Researchers from Specally (Wuhan) Life Technology Co. Ltd. have disclosed the discovery and preclinical profile of WWZ-11-098, a non-palbociclib-based, selective cyclin-dependent kinase 6 (CDK6) degrader in models of leukemia.
Mitogen-activated protein kinase kinase kinase kinase 1 (HPK1) is a serine/threonine protein kinase that is expressed in the hematopoietic compartment, exerting regulatory functions in myeloid and innate immune cells. It has been associated with decreased T-cell activation and proliferation.
Gan & Lee Pharmaceuticals Co. Ltd. has disclosed proteolysis targeting chimera (PROTAC) compounds comprising an E3 ubiquitin ligase-binding moiety covalently linked to a probable global transcription activator SNF2L2 (SMARCA2; BAF190B; SNF2-α)- and/or SMARCA4-targeting moiety.
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.
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