A. G. Coyne

A Fragment-based approach to assess the ligandability of ArgB, ArgC, ArgD and ArgF in the L-arginine biosynthetic pathway of Mycobacterium tuberculosis.

This study uses a fragment-based approach to assess the ligandability of four enzymes in the L-arginine biosynthesis pathway of M. tuberculosis, identifying potential drug targets.

Chemical validation of Mycobacterium tuberculosis phosphopantetheine adenylyltransferase using fragment linking and CRISPR interference

This study identifies inhibitors of MtbPPAT, a key enzyme in CoA biosynthesis, using fragment linking and CRISPR interference to validate it as a potential anti-TB drug target.

A small-molecule inhibitor of the BRCA2-RAD51 interaction modulates RAD51 assembly and potentiates DNA damage-induced cell death

The paper identifies CAM833, a small-molecule inhibitor of BRCA2-RAD51 interaction, which disrupts RAD51 assembly and enhances DNA damage-induced cell death in BRCA2-wildtype cells.

Using a fragment-based approach to identify novel chemical scaffolds targeting the dihydrofolate reductase (DHFR) from Mycobacterium tuberculosis

This study uses fragment-based drug discovery to identify novel chemical scaffolds targeting Mycobacterium tuberculosis DHFR, revealing a new binding mode and low micromolar affinity compounds.

Inhibiting Mycobacterium tuberculosis CoaBC by targeting a new allosteric site.

The paper identifies potent inhibitors of Mycobacterium tuberculosis CoaB by targeting a novel allosteric site, based on structural and biochemical analyses of CoaBC.

Fragment-based discovery of a new class of inhibitors targeting mycobacterial tRNA modification

This study identifies new TrmD inhibitors for mycobacterial infections using fragment-based drug discovery, showing activity against multiple mycobacterial species in vitro and in macrophage models.