Category: NSCLC

Sotorasib (AMG-510) is an Orally Bioavailable KRAS G12C Covalent Inhibitor

The KRAS oncoprotein is a GTPase and an essential mediator of intracellular signaling pathways. KRAS oncoprotein regulates tumor cell growth and survival. However, KRAS also is the most frequently mutated oncogene in cancer and encodes a key signaling protein in tumors. In addition, KRASG12C mutant is present in approximately...

Talotrexin, A RFC Specific Inhibitor, Targets DHFR to Inhibit Tumor Growth

In this article, we will introduce a potent RFC (reduced folate carrier) specific inhibitor Talotrexin (PT523). Talotrexin, an analog of Aminopterin, is a nonpolyglutamatable classic antifolate. Additionally, it selectively inhibits RFC transport. Mammals cannot synthesize folates de novo, their cellular uptake from the extracellular milieu is essential. Besides, The...

Opnurasib (JDQ-443) is an Orally Active KRAS G12C Inhibitor

Kirsten rat sarcoma (KRAS) is a member of the RAS family. KRAS is a key regulator of signaling pathways responsible for cell proliferation, differentiation, and survival. KRAS mutations are genetic drivers of multiple cancer types, especially colorectal cancer (CRC), pancreatic ductal adenocarcinoma (PDAC), and non-small cell lung cancer (NSCLC)....