NIH R01 · 2024
Molecular Glues to Target RAS-MAPK Driven Cancers
SUMMARY We seek to develop a new class of drugs for RAS-MAPK driven cancers by targeting the interfacial binding sites of key regulatory complexes within the cascade. By moving away from conventional active site-based drugs, we have the potential for a unique class of compounds with advantages in terms of selectivity, target engagement, therapeutic index, and combinatorial activity to mitigate the emergence of drug resistance. The MAPK/ERK Kinase (MEK) MEK is a shared effector of KRAS and BRAF, which are among the most frequently mutated oncogenes and protein kinases across all human cancers. As such, MEK has long been pursued as a drug target in oncology, and more recently in immunotherapy…
From the public funding record at NIH RePORTER. Describes the funded project, not the reviews below.