Littérature scientifique sur le sujet « Irreversible inhibitor »
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Articles de revues sur le sujet "Irreversible inhibitor"
Buneeva, O. A., L. N. Aksenova et A. E. Medvedev. « A Simple Approach for Pilot Analysis of Time-dependent Enzyme Inhibition : Discrimination Between Mechanism-based Inactivation and Tight Binding Inhibitor Behavior ». Biomedical Chemistry : Research and Methods 3, no 1 (2020) : e00115. http://dx.doi.org/10.18097/bmcrm00115.
Texte intégralGledhill, L., P. Williams et B. W. Bycroft. « Irreversible inactivation of β-lactamase I from Bacillus cereus by chlorinated 6-spiroepoxypenicillins ». Biochemical Journal 276, no 3 (15 juin 1991) : 801–7. http://dx.doi.org/10.1042/bj2760801.
Texte intégralRožman, Kaja, Evan M. Alexander, Eva Ogorevc, Krištof Bozovičar, Izidor Sosič, Courtney C. Aldrich et Stanislav Gobec. « Psoralen Derivatives as Inhibitors of Mycobacterium tuberculosis Proteasome ». Molecules 25, no 6 (12 mars 2020) : 1305. http://dx.doi.org/10.3390/molecules25061305.
Texte intégralMorgan, Hugh P., Martin J. Walsh, Elizabeth A. Blackburn, Martin A. Wear, Matthew B. Boxer, Min Shen, Henrike Veith et al. « A new family of covalent inhibitors block nucleotide binding to the active site of pyruvate kinase ». Biochemical Journal 448, no 1 (18 octobre 2012) : 67–72. http://dx.doi.org/10.1042/bj20121014.
Texte intégralVerdugo, Anael, P. K. Vinod, John J. Tyson et Bela Novak. « Molecular mechanisms creating bistable switches at cell cycle transitions ». Open Biology 3, no 3 (mars 2013) : 120179. http://dx.doi.org/10.1098/rsob.120179.
Texte intégralViczjan, Gabor, Tamas Erdei, Ignac Ovari, Nora Lampe, Reka Szekeres, Mariann Bombicz, Barbara Takacs et al. « A Body of Circumstantial Evidence for the Irreversible Ectonucleotidase Inhibitory Action of FSCPX, an Agent Known as a Selective Irreversible A1 Adenosine Receptor Antagonist So Far ». International Journal of Molecular Sciences 22, no 18 (11 septembre 2021) : 9831. http://dx.doi.org/10.3390/ijms22189831.
Texte intégralKondža, Martin, Mirza Bojić, Ivona Tomić, Željan Maleš, Valentina Rezić et Ivan Ćavar. « Characterization of the CYP3A4 Enzyme Inhibition Potential of Selected Flavonoids ». Molecules 26, no 10 (19 mai 2021) : 3018. http://dx.doi.org/10.3390/molecules26103018.
Texte intégralEspín, J. C., et J. Tudela. « Experimental approach to the kinetic study of unstable site-directed irreversible inhibitors : kinetic origin of the apparent positive co-operativity arising from inactivation of trypsin by p-amidinophenylmethanesulphonyl fluoride ». Biochemical Journal 299, no 1 (1 avril 1994) : 29–35. http://dx.doi.org/10.1042/bj2990029.
Texte intégralBitonti, A. J., P. J. Casara, P. P. McCann et P. Bey. « Catalytic irreversible inhibition of bacterial and plant arginine decarboxylase activities by novel substrate and product analogues ». Biochemical Journal 242, no 1 (15 février 1987) : 69–74. http://dx.doi.org/10.1042/bj2420069.
Texte intégralLiyanage, Piyumi Dinusha, Pabudi Weerathunge, Mandeep Singh, Vipul Bansal et Rajesh Ramanathan. « L-Cysteine as an Irreversible Inhibitor of the Peroxidase-Mimic Catalytic Activity of 2-Dimensional Ni-Based Nanozymes ». Nanomaterials 11, no 5 (13 mai 2021) : 1285. http://dx.doi.org/10.3390/nano11051285.
