Jiangsu Hengrui Pharmaceuticals Co. Ltd. has patented new proteolysis targeting chimera (PROTACs) compounds comprising an E3 ubiquitin ligase-binding moiety covalently linked to cyclin-dependent kinase 7 (CDK7) targeting moiety potentially useful for the treatment of cancer, inflammatory and autoimmune diseases.
Arvinas Inc. has identified new proteolysis targeting chimeras (PROTACs) comprising an E3 ubiquitin ligase coupled to a mitogen-activated protein kinase kinase kinase kinase 1 (MAP4K1; HPK1; MEKKK1)-targeting moiety acting as HPK1 degradation inducers designed for use in the treatment of cancer.
Transient receptor potential melastatin 3 (TRPM3) is a calcium-permeable TRP channel that is highly expressed in somatosensory neurons, including nociceptors of rodents and humans. Its activation triggers acute pain, making drugs that target TRPM3 a potential approach to alleviate pain. Biohaven Ltd.’s BHV-2100 is the only selective TRPM3 antagonist in clinical development. The company recently disclosed the work leading to its discovery and early development, as well as the chemical structure.
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.
Microtubule-associated serine/threonine kinase-like protein (MASTL) is a key regulator of mitotic progression and cell-cycle control. Researchers from the Korea Institute of Radiological and Medical Sciences reported the preclinical efficacy of MKI-3, a selective MASTL inhibitor.
Mabwell (Shanghai) Bioscience Co. Ltd. has announced that SST-001 (18F-FD4), an α-synuclein-targeted PET tracer developed by Mabwell’s incubated company Synusight Biotech, has received clinical trial clearance from China’s National Medical Products Administration (NMPA). The planned phase I trial will enroll healthy volunteers, patients with multiple system atrophy (MSA), and patients with Parkinson’s disease.
Glyconex Inc. has received approval from Japan’s Pharmaceuticals and Medical Devices Agency (PMDA) for the initiation of a first-in-human phase I trial of GNX-1021, the company’s lead antibody-drug conjugate (ADC) candidate, in patients with advanced gastrointestinal (GI) cancers.
While most human papillomavirus (HPV) infections are cleared by the host immune system, persistent infection with high-risk HPV genotypes, particularly HPV16 and HPV18, can promote cervical cancer development. Researchers from Huazhong University of Science and Technology reported the development and preclinical characterization of KDTV-001, an HPV vaccine comprising a nonreplicating adenovirus type 5 vector encoding a codon-optimized fusion protein of the early antigens E6 and E7 derived from HPV genotypes 16, 18 and 52.
Haisco Pharmaceutical Group Co. Ltd. has disclosed new lysophosphatidic acid receptor 1 (LPAR1; EDG2) antagonists reported to be useful for the treatment of idiopathic pulmonary fibrosis.
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