Work at Dark Blue Therapeutics Ltd. has led to the development of new proteolysis targeting chimera (PROTAC) compounds comprising a E3 ubiquitin ligase-binding moiety coupled to a protein ENL (MLLT1; YEATS1) and/or protein AF-9 (MLLT3; AF9)-targeting moiety through a linker. They are reported to be useful for the treatment of cancer.
CD276, also known as B7-H3, is an antigen highly expressed in several cancer types, including hepatocellular carcinoma (HCC, 79%-94% expression) and closely tied to aggressiveness and poor survival, but shows very low expression in normal tissues. Increasing evidence exists indicating B7-H3 has immune inhibitory functions, thus reducing interferon levels released by T cells and suppressing cytotoxic activity of natural killer cells, thereby aiding in tumor immune evasion.
Bispecific T-cell engagers (TCEs) aim to combat cancer by simultaneously binding T cells and tumor cells in order to induce the first to kill the second. This approach has failed to work effectively against many solid tumors because the exogenous engager proteins do not penetrate into tumors at sufficiently high concentrations.
Tahoe Therapeutics and Alloy Therapeutics Inc. are forming a jointly seeded new company focused on developing first-in-class antibody-drug conjugates (ADCs) for patients with hard-to-treat cancers. The joint venture will advance two ADC programs directed at novel tumor targets discovered by Tahoe using its proprietary Mosaic platform and large-scale, perturbative single-cell datasets.
The colchicine-binding domain (CBD) of tubulin, one of the earliest identified regulatory sites, remains underexplored in oncology despite its proven success in other therapeutic areas. Drugs targeting CBD are widely used for gout, parasitic infections or actinic keratosis. However, no CBD-directed agents have reached clinical use for cancer, highlighting a significant opportunity to exploit this domain for novel anticancer strategies.
Hainan Simcere Pharmaceutical Co. Ltd. has described N-myristoyltransferase 1 (NMT1) and NMT2 inhibitors reported to be useful for the treatment of cancer.
Shenzhen Forward Pharmaceutical Co. Ltd. has synthesized quinazoline derivatives acting as GTPase KRAS G12C, G12D and G12V mutant inhibitors reported to be useful for the treatment of pancreatic cancer.
Swiss Rockets AG and Alloy Therapeutics Inc. have signed a master research agreement establishing a multitarget collaboration to discover and develop next-generation radioligand therapeutics (RLTs) for oncology.
Researchers from Stanford School of Medicine and Yonsei University College of Medicine reported the discovery and preclinical characterization of novel KLHDC2-mediated CDK6-selective degraders.
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