Auswahl der wissenschaftlichen Literatur zum Thema „Irreversible inhibitor“
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Zeitschriftenartikel zum Thema "Irreversible inhibitor"
Buneeva, O. A., L. N. Aksenova und 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, Nr. 1 (2020): e00115. http://dx.doi.org/10.18097/bmcrm00115.
Der volle Inhalt der QuelleGledhill, L., P. Williams und B. W. Bycroft. „Irreversible inactivation of β-lactamase I from Bacillus cereus by chlorinated 6-spiroepoxypenicillins“. Biochemical Journal 276, Nr. 3 (15.06.1991): 801–7. http://dx.doi.org/10.1042/bj2760801.
Der volle Inhalt der QuelleRožman, Kaja, Evan M. Alexander, Eva Ogorevc, Krištof Bozovičar, Izidor Sosič, Courtney C. Aldrich und Stanislav Gobec. „Psoralen Derivatives as Inhibitors of Mycobacterium tuberculosis Proteasome“. Molecules 25, Nr. 6 (12.03.2020): 1305. http://dx.doi.org/10.3390/molecules25061305.
Der volle Inhalt der QuelleMorgan, 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, Nr. 1 (18.10.2012): 67–72. http://dx.doi.org/10.1042/bj20121014.
Der volle Inhalt der QuelleVerdugo, Anael, P. K. Vinod, John J. Tyson und Bela Novak. „Molecular mechanisms creating bistable switches at cell cycle transitions“. Open Biology 3, Nr. 3 (März 2013): 120179. http://dx.doi.org/10.1098/rsob.120179.
Der volle Inhalt der QuelleViczjan, 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, Nr. 18 (11.09.2021): 9831. http://dx.doi.org/10.3390/ijms22189831.
Der volle Inhalt der QuelleKondža, Martin, Mirza Bojić, Ivona Tomić, Željan Maleš, Valentina Rezić und Ivan Ćavar. „Characterization of the CYP3A4 Enzyme Inhibition Potential of Selected Flavonoids“. Molecules 26, Nr. 10 (19.05.2021): 3018. http://dx.doi.org/10.3390/molecules26103018.
Der volle Inhalt der QuelleEspín, J. C., und 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, Nr. 1 (01.04.1994): 29–35. http://dx.doi.org/10.1042/bj2990029.
Der volle Inhalt der QuelleBitonti, A. J., P. J. Casara, P. P. McCann und P. Bey. „Catalytic irreversible inhibition of bacterial and plant arginine decarboxylase activities by novel substrate and product analogues“. Biochemical Journal 242, Nr. 1 (15.02.1987): 69–74. http://dx.doi.org/10.1042/bj2420069.
Der volle Inhalt der QuelleLiyanage, Piyumi Dinusha, Pabudi Weerathunge, Mandeep Singh, Vipul Bansal und Rajesh Ramanathan. „L-Cysteine as an Irreversible Inhibitor of the Peroxidase-Mimic Catalytic Activity of 2-Dimensional Ni-Based Nanozymes“. Nanomaterials 11, Nr. 5 (13.05.2021): 1285. http://dx.doi.org/10.3390/nano11051285.
Der volle Inhalt der QuelleDissertationen zum Thema "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/.
Der volle Inhalt der QuelleSmar, 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.
Der volle Inhalt der QuelleBorrello, Maria Teresa. „Reversible and irreversible LSD1 inhibitors“. Thesis, University of East Anglia, 2016. https://ueaeprints.uea.ac.uk/59682/.
Der volle Inhalt der QuelleBurger, Alain. „Inhibiteurs irreversibles de la biosynthese de l'ecdysone“. Université Louis Pasteur (Strasbourg) (1971-2008), 1988. http://www.theses.fr/1988STR13081.
Der volle Inhalt der QuelleCoxon, 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.
Der volle Inhalt der QuelleSnider, 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.
Der volle Inhalt der QuelleBerabez, 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.
Der volle Inhalt der QuelleNeurofibromatosis 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.
Der volle Inhalt der QuelleAcid 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.
Der volle Inhalt der QuelleÄbelö, 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.
Der volle Inhalt der QuelleBücher zum Thema "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.
Den vollen Inhalt der Quelle findenS, Gray Nathanael, Janne Pasi A und Saghatelian Alan, Hrsg. Targeting `Undruggable' Cancer Proteins with Irreversible Small Molecule Inhibitors: Her3 and KRas. 2014.
Den vollen Inhalt der Quelle findenLambert, David G. Mechanisms and determinants of anaesthetic drug action. Herausgegeben von Michel M. R. F. Struys. Oxford University Press, 2017. http://dx.doi.org/10.1093/med/9780199642045.003.0013.
Der volle Inhalt der QuelleBuchteile zum Thema "Irreversible inhibitor"
Reed, Jessica E., und 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.
Der volle Inhalt der QuelleVerma, 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.
Der volle Inhalt der QuelleKeillor, Jeffrey W., Nicolas Chabot, Isabelle Roy, Amina Mulani, Olivier Leogane und 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.
Der volle Inhalt der QuelleEremenko, Arkadiy, Il'ya Kurochkin und 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.
Der volle Inhalt der QuelleEremenko, Arkadiy, Il'ya Kurochkin und 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.
Der volle Inhalt der QuelleMohutsky, Michael, und 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.
Der volle Inhalt der QuelleMohutsky, Michael, und 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.
Der volle Inhalt der QuelleWaring, 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.
Der volle Inhalt der Quellevan Ommen, Ben, Jan J. P. Bogaards, Jan Peter Ploemen, J. van der Greef und 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.
Der volle Inhalt der QuelleMoore, Michael L., Stephen A. Fakhoury, William M. Bryan, Heidemarie G. Bryan, Thaddeus A. Tomaszek, Stephan K. Grant, Thomas D. Meek und 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.
Der volle Inhalt der QuelleKonferenzberichte zum Thema "Irreversible inhibitor"
Visser, A., und 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.
Der volle Inhalt der QuelleIwamoto, M., N. Sugiyama, T. Sasaki und 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.
Der volle Inhalt der QuelleQiao, 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.
Der volle Inhalt der QuelleCarrell, R. W., P. D. Christey und 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.
Der volle Inhalt der QuelleBennett, Ruth, Merel Gijsen und 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.
Der volle Inhalt der QuelleKaliszczak, Maciej, Meg Perumal und 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.
Der volle Inhalt der QuelleVenetsanakos, 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.
Der volle Inhalt der QuelleSmaill, 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.
Der volle Inhalt der QuelleErcan, Dalia, Wenjun Zhou, Masahiko Yanagita, Marzia Capelletti, Andrew Rogers, Yun Xiao, Nathanael S. Gray und 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.
Der volle Inhalt der QuelleHolmes, W. E., H. R. Lijnen und 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.
Der volle Inhalt der QuelleBerichte der Organisationen zum Thema "Irreversible inhibitor"
Terskikh, Alexey V. Development of Irreversible Inhibitors of MELK Kinase. Fort Belvoir, VA: Defense Technical Information Center, August 2008. http://dx.doi.org/10.21236/ada492687.
Der volle Inhalt der QuelleOhad, Itzhak, und Himadri Pakrasi. Role of Cytochrome B559 in Photoinhibition. United States Department of Agriculture, Dezember 1995. http://dx.doi.org/10.32747/1995.7613031.bard.
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