Aurigene Oncology Ltd. has identified proteolysis targeting chimera (PROTAC) compounds comprising an E3 ubiquitin ligase protein binding moiety covalently linked to probable global transcription activator SNF2L2 (SMARCA2; BAF190B; SNF2-α) and/or transcription activator BRG1 (SMARCA4; BAF190A; SNF2-β) binding moieties through a linker reported to be useful for the treatment of cancer.
Sichuan Kelun-Biotech Biopharmaceutical Co. Ltd. has synthesized proteolysis targeting chimera (PROTAC) compounds comprising a Von Hippel-Lindau disease tumor suppressor (VHL)-binding moiety covalently linked to a GTPase KRAS G12D mutant-targeting moiety through a linker reported to be useful for the treatment of cancer.
Chia Tai Tianqing Pharmaceutical Group Co. Ltd. has disclosed proteolysis targeting chimeric (PROTAC) compounds comprising cereblon (CRBN) ligands covalently bonded to a B-cell lymphoma 6 protein (BCL6)-targeting moiety through a linker.
Beijing DP Technology Co. Ltd. has divulged proteolysis targeting chimera (PROTAC) compounds comprising an E3 ubiquitin ligase-binding moiety covalently bonded to a Myc proto-oncogene protein (c-Myc)-targeting moiety through a linker reported to be useful for the treatment of cancer, viral infections, and cardiovascular, immunological and cerebrovascular disorders.
Prelude Therapeutics Inc. has prepared and tested new proteolysis targeting chimera (PROTAC) compounds comprising an E3 ubiquitin ligase-binding moiety coupled to probable global transcription activator SNF2L2 (SMARCA2; BAF190B; SNF2-α) and SMARCA4-targeting moiety through a linker.
Hangzhou Polymed Biopharmaceuticals Inc. has identified proteolysis targeting chimera (PROTAC) compounds comprising a Von Hippel-Lindau disease tumor suppressor (VHL) ligase binding moiety covalently linked to a GTPase KRAS (G12D mutant) targeting moiety via a linker reported to be useful for the treatment of cancer.
Merck KGaA has synthesized proteolysis targeting chimera (PROTAC) compounds comprising an E3 ubiquitin-protein ligase-binding moiety covalently bonded to a mitogen-activated protein kinase kinase kinase kinase 1 (MAP4K1; HPK1; MEKKK1)-targeting moiety through a linker reported to be useful for the treatment of cancer.
Chia Tai Tianqing Pharmaceutical Group Co. Ltd. has synthesized proteolysis targeting chimera (PROTAC) compounds comprising an E3 ubiquitin ligase binding moiety covalently linked to a eukaryotic peptide chain release factor GTP-binding subunit ERF3A (GSPT1) targeting moiety via a linker reported to be useful for the treatment of cancer.
Cyclin-dependent kinase 6 (CDK6) plays a crucial role in the G1 phase to S phase transition of the cell cycle. Aberrant activation of CDK6 has been linked with the development and progression of cancers such as leukemia, lymphoma and solid tumors. A recent study published in Bioorganic & Medicinal Chemistry aimed to discover novel proteolysis-targeting chimera (PROTAC) molecules as CDK6 inhibitors.