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Journal articles on the topic "Inhibitors"

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Chen, Xingchen, Darren Leahy, Jessica Van Haeften, Perry Hartfield, Peter J. Prentis, Chloé A. van der Burg, Joachim M. Surm, et al. "A Versatile and Robust Serine Protease Inhibitor Scaffold from Actinia tenebrosa." Marine Drugs 17, no. 12 (December 12, 2019): 701. http://dx.doi.org/10.3390/md17120701.

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Serine proteases play pivotal roles in normal physiology and a spectrum of patho-physiological processes. Accordingly, there is considerable interest in the discovery and design of potent serine protease inhibitors for therapeutic applications. This led to concerted efforts to discover versatile and robust molecular scaffolds for inhibitor design. This investigation is a bioprospecting study that aims to isolate and identify protease inhibitors from the cnidarian Actinia tenebrosa. The study isolated two Kunitz-type protease inhibitors with very similar sequences but quite divergent inhibitory potencies when assayed against bovine trypsin, chymostrypsin, and a selection of human sequence-related peptidases. Homology modeling and molecular dynamics simulations of these inhibitors in complex with their targets were carried out and, collectively, these methodologies enabled the definition of a versatile scaffold for inhibitor design. Thermal denaturation studies showed that the inhibitors were remarkably robust. To gain a fine-grained map of the residues responsible for this stability, we conducted in silico alanine scanning and quantified individual residue contributions to the inhibitor’s stability. Sequences of these inhibitors were then used to search for Kunitz homologs in an A. tenebrosa transcriptome library, resulting in the discovery of a further 14 related sequences. Consensus analysis of these variants identified a rich molecular diversity of Kunitz domains and expanded the palette of potential residue substitutions for rational inhibitor design using this domain.
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Luan, Hengjie, Mingkang Liu, Qinglin Shan, Yujing Jiang, Peng Yan, and Xiaoyu Du. "Experimental Study on the Effect of Mixed Thermodynamic Inhibitors with Different Concentrations on Natural Gas Hydrate Synthesis." Energies 17, no. 9 (April 26, 2024): 2078. http://dx.doi.org/10.3390/en17092078.

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Natural gas hydrate (NGH) is a potential future energy resource. More than 90% of NGH resources exist in the pore medium of seafloor sediments. During the development of deep-sea oil and gas fields, wellbore pipelines are often clogged due to the synthesis of gas hydrates, and the addition of thermodynamic inhibitors is a common solution to prevent hydrate synthesis. In this paper, the effects of two single inhibitors, sodium chloride and ethylene glycol, as well as hybrid inhibitors combining these two inhibitors on the synthesis of methane hydrates were investigated using the self-developed one-dimensional gas hydrate exploitation simulation test apparatus. The effects of single and hybrid inhibitors were investigated in terms of the hydrate synthesis volume and gas–water two-phase conversion rate. The results show that the hybrid inhibitor has a better inhibitory effect on hydrate synthesis with the same initial synthesis driving force. When the concentration of inhibitors is low, salt inhibitors can have a better inhibitory effect than alcohol inhibitors. However, in the mixed inhibitor experiment, increasing the proportion of ethylene glycol in the mixed inhibitor can more effectively inhibit the synthesis of hydrates than increasing the proportion of sodium chloride in the mixed inhibitor.
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Jasim, Haider Hadi, Read Abd Al-Hussain, and Ahmed Shawqi Sadeq. "Evaluation the Efficiency of Various Types of Corrosion Inhibitors Used for Basrah Water Storage Tanks." Al-Nahrain Journal for Engineering Sciences 23, no. 3 (November 21, 2020): 267–76. http://dx.doi.org/10.29194/njes.23030267.

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In this paper, the efficiency of six different types of corrosion inhibitors used in Basrah drinking water tanks was assessed using a potentiostatic test method. The mechanism of adsorption of silicate and phosphate inhibitors in AISI 316 stainless steel surfaces and the effects of different water components in inhibitors are discussed in detail. The values of corrosion rate obtained from the Potentiostatic test showed that the protection against corrosion in the presence of inhibitors is better compared to the case of absence of inhibitors. The results of the six types of corrosion inhibitors tested showed that the inhibitory efficacy is higher below the temperatures 45oC, but when raise the temperature above 45oC the inhibitory efficiency becomes to decrease. Also, the test results indicated that the corrosion inhibitor involves silicate products provided more inhibited efficiency compared to the phosphate inhibitor alone or used the combined silicate/phosphate corrosion inhibitor. The inspection of the surface of the tested samples using optical methods shows that the pitting corrosion is demonstrated on the specimen surfaces after testing with or without inhibitors.
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Arita, Minetaro, Takaji Wakita, and Hiroyuki Shimizu. "Cellular kinase inhibitors that suppress enterovirus replication have a conserved target in viral protein 3A similar to that of enviroxime." Journal of General Virology 90, no. 8 (August 1, 2009): 1869–79. http://dx.doi.org/10.1099/vir.0.012096-0.

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Previously, we identified a cellular kinase inhibitor, GW5074, that inhibits poliovirus (PV) and enterovirus 71 replication strongly, although its target has remained unknown. To identify the target of GW5074, we searched for cellular kinase inhibitors that have anti-enterovirus activity similar or related to that of GW5074. With this aim, we performed screenings to identify cellular kinase inhibitors that could inhibit PV replication cooperatively with GW5074 or synthetically in the absence of GW5074. We identified MEK1/2 inhibitors (SL327 and U0126), an EGFR inhibitor (AG1478) and a phosphatidylinositol 3-kinase inhibitor (wortmannin) as compounds with a cooperative inhibitory effect with GW5074, and an Akt1/2 inhibitor (Akt inhibitor VIII) as a compound with a synthetic inhibitory effect with MEK1/2 inhibitors and AG1478. Individual treatment with the identified kinase inhibitors did not affect PV replication significantly, but combined treatment with MEK1/2 inhibitor, AG1478 and Akt1/2 inhibitor suppressed the replication synthetically. The effect of AG1478 in this synthetic inhibition was compensated by other receptor tyrosine kinase inhibitors (IGF-1R inhibitor II and Flt3 inhibitor II). We isolated mutants resistant to Flt3 inhibitor II and GW5074 and found that these mutants had cross-resistance to each treatment. These mutants had a common mutation in viral protein 3A that results in an amino acid change at position 70 (Ala to Thr), a mutation that was previously identified in mutants resistant to a potent anti-enterovirus compound, enviroxime. These results suggest that cellular kinase inhibitors and enviroxime have a conserved target in viral protein 3A to suppress enterovirus replication.
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Cheng, Liwei, Limin Wang, Zhi Li, Bei Liu, and Guangjin Chen. "Inhibition Effect of Kinetic Hydrate Inhibitors on the Growth of Methane Hydrate in Gas–Liquid Phase Separation State." Energies 12, no. 23 (November 25, 2019): 4482. http://dx.doi.org/10.3390/en12234482.

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The effect of kinetic hydrate inhibitors (KHIs) on the growth of methane hydrate in the gas–liquid phase separation state is studied at the molecular level. The simulation results show that the kinetic inhibitors, named PVP and PVP-A, show good inhibitory effects on the growth of methane hydrate under the gas–liquid phase separation state, and the initial position of the kinetic hydrate inhibitors has a major effect on the growth of methane hydrates. In addition, inhibitors at different locations exhibit different inhibition performances. When the inhibitor molecules are located at the gas–liquid phase interface, increasing the contact area between the groups of the inhibitor molecules and methane is beneficial to enhance the inhibitory performance of the inhibitors. When inhibitor molecules are located at the solid–liquid phase interface, the inhibitor molecules adsorbed on the surface of the hydrate nucleus and decreased the direct contact of hydrate nucleus with the surrounding water and methane molecules, which would delay the growth of hydrate nucleus. Moreover, the increase of hydrate surface curvature and the Gibbs–Thomson effect caused by inhibitors can also reduce the growth rate of methane hydrate.
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Kunitada, Satoshi, and Takayasu Nagahara. "Factor Xa Inhibitors." Current Pharmaceutical Design 2, no. 5 (October 1996): 531–42. http://dx.doi.org/10.2174/1381612802666221004174926.

