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Novel Chemical Scaffolds for Inhibition of Rifamycin-Resistant RNA Polymerase Discovered from High-Throughput Screening.

SLAS discovery : advancing life sciences R & D - 1 Mar 2017

Scharf Nathan T, Molodtsov Vadim, Kontos Arrin, Murakami Katsuhiko S, Garcia George A

Abstract excerpt

Rifampin has been a cornerstone of tuberculosis (TB) treatment since its introduction. The rise of multidrug-resistant and extensively drug-resistant TB makes the development of novel therapeutics effective against these strains an urgent need. Site-specific mutations in the target enzyme of rifampin, RNA polymerase (RNAP) comprises the majority (~97%) of rifamycin-resistant (RifR) strains of Mycobacterium...

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Identifiers

PMID: 28027449
DOI: 10.1177/2472555216679994
PMCID: PMC5323270

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