Jiangsu Hengrui Pharmaceuticals Co. Ltd. and Shanghai Hengrui Pharmaceutical Co. Ltd. have identified new proteolysis targeting chimera (PROTACs) compounds comprising an E3 ubiquitin ligase-binding moiety coupled to a B-cell lymphoma 6 protein (BCL6)-targeting moiety through a linker.
Shenzhen Targetrx Inc. has designed new proteolysis targeting chimeric (PROTACs) compounds comprising cereblon (CRBN) ligands covalently bonded to an EGFR L858R-, L858R/T790M double mutant- and L858R/T790M/C797S triple mutant-targeting moiety through a linker reported to useful for the treatment of non-small-cell lung cancer.
Ascentage Pharma Group Corp. Ltd. and Ascentage Pharma (Suzhou) Co. Ltd. have disclosed proteolysis targeting chimera (PROTAC) compounds comprising E3 ubiquitin ligase-binding moiety covalently linked to a Bruton tyrosine kinase (BTK)-targeting moiety. They are reported to be useful for the treatment of cancer.
Scientists from Adlai Nortye Biopharma Co. Ltd. and Adlai Nortye Pte Ltd. have prepared and tested proteolysis targeting chimera (PROTAC) compounds comprising an E3 ubiquitin ligase-binding moiety coupled to a signal transducer and activator of transcription 6 (STAT6)- or STAT3-targeting moiety.
Uppthera Inc. has patented new proteolysis targeting chimera (PROTAC) compounds comprising cereblon E3 ubiquitin ligase-binding moiety covalently linked to Aurora kinase A (AURKA; ARK1)-targeting moiety. They are reported to be useful for the treatment of cancer.
Inflammatory bowel disease (IBD), including ulcerative colitis and Crohn’s disease, is a chronic immune-mediated inflammatory disorder with limited long-term therapeutic options. Proteolysis-targeting chimeras (PROTACs) offer a promising strategy for IBD by enabling selective degradation of disease-relevant proteins and potentially improving efficacy and safety.
University of Florida researchers have synthesized proteolysis targeting chimeras (PROTACs) comprising an E3 ubiquitin ligase-binding moiety coupled to Bcl-2-like protein 1 (Bcl-xl; Bcl-X; BCL2L1)- and apoptosis regulator Bcl-2-targeting moiety.
Shanghai Haiyan Pharmaceutical Technology Co. Ltd. and Yangtze River Pharmaceutical Group have divulged new isoindoline proteolysis targeting chimeric (PROTAC) compounds comprising cereblon (CRBN) ligands covalently linked to a eukaryotic peptide chain release factor GTP-binding subunit ERF3A (GSPT1)-targeting moiety. They are reported to be useful for the treatment of cancer.
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.
