Researchers from Therapex Co. Ltd. recently reported the discovery and preclinical evaluation of a novel fourth-generation epidermal growth factor receptor (EGFR) inhibitor for overcoming C797S mutation-mediated acquired resistance in non-small-cell lung cancer (NSCLC), which has been reported as the most common acquired resistance mechanism in NSCLC.
Kymera Therapeutics Inc. has described proteolysis targeting chimeras (PROTACs) comprising an E3 ubiquitin ligase binding moiety covalently linked to an MDM2 targeting moiety through a linker and reported to be useful for the treatment of cancer.
Therabest Co. Ltd. has identified glutathione (GSH) or hydrogen peroxide (H2O2)-activated prodrugs comprising obeticholic acid dimers conjugated via linkers and their nanogels coated with fucoidan reported to be useful for the treatment of liver diseases.
Xenon Pharmaceuticals Inc. has synthesized pyridinyl derivatives acting as sodium channel protein type 1 subunit α (SCN1A; Nav1.1) activators reported to be useful for the treatment of epilepsy.
The isocitrate dehydrogenase (IDH) enzyme family catalyzes the oxidative decarboxylation of isocitrate to produce α-ketoglutarate (α-KG). IDH1 and IDH2 mutants use the latter to generate the oncogenic metabolite R-2-hydroxyglutarate (2-HG). IDH mutations are highly prevalent in gliomas.
Veneno Technologies Co. Ltd. has entered into a joint research agreement with Sumitomo Pharma Co. Ltd. under which Veneno will conduct a program to obtain functional peptides (disulfide-rich peptides) for ion channels targeted by Sumitomo Pharma.