Shanghai Qilu Pharmaceutical Research and Development Centre Ltd. has described proteolysis targeting chimera (PROTAC) compounds comprising an E3 ubiquitin ligase-binding moiety covalently linked to epidermal growth factor receptor (EGFR)-binding moiety through linker reported to be useful for the treatment of cancer.
Medshine Discovery Inc. has presented furan fused ring-substituted glutarimides as proteolysis targeting chimera (PROTAC) compounds comprising an E3 ubiquitin ligase-binding moiety covalently linked to androgen receptor-targeting moiety reported to be useful for the treatment of prostate cancer.
Proteolysis targeting chimeras (PROTACs) are drugs that use cancer cells’ own proteasome to selectively degrade essential tumor-driver molecules through E3 ubiquitin ligase binding. Resistance to PROTAC therapy in cultured cells has been shown to involve genomic alterations in their E3 ligase targets.
University of Michigan has described new proteolysis targeting chimeric (PROTACs) compounds comprising cereblon (CRBN) ligands covalently bonded to CREB-binding protein (CBP) and/or histone acetyltransferase KAT3B (p300)-targeting moiety through linker reported to be useful for the treatment of cancer.
The University of Michigan has synthesized new proteolysis targeting chimera (PROTAC) compounds comprising an E3 ubiquitin ligase binding moiety covalently linked estrogen receptor (ER) targeting moiety reported to be useful for the treatment of breast cancer.
