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.
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).
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.
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.
Daiichi Sankyo Co. Ltd. has disclosed new proteolysis targeting chimera (PROTAC) compounds comprising an E3 ubiquitin ligase-binding moiety covalently linked to a steroidogenic factor 1 (SF-1)-targeting moiety. They are reported to be potentially useful for the treatment of primary aldosteronism, Cushing syndrome and cancer.
Treeline Biosciences Inc. has synthesized new proteolysis targeting chimera (PROTAC) compounds comprising an E3 ubiquitin ligase-binding moiety covalently linked to transcriptional enhancer factor TEF (TEAD)-targeting moiety potentially useful for the treatment of cancer.
A University of Texas System patent describes new YAP1 degradation inducing proteolysis targeting chimeras (PROTACs) designed for use in the treatment of cancer.
A patent from Gilead Sciences Inc. has divulged GTPase KRAS (G12D mutant) inhibitors and proteolysis targeting chimeras (PROTACS) comprising an E3 ubiquitin ligase-binding moiety covalently linked to a GTPase KRAS (G12D mutant)-targeting moiety through linker.
A Risen (Shanghai) Pharma Eng Co. Ltd. and Risen (Suzhou) Pharma Tech Co. Ltd. patent describes the discovery of new proteolysis targeting chimera (PROTAC) compounds comprising a E3 ubiquitin ligase-binding moiety covalently linked to a GTPase KRAS-targeting moiety. They are reported to be useful for the treatment of cancer.
