A patent from Gilead Sciences Inc. has divulged GTPase KRAS (G12D mutant) inhibitors and proteolysis targeting chimeras (PROTACS) comprising an E3 ubiquitin ligase-binding moiety covalently linked to a GTPase KRAS (G12D mutant)-targeting moiety through linker.
A Risen (Shanghai) Pharma Eng Co. Ltd. and Risen (Suzhou) Pharma Tech Co. Ltd. patent describes the discovery of new proteolysis targeting chimera (PROTAC) compounds comprising a E3 ubiquitin ligase-binding moiety covalently linked to a GTPase KRAS-targeting moiety. They are reported to be useful for the treatment of cancer.
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.
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