The discovery and development of new histone lysine acetyltransferase KAT6 inhibitors is a significant advancement in the management of breast cancer. Investigators from Olema Pharmaceuticals Inc. and Aurigene Oncology Ltd. recently presented data for their KAT6 inhibitor, OP-3136, as an approach for breast cancer.
Aurigene Oncology Ltd. and Olema Pharmaceuticals Inc. have disclosed new proteolysis targeting chimera (PROTAC) compounds comprising an E3 ubiquitin ligase CBL-B (CBLB)-binding moiety coupled to a histone acetyltransferase KAT6A (MOZ; MYST-3)-targeting moiety. They are described as potentially useful for the treatment of cancer.
Aurigene Oncology Ltd. has identified compounds acting as E3 ubiquitin-protein ligase CBL-B (CBLB) inhibitors reported to be useful for the treatment of cancer.
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.
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.
Aurigene Oncology Ltd. has identified proteolysis targeting chimera (PROTAC) compounds comprising an E3 ubiquitin ligase protein binding moiety covalently linked to probable global transcription activator SNF2L2 (SMARCA2; BAF190B; SNF2-α) and/or transcription activator BRG1 (SMARCA4; BAF190A; SNF2-β) binding moieties through a linker reported to be useful for the treatment of cancer.
Aurigene Oncology Ltd. has patented new proteolysis targeting chimera (PROTACs) compounds comprising a protein cereblon (CRBN)-binding moiety covalently bound to a CREB-binding protein (CREBBP; CBP)-targeting moiety through a linker.
Aurigene Oncology Ltd. has described proteolysis targeting chimeras (PROTACs) comprising an E3 ubiquitin ligase binding moiety coupled to a probable global transcription activator SNF2L2 (SMARCA2; BAF190B; SNF2-α) and/or transcription activator BRG1 (SMARCA4; BAF190A; SNF2-β) targeting moiety via a linker acting as SMARCA2 and/or SMARCA4 degradation inducers reported to be useful for the treatment of cancer.