Zobrazeno 1 - 10
of 71
pro vyhledávání: '"Petr Kuzmic"'
Autor:
Deviprasad R. Gollapalli, Gregory D. Cuny, Adhar C. Manna, Natalia Maltseva, Barry B. Snider, Yubo Zhang, Mohana Rao Vippila, Ann P. Lawson, Lizbeth Hedstrom, Minjia Zhang, Youngchang Kim, David M Rothstein, Shibin Chacko, Petr Kuzmic, Xingyou Wang, Andrzej Joachimiak, Ryan T Cullinane, Gyan Modi, Gary M Marqus, Ambrose L. Cheung, Judy L.M. Kotler
Publikováno v:
ACS Infectious Diseases. 7:3062-3076
Many bacterial pathogens, including Staphylococcus aureus, require inosine 5'-monophosphate dehydrogenase (IMPDH) for infection, making this enzyme a promising new target for antibiotics. Although potent selective inhibitors of bacterial IMPDHs have
Autor:
Petr Kuzmic
The mathematics and geometry of the "kobs" method under the tight-binding experimental conditions, when inhibitor depletion is significant, has not been fully explored in the existing biochemical kinetic literature. It is shown here that under tight-
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1d2f3d8215580e0435949b93e6ba0681
https://doi.org/10.26434/chemrxiv-2022-n3z0m-v2
https://doi.org/10.26434/chemrxiv-2022-n3z0m-v2
Autor:
Gyan, Modi, Gary M, Marqus, Mohana Rao, Vippila, Deviprasad R, Gollapalli, Youngchang, Kim, Adhar C, Manna, Shibin, Chacko, Natalia, Maltseva, Xingyou, Wang, Ryan T, Cullinane, Yubo, Zhang, Judy L M, Kotler, Petr, Kuzmic, Minjia, Zhang, Ann P, Lawson, Andrzej, Joachimiak, Ambrose, Cheung, Barry B, Snider, David M, Rothstein, Gregory D, Cuny, Lizbeth, Hedstrom
Publikováno v:
ACS Infect Dis
Many bacterial pathogens, including Staphylococcus aureus, require inosine 5’-monophosphate dehydrogenase (IMPDH) for infection, making this enzyme a promising new target for antibiotics. Although potent selective inhibitors of bacterial IMPDHs hav
Publikováno v:
The FASEB Journal. 35
Autor:
Petr Kuzmic
Covalent (irreversible) enzyme inhibitors are an important group of actual or potential therapeutics. For example, Aspirin is an irreversible inhibitor of the cyclooxygenase enzyme. Evaluating covalent inhibitors in the drug discovery is exceptionall
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::6e14148c2f012b67dde4ea89a2b6d6a9
https://doi.org/10.26434/chemrxiv.12407105
https://doi.org/10.26434/chemrxiv.12407105
Autor:
Petr Kuzmic
Irreversible (covalent) enzyme inhibitors cannot be unambiguously ranked for biochemical potency by using IC50 values determined at a single point in time, because the same IC50 value could originate either from relatively low initial binding affinit
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::9dbb86aa6a5d7343adf1fd948cb78cc6
https://doi.org/10.1101/2020.06.25.171207
https://doi.org/10.1101/2020.06.25.171207
Autor:
Petr Kuzmic
This report describes an algebraic equation for the time course of irreversible enzyme inhibition following a two-step mechanism. In the first step, the enzyme and the inhibitor associate reversibly to form a non-covalent complex. In the second step,
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::3e5c9677bb1708eddf97aaeee017bc4e
https://doi.org/10.1101/2020.06.10.144220
https://doi.org/10.1101/2020.06.10.144220
Autor:
Petr Kuzmic
This report describes an algebraic formula to calculate the optimal duration of the pre-incubation phase in enzyme-inhibition experiments, based on the assumed range of expected values for the dissociation equilibrium constant of the enzyme–inhibit
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::78dabad2d46b0feeb9923f0849ce8fd3
https://doi.org/10.26434/chemrxiv.12016974
https://doi.org/10.26434/chemrxiv.12016974
Autor:
Petr Kuzmic, Mey Ling Reytor González, Lizbeth Hedstrom, Maday Alonso-del-Rivero Antigua, José R. Pires
Publikováno v:
Biochimie. 150:37-47
Multi-domain inhibitors capable to block the activity of different classes of proteases are not very common in nature. However, these kinds of molecules are attractive systems for biomedical or biotechnological applications, where two or more differe
Autor:
Brandon A. Wright, Samuel Carlson, Elizabeth May, Vincent Chu, Petr Kuzmic, Shilpa Rani, Joseph D. Panarese, Rachelle Gaudet, Matthew D. Shair, Sreekanth Dittakavi, Danny T. C. Huang, Rocco L. Policarpo, Saravanakumar Dhakshinamoorthy, Aimo Kannt, Ludovic Decultot
Publikováno v:
J Med Chem
In this work, structure-based rational design led to the development of potent and selective alkynyl bisubstrate inhibitors of NNMT. The reported nicotinamide-SAM conjugate (named NS1) features an alkyne as a key design element that closely mimics th
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::4a04d8b7ae89b4cb800493a0e4df32f6
https://europepmc.org/articles/PMC7955893/
https://europepmc.org/articles/PMC7955893/