Chengdu Easton Biopharmaceuticals Co. Ltd. has synthesized oxalamide derivatives acting as protein arginine N-methyltransferase 5 (PRMT5) inhibitors reported to be useful for the treatment of cancer.
Tumor cells use metabolic reprogramming for their survival and to fuel and boost their proliferation. Only 15% of patients with colorectal cancer (CRC) benefit from immune checkpoint blockade therapy, mainly due to tumor microenvironment changes to promote CD8+ T-cell exhaustion and inactivation allowing tumor cells to escape from immunity.
Transposable elements (TEs) are DNA sequences involved in the epigenetic regulation of tumors. KDM1A is an epigenetic regulator overexpressed in liver cancer that suppresses the methylation of histone H3 Lys4 (H3K4) in liver-TEs and as a result, HNF4A expression is silenced and hepatocellular carcinoma (HCC) growth is promoted.
Mutations in the metabolic enzyme isocitrate dehydrogenase 1 (IDH1) induce tumorigenesis due to generation of the oncometabolite (R)-2-hydroxyglutarate (R-2HG). A hallmark of solid tumors carrying mutations in IDH1 is immune evasion by T-cell exclusion and altered epigenetic state. Researchers from the Center for Cancer Research, Massachusetts General Hospital have published a study in Science on July 12, 2024, in which they demonstrate that inhibiting mutant IDH1 restored antitumoral immunity.
University of Regensburg has described water-soluble FLT3 (FLK2/STK1) inhibitors and their prodrugs reported to be useful for the treatment of acute myeloid leukemia (AML).
Hangzhou Zhongmei Huadong Pharmaceutical Co. Ltd. has synthesized proteolysis targeting chimera (PROTAC) compounds comprising an E3 ubiquitin ligase binding moiety covalently bonded to a GTPase KRAS (G12D mutant) targeting moiety through a linker reported to be useful for the treatment of cancer.
The bromodomain and extraterminal (BET) subfamily contain two similar tandem bromodomains (BD1 and BD2). Selective inhibition of BD2 has been deeply explored; however, the obtention of selective and potent BD1 inhibitors is essential and still lacking.
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