An article Pyrazinamide triggers degradation of its target aspartate decarboxylase WOS:000564272800001 published article about TUBERCULOSIS; RESISTANCE; MUTATIONS; PROTEASE; COMPLEX in [Gopal, Pooja; Sarathy, Jickky Palmae] Natl Univ Singapore, Yong Loo Lin Sch Med, Dept Med, Singapore, Singapore; [Yee, Michelle; Dick, Thomas] Natl Univ Singapore, Yong Loo Lin Sch Med, Dept Microbiol & Immunol, Singapore, Singapore; [Ragunathan, Priya; Shin, Joon; Bhushan, Shashi; Grueber, Gerhard] Nanyang Technol Univ, Sch Biol Sci, Singapore, Singapore; [Zhu, Junhao; Akopian, Tatos; Kandror, Olga; Rubin, Eric J.] Harvard Univ, Harvard TH Chan Sch Publ Hlth, Dept Immunol & Infect Dis, Boston, MA 02115 USA; [Lim, Teck Kwang; Lin, Qingsong] Natl Univ Singapore, Dept Biol Sci, Singapore, Singapore; [Gengenbacher, Martin; Dick, Thomas] Hackensack Meridian Hlth, Ctr Discovery & Innovat, Nutley, NJ 07110 USA; [Gengenbacher, Martin; Dick, Thomas] Seton Hall Univ, Dept Med Sci, Hackensack Meridian Med Sch, Nutley, NJ 07110 USA; [Gopal, Pooja] Merck Res Labs, MSD Translat Med Res Ctr, Singapore, Singapore in 2020, Cited 29. The Name is Pyrazine-2-carboxylic acid. Through research, I have a further understanding and discovery of 98-97-5. Recommanded Product: 98-97-5
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.
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Reference:
Patent; Chevron Research Company; US4732894; (1988); A;,
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