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Thrombin occupies a central position in thrombus formation and eventually has been a target to develop anticoagulant agents. Although both heparin and warfarin have been used as anticoagulants, a more useful, ideal anticoagulant is desired at bedside. Numerous efforts to develop a direct inhibitor of thrombin led to the discovery of improved anticoagulants including argatoroban. However, no orally available agent has been developed yet. FXa is responsible for prothrombin activation to generate thrombin and provides an alternative strategy to inhibit the coagulation cascade. In contrast with ATIII-dependent type FXa inhibitor, direct ATIII­ independent type inhibitors, such as tick anticoagulant peptide and antistasin, showed an inhibitory effect on arterial as well as venous thrombosis models, which was comparable to the effects of thrombin direct inhibitors or glycoprotein llb/Illa inhibitors. We synthesized a low molecular weight, orally active FXa inhibitor, DX- 9065l!, which also showed antithrombotic effect in various kind of thrombosis models. Further, FXa inhibitors have been known to have unique characteristics preferable to those of thrombin inhibitors. In this article, we review the pharmacological profile and structure-activity relationships of FXa inhibitors, ranging from naturally occuring to synthetic small molecular types.
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Milner, Malgorzata, Jadwiga Chroboczek, and Wlodzimierz Zagorski-Ostoja. "Engineered resistance against proteinases." Acta Biochimica Polonica 54, no. 3 (September 6, 2007): 523–36. http://dx.doi.org/10.18388/abp.2007_3226.

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Exogenous proteinase inhibitors are valuable and economically interesting protective biotechnological tools. We examined whether small proteinase inhibitors when fused to a selected target protein can protect the target from proteolytic degradation without simultaneously affecting the function and activity of the target domain. Two proteinase inhibitors were studied: a Kazal-type silk proteinase inhibitor (SPI2) from Galleria mellonella, and the Cucurbita maxima trypsin inhibitor I (CMTI I). Both inhibitors target serine proteinases, are small proteins with a compact structure stabilized by a network of disulfide bridges, and are expressed as free polypeptides in their natural surroundings. Four constructs were prepared: the gene for either of the inhibitors was ligated to the 5' end of the DNA encoding one or the other of two selected target proteins, the coat protein (CP) of Potato potyvirus Y or the Escherichia coli beta-glucuronidase (GUS). CMTI I fused to the target proteins strongly hampered their functions. Moreover, the inhibitory activity of CMTI I was retained only when it was fused to the CP. In contrast, when fused to SPI2, specific features and functions of both target proteins were retained and the inhibitory activity of SPI2 was fully preserved. Measuring proteolysis in the presence or absence of either inhibitor, we demonstrated that proteinase inhibitors can protect target proteins used either free or as a fusion domain. Interestingly, their inhibitory efficiency was superior to that of a commercial inhibitor of serine proteinases, AEBSF.
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Shi, Qizhen, Erin L. Kuether, Jocelyn A. Schroeder, Crystal L. Perry, Scot A. Fahs, and Robert R. Montgomery. "Factor VIII Inhibitors: Von Willebrand Factor Makes A Difference In Vitro and In Vivo." Blood 116, no. 21 (November 19, 2010): 709. http://dx.doi.org/10.1182/blood.v116.21.709.709.

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Abstract Abstract 709 The important association between von Willebrand factor (VWF) and factor VIII (FVIII) has been investigated for decades, but the effect of VWF on FVIII inhibitors is still controversial. Studies have demonstrated that some anti-FVIII inhibitory antibodies inhibit VWF-FVIII interaction, while others rely on the presence of VWF to inhibit FVIII activities. The influence of VWF on the Bethesda assay, which is routinely used in the clinic to determine the titer of FVIII-neutralizing inhibitors, is still uncertain because the plasma from hemophilia A patients with inhibitors contains normal levels of VWF. To explore the effect of VWF on the reactivity of FVIII inhibitors, we immunized VWF and FVIII double knockout (VWFnullFVIIInull) mice with recombinant human B-domain deleted FVIII (rhFVIII) to induce anti-FVIII inhibitory antibody development. Inhibitory plasma was collected and the titer of inhibitors was determined by Bethesda assay. Murine plasma-derived VWF (from FVIIInull mice) or recombinant human VWF (rhVWF) was used to study the influence of VWF on inhibitor inactivation of FVIII activity (FVIII:C). The remaining FVIII:C after inactivation was determined by chromogenic assay. When inhibitory plasma was incubated with rhFVIII in the presence of 1 U/ml VWF, the residual FVIII activity recovered was higher than in the absence of VWF, resulting in 6.82 ± 1.12 (n = 27) fold lower apparent inhibitor titers. This protective effect is VWF dose dependent. The source of VWF (plasma-derived murine VWF vs. rhVWF) did not affect its protection of FVIII from inhibitor inactivation and VWF does not affect FVIII:C measured in the chromogenic assay in the absence of inhibitors. Interestingly, we found that inhibitor inactivation of FVIII:C in the absence of VWF occurred much faster than in its presence. When the usual 2 hr. incubation at 37°C was omitted from the Bethesda assay, adding rhVWF to rFVIII before mixing with inhibitory plasma resulted in 67.29 ± 20.18 (n = 5) fold lower apparent inhibitor titers than without added VWF. In contrast, if VWF was added to inhibitory plasma first and then mixed with rhFVIII, the inhibitor titers were only 11.04 ± 3.56 (n = 5) fold lower than without added VWF. These results indicate that rhFVIII present in a preformed VWF-FVIII complex is protected from inhibitory antibody inactivation. Conversely, when VWF and inhibitory plasma are added to rhFVIII at the same time, the VWF and inhibitors appear to compete to bind to rhFVIII. Inhibitor titers were lower than in the absence of VWF, but the protective effect is not as efficient as when VWF and rhFVIII were already associated with one another before encountering inhibitors. To confirm the protective effect of VWF on FVIII from inhibitor inactivation, we infused FVIIInull or VWFnullFVIIInull mice with inhibitory plasma and rhFVIII followed by a tail clip survival test. When rhFVIII was infused into FVIIInull mice to 2% followed by inhibitory plasma infusion, all mice with inhibitor titer of 2.5 BU/ml (n = 4) survived tail clipping, and 2 of 4 survived with either 25 BU/ml or 250 BU/ml. If inhibitory plasma was infused first followed by rhFVIII infusion, then only 2 of 6 mice with inhibitor titers of 2.5 BU/ml survived tail clip challenge and none survived with 25 BU/ml and 250 BU/ml. In the first set of mice the infused FVIII was able to form a protective complex with endogenous VWF before encountering inhibitors, while in the second set FVIII is exposed to VWF and pre-infused inhibitory antibodies at the same time, a competitive binding that appears to reduce VWF's protective effect. In contrast, when rhFVIII was infused into VWFnullFVIIInull mice followed by inhibitory plasma infusion, no animals (n = 4 for each group) survived tail clipping with inhibitor titers of 2.5 BU/ml or higher. In summary, our studies demonstrate that VWF exerts a protective effect, reducing inhibitor inactivation of FVIII, both in vitro and in vivo. While the role of VWF in stabilizing plasma FVIII in a milieu rich in proteases has been appreciated for decades, our results indicate that treatment utilizing products containing a complex of FVIII with VWF may be especially beneficial in hemophilia A patients with inhibitors. Disclosures: No relevant conflicts of interest to declare.
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Savitri, Erna Noor, Putut Marwoto, and Sunyoto Eko Nugroho. "The Effectiveness of a Combination of Lime (Citrus aurantifolia.), Lerak (Sapindus rarak) and Jasmine Flower (Jasminum nudiflorum) Extracts as and Environmentally Friendly Corrosion Inhibitor." Jurnal Penelitian Pendidikan IPA 10, no. 3 (March 30, 2024): 1019–24. http://dx.doi.org/10.29303/jppipa.v10i3.6364.

