Drug Discovery Seminar - Robert Abramovitch, PhD

Release Date: Nov 17, 2021
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Inhibitors of the MmpL3 transporter in M. tuberculosis and non-tuberculous mycobacteria

Infections by Mycobacterium tuberculosis (Mtb) and non-tuberculous mycobacteria (NTMs) are challenging to treat and evolving drug resistance. Discovering and developing new drugs with new targets could play an important role in improving treatment outcomes for these diseases. The MmpL3 mycolate transporter is essential for Mtb and NTM survival, making MmpL3 an attractive new drug target. Our team conducted targeted and untargeted whole cell phenotypic screens for inhibitors of Mtb MmpL3. The screens successfully identified over 10 new inhibitors of Mtb MmpL3, several of which are also active against NTMs. Resistant mutants were isolated for several of the inhibitors and identified key domains of the MmpL3 structure associated with differential resistance. Efforts are now underway, including medicinal chemistry, PK and in vivo efficacy studies, to optimize prioritized hits for further development.

Date: Friday, November 19

Time 09:00 AM

Location: IQ Lobby

Zoom: https://msu.zoom.us/j/98508621581

Passcode: 083646

Host: Dr. Edmund Ellsworth (ellswo59@msu.edu)