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).
Biofront Ltd. has designed new proteolysis targeting chimeras (PROTACs) comprising an E3 ubiquitin ligase-binding moiety coupled to a mitogen-activated protein kinase kinase kinase kinase 1 (MAP4K1; HPK1; MEKKK1)-targeting moiety as HPK1 degradation inducers. They are described as potentially useful for the treatment of cancer.
In both acute myeloid leukemia (AML) and synovial sarcoma (SS), targeting BRD9 disrupts oncogenic transcriptional programs, including MYC, leading to reduced proliferation and induction of apoptosis. Researchers from Pamplona Therapeutics (Shenzhen) Co. Ltd. reported the discovery and preclinical efficacy profile of XYD-270, a BRD9-targeting PROTAC, in models of SS and AML.
IKZF1-4 are transcription factors that regulate cellular differentiation, proliferation and survival. At the American Chemical Society (ACS) Spring 2026 meeting this week in Atlanta, Bristol Myers Squibb Co. detailed the identification and preclinical profile of BMS-986482, a next-generation investigational cereblon E3 ligase modulator (CELMoD) degrader designed to target IKZF1-4 factors.
Arvinas Operations Inc. has disclosed proteolysis targeting chimera (PROTACs) compounds comprising a cereblon (CRBN) E3 ubiquitin ligase-binding moiety covalently linked to a B-cell lymphoma 6 protein (BCL-6)-targeting moiety through a linker with potential for use in the treatment of cancer.
Shanghai Qilu Pharmaceutical Research and Development Centre Ltd. has prepared and tested molecular glue degraders comprising E3 ubiquitin-protein ligases acting as proto-oncogene Vav (VAV1) degradation inducers reported to be useful for the treatment of inflammation and autoimmune diseases.
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