Chia Tai Tianqing Pharmaceutical Group Co. Ltd. has disclosed proteolysis targeting chimeric (PROTAC) compounds comprising a E3 ubiquitin ligase-binding moiety covalently linked to an estrogen receptor-α (ERα)-targeting moiety. They are reported to be useful for the treatment of breast cancer.
Ovarian cancer is a highly lethal gynecological malignancy with limited therapeutic options for recurrent and drug-resistant disease. Sirtuin 2 (SIRT2) promotes tumor cell proliferation, migration and invasion by regulating multiple oncogenic signaling pathways. Although SIRT2 has emerged as a promising therapeutic target, conventional inhibitors often result in incomplete and transient suppression of its activity.
Gachon University and Jeonbuk National University Industry Foundation have disclosed proteolysis targeting chimera (PROTAC) compounds comprising a cereblon (CRBN) E3 ubiquitin ligase-binding moiety coupled to a serine/threonine-protein kinase PAK4-targeting moiety through a linker potentially useful for the treatment of cancer.
Hanmi Holdings Co. Ltd. has patented proteolysis targeting chimeras (PROTACs) comprising a cereblon (CRBN)-binding moiety coupled to a histone acetyltransferase p300 (EP300)-targeting moiety through a linker acting as EP300 degradation inducers reported to be useful for the treatment of cancer.
Gan & Lee Pharmaceuticals Co. Ltd. has prepared and tested proteolysis targeting chimera (PROTAC) compounds comprising an E3 ubiquitin ligase binding moiety covalently linked to an estrogen receptor α(ER-α; ESR1) targeting moiety via a linker reported to be useful for the treatment of cancer.
Work at Dark Blue Therapeutics Ltd. has led to the development of new proteolysis targeting chimera (PROTAC) compounds comprising a E3 ubiquitin ligase-binding moiety coupled to a protein ENL (MLLT1; YEATS1) and/or protein AF-9 (MLLT3; AF9)-targeting moiety through a linker. They are reported to be useful for the treatment of cancer.
Hangzhou Polymed Biopharmaceuticals Inc. has disclosed proteolysis targeting chimeric (PROTAC) compounds comprising cereblon (CRBN) ligands covalently bonded to an EGFR del19/Thr790Met/Cys797Ser triple mutant and/or EGFR Leu858Arg/Thr790Met/Cys797Ser triple mutant-targeting moiety through a linker reported to be useful for the treatment of cancer.
Ascentage Pharma Group International has obtained IND approval from the FDA for its BTK-targeted protein degrader APG-3288. A phase I study will be conducted in patients with relapsed or refractory B-cell malignancies.
Convergen (Suzhou) Pharmaceutical Co. Ltd. has described proteolysis targeting chimera (PROTAC) compounds comprising a cereblon (CRBN) E3 ubiquitin ligase-binding moiety coupled to a serine/threonine-protein kinase PAK4-targeting moiety through a linker reported to be useful for the treatment of cancer.
Shenzhen Targetrx Inc. has divulged proteolysis targeting chimera (PROTAC) compounds comprising a cereblon (CRBN)-binding moiety covalently linked to Raf kinase B (V600E mutant)-targeting moiety through linker reported to be useful for the treatment of cancer.
