Department of Chemistry, Brooklyn College and The Graduate Center of The City University of New York, 2900 Bedford Avenue, Brooklyn, NY 11210, USA.
Chem Commun (Camb). 2013 Dec 25;49(99):11650-2. doi: 10.1039/c3cc47022a.
Peroxidatic activation of the anti-tuberculosis pro-drug isoniazid by Mycobacterium tuberculosis catalase-peroxidase (KatG) is regulated by gating residues of a heme access channel. The steric restriction at the bottleneck of this channel is alleviated by replacement of residue Asp137 with Ser, according to crystallographic and kinetic studies.
分枝杆菌过氧化氢酶-过氧化物酶(KatG)对结核前药异烟肼的过氧活化作用受到血红素进入通道门控残基的调节。根据晶体学和动力学研究,用丝氨酸取代该通道瓶颈处的残基天冬氨酸 137 可以减轻空间位阻。