Hangzhou Zhongmei Huadong Pharmaceutical Co. Ltd. has described E3 ubiquitin-protein ligase CBL-B (CBLB) inhibitors reported to be useful for the treatment of cancer.
Beijing Infinite Intelligence Pharmaceutical Technology Co. Ltd. and Suzhou Fish-Summoning Biotechnology Co. Ltd. have identified compounds acting as Bcr-Abl (Bcr-Abl1) kinase inhibitors reported to be useful for the treatment of cancer, viral infections and neurological disorders.
Shanghai Leadingtac Pharmaceutical Co. Ltd. has synthesized proteolysis targeting chimera (PROTAC) compounds comprising an E3 ubiquitin ligase-binding moiety covalently linked to a GTPase KRAS (G12D mutant)-targeting moiety via a linker reported to be useful for the treatment of cancer.
Evopoint Biosciences Co. Ltd. has obtained clinical trial clearance in China for XNW-34017, an oral protein degrader that targets Aurora kinase A (AURKA) while simultaneously degrading MYC.
Researchers at Keimyung University and its medical school generated various candidate quinazolin-4-one derivatives, the most promising of which inhibited HDAC6 with an IC50 of 17 nM, 19-fold more strongly than it inhibited the off-target deacetylase HDAC1.
Researchers from Prospect Therapeutics Inc. have discovered PSTA-5204, a novel oral KRAS G12D(ON) inhibitor that exhibits potent in vitro activity, strong in vivo efficacy and high selectivity over wild-type KRAS.
Aurigene Oncology Ltd. recently provided details on the discovery and preclinical characterization of AUR-243, a novel CBL-B inhibitor with a distinct therapeutic profile and best-in-class potential compared to other inhibitors. AUR-243 was described as a structurally distinct, oral small molecule demonstrating excellent potency, functional activity and superior efficacy.
A team from the University of Missouri and collaborating institutions aimed to investigate the role of ABTB2 expression in pancreatic ductal adenocarcinoma cells. To do that, they applied a comprehensive suite of functional genomics tools, including siRNA/shRNA knockdown, CRISPR-Cas9 knockout, plasmid-based overexpression and a Cre-LoxP transgenic mouse model to modulate ABTB2 expression.
Researchers from Nankai University and collaborating institutions have identified a novel proteolysis targeting chimera (PROTAC) molecule that effectively and selectively degrades multiple cyclin-dependent kinases (CDKs) to inhibit the proliferation of triple-negative breast cancer (TNBC) cells, offering a potential targeted therapy for this form of breast cancer.
Researchers at Triana Biomedicines Inc. presented the preclinical characterization of TRI-611, a CNS-penetrant molecular glue degrader targeting ALK in models of ALK fusion-positive non-small-cell lung cancer.
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