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Corrosion can also be defined as the forced destruction of metal by the surrounding medium which is usually a liquid (corrosive agent). Corrosion prevention processes can be carried out, including by coating the metal surface, cathodic protection, adding corrosion inhibitors and so on. Several types of inhibitors that have been widely used in industrial applications are synthetic chemical inhibitors. However, the compounds of inhibitors are environmentally unfriendly, toxic and expensive. To overcome this problem, it is necessary to develop an environmentally friendly alternative corrosion inhibitor or better known as a green inhibitor. This research aims to test the effectiveness of using a combination of lime (Citrus aurantifolia.), Lerak (Sapindus rarak) and jasmine flower (Jasminum nudiflorum) extracts as an environmentally friendly corrosion inhibitor. The results obtained were inhibitors in the form of a combination which were added to the corrosive medium HCl which could reduce the rate of aluminum corrosion. This research also shows that time and concentration influence the corrosion rate. A higher concentration (200 ppm) has a greater inhibitory power than a concentration of 100 ppm. The best inhibitory power is found in 200 ppm inhibitor with a soaking time of 20 minutes
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Zeng, Peng, and Alvin Schmaier. "Ponatinib and other CML Tyrosine Kinase Inhibitors in Thrombosis." International Journal of Molecular Sciences 21, no. 18 (September 8, 2020): 6556. http://dx.doi.org/10.3390/ijms21186556.

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Abl1 kinase has important biological roles. The Bcr-Abl1 fusion protein creates undesired kinase activity and is pathogenic in 95% of chronic myeloid leukemia (CML) and 30% of acute lymphoblastic leukemia (ALL) patients. Targeted therapies to these diseases are tyrosine kinase inhibitors. The extent of a tyrosine kinase inhibitor’s targets determines the degree of biologic effects of the agent that may influence the well-being of the patient. This fact is especially true with tyrosine kinase inhibitor effects on the cardiovascular system. Thirty-one percent of ponatinib-treated patients, the tyrosine kinase inhibitor with the broadest inhibitory spectrum, have thrombosis associated with its use. Recent experimental investigations have indicated the mechanisms of ponatinib-associated thrombosis. Further, an antidote to ponatinib is in development by re-purposing an FDA-approved medication.
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Dissertations / Theses on the topic "Inhibitors"

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Miyazaki, Hiroshi. "Studies on Inhibitors of Plasminogen Activator Inhibitor-1(PAI-1) and Inhibitors of PAI-1 Production as Antithrombotic Agents." 京都大学 (Kyoto University), 2010. http://hdl.handle.net/2433/126818.

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Bodhe, A. M. "Enzyme inhibitors." Thesis(Ph.D.), CSIR-National Chemical Laboratory, Pune, 1988. http://dspace.ncl.res.in:8080/xmlui/handle/20.500.12252/3302.

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Rioja, Alphonso Sid. "Synthesis of prenyl transferase inhibitors and histone deacetylase inhibitors." Thesis, University College London (University of London), 2002. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.418246.

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Trivedi-Parmar, Vinay. "Synthesis and Optimization of Non-Phenolic Inhibitors of Macrophage Migration Inhibitory Factor." Thesis, Yale University, 2019. http://pqdtopen.proquest.com/#viewpdf?dispub=13851921.

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Macrophage migration inhibitory factor (MIF) is a pleiotropic cytokine and an upstream regulator of inflammation and cell proliferation. Interestingly, MIF is also an enzyme that functions as a keto-enol tautomerase, though this function is believed to be vestigial in humans. Implicated in the pathogenesis of multiple infectious and autoimmune diseases, including rheumatoid arthritis and cancer, MIF has emerged as an attractive drug target, with the tautomerase active site serving as a convenient binding pocket for small molecule inhibitors. Most MIF inhibitors include a phenol ring, which forms an essential hydrogen bond with an asparagine residue at the back of the binding pocket. While phenol is not an uncommon moiety in approved dugs, it is particularly susceptible to rapid phase 11 metabolic processes and excretion from biological systems, resulting in low oral bioavailability and short half-life. Therefore, potent non-phenolic MIF inhibitors are desirable. Two series of MIF inhibitors lacking the commonly employed phenol group were pursued and are described in this thesis.

The first was a series of benzoxazolone inhibitors. Attempts at lead optimization were stymied by sensitivity of tautomerase assay results to protein source and incubation conditions, inconsistencies between molecular modeling studies and experimental activity data, and the inability to obtain a crystal structure of the protein–inhibitor complex. A binding mode could not be resolved for the scaffold, preventing a rational, structure-based approach to drug development. Nevertheless, a methodical medicinal chemistry strategy was employed to elaborate the structure-activity relationships (SAR) of the series and discover potent inhbitors. A circa 5 µM inhibitor was obtained, but when further attempts to optimize the series proved ineffective, attention was turned to a new scaffold.

The second series of MIF inhibitors pursued involved bioisosteric replacement of phenol with a pyrazole, which is capable of forming dual hydrogen bonds with the asparagine residue at the back of the binding pocket. From a 113-µM virtual screening hit, a structure-based, computer-aided lead optimization strategy was employed. X-ray crystal structures of MIF-inhibitor complexes and molecular modeling results guided effective selection and placement of substituents on the scaffold. Methodical derivitization and expansion of the scaffold to include auxiliary aryl functionality near the rim of the binding pocket and recognition of the benefit of pyrazole fluorination were essential breakthroughs in optimizing this series, resulting in inhibitors with potencies around 60-70 nm. From a metabolic perspective, bioisosteric replacement of a salt bridge-forming carboxylate group on the scaffold with a pharmacologically favorable sulfonamide was found to be well tolerated. Additionally, modification of the solvent-exposed region of the scaffold with solubilizing groups was shown to improve aqueous solubility without affecting activity. The pyrazoles are the only the second series of MIF inhibitors to be optimized from an initial screening hit to give inhibitors with nanomolar potency. With their high potencies and expected favorable metabolism, compounds in this series have the potential to be developed into true MIF-directed therapeutics.

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Mamone, Marius. "N-fluoroalkyles et CF3-cyclopropanes; vers de nouvelles unités peptidomimétiques." Thesis, Université Paris-Saclay (ComUE), 2015. http://www.theses.fr/2015SACLS276.

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Grâce à des propriétés physico-chimiques particulières, le fluor prend de plus en plus d’importance dans la chimie médicinale et plus particulièrement dans les peptidomimétiques. Dans ce mémoire, deux classes de peptidomimétiques fluorées ont été étudiées.Dans la première partie, de nouveaux groupements N-Rf ; les hydrazines difluoro ou trifluorométhylées et les 1,2,3 triazoles N-difluorométhylés ont été préparés et des études de leurs propriétés structurales ont montré l’intérêt de l’incorporation du fluor sur la conformation des pseudopeptides via des interactions NH-F.Dans la seconde partie, de nouveaux peptidomimétiques comportant des groupements cyclopropanes trifluorométhylés ont été conçus et synthétisés en tant qu’inhibiteurs potentiels du protéasome 26S (un macro-complexe protéique impliqué dans la dégradation de nombreuses protéines intracellulaires et qui a fait ses preuves en tant que cible pour le traitement de cancers)
Through special physico-chemical properties, fluorine is becoming increasingly important in medicinal chemistry and particularly in peptidomimetics. In this paper, two classes of fluorinated peptidomimetics were studied.In the first part, new N-Rf moieties; difluoro or trifluoromethylated hydrazines and N-difluoromethyl 1,2,3 triazoles were prepared and the study of their structural properties have shown the benefit of the incorporation of fluorine on the conformation of the peptidomimetics via NH-F interactions.In the second part, new trifluoromethylated cyclopropanes containing peptidomimetics were designed and synthesized as potential inhibitors of the 26S proteasome, a macro-complex protein involved in the degradation of many intracellular proteins and which has been recognized as a target for cancer treatment
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Paren, Helen. "Inhibitors of metalloproteases." Thesis, University of Oxford, 1995. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.260150.

