Article
Discovery of Novel Coumarin-quinolinium Derivatives as Pan-KRAS Translation Inhibitors by Targeting 5'-UTR RNA G-Quadruplexes.
Journal of medicinal chemistry - 8 Feb 2024
Li Mao-Lin, Dai Le-Tian, Gao Zhuo-Yu, Yan Jia-Tong, Xu Shu-Min, Tan Jia-Heng, Huang Zhi-Shu, Chen Shuo-Bin, Chen Xiu-Cai
Abstract excerpt
Hyperactivated KRAS mutations fuel tumorigenesis and represent attractive targets for cancer treatment. While covalent inhibitors have shown clinical benefits against the KRASG12C mutant, advancements for non-G12C mutants remain limited, highlighting the urgent demand for pan-KRAS inhibitors. RNA G-quadruplexes (rG4s) in the 5'-untranslated region of KRAS mRNA can regulate KRAS translation, making them promising...
Read the complete abstract on PubMedTopics
Share this publication in a Topic to start or enrich a Post.