Texte intégralThèses sur le sujet "Irreversible inhibitor"
Büchold, Christian. « Synthese und Testung cis-konfigurierter Aziridine als pseudo-irreversible Inhibitoren der sekretorischen Aspartatproteasen von Candida albicans ». kostenfrei, 2009. http://www.opus-bayern.de/uni-wuerzburg/volltexte/2009/3935/.
Texte intégralSmar, Michael William. « Part 1 : Reversible and irreversible inhibitors of aldose reductase as probes of the inhibitor binding site. Part 2 : Synthesis of permanently charged and permanently uncharged dopamine agonists / ». The Ohio State University, 1988. http://rave.ohiolink.edu/etdc/view?acc_num=osu1487597424138323.
Texte intégralBorrello, Maria Teresa. « Reversible and irreversible LSD1 inhibitors ». Thesis, University of East Anglia, 2016. https://ueaeprints.uea.ac.uk/59682/.
Texte intégralBurger, Alain. « Inhibiteurs irreversibles de la biosynthese de l'ecdysone ». Université Louis Pasteur (Strasbourg) (1971-2008), 1988. http://www.theses.fr/1988STR13081.
Texte intégralCoxon, Christopher Robert. « Design and synthesis of irreversible inhibitors of Nek2 kinase ». Thesis, University of Newcastle Upon Tyne, 2010. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.627743.
Texte intégralSnider, Catherine E. « Synthesis and biochemical evaluation of irreversible inhibitors of aromatase / ». The Ohio State University, 1986. http://rave.ohiolink.edu/etdc/view?acc_num=osu1487266362338344.
Texte intégralBerabez, Rayan. « Conception et validation préclinique de nouveaux inhibiteurs de LIMK pour le traitement de la Neurofibromatose de type 1 ». Electronic Thesis or Diss., Orléans, 2023. http://www.theses.fr/2023ORLE1070.
Texte intégralNeurofibromatosis type 1 (NF1) is a genetic disease characterized by the development of cutaneous neurofibromas (cNF) (benign tumors) located at nerve endings. LIM kinases (LIMKs), enzymes responsible for cytoskeleton dynamics, have emerged in recent years as valid therapeutic targets for this disease. These enzymes are overactivated in several pathologies including NF1, glioblastoma or osteosarcoma. A medicinal chemistry project was therefore initiated with the aim of designing new selective inhibitors of LIMKs. Initially, structure-activity relationship (SAR) studies were conducted on the 3 main pharmacomodulation sites of the pyrrolopyrimidine-type compounds previously developed by our team. The development of various synthetic strategies was undertaken, allowing efficient access to a large number of final products (84). Optimization of the aniline portion of the compounds led to the synthesis of 49 LIMKs inhibitors, with inhibition constants lower than 5 nM for several derivatives. Subsequently, an optimized 15 steps synthetic route was developed to replace the previously unchanged central ring 3,6-dihydropyridine with a derivative of 1-aminocyclohex-3-ene-1-carboxylic acid. Finally, a new series of inhibitors was developed by replacing the heterocyclic pyrrolo[2,3-d]pyrimidine base by 7-azaindole derivatives. Improved LIMK vs. ROCK selectivity was observed among the 23 obtained products. Following extensive in vitro evaluation of our best inhibitors on several cell lines, two compounds were selected for in vivo trials on an original mouse model of NF1. In parallel, new modes of LIMKs inhibition were developed with the synthesis of an irreversible inhibitor targeting LIMK1, as well as 4 PROTACs that induced LIMKs degradation through the ubiquitin-proteasome system in several cell lines
Äbelö, Angela. « Pharmacodynamic Modelling of Irreversible and Reversible Gastric Proton Pump Inhibitors ». Doctoral thesis, Uppsala University, Division of Pharmacokinetics and Drug Therapy, 2003. http://urn.kb.se/resolve?urn=urn:nbn:se:uu:diva-3778.
