Sulfonylurea is a Non-competitive Inhibitor of Acetohydroxyacid Synthase from Mycobacterium tuberculosis
- Title
- Sulfonylurea is a Non-competitive Inhibitor of Acetohydroxyacid Synthase from Mycobacterium tuberculosis
- Author
- 김정림
- Keywords
- acetohydroxyacid synthase; Mycobacterium tuberculosis; inhibition mechanism; sulfonylurea
- Issue Date
- 2006-10
- Publisher
- KOREAN CHEMICAL SOC
- Citation
- BULLETIN OF THE KOREAN CHEMICAL SOCIETY, v. 27, No. 10, Page. 1697-1700
- Abstract
- Acetohydroxyacid synthase (AHAS EC2.2.1.6) catalyses the first step in the biosynthesis of
branched-chain aminoacids (BCAAs). AHAS catalyzes the condensation of two molecules of
pyruvate to form 2-acetolactate in the biosynthasis of valine and leucine or the condensation
of pyruvate and 2-ketobutyrate to form 2-aceto-2-hydroxybutyrate in the biosynthesis of
isoleucine. AHAS consists of two subunits, the catalytic subunits and the regulatory subunits.
The enzymatic activity of AHAS is produced from the catalytic subunit, while the regulatory
subunit affects feedback regulation and activation of the catalytic subunit. AHAS repuires
three cofactors for activity thiamin diphospate (ThDP), divalent metal ion (usually Mg2+),
and flavin adenine dinucleotide(FAD). The first two cofactors are typical for the ThDP-
depenent enzymes in the catalysis. In this study, we observed that inhibition of AHAS from
Mycobacterium tuberculosis by sulfonylurea in non-cpmpetitive. So we can, at least, estimate
that the sulfonylurea can bind to either free enzyme or substrate binding enzyme in the
active site. This approach for understanding the mechanism of inhibition will extend the
possibilities for the design of new inhibitors and the development of new anti-TB drugs.
- URI
- http://www.kci.go.kr/kciportal/ci/sereArticleSearch/ciSereArtiView.kci?sereArticleSearchBean.artiId=ART001028455https://repository.hanyang.ac.kr/handle/20.500.11754/108632
- ISSN
- 0253-2964
- Appears in Collections:
- COLLEGE OF SCIENCE AND CONVERGENCE TECHNOLOGY[E](과학기술융합대학) > CHEMICAL AND MOLECULAR ENGINEERING(화학분자공학과) > Articles
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