Literatura científica selecionada sobre o tema "Irreversible inhibitor"
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Artigos de revistas sobre o assunto "Irreversible inhibitor"
Buneeva, O. A., L. N. Aksenova e 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, n.º 1 (2020): e00115. http://dx.doi.org/10.18097/bmcrm00115.
Texto completo da fonteGledhill, L., P. Williams e B. W. Bycroft. "Irreversible inactivation of β-lactamase I from Bacillus cereus by chlorinated 6-spiroepoxypenicillins". Biochemical Journal 276, n.º 3 (15 de junho de 1991): 801–7. http://dx.doi.org/10.1042/bj2760801.
Texto completo da fonteRožman, Kaja, Evan M. Alexander, Eva Ogorevc, Krištof Bozovičar, Izidor Sosič, Courtney C. Aldrich e Stanislav Gobec. "Psoralen Derivatives as Inhibitors of Mycobacterium tuberculosis Proteasome". Molecules 25, n.º 6 (12 de março de 2020): 1305. http://dx.doi.org/10.3390/molecules25061305.
Texto completo da fonteMorgan, 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, n.º 1 (18 de outubro de 2012): 67–72. http://dx.doi.org/10.1042/bj20121014.
Texto completo da fonteVerdugo, Anael, P. K. Vinod, John J. Tyson e Bela Novak. "Molecular mechanisms creating bistable switches at cell cycle transitions". Open Biology 3, n.º 3 (março de 2013): 120179. http://dx.doi.org/10.1098/rsob.120179.
Texto completo da fonteViczjan, 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, n.º 18 (11 de setembro de 2021): 9831. http://dx.doi.org/10.3390/ijms22189831.
Texto completo da fonteKondža, Martin, Mirza Bojić, Ivona Tomić, Željan Maleš, Valentina Rezić e Ivan Ćavar. "Characterization of the CYP3A4 Enzyme Inhibition Potential of Selected Flavonoids". Molecules 26, n.º 10 (19 de maio de 2021): 3018. http://dx.doi.org/10.3390/molecules26103018.
Texto completo da fonteEspín, J. C., e 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, n.º 1 (1 de abril de 1994): 29–35. http://dx.doi.org/10.1042/bj2990029.
Texto completo da fonteBitonti, A. J., P. J. Casara, P. P. McCann e P. Bey. "Catalytic irreversible inhibition of bacterial and plant arginine decarboxylase activities by novel substrate and product analogues". Biochemical Journal 242, n.º 1 (15 de fevereiro de 1987): 69–74. http://dx.doi.org/10.1042/bj2420069.
Texto completo da fonteLiyanage, Piyumi Dinusha, Pabudi Weerathunge, Mandeep Singh, Vipul Bansal e Rajesh Ramanathan. "L-Cysteine as an Irreversible Inhibitor of the Peroxidase-Mimic Catalytic Activity of 2-Dimensional Ni-Based Nanozymes". Nanomaterials 11, n.º 5 (13 de maio de 2021): 1285. http://dx.doi.org/10.3390/nano11051285.
Texto completo da fonteTeses / dissertações sobre o assunto "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/.
Texto completo da fonteSmar, 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.
Texto completo da fonteBorrello, Maria Teresa. "Reversible and irreversible LSD1 inhibitors". Thesis, University of East Anglia, 2016. https://ueaeprints.uea.ac.uk/59682/.
Texto completo da fonteBurger, Alain. "Inhibiteurs irreversibles de la biosynthese de l'ecdysone". Université Louis Pasteur (Strasbourg) (1971-2008), 1988. http://www.theses.fr/1988STR13081.
Texto completo da fonteCoxon, 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.
Texto completo da fonteSnider, 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.
Texto completo da fonteBerabez, 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.
Texto completo da fonteNeurofibromatosis 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.
Texto completo da fonteAcid 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.
Texto completo da fonteÄbelö, 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.
Texto completo da fonteLivros sobre o assunto "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.
Encontre o texto completo da fonteS, Gray Nathanael, Janne Pasi A e Saghatelian Alan, eds. Targeting `Undruggable' Cancer Proteins with Irreversible Small Molecule Inhibitors: Her3 and KRas. 2014.
Encontre o texto completo da fonteLambert, David G. Mechanisms and determinants of anaesthetic drug action. Editado por Michel M. R. F. Struys. Oxford University Press, 2017. http://dx.doi.org/10.1093/med/9780199642045.003.0013.
Texto completo da fonteCapítulos de livros sobre o assunto "Irreversible inhibitor"
Reed, Jessica E., e Jeff B. Smaill. "The Discovery of Dacomitinib, a Potent Irreversible EGFR Inhibitor". In 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.
Texto completo da fonteVerma, Ajit K. "Inhibition of Tumor Promotion by DL-α-Difluoromethylornithine, A Specific Irreversible Inhibitor of Ornithine Decarboxylase". In Antimutagenesis and Anticarcinogenesis Mechanisms II, 195–204. Boston, MA: Springer US, 1990. http://dx.doi.org/10.1007/978-1-4615-9561-8_16.
Texto completo da fonteKeillor, Jeffrey W., Nicolas Chabot, Isabelle Roy, Amina Mulani, Olivier Leogane e Christophe Pardin. "Irreversible Inhibitors of Tissue Transglutaminase". In 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.