Texte intégralAcid related diseases like GERD, duodenal-and gastric ulcers and H. Pylori-positive peptic ulcer disease are primarily managed by reducing gastric acidity. Irreversible proton pump inhibitors (PPIs) inhibit gastric acid secretion effectively throughout the day by irreversibly inhibiting the gastric proton pump, H+, K+-ATPase, in the parietal cells. Reversible gastric proton pump inhibitors are under development, but have not yet reached clinical use.
The pharmacokinetic/pharmacodynamic (PK/PD) relationships of these compounds are nonlinear, with a delay in the effect-time profile compared to the plasma concentration-time course. PK/PD-modelling was used to characterize and quantify the pharmacological effect with regard to onset, intensity and duration of effect. Models based on functional data, that discriminate between drug-and system-specific parameters, were developed.
In general, the plasma concentration-time course for each individual was approximated by linear interpolation between time-points and served as input into the pharmacodynamic models. A turnover model of irreversible inhibition of gastric acid secretion by omeprazole in the dog described the data well. The model was challenged and found to be robust under different experimental conditions. This model could predict the effect following different exposure of omeprazole and following different histamine provocation. Different fitting approaches (naïve pooling, standard two-stage and nonlinear mixed effects modelling) were compared and resulted in similar parameter estimates. For the reversible inhibitors, a kinetic binding model was finally selected. With a binding model the delay in the effect-time profile is explained by prolonged binding to the enzyme.
Use of these results in drug development can be helpful with regard to selection of drugs for further development and to predict the first clinical dose.
Ekici, Ozlem Dogan. « Design, synthesis, and evaluation of novel irreversible inhibitors for caspases ». Diss., Georgia Institute of Technology, 2003. http://hdl.handle.net/1853/5333.
Texte intégralÄbelö, Angela. « Pharmacodynamic modelling of irreversible and reversible gastric proton pump inhibitors / ». Uppsala : Acta Universitatis Upsaliensis : Univ.-bibl. [distributör], 2003. http://urn.kb.se/resolve?urn=urn:nbn:se:uu:diva-3778.
Texte intégralLivres sur le sujet "Irreversible inhibitor"
Isaacs, Stuart Neal. Premeditated enzyme inactivation : The development of mechanism-based irreversible inhibitors of glyoxalase I as potential anti-cancer agents. [New Haven : s.n.], 1985.
Trouver le texte intégralS, Gray Nathanael, Janne Pasi A et Saghatelian Alan, dir. Targeting `Undruggable' Cancer Proteins with Irreversible Small Molecule Inhibitors : Her3 and KRas. 2014.
Trouver le texte intégralLambert, David G. Mechanisms and determinants of anaesthetic drug action. Sous la direction de Michel M. R. F. Struys. Oxford University Press, 2017. http://dx.doi.org/10.1093/med/9780199642045.003.0013.
Texte intégralChapitres de livres sur le sujet "Irreversible inhibitor"
Reed, Jessica E., et Jeff B. Smaill. « The Discovery of Dacomitinib, a Potent Irreversible EGFR Inhibitor ». Dans Comprehensive Accounts of Pharmaceutical Research and Development : From Discovery to Late-Stage Process Development Volume 1, 207–33. Washington, DC : American Chemical Society, 2016. http://dx.doi.org/10.1021/bk-2016-1239.ch008.
Texte intégralVerma, Ajit K. « Inhibition of Tumor Promotion by DL-α-Difluoromethylornithine, A Specific Irreversible Inhibitor of Ornithine Decarboxylase ». Dans Antimutagenesis and Anticarcinogenesis Mechanisms II, 195–204. Boston, MA : Springer US, 1990. http://dx.doi.org/10.1007/978-1-4615-9561-8_16.
Texte intégralKeillor, Jeffrey W., Nicolas Chabot, Isabelle Roy, Amina Mulani, Olivier Leogane et Christophe Pardin. « Irreversible Inhibitors of Tissue Transglutaminase ». Dans Advances in Enzymology - and Related Areas of Molecular Biology, 415–47. Hoboken, NJ, USA : John Wiley & Sons, Inc., 2011. http://dx.doi.org/10.1002/9781118105771.ch10.
