KRAS Oncogene Inhibitor
JHU Ref #: C16567
Value Proposition
· KRAS oncogene function inhibitor
· 24 amino acid peptide synthesized from KRAS4B structure
· Enables development of KRAS-driven cancer therapeutics
Unmet Need
KRAS is an oncoprotein involved in cell division regulation with gene mutations leading to cellular transformations and increased resistance to chemotherapy and therapies targeting epidermal growth factor receptors. Alterations in the KRAS coding region are among the most frequent gain-of-function mutations in patients with cancer. The oncogenic form of KRAS is found in >80% of pancreatic carcinomas, 40-50% of colon carcinomas, and 30-50% of lung carcinomas (Jancik). Current drugs are specific to KRAS G12C mutants and have structural limitations. Thus, the development of a drug for the global inhibition of KRAS function is necessary for targeting KRAS-driven cancers.
Technology Description
KRAS belongs to the RAS superfamily of GTP-binding proteins. KRAS has two variants: KRAS4A and KRAS4B, with KRAS4B being the dominant and highly expressed form. JHU researchers have found a 24 amino acid peptide from the C-terminal region of KRAS4B able to inhibit its function. The researchers used their peptide in a dose-dependent manner to test its effect on KRAS4B and RHOA (another GTPase) interactions in vitro.
Stage of Development
· In vitro studies have been published.
Data Availability
· Data available at below publication.
Publication
https://doi.org/10.1016/j.molcel.2021.09.001
