Researchers from Bridge Biotherapeutics Inc. have presented the discovery and preclinical characterization of BBT-4437, a novel brain-penetrable and reversible pan-transcriptional enhancer factor (TEAD) inhibitor, designed to target the Hippo signaling pathway in solid tumors.
Increasing knowledge of the cancer glycome and the need for new options to overcome resistance to immune checkpoint inhibitors are leading to an expansion of glycoimmunology. Stanford University professor Carolyn Bertozzi demonstrated that cell-surface glycans may be tagged to become targetable glyco-immune checkpoints.
Huadong Medicine Co. Ltd. recently detailed the discovery and preclinical characterization of a potent and selective small-molecule glucagon-like peptide-1 receptor (GLP-1R) agonist, HDM-1002, under investigation for the treatment of type 2 diabetes and obesity.
Research at Aurigene Oncology Ltd. has led to the discovery of a mucosa-associated lymphoid tissue lymphoma translocation protein 1 (MALT1) inhibitor AU-MALT1-01 for the potential treatment of B-cell lymphomas including diffuse large B-cell lymphoma (DLBCL).
Structure-guided lead optimization at Merck & Co. Inc. has led to the discovery of MK-1084 as a highly potent and selective KRAS G12C-GDP inhibitor. As reported at the recent AACR-NCI-EORTC conference, the candidate demonstrated an excellent off-target and ion channel profile, with low potential for bile salt export pump (BSEP) inhibition.
Vividion Therapeutics Inc. has disclosed VVD-065, a novel, first-in-class, allosteric molecular glue of the KEAP1-CUL3 E3-ligase complex, for the potential treatment of NRF2-activated cancers. NRF2 (nuclear factor erythroid 2-related factor 2) is a significant mediator of antioxidant response.
Researchers from Biolexis Therapeutics Inc. presented the development of a potent and highly selective CDK9 inhibitor, BLX-3030, and its analogues for the treatment of N-Myc and c-Myc-driven cancers.
Researchers from Generate Biomedicines Inc. have detailed the discovery and preclinical characterization of GB-0669, a spike S2-targeted monoclonal antibody (MAb) being developed for the prophylaxis of SARS-CoV-2 infection. Machine learning models were used to identify MAbs targeting the conserved S2 stem helix and RBD class IV region of spike.
Researchers from Astellas Pharma Inc. presented preclinical data for the novel small-molecule diacylglycerol kinase ζ (DGKζ) inhibitor ASP-1570, currently in phase I development for the treatment of solid tumors (NCT05083481).
KRAS is a GTP-binding protein involved in cell growth control that requires post-translational farnesylation to be active. KRAS G12D mutations are mostly associated with pancreatic, colorectal and non-small-cell lung cancers and occur less commonly in other cancers. There are currently no therapies approved to specifically target this mutation.
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