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...
FGTI-2734, a Dual FTase and GGTase Inhibitor, Has Potential to Treat KRAS-mutant Cancer
The KRAS gene belongs to a class of genes known as oncogenes. When mutated, oncogenes have the potential to cause normal cells to become cancerous. The KRAS gene is in the Ras family of oncogenes, which also includes two other genes: HRAS and NRAS. These proteins play important roles...
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...