2NV6

Mycobacterium tuberculosis InhA (S94A) bound with INH-NAD adduct

2NV6 の概要

• エントリーDOI: 10.2210/pdb2nv6/pdb
• 分子名称: Enoyl-[acyl-carrier-protein] reductase [NADH, ISONICOTINIC-ACETYL-NICOTINAMIDE-ADENINE DINUCLEOTIDE (3 entities in total)
• 機能のキーワード: inha, s94a, tuberculosis, isoniazid, oxidoreductase
• 由来する生物種: Mycobacterium tuberculosis
• タンパク質・核酸の鎖数: 1
• 化学式量合計: 29146.08

構造登録者

Wang, F.,Sacchettini, J.C. (登録日: 2006-11-10, 公開日: 2006-11-21, 最終更新日: 2023-08-30)

主引用文献

Vilcheze, C.,Wang, F.,Arai, M.,Hazbon, M.H.,Colangeli, R.,Kremer, L.,Weisbrod, T.R.,Alland, D.,Sacchettini, J.C.,Jacobs Jr., W.R.
Transfer of a point mutation in Mycobacterium tuberculosis inhA resolves the target of isoniazid.
NAT.MED. (N.Y.), 12:1027-1029, 2006

PubMed Abstract: Isoniazid is one of the most effective antituberculosis drugs, yet its precise mechanism of action is still controversial. Using specialized linkage transduction, a single point mutation allele (S94A) within the putative target gene inhA was transferred in Mycobacterium tuberculosis. The inhA(S94A) allele was sufficient to confer clinically relevant levels of resistance to isoniazid killing and inhibition of mycolic acid biosynthesis. This resistance correlated with the decreased binding of the INH-NAD inhibitor to InhA, as shown by enzymatic and X-ray crystallographic analyses, and establishes InhA as the primary target of isoniazid action in M. tuberculosis.

PubMed: 16906155
DOI: 10.1038/nm1466

実験手法

X-RAY DIFFRACTION (1.9 Å)