Category: Pyrazines. Recently I am researching about TUBERCULOSIS; RESISTANCE; MUTATIONS; PROTEASE; COMPLEX, Saw an article supported by the Singapore Ministry of Health’s National Medical Research CouncilNational Medical Research Council, Singapore [NMRC/TCR/011-NUHS/2014, NMRC/CG/013/2013]; Yong Loo Lin School of Medicine graduate scholarship; National Institute of Allergy and Infectious Diseases of the National Institutes of HealthUnited States Department of Health & Human ServicesNational Institutes of Health (NIH) – USANIH National Institute of Allergy & Infectious Diseases (NIAID) [2R01AI10639805, P01AI095208]; Bill and Melinda Gates FoundationBill & Melinda Gates Foundation [OPP1181211]; National Research Foundation (NRF) SingaporeNational Research Foundation, Singapore [NRF-CRP18-2017-01]. Published in NATURE PUBLISHING GROUP in LONDON ,Authors: Gopal, P; Sarathy, JP; Yee, M; Ragunathan, P; Shin, J; Bhushan, S; Zhu, JH; Akopian, T; Kandror, O; Lim, TK; Gengenbacher, M; Lin, QS; Rubin, EJ; Gruber, G; Dick, T. The CAS is 98-97-5. Through research, I have a further understanding and discovery of Pyrazine-2-carboxylic acid
Pyrazinamide is a sterilizing first-line tuberculosis drug. Genetic, metabolomic and biophysical analyses previously demonstrated that pyrazinoic acid, the bioactive form of the prodrug pyrazinamide (PZA), interrupts biosynthesis of coenzyme A in Mycobacterium tuberculosis by binding to aspartate decarboxylase PanD. While most drugs act by inhibiting protein function upon target binding, we find here that pyrazinoic acid is only a weak enzyme inhibitor. We show that binding of pyrazinoic acid to PanD triggers degradation of the protein by the caseinolytic protease ClpC1-ClpP. Thus, the old tuberculosis drug pyrazinamide exerts anti-bacterial activity by acting as a target degrader, a mechanism of action that has recently emerged as a successful strategy in drug discovery across disease indications. Our findings provide the basis for the rational discovery of next generation PZA.
Category: Pyrazines. Welcome to talk about 98-97-5, If you have any questions, you can contact Gopal, P; Sarathy, JP; Yee, M; Ragunathan, P; Shin, J; Bhushan, S; Zhu, JH; Akopian, T; Kandror, O; Lim, TK; Gengenbacher, M; Lin, QS; Rubin, EJ; Gruber, G; Dick, T or send Email.
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Patent; Chevron Research Company; US4732894; (1988); A;,
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