In glioblastoma multiforme, MTAP loss leads to MTA accumulation, which partially inhibits PRMT5, making the cells reliant on residual PRMT5 activity for survival. Targeting this remaining PRMT5 with MTA-cooperative inhibitors induces synthetic lethality, representing a promising targeted approach for MTAP-deleted gliomas. Researchers from Ryvu Therapeutics SA reported the preclinical profile of RVU-305, a PRMT5 inhibitor, in MTAP-deleted cancer models.
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.
Hutchmed (China) Ltd. has developed HMPL-A251, a novel HER2 antibody-drug conjugate (ADC) designed to deliver a potent PI3K/PIKK inhibitor directly to tumor cells.
CIS Biopharma AG recently presented an antibody-drug conjugate (ADC) targeting the L1 cell adhesion molecule (L1CAM/CD171) as a potential candidate for the treatment of advanced tumors.
Pinotbio Inc. recently reported a novel antibody-drug conjugate (ADC), named PBX-004, consisting of an ITGB6-targeting antibody conjugated to a potent topoisomerase I (TOP1) inhibitor payload.
Researchers from Prospect Therapeutics Inc. have discovered PSTA-5204, a novel oral KRAS G12D(ON) inhibitor that exhibits potent in vitro activity, strong in vivo efficacy and high selectivity over wild-type KRAS.
Aurigene Oncology Ltd. recently provided details on the discovery and preclinical characterization of AUR-243, a novel CBL-B inhibitor with a distinct therapeutic profile and best-in-class potential compared to other inhibitors. AUR-243 was described as a structurally distinct, oral small molecule demonstrating excellent potency, functional activity and superior efficacy.
Researchers at Triana Biomedicines Inc. presented the preclinical characterization of TRI-611, a CNS-penetrant molecular glue degrader targeting ALK in models of ALK fusion-positive non-small-cell lung cancer.
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