Texte intégralEremenko, Arkadiy, Il'ya Kurochkin et Nataliya Nechaeva. « Bioanalytical systems based on cholinesterases for detection of organophosphates ». Dans ORGANOPHOSPHORUS NEUROTOXINS, 205–18. ru : Publishing Center RIOR, 2020. http://dx.doi.org/10.29039/32_205-218.
Texte intégralEremenko, Arkadiy, Il'ya Kurochkin et Nataliya Nechaeva. « Bioanalytical systems based on cholinesterases for detection of organophosphates ». Dans Organophosphorous Neurotoxins, 0. ru : Publishing Center RIOR, 2020. http://dx.doi.org/10.29039/chapter_5e4132b6096d14.18045940.
Texte intégralMohutsky, Michael, et Stephen D. Hall. « Irreversible Enzyme Inhibition Kinetics and Drug–Drug Interactions ». Dans Methods in Molecular Biology, 57–91. Totowa, NJ : Humana Press, 2014. http://dx.doi.org/10.1007/978-1-62703-758-7_5.
Texte intégralMohutsky, Michael, et Stephen D. Hall. « Irreversible Enzyme Inhibition Kinetics and Drug–Drug Interactions ». Dans Methods in Molecular Biology, 51–88. New York, NY : Springer US, 2021. http://dx.doi.org/10.1007/978-1-0716-1554-6_3.
Texte intégralWaring, Michael J. « The Discovery of Osimertinib (TAGRISSO™) : An Irreversible Inhibitor of Activating and T790M Resistant Forms of the Epidermal Growth Factor Receptor Tyrosine Kinase for the Treatment of Non-Small Cell Lung Cancer ». Dans Successful Drug Discovery, 341–57. Weinheim, Germany : Wiley-VCH Verlag GmbH & Co. KGaA, 2018. http://dx.doi.org/10.1002/9783527808694.ch12.
Texte intégralvan Ommen, Ben, Jan J. P. Bogaards, Jan Peter Ploemen, J. van der Greef et Peter J. van Bladeren. « Quinones and their Glutathione Conjugates as Irreversible Inhibitors of Glutathione S-Transferases ». Dans Advances in Experimental Medicine and Biology, 403–6. Boston, MA : Springer New York, 1991. http://dx.doi.org/10.1007/978-1-4684-5877-0_54.
Texte intégralMoore, Michael L., Stephen A. Fakhoury, William M. Bryan, Heidemarie G. Bryan, Thaddeus A. Tomaszek, Stephan K. Grant, Thomas D. Meek et William F. Huffman. « Peptidyl epoxides as potent, active site-directed irreversible inhibitors of HIV-1 protease ». Dans Peptides, 781–82. Dordrecht : Springer Netherlands, 1992. http://dx.doi.org/10.1007/978-94-011-2264-1_315.
Texte intégralActes de conférences sur le sujet "Irreversible inhibitor"
Visser, A., et D. G. Meuleman. « IRREVERSIBLE INHIBITION OF THE THROMBIN-MEDIATED SIGNAL TRANSFER ». Dans XIth International Congress on Thrombosis and Haemostasis. Schattauer GmbH, 1987. http://dx.doi.org/10.1055/s-0038-1644808.
Texte intégralIwamoto, M., N. Sugiyama, T. Sasaki et Y. Abiko. « DOMAIN OF BINDING ACTIVITY WITH PLASMIN KRINGLE IN SYNTHESIZED C-TERMINAL PEPTIDES , OF α2-PLASMIN INHIBITOR ». Dans XIth International Congress on Thrombosis and Haemostasis. Schattauer GmbH, 1987. http://dx.doi.org/10.1055/s-0038-1644612.
Texte intégralQiao, Lixin, Mariana Nacht, Michael P. Sheets, Thia St Martin, Matthew Labenski, Hormoz Mazdiyasni, Zhendong Zhu et al. « Abstract 4482 : Discovery of an irreversible PI3Kα-specific Inhibitor ». Dans Proceedings : AACR 102nd Annual Meeting 2011‐‐ Apr 2‐6, 2011 ; Orlando, FL. American Association for Cancer Research, 2011. http://dx.doi.org/10.1158/1538-7445.am2011-4482.
