Department of Pharmacoinformatics, National Institute of Pharmaceutical Education and Research (NIPER)-Kolkata, Chunilal Bhawan, 168 Maniktala Main Road, Kolkata, West Bengal, 700054, India.
Mol Divers. 2022 Oct;26(5):2949-2965. doi: 10.1007/s11030-021-10335-y. Epub 2021 Nov 11.
The terminal oxidases of the oxidative phosphorylation pathway play a significant role in the survival and growth of M. tuberculosis, targeting these components lead to inhibition of M. tuberculosis. Many drug candidates targeting various components of the electron transport chain in M. tuberculosis have recently been discovered. The cytochrome bc-aa supercomplex is one of the most important components of the electron transport chain in M. tuberculosis, and it has emerged as the novel target for several promising candidates. There are two cryo-electron microscopy structures (PDB IDs: 6ADQ and 6HWH) of the cytochrome bc-aa supercomplex that aid in the development of effective and potent inhibitors for M. tuberculosis. In recent years, a number of potential candidates targeting the QcrB subunit of the cytochrome bc complex have been developed. In this review, we describe the recently identified inhibitors that target the electron transport chain's terminal oxidase enzyme in M. tuberculosis, specifically the QcrB subunit of the cytochrome bc complex.
氧化磷酸化途径的末端氧化酶在结核分枝杆菌的存活和生长中起着重要作用，针对这些成分的药物会抑制结核分枝杆菌。最近发现了许多针对结核分枝杆菌电子传递链中各种成分的药物候选物。细胞色素 bc-aa 超复合体是结核分枝杆菌电子传递链的最重要组成部分之一，它已成为几种有前途的候选物的新靶标。有两个细胞色素 bc-aa 超复合体的低温电子显微镜结构（PDB ID：6ADQ 和 6HWH），有助于开发针对结核分枝杆菌的有效和强效抑制剂。近年来，已经开发出许多针对细胞色素 bc 复合物的 QcrB 亚基的潜在候选物。在这篇综述中，我们描述了最近发现的针对结核分枝杆菌电子传递链末端氧化酶的抑制剂，特别是细胞色素 bc 复合物的 QcrB 亚基。
