Structure of tuberculosis drug target determined

Scientists have determined the three-dimensional structure of the target of the first-line anti-tuberculosis drug rifampin. They have also discovered a new class of potential anti-tuberculosis drugs that kill rifampin-resistant and multi-drug-resistant tuberculosis bacteria. Tuberculosis (TB) bacteria infect a third of the world's population and the disease kills 1.8 million people annually.
In a paper published online in Molecular Cell, scientists report the three-dimensional structures of Mtb RNA polymerase (Mtb RNAP) and Mtb RNAP bound to rifampin. The structures were determined by use of X-ray crystallography and are at a resolution sufficient to define the positions, conformations and interactions of individual amino acid residues of Mtb RNAP. The results reveal the interactions between Mtb RNAP and rifampin, reveal the mechanism by which rifampin inhibits Mtb RNAP, and enable rational, structure-based design of improved rifampin derivatives for inhibition of Mtb RNAP.
Source : www.sciencedaily.com      2017/4/18 08:44

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