Mycobacterium Cytidylate Kinase Appears to Be an Undruggable Target.

ABSTRACT: New and improved drugs against tuberculosis are urgently needed as multi-drug-resistant forms of the disease become more prevalent. Mycobacterium tuberculosis cytidylate kinase is an attractive target for screening due to its essentiality and different substrate specificity to the human orthologue. However, we selected the Mycobacterium smegmatis cytidylate kinase for screening because of the availability of high-resolution X-ray crystallographic data defining its structure and the high likelihood of active site structural similarity to the M. tuberculosis orthologue. We report the development and implementation of a high-throughput luciferase-based activity assay and screening of 19,920 compounds derived from small-molecule libraries and an in silico screen predicting likely inhibitors of

SUBMITTER: Craig JK 

PROVIDER: S-EPMC8565994 | biostudies-literature | 2016 Aug

REPOSITORIES: biostudies-literature