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Tan, Swee Hain. "Organic corrosion inhibitors." Thesis, Tan, Swee Hain (1991) Organic corrosion inhibitors. PhD thesis, Murdoch University, 1991. https://researchrepository.murdoch.edu.au/id/eprint/333/.

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The overall aims of this thesis were to conduct a broad survey of possible organic corrosion inhibitors in near-neutral chloride solutions and to elucidate the mechanisms of such action. Altogether, 130 organic compounds were studied as possible corrosion inhibitors for pure iron, mild steel, copper and aluminium in aerated near-neutral (pH = 8.4) solutions containing 500 ppm NaCl and 100 ppm NaHCO, conditions often encountered in water-based automotive engine coolants. Inhibitor behaviour was investigated using steady-state electrochemical techniques including polarisation curves, Stern-Geary and corrosion potential (Em,) measurements. The organic compounds examined were found to be highly specific in their inhibitive action toward the metals studied. Typical examples of highly effective corrosion inhibitors were: sebacate and octanoate for pure iron; oleate and sebacate for mild steel; benzotriazole and 2-mercaptobenzothiazole for copper; and laurate and oleate for aluminium. E, was found to provide a rapid and convenient screening test for evaluating the inhibitor performance of organic compounds toward pure iron, mild steel and aluminium but was less useful for copper. Good organic inhibitors were found to act as anodic inhibitors toward pure iron and mild steel but as anodic or mixed-type inhibitors toward copper. For aluminium, the majority of the compounds studied were found to act as anodic inhibitors. However,However, it was also found that only pit initiation was inhibited, i.e. existing pits were not prevented from developing. Optical microscopy of pitted aluminium surfaces indicated their nature varied considerably with inhibition efficiency. The role of complex formation in organic corrosion inhibitors was found to vary with the metal. Complexation of either iron(I1) or iron(II1) ions was found to have an insignificant effect on mild steel. The corrosion rate of copper was found to increase with the copper(LI) complex stability, thus indicating complex formation to be the rate-determining step. For aluminium, the observed effects were found to depend on complex stability. For weak to moderate complexants, inhibitor efficiency (measured as E,,) increased with increasing complexation. However, very strong complexing agents were sufficiently stable to dissolve the aluminium oxide surface, leading to poor inhibition. Aluminium pit morphology was found, using scanning electron microscopy, to change from hemispherical in the uninhibited solution to irregular in the presence of complexing inhibitors. No simple relationships between inhibitor efficiency and molecular structure were found. However, carbon chain length, the nature of functional group(s) and their location in the molecule were found to be important but varied according to the metal. The inhibiting ability of sebacate (a straight chain C, dicarboxylate) was found not to be compromised by water movement (stirring) or pre-existing corrosion product layers. Immersion tests showed that passive film formation on mild steel in sebacate solution involved two stages and was complete only after -100 h immersion. The ion selective properties of several iron(II1) carboxylates and hydrated iron(II1) oxide films were studied by membrane potential measurements in neutral sodium chloride solutions. Some specimens were also studied by Mossbauer spectroscopy. These results show that dicarboxylates are good inhibitors toward mild steel because they form impermeable films. Poor inhibitor performance is associated with the anion selectivity of the film which in turn appears to be related to the film purity. A model is suggested for the inhibition mechanism of mild steel corrosion by dicarboxylates in aerated near-neutral chloride solutions.
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Tan, Swee Hain. "Organic corrosion inhibitors." Murdoch University, 1991. http://wwwlib.murdoch.edu.au/adt/browse/view/adt-MU20060818.150145.

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The overall aims of this thesis were to conduct a broad survey of possible organic corrosion inhibitors in near-neutral chloride solutions and to elucidate the mechanisms of such action. Altogether, 130 organic compounds were studied as possible corrosion inhibitors for pure iron, mild steel, copper and aluminium in aerated near-neutral (pH = 8.4) solutions containing 500 ppm NaCl and 100 ppm NaHCO,, conditions often encountered in water-based automotive engine coolants. Inhibitor behaviour was investigated using steady-state electrochemical techniques including polarisation curves, Stern-Geary and corrosion potential (Em,) measurements. The organic compounds examined were found to be highly specific in their inhibitive action toward the metals studied. Typical examples of highly effective corrosion inhibitors were: sebacate and octanoate for pure iron; oleate and sebacate for mild steel; benzotriazole and 2-mercaptobenzothiazole for copper; and laurate and oleate for aluminium. E, was found to provide a rapid and convenient screening test for evaluating the inhibitor performance of organic compounds toward pure iron, mild steel and aluminium but was less useful for copper. Good organic inhibitors were found to act as anodic inhibitors toward pure iron and mild steel but as anodic or mixed-type inhibitors toward copper. For aluminium, the majority of the compounds studied were found to act as anodic inhibitors. However,However, it was also found that only pit initiation was inhibited, i.e. existing pits were not prevented from developing. Optical microscopy of pitted aluminium surfaces indicated their nature varied considerably with inhibition efficiency. The role of complex formation in organic corrosion inhibitors was found to vary with the metal. Complexation of either iron(I1) or iron(II1) ions was found to have an insignificant effect on mild steel. The corrosion rate of copper was found to increase with the copper(LI) complex stability, thus indicating complex formation to be the rate-determining step. For aluminium, the observed effects were found to depend on complex stability. For weak to moderate complexants, inhibitor efficiency (measured as E,,) increased with increasing complexation. However, very strong complexing agents were sufficiently stable to dissolve the aluminium oxide surface, leading to poor inhibition. Aluminium pit morphology was found, using scanning electron microscopy, to change from hemispherical in the uninhibited solution to irregular in the presence of complexing inhibitors. No simple relationships between inhibitor efficiency and molecular structure were found. However, carbon chain length, the nature of functional group(s) and their location in the molecule were found to be important but varied according to the metal. The inhibiting ability of sebacate (a straight chain C, dicarboxylate) was found not to be compromised by water movement (stirring) or pre-existing corrosion product layers. Immersion tests showed that passive film formation on mild steel in sebacate solution involved two stages and was complete only after -100 h immersion. The ion selective properties of several iron(II1) carboxylates and hydrated iron(II1) oxide films were studied by membrane potential measurements in neutral sodium chloride solutions. Some specimens were also studied by Mossbauer spectroscopy. These results show that dicarboxylates are good inhibitors toward mild steel because they form impermeable films. Poor inhibitor performance is associated with the anion selectivity of the film which in turn appears to be related to the film purity. A model is suggested for the inhibition mechanism of mild steel corrosion by dicarboxylates in aerated near-neutral chloride solutions.
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Menon, V. "Molecular and functional aspects of hydrolyases / inhibitors with emphasis on aspartic protease inhibitor." Thesis(Ph.D.), CSIR-National Chemical Laboratory, Pune, 2012. http://dspace.ncl.res.in:8080/xmlui/handle/20.500.12252/2401.

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Hirst, Claire Elizabeth 1971. "Tissue distribution and regulation of the granzyme B inhibitor, proteinase inhibitor 9." Monash University, Dept. of Biochemistry and Molecular Biology, 2002. http://arrow.monash.edu.au/hdl/1959.1/8488.

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Books on the topic "Inhibitors"

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Iqbal, Choudhary Muhammad, ed. Biological inhibitors. Amsterdam: Harwood Academic Publishers, 1996.

