Genfleet Therapeutics Co. Ltd. has presented preclinical data on their KRAS G12C inhibitor fulzerasib, also known as GFH-925, the third approved KRAS G12C inhibitor for treating non-small-cell lung cancer (NSCLC).
Dysregulation of the polycomb repressive complex 2 (PRC2) is associated with epigenetic silencing of tumor suppressor genes, leading to alterations in cell proliferation, differentiation and survival that contribute to cancer progression.
RAS is the most mutated oncogene in cancer (about 30% rate), where mutations in KRAS are the most prevalent. The approval of covalent KRAS G12C inhibitors has shown allosteric inhibition of KRAS to be a feasible therapeutic strategy, and there is interest in developing new KRAS-directed therapies to target additional KRAS mutants. Amgen has presented data regarding its pan-KRAS inhibitor AMG-410.
Bladder cancer is among the 10 most frequent cancers around the world. While potentially effective treatments exist, they do not benefit all patients, so investigators continue to search for new targets. Researchers at Nanjing Drum Tower Hospital have identified sideroflexin 1 (SFXN1) as a potential therapeutic target.
Esophageal carcinoma (EC) is a tumor type of the digestive tract that accounts for about 300,000 deaths worldwide annually, with high aggressiveness and poor prognosis. Chinese researchers have investigated the implication of the enzyme aldehyde dehydrogenase 18 family member A1 (ALDH18A1) in EC.
Sorafenib is a widely used treatment for hepatocellular carcinoma that has advanced beyond surgical resection, but only 30% of patients respond and many develop resistance within half a year. The resistance has been linked to showing greater ‘stemness’ characteristics of tumor cells, such as activation of signaling pathways mediated by Wnt/b-catenin, Hedgehog and PI3K-Akt.
Researchers at Wenzhou Medical University reported the synthesis and preclinical evaluation of a novel series of betulin-succinate derivatives developed as potential anticancer agents. Betulin is a naturally occurring triterpene that shows significant potential as a lead compound for the development of novel antitumor agents, owing to its selective cytotoxicity against cancer cells and low toxicity toward normal cells.
Mutations in the GTPase KRAS drive proliferation of many types of tumors, and daraxonrasib (RMC-6236), which inhibits various KRAS mutants, can slow growth of pancreatic and lung cancers. Researchers at City University of New York and Weill Cornell Medical College have demonstrated that it also showed effects in osteosarcoma models expressing mutated KRAS.
Researchers from China Pharmaceutical University and collaborators have identified various naphthalene and indane derivatives as selective USP7 inhibitors.
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