Betta Pharmaceuticals Co. Ltd. has described proteolysis targeting chimera (PROTAC) compounds comprising a VHL-binding agent coupled to a GTPase KRAS-targeting moiety through a linker acting as KRAS degradation inducers reported to be useful for the treatment of cancer.
Treeline Biosciences Inc. has divulged proteolysis targeting chimeras (PROTACs) comprising cereblon (CRBN) ligands coupled to a Bcl-2-like protein 1 (Bcl-xl; Bcl-X; BCL2L1) targeting moiety via a linker acting as Bcl-xl degradation inducers reported to be useful for the treatment of cancer.
Bristol Myers Squibb Co. has disclosed proteolysis targeting chimera (PROTAC) compounds comprising a cereblon (CRBN) E3 ubiquitin ligase-binding moiety covalently bonded to a B-cell lymphoma 6 protein (BCL-6)-targeting moiety through a linker. They are reported to be useful for the treatment of cancer and autoimmune diseases.
Shenzhen Zhongge Biotechnology Co. Ltd. has described proteolysis targeting chimera (PROTAC) compounds comprising an E3 ubiquitin ligase binding agent coupled to interleukin-1 receptor-associated kinase 4 (IRAK-4) targeting moiety via linkers acting as IRAK-4 degradation inducers reported to be useful for the treatment of cancer, autoimmune disease, inflammatory disorders, transplant rejection, thromboembolism, atherosclerosis, myocardial infarction and metabolic syndrome.
Targeted protein degradation has yet to notch its first approval. But with more than two dozen agents now in clinical trials, the strategy’s ultimate clinical validation appears to be a matter of time.
Summit Therapeutics Inc. has identified proteolysis targeting chimera (PROTAC) compounds comprising an E3 ubiquitin ligase binding moiety coupled to a GTPase KRAS (G12D) targeting moiety through a linker acting as KRAS (G12D) inhibitors and degradation inducers reported to be useful for the treatment of cancer.
CSPC Zhongqi Pharmaceutical Technology (Shijiazhuang) Co. Ltd. has identified proteolysis targeting chimeras (PROTACs) comprising an E3 ubiquitin ligase cereblon binding moiety coupled to an EGFR-targeting moiety via a linker reported to be useful for the treatment of non-small-cell lung cancer.
Oxford University Innovations Ltd. has synthesized hypoxia-activated proteolysis targeting chimeras (hypoxia-activated PROTACs; HAP-TAC) comprising a hypoxia-activated moiety modified E3 ubiquitin ligase-binding moiety coupled to a protein targeting moiety through a linker reported to be useful for the treatment of cancer.
Kymera Therapeutics Inc. has described proteolysis targeting chimera (PROTACs) compounds comprising an E3 ubiquitin ligase-binding moiety covalently linked to a signal transducer and activator of transcription 6 (STAT6)-targeting moiety.
