9:27 AM
Jun 12, 2018
 |  BioCentury  |  Emerging Company Profile

A Cancer Target Revolution

How Revolution atypically inhibits SHP-2 and other difficult-to-drug targets for cancer

Revolution Medicines Inc. is developing inhibitors that target non-catalytic sites on proteins to block cell signaling pathways, such as Ras, that drive cancer cell proliferation.

The company’s platform combines synthetic and medicinal chemistry, biochemistry, and structural and computational biology components to design and build complex compounds from chemical fragments. CEO Mark Goldsmith told BioCentury that the use of modular methods allows systematic and repetitive coupling of fragments to build variants of a compound and optimize their biological properties.

According to Goldsmith, the platform enabled the company to focus on atypical sites once considered “undruggable.”

“We’re picking targets that your typical drug discovery company wouldn’t focus on,” he said.

Revolution’s lead candidate, RMC-4630, is an allosteric inhibitor of src homology protein tyrosine phosphatase 2 (SHP-2; SHPTP2; PTPN11), a scaffold protein that functions downstream of multiple receptor tyrosine kinases (RTKs) and upstream of the Ras/MAP kinase (MAPK; ERK) pathway.


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