Couto M, Mastandrea I, Cabrera M, Cabral P, Teixidor F, Cerecetto H, Vinas C. Small- molecule kinase-inhibitors-loaded boron cluster as hybrid agents for glioma-cell-target- ing therapy. Chemistry. 2017;23:9233-9238. DOI: 10.1002/chem.201701965...
Pao W and Miller VA (2005) Epidermal growth factor receptor mutations, small-molecule kinase inhibitors, and non-small-cell lung cancer: current knowledge and future directions. J Clin Oncol 23: 2556–2568 Article CAS Google Scholar Airaksinen MS and Saarma M (2002) The GDNF family: signalli...
To date, the US FDA has approved 28 small-molecule kinase inhibitors, half of which were approved in the past 3 years. While the clinical data of these approved molecules are widely presented and structure–activity relationship (SAR) has been reported for individual molecules, an updated review...
The only binding interaction observed was between TRK-A kinase and AM-5308 tested at 1 µM (Extended Data Fig. 3a). We next investigated whether our KIF18A inhibitors affected tubulin polymerization in vitro in the absence of the KIF18A motor. All four KIF18A compounds had tubulin-...
Protein Kinase InhibitorsMicrochemistryProtein Interaction MappingProtein BindingDrug DesignKinase inhibitors show great promise as a new class of therapeutics. Here we describe an efficient way to determine kinase inhibitor specificity by measuring binding of small molecules to the ATP site of kinases. We...
At least, 11 kinase inhibitors have received FDA approval to be used as cancer treatments, and there are continuous efforts to bring more candidates from laboratory benches to the clinic. Although many protein kinase inhibitors directly interact with the ATP binding site, other can alter the ...
Discovery of Novel Small-Molecule Tyrosine Kinase Inhibitors of Egfr and Her-2 by Ligand Based Virtual Screening.Pharmacophore ModelEGFRHER2ADMETDockingAbnormal signaling from the Protein tyrosine kinase (PTK) like receptor tyrosine kinase and intracellular tyrosine kinase can lead to diseases such as ...
Type I inhibitors bind to the active protein kinase conformation (DFG-Asp in, αC-helix in). Type I½ inhibitors bind to a DFG-Asp in inactive conformation while Type II inhibitors bind to a DFG-Asp out inactive conformation. Type I, I½, and type II inhibitors occupy part of the ...
The closely related casein kinase 1 epsilon (CK1e) which has a virtually identical ATP binding site has also been shown to regulate gamma-secretase activity and thus the production of toxic amyloid. Methods Using in silico modelling of the CK1d ATP binding site we have developed a series of ...
kinaseactivationandinsulinreceptorsubstrate1 serinephosphorylationinvitroandinvivo.In addition,treatmentwithbothPKRinhibitors reducedadiposetissueinflammation,improved insulinsensitivity,andimprovedglucose intoleranceinmiceaftertheestablishmentof obesityandinsulinresistance.Ourfindings ...