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.
Commit Biologics ApS has released promising results from a nonhuman primate (NHP) study demonstrating proof of concept for its proprietary bispecific complement engager (BiCE) platform.
Kolm Therapeutics Inc. has disclosed heterobifunctional compounds comprising a disease-dependent protein binding moiety (particularly, CREB-binding protein [CREBBP; CBP] or histone acetyltransferase p300 [EP300]) covalently linked to a disease protein (particularly, androgen receptor) through a linker.
San Francisco Bay Area researchers from UC Berkeley, UC San Francisco and Stanford University have combined their technologies to create Azalea Therapeutics Inc., a company focused on editing cells in vivo.
Shanghai Leadingtac Pharmaceutical Co. Ltd. has divulged proteolysis targeting chimera (PROTAC) compounds comprising an E3 ubiquitin ligase-binding moiety covalently linked to a pan-KRAS-targeting moiety through a linker.
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