期刊
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
卷 222, 期 -, 页码 -出版社
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2021.113568
关键词
Tuberculosis; MDR-TB; XDR-TB; Mur ligase
资金
- Indian Council of Medical Research (ICMR), New Delhi, Govt. of India [ISRM/12(11)/2019]
Tuberculosis transmitted by Mycobacterium tuberculosis is a global concern, with drug resistance posing a significant challenge. Targeting the Mtb cell wall peptidoglycan synthesis is an attractive strategy to combat drug resistance, with Mur enzymes serving as potential targets.
Tuberculosis: (TB) transmitted by Mycobacterium tuberculosis (Mtb) is one of the top 10 causes of death globally. Currently, the widespread occurrence of resistance toward Mtb strains is becoming a significant concern to public health. This scenario exaggerated the need for the discovery of novel targets and their inhibitors. Targeting the Mtb cell wall peptidoglycan synthesis is an attractive strategy to overcome drug resistance. Mur enzymes (MurA-MurF) play essential roles in the peptidoglycan synthesis by catalyzing the ligation of key amino acid residues to the stem peptide. These enzymes are unique and confined to the eubacteria and are absent in humans, representing potential targets for anti-tubercular drug discovery. Mtb Mur ligases with the same catalytic mechanism share conserved amino acid regions and structural features that can conceivably exploit for the designing of the inhibitors, which can simultaneously target more than one isoforms (MurC-MurF) of the enzyme. In light of these findings in the current review, we have discussed the recent advances in medicinal chemistry of Mtb Mur enzymes (MurA-MurF) and their inhibitors, offering attractive multi-targeted strategies to combat the problem of drug-resistant in M. tuberculosis. (C) 2021 Elsevier Masson SAS. All rights reserved.
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