Synnovation Therapeutics Inc. has discovered new proteolysis targeting chimera (PROTAC) compounds comprising an E3 ubiquitin-protein ligases binding moiety coupled to nuclear factor erythroid 2-related factor 2 (NFE2L2; NRF2)-targeting moiety potentially useful for the treatment of cancer.
Treeline Biosciences Inc. has patented new tetrahydroisoquinoline heterobifunctional proteolysis targeting chimera (PROTAC) compounds comprising an E3 ubiquitin ligase-binding moiety coupled to a Bcl-2-like protein 1 (Bcl-xl; Bcl-X; BCL2L1)-targeting moiety potentially useful for the treatment of cancer.
Prelude Therapeutics Inc. has identified new proteolysis targeting chimera (PROTAC) compounds comprising an E3 ubiquitin ligase Von Hippel-Lindau disease tumor suppressor (VHL)-binding moiety coupled to a probable global transcription activator SNF2L2 (SMARCA2; BAF190B; SNF2-α)- and SMARCA4-targeting moiety.
Chinese researchers reported the discovery and preclinical characterization of a novel PROTAC degrader designed to target SAMHD1 and intended for the treatment of pulmonary fibrosis.
The University of California has identified proteolysis targeting chimera (PROTAC) compounds comprising an E3 ubiquitin ligase Von Hippel-Lindau disease tumor suppressor (VHL)-binding moiety coupled to cAMP-dependent protein kinase catalytic subunit α (PRKACA) targeting moiety through a linker.
A month ahead of its June 5 PDUFA date, Arvinas Inc.’s vepdegestrant gained U.S. FDA approval for use in a specific type of advanced or metastatic breast cancer, becoming the first proteolysis targeting chimera, or PROTAC, drug to reach the market.
Gilead Sciences Inc. has identified new 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 potentially useful for the treatment of cancer.
K2 Medicines (Nanjing) Co. Ltd. has identified new proteolysis targeting chimera (PROTAC) compounds comprising an E3 ubiquitin ligase-binding moiety coupled to a cyclin-dependent kinase 4 (CDK4)- and/or CDK4/6 dual-targeting moiety. They are designed for use in the treatment of cancer, neurodegeneration, viral infection, cardiovascular and inflammatory disorders.
A Beone Medicines I GmbH and Beone Pharmaceutical (Suzhou) Co. Ltd. patent details new proteolysis targeting chimera (PROTAC) compounds comprising an E3 ubiquitin ligase-binding moiety coupled to an interleukin-1 receptor-associated kinase 1 (IRAK-1)- and IRAK-4-targeting moiety. They are described as useful for the treatment of cancer, inflammatory disorders and autoimmune diseases.
