NIH R01 · 2025
Repurposing human kinase inhibitor chemotypes for Neglected Tropical Diseases
SUMMARY/ABSTRACT Human African trypanosomiasis (HAT) and Chagas disease (CD) are neglected tropical diseases (NTDs). Current drugs show increasing numbers of treatment failure, low efficacy, difficult treatment regimens or severe side effects. In a unique industrial-academic collaboration, the PIs, in collaboration with GSK, ran a high-throughput screen (HTS) of ~46,000 kinase-targeted inhibitors against Trypanosoma brucei, the causative agent of HAT. This resulted in the discovery of 797 potent (T brucei EC50<1 μM; pEC50 6) and selective hits (>100-fold over HepG2 cells) that were sorted into 59 structural clusters, plus 53 singletons. 14 chemotypes including 13 clusters and 1 singleton…
From the public funding record at NIH RePORTER. Describes the funded project, not the reviews below.