About 15% of all cancers have co-deletion of both the MTAP and CDKN2A genes, which results in sensitization to MAT2A inhibitors, thus opening a therapeutic window in these cancer types. MAT2A inhibitors have demonstrated efficacy in MTAD-deficient cancers. Shouyao Holdings (Beijing) Co. Ltd. has developed and released data for their MAT2A inhibitor SY-9453 for the treatment of MTAP-deficient cancers.
Researchers at North China Electric Power University and collaborators have developed novel radiolabels for the membrane-bound monoamine oxidase-B that feature a coumarin core.
Researchers from Fudan University and their collaborators reported the synthesis and preclinical characterization of novel Bruton’s tyrosine kinase (BTK)-targeting proteolysis-targeting chimeras (PROTACs) based on ARQ-531, a potent, reversible, noncovalent BTK inhibitor.