Type I protein arginine methyltransferases (PRMTs) are an attractive target for inhibiting growth of triple-negative breast cancer. Several small-molecule inhibitors of these enzymes are in various stages of preclinical development, while clinical trials of the inhibitor GSK-3368715 had to be terminated early because of poor efficacy and toxicity.
The inhibition of PD-L1 and VEGF individually or in combination has shown efficacy across several solid tumor types, but not all patients respond to therapy or respond for short duration. IMM-2510 is a novel bispecific antibody developed by Immuneonco Biopharmaceuticals Inc. that targets both PD-L1 and VEGF, thus achieving both angiogenesis inhibition and immune checkpoint blockade.
Researchers from Tango Therapeutics Inc. presented preclinical efficacy data on TNG-260, an inhibitor of the co-repressor of repressor element-1 silencing transcription (CoREST) deacetylase complex, designed to treat immunotherapy-resistant STK11-mutant tumors.
Novartis AG has described peptide-drug conjugates comprising cyclic peptides targeting HER2 (erbB2) covalently linked to a radiolabeled metal chelator through a linker reported to be useful for diagnosis and treatment of cancer.
Nanjing Zaiming Pharmaceutical Co. Ltd. has synthesized Werner syndrome ATP-dependent helicase (WRN; RECQ3; RECQL2) inhibitors reported to be useful for the treatment of cancer.
Shouyao Holdings (Beijing) Co. Ltd. has disclosed mucosa-associated lymphoid tissue lymphoma translocation protein 1 (MALT1) inhibitors reported to be useful for the treatment of cancer, rheumatoid arthritis, multiple sclerosis, psoriasis, Sjögren’s syndrome, systemic lupus erythematosus, erythema and vasculitis.
During the AACR-NCI-EORTC International Conference on Molecular Targets and Cancer Therapeutics, scientists from Plexium Inc. presented the identification of a new class of potent, selective, cereblon (CRBN)-based molecular glue degraders of CDK2 using its proprietary monovalent degrader platform.
At the recent AACR-NCI-EORTC International Conference on Molecular Targets and Cancer Therapeutics, researchers from Aurigene Oncology Ltd. presented the discovery and clinical characterization of novel macrocyclic KIF18A inhibitors.
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