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Zollner, Helmward. Handbook of enzyme inhibitors. 2nd ed. Weinheim, Federal Republic of Germany: VCH, 1993.

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Zollner, Helmward. Handbook of enzyme inhibitors. 3rd ed. Weinheim: New York, 1999.

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Zollner, Helmward. Handbook of enzyme inhibitors. Weinheim, Federal Republic of Germany: VCH, 1989.

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Laufer, Stefan, ed. Proteinkinase Inhibitors. Cham: Springer International Publishing, 2021. http://dx.doi.org/10.1007/978-3-030-68180-7.

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D’Orléans-Juste, Pedro, and Gérard E. Plante, eds. ACE Inhibitors. Basel: Birkhäuser Basel, 2001. http://dx.doi.org/10.1007/978-3-0348-7579-0.

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Kuster, Bernhard, ed. Kinase Inhibitors. Totowa, NJ: Humana Press, 2012. http://dx.doi.org/10.1007/978-1-61779-337-0.

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Furr, Barrington J. A., ed. Aromatase Inhibitors. Basel: Birkhäuser Basel, 2006. http://dx.doi.org/10.1007/3-7643-7418-7.

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Furr, Barrington J. A., ed. Aromatase Inhibitors. Basel: Birkhäuser Basel, 2008. http://dx.doi.org/10.1007/978-3-7643-8693-1.

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Hayes, Teresa L. Corrosion inhibitors. Cleveland, Ohio: Freedonia Group, 2002.

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Book chapters on the topic "Inhibitors"

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Kumar, Varun, and Kanwate Balaji. "Enzymatic Inhibitors (Protease inhibitors, Amylase inhibitors, Cholinesterase Inhibitors)." In Handbook of Plant and Animal Toxins in Food, 217–38. Boca Raton: CRC Press, 2022. http://dx.doi.org/10.1201/9781003178446-12.

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Quaranta, Vito. "Inhibitors." In Encyclopedia of Systems Biology, 1033. New York, NY: Springer New York, 2013. http://dx.doi.org/10.1007/978-1-4419-9863-7_1075.

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Vane, John R. "The history of inhibitors of angiotensin converting enzyme." In ACE Inhibitors, 1–10. Basel: Birkhäuser Basel, 2001. http://dx.doi.org/10.1007/978-3-0348-7579-0_1.

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de Champlain, Jacques, and Pedro D’Orléans-Juste. "Role of the renin-angiotensin system on the central and peripheral autonomic nervous system." In ACE Inhibitors, 145–53. Basel: Birkhäuser Basel, 2001. http://dx.doi.org/10.1007/978-3-0348-7579-0_10.

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Fink, Cynthia A. "Dual inhibitors of angiotensin converting enzyme and neutral endopeptidase." In ACE Inhibitors, 155–62. Basel: Birkhäuser Basel, 2001. http://dx.doi.org/10.1007/978-3-0348-7579-0_11.

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Orfanos, Stylianos E., Linhua Zou, and John D. Catravas. "Pharmacodynamics, tissue-specificity of ACE inhibitors." In ACE Inhibitors, 163–70. Basel: Birkhäuser Basel, 2001. http://dx.doi.org/10.1007/978-3-0348-7579-0_12.

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Nawar, Tewfik, Eve-Reine Gagné, Raymonde Turcotte, and Gérard E. Plante. "Effect of angiotensin converting enzyme inhibition on thirst and salt-appetite." In ACE Inhibitors, 171–76. Basel: Birkhäuser Basel, 2001. http://dx.doi.org/10.1007/978-3-0348-7579-0_13.

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Cooper, Mark E. "ACE and diabetes." In ACE Inhibitors, 177–84. Basel: Birkhäuser Basel, 2001. http://dx.doi.org/10.1007/978-3-0348-7579-0_14.

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Lajemi, Malika, and Athanase Benetos. "Genetics of the renin-angiotensin-aldosterone system and risk of arterial disease." In ACE Inhibitors, 11–27. Basel: Birkhäuser Basel, 2001. http://dx.doi.org/10.1007/978-3-0348-7579-0_2.

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Wohlfart, Paulus, Gabriele Wiemer, Wolfgang Linz, and Bernward A. Schölkens. "Crosstalk between ACE inhibitors, B2 kinin receptor and nitric oxide in endothelial cells." In ACE Inhibitors, 29–36. Basel: Birkhäuser Basel, 2001. http://dx.doi.org/10.1007/978-3-0348-7579-0_3.

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Conference papers on the topic "Inhibitors"

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Krunić, Mihajlo J., Jelena Z. Penjišević, Slađana Kostić-Rajačić, Vladimir B. Šukalović, Deana B. Andrić, and Ivana I. Jevtić. "Pyrazole/tacrine derivatives as potential cholinesterase inhibitors." In 2nd International Conference on Chemo and Bioinformatics. Institute for Information Technologies, University of Kragujevac, 2023. http://dx.doi.org/10.46793/iccbi23.567k.

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Two new tacrine/pyrazole conjugates were designed, synthesized, and pharmacologically evaluated for their inhibitory activity toward acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE). A scalable and cost-efficient synthetic route was developed, and key reaction steps for the synthesis of compounds 4a,b were nucleophilic substitution of α-aroylketene dithioacetals with tacrine intermediates, followed by cyclocondensation of respective N,S-acetals with hydrazine hydrate. The preliminary pharmacological evaluation revealed high inhibitory activities of 4a,b toward AChE (180 and 259 nM, respectively) and BuChE (51 and 95 nM, respectively) as compared with known inhibitor, tacrine. Overall, both compounds were more efficient BuChE inhibitors while 4a, with a shorter linker connecting tacrine and phenylpyrazole moieties, showed higher inhibitory activity toward both enzymes. Molecular docking analysis strongly corroborated pharmacological results since both compounds interacted favorably with target enzymes. Calculated pharmacokinetic properties (absorption, distribution, metabolism, and excretion (ADME) showed that 4a,b obey Lipinski’s rule of druglikeness and are promising lead compounds for the development of new drug candidates.
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Beretz, A., F. Lanza, A. Stierlé, and J.-P. Cazenave. "CYCLIC NUCLEOTIDE PHOSPHODIESTERASE INHIBITORS PREVENT AGGREGATION AND SECRETION OF HUMAN PLATELETS BY RAISING CYCLIC AMP AND REDUCING CYTOPLASMIC FREE CALCIUM MOBILIZATION." In XIth International Congress on Thrombosis and Haemostasis. Schattauer GmbH, 1987. http://dx.doi.org/10.1055/s-0038-1643586.

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Drugs that raise platelet cyclic AMP (cAMP) are potent inhibitors of platelet activation. We have studied the effects of 5 inhibitors of cyclic nucleotide phosphodiesterase (PDE) of different chemical structures (quercetin, Ro 15-2041, HL-725, cilostamide and MY-5445), which are all potent inhibitors of platelet function. The concentrations that inhibit by 50 % crude cAMP-PDE activity (IC50) from human platelets are: 0.06 μM(HL-725), 0.15 μM(Ro 15-2041 ), 0.23 μM(cilostamide), 6.9 μM(MY-5445) and 44.4 μM(quercetin). We measured on the same preparation of washed human platelets loaded with quin2, the aggregation and the increase in intracellular Ca2+ ([Ca2+]i) induced by 5 μM ADP alone or in the presence of PDE inhibitors.PGE1 (2 nM) potentiates significantly (1.6 to 3.3 fold) the inhibitory effects of PDE inhibitors on [Ca2+]i rises and platelet aggregation. Adrenaline, an inhibitor of adenylate cylase, prevents the effect of PDE inhibitors on ADP-induced [Ca2+]i rise and platelet aggregation. These results suggest that these compounds inhibit [Ca2+]i mobilization and subsequent ADP-induced aggregation through a rise in cAMP, because both effects are potentiated by PGE1 and inhibited by adrenaline. The inhibitor concentrations which potentiate the action of PGE1, on [ Ca2+]i levels also potentiate the rise in platelet cAMP induced by PGE-<. These results suggest that PDE inhibitors inhibit platelet aggregation Ly raising cAMP levels and subsequently inhibiting [Ca2+]i mobilization.
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Liu, Keshun, and Mike Woolman. "Developing an optimized method for measuring chymotrypsin inhibitor activity in protein products." In 2022 AOCS Annual Meeting & Expo. American Oil Chemists' Society (AOCS), 2022. http://dx.doi.org/10.21748/yucc6741.

