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.
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.
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.
Scientists from Adlai Nortye Biopharma Co. Ltd. and Adlai Nortye Pte Ltd. have discovered new GTPase KRAS and/or GTPase KRAS (mutant) inhibitors that are potentially useful for the treatment of cancer, autoimmune disorders and inflammation.
Researchers from Jiangsu Hengrui Pharmaceuticals Co. Ltd. and Shanghai Hengrui Pharmaceutical Co. Ltd. have synthesized new protein arginine N-methyltransferase 5 (PRMT5) inhibitors reported to be useful for the treatment of cancer.
KMT2A-rearranged acute myeloid leukemia (AML) is a highly aggressive leukemia subtype characterized by poor prognosis and high relapse rates. Because the menin-MLL interaction is essential for the stability and transcriptional activity of MLL fusion complexes, targeting this protein-protein interaction represents a promising therapeutic strategy for this aggressive form of AML. Researchers from Zhejiang University reported the discovery and preclinical characterization of [I], a novel menin inhibitor, designed for the treatment of AML.
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