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UnknownJND4135, a New Type II TRK Inhibitor, Overcomes TRK xDFG and Other Mutation Resistance In Vitro and In Vivo.
The tropomyosin receptor kinases (TRKs) have been validated as effective targets in anticancer drug discovery. Two first-generation TRK inhibitors have been approved into market and displayed an encouraging therapeutic response in cancer patients harboring TRK fusion proteins. However, acquired resi...
S-EPMC9570838 | biostudies-literature
UnknownYL143, a novel mutant selective irreversible EGFR inhibitor, overcomes EGFRL858R, T790M -mutant resistance in vitro and in vivo.
YL143 was identified as a novel wild-type sparing EGFRT790M inhibitor with good pharmacokinetic properties. It potently suppresses EGFRL858R/T790M with an 50% inhibitory concentration (IC50 ) value of 2.0 ± 0.3 nmol/L, but is approximately 92-folds less potent agains...
S-EPMC5911580 | biostudies-literature
UnknownInvestigation of Covalent Warheads in the Design of 2-Aminopyrimidine-based FGFR4 Inhibitors.
Covalent kinase inhibitors are rapidly emerging as a class of therapeutics with clinical benefits. Herein we report a series of selective 2-aminopyrimidine-based fibroblast growth factor receptor 4 (FGFR4) inhibitors exploring different types of cysteine-targeting warheads. The structure-activity re...
S-EPMC8040253 | biostudies-literature
MetabolomicsEnterobacter ludwigii protects DSS-induced colitis through choline-mediated immune tolerance
Commensal intestinal bacteria play key roles in regulating cells mediating immune tolerance; however, bacterial strains and related metabolites directly involved in this regulation are largely unknown. Here, using a mouse model of dextran sulfate sodium (DSS)-induced colitis combined with different ...
2024-08-05 | MTBLS5585 | MetaboLights
ProteomicsA novel variant of Salmonella enterica serovar Typhimurium with a rough colony morphology and multidrug resistance
Salmonella enterica serovar Typhimurium (S. Typhimurium) is a major cause of salmonellosis, with various multidrug-resistant pathovariants emerging. Here, we investigated a distinct rough colony variant with potentially enhanced environmental adaptation in China. Whole-genome sequencing of 2,212 Chi...
ORGANISM(S): Salmonella Enterica Subsp. Enterica Serovar Typhimurium Str. Lt2 
PXD047483 |
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