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Protease inhibitors of protein nature, such as trypsin inhibitors and chymotrypsin inhibitors, are rich in seeds of legume crops. Soybeans contain Kunitz inhibitor and Bowman-Birk inhibitor. The former mainly inhibits trypsin, while the latter inhibits both trypsin and chymotrypsin. Other legumes contain similar types. Historically, trypsin inhibitor activity in legume products has been of primary interest for measurement due to its antinutritional implication. However, Bowman-Birk inhibitor has been shown therapeutic. It is also more resistant to heat than Kunitz inhibitor. As increasing volumes of plant proteins are being used for food or feed in recent years, there is a growing interest in monitoring chymotrypsin inhibitor activity (CIA) in these products as well. Yet, reported methods for CIA assay vary greatly, with no standard method being available. Three years ago, at our USDA lab, we developed an improved method for measuring trypsin inhibitor activity, which was later adopted as AOCS Official Method, Ba 12a-2020. This presentation reports our new effort in developing a method for measuring CIA, using N-benzoyl-L-tyrosine p-nitroanilide (BTpNA) as a substrate. Unlike the substrate for measuring trypsin inhibitor activity, BTpNA is not water soluble, an organic solvent that is miscible with water must be present. Therefore, the assay system for measuring CIA was much more complicated than that for measuring trypsin inhibitor activity. This made the method development more difficult than originally thought. After investigating effects of many assay parameters, such as organic solvent, the sequence of adding reagents, % chymotrypsin inhibition, etc., an optimized method for CIA measurement was finally developed. It featured dimethylformamide as the organic solvent, the enzyme-last sequence, 5 mL total assay volume, and calculation of the inhibitor activity based on % chymotrypsin inhibition. The proposed method was reliable and robust and could be standardized for measuring CIA in various protein products.
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Carrell, R. W., P. D. Christey, and D. R. Boswell. "SERPINS: ANTITHROMBIN AND OTHER INHIBITORS OF COAGULATION AND FIBRINOLYSIS. EVIDENCE FROM AMINO ACID SEQUENCES." In XIth International Congress on Thrombosis and Haemostasis. Schattauer GmbH, 1987. http://dx.doi.org/10.1055/s-0038-1642896.

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A number of the key inhibitors of coagulation and fibrinolysis have recently been shown to be members of the same superfamily of serine protease inhibitors, the serpins. The archetypes of the group are alpha-l-antitrypsin and antithrombin and it includes antiplasmin, C1-inhibitor, heparin cofactor II and the newly recognised inhibitors of plasminogen activators and activated Protein C. Alignment of their structures shows that they have the same skeletal three-dimensional conformation and, by inference, the same general function mechanisms.The serpins have a reactive centre, primarily dependent on a single amino acid, exteriorly placed on a stressed peptide loop. This functions by offering the cognate protease a high-affinity substrate that resists complete cleavage to form a tight 1:1 complex of inhibitor and protease that is subsequently removed from the circulation. The loop is vulnerable to cleavage with resulting loss of inhibitory activity. This irreversible switch is utilised: pathologically by venom and invasive bacterial proteases; and physiologically by the neutrophil leucocyte to modify local inflammatory responses. These mechanisms contribute to the changes seen in DIC and the shock syndromes.Modelling of antithrombin indicates the likely topological features involved in the binding of heparin, namely a sphere of positive charge centred on the A and D helices and involving Arg 47, Lys 125, Arg 129 and probably Arg 132 and Lys 133.Because the serpins are largely dependent for their specificityon a single amino acid it is now possible to precisely tailor inhibitory activity by site specific mutation. This has been used to produce recombinant antitrypsins that function as an improved inhibitor of neutrophil proteases (valine or leucine reactive centre), or as an analogue of antithrombin (arginine reactive centre). An elegant application of this approach is the engineered mutants of antiplasmin recently described by Holmes, Collen and colleagues (Leuven).
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Donaldson, V. H., and M. D. B. H. Mitchell. "INTERACTIONS OF DYSFUNCTIONAL Cl-INHIBITORS FROM PATIENTS WITH TYPE II HEREDITARY ANGIONEUROTIC EDEMA (HANE) WITH ACTIVATED HAGEMAN FACTOR (FACTOR XIIa)." In XIth International Congress on Thrombosis and Haemostasis. Schattauer GmbH, 1987. http://dx.doi.org/10.1055/s-0038-1643302.

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Type II HANE is characterized by a deficiency of Cl-inhibitor (Cl-INH) activity in serum which is associated with a dysfunctional inhibitor protein having a normal or increased quantity o|_the antigenic properties of normal serum Cl-inhibitor. Dysfunctional Cl-INH proteins were purified from members_of eight different kindred with Type II HANE and compared to normal Cl-inhibitor with respect to their inhibitory activity directed against the amidolytic and clot-promoting properties of purified activated Hageman factor. All but one dysfunctional Cl-inhibitor blocked the amidolytic activity of ellagic acid-activated Hageman factor; all eight blocked the clot-promoting activity of Hageman factor activated in solutions of sulfatides and BSA. The inhibition _of amidolytic activity was equal to or greater than that of normal Cl-INH (Donaldson, et al., 3. Clin. Invest. 75:124,1985). The impairment of the specific Hageman factor coagulant activity of activated Hageman factor by six^f the eight dysfunctional inhibitors was less than that of the normal Cl-inhibitor, although readily measured. Dysfunctional Cl-inhibitor proteins were also heterogeneous with respect to their formation of stable complexes and their susceptibility to cleavage by Hageman factor activated with BSA-sulfatides when analyzed in SDS-gel electrophoresis. Although these observatons cannot be directly applied to in vivo pathophysiologic changes in plasma, dysfunctional Cl-inhibitors do have the potential of regulating activated Hageman factor.
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Yao, Xuanzhu, Xin Wang, Saebom Ko, Cianna Leschied, Yu Yi Shen, Daniel Pimentel, Chanaka Navarathna, et al. "Fate and Transport of Sulfonated Polymeric Inhibitors in the Reservoir: Studied by Column Experiments With Calcite Media." In SPE International Conference on Oilfield Chemistry. SPE, 2023. http://dx.doi.org/10.2118/213787-ms.

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Abstract Sulfonated polymers are frequently used in the oil and gas industry to prevent inorganic scale damage, but studying their fate and transport in reservoirs has been difficult due to the challenges in analyzing them at effective concentrations. Recycling inhibitors in reservoirs necessitates inhibitors that do not adhere strongly to mineral surfaces, making polymeric inhibitors a promising option. This research aims to examine the sorption and transport of sulfonated polymeric inhibitors in calcite-packed columns using the Brine Chemistry Inhibitor (BCIn) technique, with the goal of recycling the inhibitors, specifically in the Permian basin. The BCIn method was used in this study to determine concentrations of sulfonated inhibitors, which had been shown to be reliable for measuring polymeric inhibitors at near ppm levels. The study began with conducting batch experiments on barite and calcite salts to gain initial insights into the adsorption properties of inhibitors. Next, flow-through experiments were performed where sulfonated inhibitors were injected into a column packed with calcite, followed by a flow-back test. Different sulfonated polymeric inhibitors were tested under various temperatures in the lab’s synthetic brine matrices. The concentrations of sulfonates versus injected time were plotted to assess the retention of inhibitors on rock surfaces. A commonly used phosphonate scale inhibitor (DTPMP) was included for comparison of adsorption characteristics. The experimental findings suggest that sulfonated polymeric inhibitors exhibit limited adsorption capacity but strong binding between inhibitor molecules and mineral surfaces. An inhibitor treatment scenario is proposed, where the first injection is used to saturate the surfaces of rocks, and subsequently, produced water containing low-concentration inhibitors can be recycled. The research expands our understanding of sulfonated polymeric scale inhibitors’ fate and transport in reservoirs, overcoming the challenge of analyzing polymeric inhibitors at low concentrations. The results provide evidence supporting the potential of applying polymeric inhibitors via injection wells for safeguarding production.
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Løge, Isaac A., Benaiah U. Anabaraonye, and Philip L. Fosbøl. "Characterizing the Effect of Scale Inhibitors on Surfaces." In SPE International Conference on Oilfield Chemistry. SPE, 2023. http://dx.doi.org/10.2118/213830-ms.