Texte intégralCarrell, R. W., P. D. Christey et D. R. Boswell. « SERPINS : ANTITHROMBIN AND OTHER INHIBITORS OF COAGULATION AND FIBRINOLYSIS. EVIDENCE FROM AMINO ACID SEQUENCES ». Dans XIth International Congress on Thrombosis and Haemostasis. Schattauer GmbH, 1987. http://dx.doi.org/10.1055/s-0038-1642896.
Texte intégralBennett, Ruth, Merel Gijsen et Anthony Kong. « Abstract 1737 : Overcoming trastuzumab resistance with the irreversible Pan-HER inhibitor neratinib ». Dans Proceedings : AACR 102nd Annual Meeting 2011‐‐ Apr 2‐6, 2011 ; Orlando, FL. American Association for Cancer Research, 2011. http://dx.doi.org/10.1158/1538-7445.am2011-1737.
Texte intégralKaliszczak, Maciej, Meg Perumal et Eric Aboagye. « Abstract 2608 : HDAC-C1A : An irreversible HDAC inhibitor with significant anti-tumor activity ». Dans Proceedings : AACR 102nd Annual Meeting 2011‐‐ Apr 2‐6, 2011 ; Orlando, FL. American Association for Cancer Research, 2011. http://dx.doi.org/10.1158/1538-7445.am2011-2608.
Texte intégralVenetsanakos, Eleni, Yan Xing, Natalie Loewenstein, J. Michael Bradshaw, Dane Karr, Jacob LaStant, Philip Nunn et al. « Abstract 2091 : PRN1371, an irreversible, covalent inhibitor of FGFR1-4 exhibits sustained pathway inhibition in cancer cell lines ». Dans Proceedings : AACR Annual Meeting 2017 ; April 1-5, 2017 ; Washington, DC. American Association for Cancer Research, 2017. http://dx.doi.org/10.1158/1538-7445.am2017-2091.
Texte intégralSmaill, Jeff B., Jagdish Jaiswal, Maria Abbattista, Guo-Liang Lu, Robert F. Anderson, Amir Ashoorzadeh, William A. Denny et al. « Abstract A247 : Mechanism of action of the hypoxia-activated irreversible pan-HER inhibitor SN29966. » Dans Abstracts : AACR-NCI-EORTC International Conference : Molecular Targets and Cancer Therapeutics--Nov 12-16, 2011 ; San Francisco, CA. American Association for Cancer Research, 2011. http://dx.doi.org/10.1158/1535-7163.targ-11-a247.
Texte intégralErcan, Dalia, Wenjun Zhou, Masahiko Yanagita, Marzia Capelletti, Andrew Rogers, Yun Xiao, Nathanael S. Gray et Pasi A. Janne. « Abstract 4736 : Amplification of ERK2 mediates resistance to the novel irreversible EGFR inhibitor WZ4002 ». Dans Proceedings : AACR 102nd Annual Meeting 2011‐‐ Apr 2‐6, 2011 ; Orlando, FL. American Association for Cancer Research, 2011. http://dx.doi.org/10.1158/1538-7445.am2011-4736.
Texte intégralHolmes, W. E., H. R. Lijnen et D. Collen. « CHARACTERIZATION OFα2-ANTIPLASMIN.REACTIVE SITE VARIANTS PRODUCED BY SITE-DIRECTED MUTAGENESIS ». Dans XIth International Congress on Thrombosis and Haemostasis. Schattauer GmbH, 1987. http://dx.doi.org/10.1055/s-0038-1644766.
Texte intégralRapports d'organisations sur le sujet "Irreversible inhibitor"
Terskikh, Alexey V. Development of Irreversible Inhibitors of MELK Kinase. Fort Belvoir, VA : Defense Technical Information Center, août 2008. http://dx.doi.org/10.21236/ada492687.
Texte intégralOhad, Itzhak, et Himadri Pakrasi. Role of Cytochrome B559 in Photoinhibition. United States Department of Agriculture, décembre 1995. http://dx.doi.org/10.32747/1995.7613031.bard.
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