Tag: KRAS

LY3214996 an Orally Active ERK1/2 Inhibitor with Potential Antineoplastic Activity

The Ras/Raf/MEK/ERK signaling cascade integrates extracellular clues from cell surface receptors to gene expression and regulation of multiple cellular proteins. Extracellular-signal-regulated kinases (ERKs) serve as key central nodes within this pathway. Simultaneous targeting of multiple effectors such as RAF, MEK, and ERK offers the potential for enhanced efficacy while...

BI-2852 is the First Highly Potent KRAS Inhibitor for the SI/II Pocket

The three human RAS genes [KRAS, NRAS and HRAS] encode four RAS proteins, with two KRAS isoforms. The two KRAS isoforms arise from alternative RNA splicing KRAS4A and KRAS4B. The 3 human RAS genes belong to the protein family of small GTPases. GTPases function as binary molecular switches involved...

MRTX-1257 is a KRAS G12C Inhibitor with Antitumor Efficacy

A study from Matthew A. Marx, et al found that, MRTX-1257 is a selective, covalent KRAS G12C inhibitor, with antitumor efficacy. KRAS (K-ras or Ki-ras) is a gene that acts as an on/off switch in cell signaling. During the last several decades, the ability to target and block the...