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Abstract Inorganic scaling imposes a significant economic burden on the oil industry. Scale management protocols typically involve the use of chemical inhibitors. Most traditional methods of investigating scale formation and inhibitor performance do not provide insights into the exact mechanisms at play. However, understanding these mechanisms is critical to designing optimal mitigation interventions. We investigate BaSO4 scale formation in flow and batch experiments in the presence of a commercial inhibitor. For the first time, we apply sensitive texture parameters to characterize scale formation in the presence of chemical inhibitors. We analyzed effluent concentrations in the bulk phase using an inductively coupled plasma (ICP) technique, performed high-resolution X-ray CT scans of the surface deposits, and applied scanning electron microscopy (SEM) imaging. We used advanced image analysis to characterize how chemical inhibitors affect the overall deposition rate. We show the impact of time and inhibitor concentrations on corrosion processes.
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Sintoorahat, Patchareeporn, Aree Wairatpanich, Suchada Chimam, Dayin Mongkholkhajornsilp, and Cheolho Kang. "Performance of Corrosion Inhibitors at High CO2 Pressures." In 2008 7th International Pipeline Conference. ASMEDC, 2008. http://dx.doi.org/10.1115/ipc2008-64114.

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The objective of this study was to evaluate the performance of two corrosion inhibitors (CI-A and CI-B) under conditions similar to the second PTT’s offshore pipeline. The experiments were carried out in flow-loop system, 36 m long, 10.16 cm diameter at 10.5 and 14 bar of carbon dioxide pressure, a temperature at 50°C. The performances of corrosion inhibitors were examined under conditions of superficial liquid velocity of 0.03 m/s and gas velocities of 6, 8 and 10 m/s in 0 and 3 degree inclinations using the ER probe and X65 weight-loss coupons for corrosion rate measurement at the top and bottom of pipe. According to flow characteristics, it was found that the smooth and wavy stratified flow occurred in 0 degree. For 3 degree inclination, wavy stratified flow with big waves was dominantly presented for all conditions. Corrosion inhibitor B showed a better performance than inhibitor A in all cases. For inhibitor B, the target corrosion rates of less than 0.1 mm/yr were achieved in all conditions with 50 ppm of inhibitor concentration whereas the amount of 75 ppm inhibitor concentration was required for CI-A. The color, turbidity, and emulsion tendency with corrosion inhibitors will be also discussed in this paper.
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Liu, Ya, Rebecca Vilain, and Dong Shen. "How Does EOR Polymer Impact Scale Control During ASP Flooding?" In SPE International Conference on Oilfield Chemistry. SPE, 2021. http://dx.doi.org/10.2118/204350-ms.

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Abstract Polymer based enhanced oil recovery (EOR) technology has drawn more and more attention in the oil and gas industry. The impacts of EOR polymer on scale formation and control are not well known yet. This research investigated the impacts of EOR polymer on calcite scale formation with and without the presence of scale inhibitors. Seven different types of scale inhibitors were tested, including four different phosphonate inhibitors and three different polymeric inhibitors. Test brines included severe and moderate calcite scaling brines. The severe calcite brine is to simulate alkaline surfactant polymer (ASP) flooding conditions with high pH and high carbonate concentration. The test method used was the 24 hours static bottle test. Visual observation and the residual calcium (Ca2+) concentration determination were conducted after bottle test finished. It was found that EOR polymer can serve as a scale inhibitor in moderate calcite scaling brines, although the required dosage was significantly higher than common scale inhibitors. Strong synergistic effects were observed between EOR polymer and phosphonate scale inhibitors on calcite control, which can significantly reduce scale inhibitor dosage and provides a solution for calcite control in ASP flooding. The impact of EOR polymer on polymeric scale inhibitors varied depending on polymer types. Antagonism was observed between EOR polymer and sulfonated copolymer inhibitor, while there was weak synergism between EOR polymer and acrylic copolymer inhibitors. Therefore, when selecting scale inhibitors for polymer flooding wells in the future, the impact of EOR polymer on scale inhibitor performance should be considered.
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Furmaniak-Kazmierczak, E., J. Jagielski, and T. Wilusz. "THE EFECT OF CMTI-I INHIBITOR ON HUMAN BLOOD CLOTTING SYSTEM." In XIth International Congress on Thrombosis and Haemostasis. Schattauer GmbH, 1987. http://dx.doi.org/10.1055/s-0038-1644327.

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Polipeptyde inhibitors for different serine proteases have been isolated from a variety of plants. Among them there are the inhibitors from squash seeds of molecular weight about 3 300 /1/. The experiments were carried out to determine the effect of one of the squash inhibitors /CMTI-I/ on human blood clotting system. The 0.1 ml of inhibitor /O,8-100 ug/ was added to 0,1 ml of normal intact plasma and incubated 0,5, 15, 30 and 60 minutes at 37°C. It was found that partial tromboplastin time /PTT/ and activated partial thromboplastin time /APTT/ were prolonged. CMTI-I did not show a progressive mode of action upon prolonged time of incubation. There was no effect of CMTI-I on prothrombin time /PT/, thrombin time /TT/ and Stypven-cephalin time /ScT/. The influence of CMTI-I on APTT of factor-XII and factor-XI deficient plasmas as well as on a plasma without factor-XII and factor-XI /exhausted plasma/ was studied. The APTTs of the factor-XII and factor-XI deficient plasmas were prolonged while the APTT of the "exhausted plasma" was unchanged. The performed experiments shown that CMTI-I inhibitor blocks the clot-promoting activity of contact activated plasma. This inhibitory action is stronger in the case of factor XI than of factor XII.1. Wieczorek M., et al., 1985, Biochem. Biophys. Res. Commun. 126:646-652.
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Reports on the topic "Inhibitors"

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Lance, Richard, and Xin Guan. Variation in inhibitor effects on qPCR assays and implications for eDNA surveys. Engineer Research and Development Center (U.S.), August 2021. http://dx.doi.org/10.21079/11681/41740.

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Aquatic environmental DNA (eDNA) surveys are sometimes impacted by polymerase chain reaction (PCR) inhibitors. We tested varying concentrations of different inhibitors (humic, phytic, and tannic acids; crude leaf extracts) for impacts on quantitative PCR (qPCR) assays designed for eDNA surveys of bighead and silver carp (Hypophthalmichthys nobilis and Hypophthalmichthys molitrix). We also tested for inhibition by high concentrations of exogenous DNA, hypothesizing that DNA from increasingly closely related species would be increasingly inhibitory. All tested inhibitors impacted qPCR, though only at very high concentrations — likely a function, in part, of having used an inhibitor-resistant qPCR solution. Closer phylogenetic relatedness resulted in inhibition at lower exogenous DNA concentrations, but not at relatively close phylogenetic scales. Inhibition was also influenced by the qPCR reporter dye used. Importantly, different qPCR assays responded differently to the same inhibitor concentrations. Implications of these results are that the inclusion of more than one assay for the same target taxa in an eDNA survey may be an important countermeasure against false negatives and that internal positive controls may not, in the absence of efforts to maximize inhibition compatibility, provide useful information about the inhibition of an eDNA assay.
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Sisler, Edward C., Raphael Goren, and Akiva Apelbaum. Controlling Ethylene Responses in Horticultural Crops at the Receptor Level. United States Department of Agriculture, October 2001. http://dx.doi.org/10.32747/2001.7580668.bard.

