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.
Hubei Bio-Pharmaceutical Industrial Technological Institute Inc. has identified new molecular glue degrader compounds acting as proto-oncogene Vav (VAV1)/protein cereblon (CRBN) interaction inducers for degradation of VAV1 reported to be useful for the treatment of inflammatory bowel disease.
Gluetacs Therapeutics (Shanghai) Co. Ltd. has discovered new proteolysis targeting chimera (PROTAC) compounds comprising a cereblon (CRBN)-binding moiety coupled to a SWI/SNF-related matrix-associated actin-dependent regulator of chromatin subfamily A member 2 (SMARCA2) and SMARCA4-targeting moiety. They are designed for use in the treatment of cancer, transplant rejection, infections, diabetes, autoimmune, neurological, inflammatory and cardiovascular disorders, among others.
Retinoid X receptor γ (RXRγ) is a key nuclear receptor that sustains androgen receptor (AR) signaling. In castration-resistant prostate cancer (CRPC), RXRγ contributes to disease progression by maintaining adaptive transcriptional networks that promote therapy resistance and tumor cell survival.
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.
Gilead Sciences Inc. has exercised its option to exclusively license KT-200, a first-in-class, oral CDK2 molecular glue degrader development candidate discovered and characterized by Kymera Therapeutics Inc. under the parties’ strategic collaboration agreement.
Protein arginine methyltransferase 1 (PRMT1) is a key enzyme that catalyzes post-translational arginine methylation, thereby regulating diverse cellular processes, including gene transcription, RNA splicing, signal transduction, and DNA damage repair. As a central epigenetic and signaling regulator, PRMT1 plays a critical role in coordinating cellular proliferation, differentiation, and survival.
Shanghai Meiyue Biotech Development Co. Ltd. has disclosed new molecular glue degraders comprising an E3 ubiquitin-protein ligase binding agents coupled to proto-oncogene Vav (VAV1) acting as VAV1 degradation inducers reported to be useful for the treatment of cancer, autoimmune diseases, cardiovascular, renal, metabolic, inflammatory and neurological disorders.
Ring finger protein 4 (RNF4) is a SUMO-targeted ubiquitin ligase that modulates proteins involved in cancer progression. Researchers from Chongqing Medical University and collaborators reported the development and preclinical characterization of [I], the first RNF4-targeting PROTAC degrader for the treatment of hepatocellular carcinoma (HCC).
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