Texto completo da fonteEremenko, Arkadiy, Il'ya Kurochkin e Nataliya Nechaeva. "Bioanalytical systems based on cholinesterases for detection of organophosphates". In ORGANOPHOSPHORUS NEUROTOXINS, 205–18. ru: Publishing Center RIOR, 2020. http://dx.doi.org/10.29039/32_205-218.
Texto completo da fonteEremenko, Arkadiy, Il'ya Kurochkin e Nataliya Nechaeva. "Bioanalytical systems based on cholinesterases for detection of organophosphates". In Organophosphorous Neurotoxins, 0. ru: Publishing Center RIOR, 2020. http://dx.doi.org/10.29039/chapter_5e4132b6096d14.18045940.
Texto completo da fonteMohutsky, Michael, e Stephen D. Hall. "Irreversible Enzyme Inhibition Kinetics and Drug–Drug Interactions". In Methods in Molecular Biology, 57–91. Totowa, NJ: Humana Press, 2014. http://dx.doi.org/10.1007/978-1-62703-758-7_5.
Texto completo da fonteMohutsky, Michael, e Stephen D. Hall. "Irreversible Enzyme Inhibition Kinetics and Drug–Drug Interactions". In Methods in Molecular Biology, 51–88. New York, NY: Springer US, 2021. http://dx.doi.org/10.1007/978-1-0716-1554-6_3.
Texto completo da fonteWaring, 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". In Successful Drug Discovery, 341–57. Weinheim, Germany: Wiley-VCH Verlag GmbH & Co. KGaA, 2018. http://dx.doi.org/10.1002/9783527808694.ch12.
Texto completo da fontevan Ommen, Ben, Jan J. P. Bogaards, Jan Peter Ploemen, J. van der Greef e Peter J. van Bladeren. "Quinones and their Glutathione Conjugates as Irreversible Inhibitors of Glutathione S-Transferases". In 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.
Texto completo da fonteMoore, Michael L., Stephen A. Fakhoury, William M. Bryan, Heidemarie G. Bryan, Thaddeus A. Tomaszek, Stephan K. Grant, Thomas D. Meek e William F. Huffman. "Peptidyl epoxides as potent, active site-directed irreversible inhibitors of HIV-1 protease". In Peptides, 781–82. Dordrecht: Springer Netherlands, 1992. http://dx.doi.org/10.1007/978-94-011-2264-1_315.
Texto completo da fonteTrabalhos de conferências sobre o assunto "Irreversible inhibitor"
Visser, A., e D. G. Meuleman. "IRREVERSIBLE INHIBITION OF THE THROMBIN-MEDIATED SIGNAL TRANSFER". In XIth International Congress on Thrombosis and Haemostasis. Schattauer GmbH, 1987. http://dx.doi.org/10.1055/s-0038-1644808.
Texto completo da fonteIwamoto, M., N. Sugiyama, T. Sasaki e Y. Abiko. "DOMAIN OF BINDING ACTIVITY WITH PLASMIN KRINGLE IN SYNTHESIZED C-TERMINAL PEPTIDES , OF α2-PLASMIN INHIBITOR". In XIth International Congress on Thrombosis and Haemostasis. Schattauer GmbH, 1987. http://dx.doi.org/10.1055/s-0038-1644612.
Texto completo da fonteQiao, 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". In 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.
Texto completo da fonteCarrell, R. W., P. D. Christey e 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.
Texto completo da fonteBennett, Ruth, Merel Gijsen e Anthony Kong. "Abstract 1737: Overcoming trastuzumab resistance with the irreversible Pan-HER inhibitor neratinib". In 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.
Texto completo da fonteKaliszczak, Maciej, Meg Perumal e Eric Aboagye. "Abstract 2608: HDAC-C1A: An irreversible HDAC inhibitor with significant anti-tumor activity". In 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.
Texto completo da fonteVenetsanakos, 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". In 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.
Texto completo da fonteSmaill, 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." In 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.
Texto completo da fonteErcan, Dalia, Wenjun Zhou, Masahiko Yanagita, Marzia Capelletti, Andrew Rogers, Yun Xiao, Nathanael S. Gray e Pasi A. Janne. "Abstract 4736: Amplification of ERK2 mediates resistance to the novel irreversible EGFR inhibitor WZ4002". In 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.
Texto completo da fonteHolmes, W. E., H. R. Lijnen e D. Collen. "CHARACTERIZATION OFα2-ANTIPLASMIN.REACTIVE SITE VARIANTS PRODUCED BY SITE-DIRECTED MUTAGENESIS". In XIth International Congress on Thrombosis and Haemostasis. Schattauer GmbH, 1987. http://dx.doi.org/10.1055/s-0038-1644766.
Texto completo da fonteRelatórios de organizações sobre o assunto "Irreversible inhibitor"
Terskikh, Alexey V. Development of Irreversible Inhibitors of MELK Kinase. Fort Belvoir, VA: Defense Technical Information Center, agosto de 2008. http://dx.doi.org/10.21236/ada492687.
Texto completo da fonteOhad, Itzhak, e Himadri Pakrasi. Role of Cytochrome B559 in Photoinhibition. United States Department of Agriculture, dezembro de 1995. http://dx.doi.org/10.32747/1995.7613031.bard.
Texto completo da fonte