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Ethylene is a plant hormone that controls many plant responses, such as growth, senescence, ripening, abscission and seed germination. Recently, 1-methy- cyclopropene (1-MCP), was shown to bind to ethylene receptor for a certain period of time and prevent ethylene action. The objectives of this research were to synthesize analogues of 1-MCP and test their potency to block the ethylene receptor and inhibit ethylene action. During the course of this project, procedures for synthesis and shipment of the cyclopropene compounds were developed as well assay procedures for each compound were worked out. Thirteen new compounds were synthesized. All of them are structural analogues of 1-MCP, with substitution in the 1-position and a side chain containing 2 to 10 carbons. After preliminary studies, nine promising compounds were selected for in-depth study. The potency of the compounds to inhibit ethylene action was tested on a wide scope of systems like: climacteric fruits (banana, avocado and tomato), the triple response (etiolated peas), and leaf abscission (citrus). As the putative inhibitors are suspected to compete for the site of binding and a competitive type of inhibition could be considered, a high concentration of ethylene (300 m1.L-1) was used to induce ripening and other physiological processes. The tests were conducted under extreme conditions which hasten ripening like treatment and storage at 22 to 25oC. There were fluctuations in the responses as related to the concentrations of the inhibitors. Some required much higher concentration to exert the same effect, while some, when applied at the same concentration, blocked the receptor for a longer period of time than the others. Some fruits and other plant organs responded differently to the same inhibitor, indicating differences in characteristics and availability of the ethylene receptors in the various tissues. The potency of the putative inhibitors was found to be greatly affected by their molecular structural and size. In addition, it was found that treatment with the inhibitor should be given before the onset of ethylene action In the case of fruit, treatment should be carried out before the pre-climacteric stage. Simultaneous treatment with ethylene and the inhibitors reduced the inhibitors' effect. The relationship between ethylene and the inhibitors is of a non-competitive nature. All the fruits treated with the putative inhibitors resumed normal ripening after recovery from the inhibition. This fact is of great importance when considering the inhibitors for practical use. The advantage of using inhibitors of ethylene action over inhibitors of ethylene production lies in the ability of the inhibitors of ethylene action to protect the tissue against both endogenous and exogenous ethylene, thus providing better overall protection. Our findings indicate that 1-MCP and its structural analogues are potent inhibitors of ethylene action capable of providing good protection against endogenous and exogenous ethylene. The fact that the compounds are in a gas phase and are non-phytotoxic, odorless and effective at minute concentrations, renders them promising candidates for commercial use. However, the development of water-soluble inhibitors will expand the potential use of the inhibitors in agriculture.
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Strobl, Jeannine S., and Anna R. Martirosyan. Novel Histone Deacetylase Inhibitors. Fort Belvoir, VA: Defense Technical Information Center, July 2002. http://dx.doi.org/10.21236/ada408095.

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Wild, James R. Detoxification of Acetylcholinesterase Inhibitors. Fort Belvoir, VA: Defense Technical Information Center, February 1987. http://dx.doi.org/10.21236/ada184892.

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Beavers, Gui, and Sridhar. PR-186-073508-R01 Environmental and Stress Factors that Produce SCC in Existing Ethanol Facilities. Chantilly, Virginia: Pipeline Research Council International, Inc. (PRCI), February 2011. http://dx.doi.org/10.55274/r0010441.

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The potential exists for stress corrosion cracking (SCC) of carbon steel pipelines transporting fuel grade ethanol (FGE) and FGE- gasoline blends. The objective of SCC 4-3 Phase 2 was determine if inhibitors are effective in preventing SCC growth under more realistic field conditions than those found in the slow strain rate (SSR) tests performed previously. The results of the research demonstrated that: 1. Un-notched SSR test results generally correlated well with the results of the crack growth tests using precracked CT specimens, although the latter test technique was somewhat more aggressive. 2. The notched SSR test technique was so aggressive that it was not useful for screening SCC inhibitors. 3. E-50, prepared with a simulated FGE was consistently more potent as a cracking agent than SFGE. 4. Some commercial inhibitors were effective in inhibiting ethanol SCC under many of the test conditions. 5. The commercial inhibitors, in general, were less effective in E-50 than in SFGE. 6. Ammonium hydroxide, at a relatively low concentration, was by far the most effective inhibitor evaluated. 7. For one commercial inhibitor, a higher concentration was needed to inhibit SCC in one lot of corn based FGE than in SFGE. 8. Water inhibited, but did not completely arrest, SCC in the crack growth tests in SFGE. 9. Sustained crack growth was observed in SFGE in which no chloride was added. 10. Evidence of loss of inhibition, at low concentrations, was observed in an inhibition scheme for batching of FGE with gasoline in which a high initial dose, followed by a low maintenance dose was used.
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Crocetto, Felice, Carlo Buonerba, Luca Bardi, Antonio Verde, Simone Cilio, Biagio Barone, Gabriele Barbato, et al. Cardiovascular adverse events in patients with kidney cancer receiving combination of angiogenesis inhibitors plus immune checkpoint inhibitors vs. angiogenesis inhibitors vs. immune checkpoint inhibitors: a network analysis of randomized controlled trials. INPLASY - International Platform of Registered Systematic Review and Meta-analysis Protocols, December 2021. http://dx.doi.org/10.37766/inplasy2021.12.0060.

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Luque, Alfonso, and Luisa Iruela-Arispe. Angiogenesis Inhibitors in Breast Cancer. Fort Belvoir, VA: Defense Technical Information Center, April 2005. http://dx.doi.org/10.21236/ada436920.

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Hammond, Scott M. MicroRNA Inhibitors as Anticancer Therapies. Fort Belvoir, VA: Defense Technical Information Center, August 2007. http://dx.doi.org/10.21236/ada475785.

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Sachs, Frederick. The Use of Inhibitors of Mechanosensitive Ion Channels as Local Inhibitors of Peripheral Pain. Fort Belvoir, VA: Defense Technical Information Center, March 2014. http://dx.doi.org/10.21236/ada611580.

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Zheng, Jiaxi, and Haihua Yang. Clinical Benefits of Immune Checkpoint Inhibitors and Predictive Value of Tumor Mutation Burden in Hepatocellular Carcinoma: A Systematic Review and Meta-Analysis. INPLASY - International Platform of Registered Systematic Review and Meta-analysis Protocols, January 2022. http://dx.doi.org/10.37766/inplasy2022.1.0008.

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Abstract:
Review question / Objective: Is immunotherapy associated with beneficial clinical outcomes for hepatocellular carcinoma (HCC) and how can combination immunotherapy be deployed to produce the best benefit? Is tumor mutation burden (TMB) a predictive biomarker for immune‐checkpoint inhibitors? Condition being studied: To this date, about 50 single-arm clinical trials and several randomized control trials (RCTs) presented final or interim results of investigations on the efficacy of PD-1/PD-L1 inhibitors for advanced HCC. In the CheckMate 459, IMbrave 050, and ORIENT-32, immunotherapies were found to significantly improve progression-free survival (PFS) and overall survival (OS) compared with sorafenib (a tyrosine-kinase inhibitor, as standard systemic treatment) in patients with advanced hepatocellular carcinoma. However, these clinical trials were different on clinical phases, sample size, and response evaluation criteria, and inconsistent clinical outcomes were shown in several trials.
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