Receptor-interacting protein kinase 1 (RIPK1) helps promote the survival of cancer cells, and degrading it can sensitize tumors to immunotherapy against PD-1. Degrading the entire protein seems to be essential: merely blocking its kinase activity does not sensitize tumors.
In a study published in Molecular Therapy, researchers from H. Lee Moffitt Cancer Center and Research Institute and the University of South Florida developed an E6-targeting proteolysis targeting chimera (PROTAC) that inhibits the growth of human papillomavirus (HPV)-positive tumors. HPV is the most prevalent sexually transmitted infection worldwide, with persistent infections causing up to six different types of cancer.
Blueprint Medicines Corp. has disclosed PROTAC compounds comprising an E3 ubiquitin ligase binding moiety covalently linked to a cyclin-dependent kinase 4 (CDK4)-targeting moiety potentially useful for the treatment of cancer.
In an effort to develop more effective estrogen receptor α (ERα) inhibitors, researchers at Nanjing University of Chinese Medicine and collaborators aimed to develop a proteolysis targeting chimera (PROTAC) against the receptor.
Nikang Therapeutics Inc. has disclosed proteolysis targeting chimera (PROTAC) compounds comprising an E3 ubiquitin ligase-binding moiety coupled to a cyclin-dependent kinase 2 (CDK2)- and/or CDK4-targeting moiety through a linker reported to be useful for the treatment of cancer.
Crossfire Oncology BV has divulged proteolysis targeting chimera (PROTAC) compounds comprising an E3 ubiquitin ligase binding moiety covalently linked to a serine/threonine-protein kinase PLK1 (STPK13) targeting moiety through a linker reported to be useful for the treatment of cancer, autoimmune diseases, transplant rejection, neurological disorders and inflammatory disorders.
Northridge Health Group (Hong Kong) Co. Ltd. has divulged proteolysis targeting chimera (PROTAC) compounds comprising an E3 ubiquitin ligase binding moiety covalently linked to a tyrosine-protein phosphatase non-receptor type 2 (PTPN2; TCPTP) and/or tyrosine-protein phosphatase non-receptor type 1 (PTPN1; PTP-1B)-targeting moiety via a linker.
Shanghai Leadingtac Pharmaceutical Co. Ltd. has synthesized proteolysis targeting chimera (PROTAC) compounds comprising an E3 ubiquitin 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.
Researchers from Nankai University and collaborating institutions have identified a novel proteolysis targeting chimera (PROTAC) molecule that effectively and selectively degrades multiple cyclin-dependent kinases (CDKs) to inhibit the proliferation of triple-negative breast cancer (TNBC) cells, offering a potential targeted therapy for this form of breast cancer.
Shanghai Leadingtac Pharmaceutical Co. Ltd. has divulged proteolysis targeting chimera (PROTAC) compounds comprising an E3 ubiquitin ligase-binding moiety covalently linked to a pan-KRAS-targeting moiety through a linker.
