T. L. Blundell

Selective inhibitors of the Aurora A-TPX2 protein-protein interaction exhibit in vivo efficacy as targeted anti-mitotic agents

The paper develops selective Aurora A-TPX2 inhibitors that show in vivo efficacy and synergy with paclitaxel in pancreatic cancer.

Mutational spectra analysis reveals bacterial niche and transmission routes

The paper analyzes mutational spectra in bacterial lineages to infer niche-specific mutagen exposure and transmission routes.

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.

Mycobacterial OtsA structures unveil substrate preference mechanism and allosteric regulation by 2-oxoglutarate and 2-phosphoglycerate

The paper reports the first mycobacterial OtsA structures from M. thermoresistibile, revealing substrate preference mechanism and allosteric regulation by 2-oxoglutarate and 2-phosphoglycerate.

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.