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.
Beactica Therapeutics AB, together with researchers at KU Leuven, has been awarded a €2.5 million (US$3.0 million) grant by the European Innovation Council (EIC) to advance BEA-17, a precision immune therapy for glioblastoma.
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.
Triple-negative breast cancer (TNBC) cells depend on the transcriptional kinases CDK12 and CDK13 to maintain DNA damage response gene expression and manage replication stress. Due to their functional overlap, inhibition of a single kinase may permit compensatory activity.
Beijing Innocare Pharma Tech Co. Ltd. has gained IND clearance in China to conduct clinical trials of ICP-538, an orally administered molecular glue degrader targeting VAV1, which is a key protein downstream of T-cell and B-cell receptors. ICP-538 is being studied for the treatment of autoimmune diseases, such as inflammatory bowel disease, systemic lupus erythematosus and multiple sclerosis.
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.
Kazia Therapeutics Ltd. has announced promising preclinical and translational data supporting the development of NDL-2, a protein degrader targeting a newly identified mechanism of immunotherapy resistance and metastatic progression.
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