Discovery and Optimization of the First ATP Competitive Type-III c-MET Inhibitor
Iacovos N. Michaelides, Gavin W. Collie, Ulf Börjesson, Christina Vasalou, Omar Alkhatib, Louise Barlind, Tony Cheung, Ian L. Dale, Kevin J. Embrey, Edward J. Hennessy, Puneet Khurana, Cheryl M. Koh, Michelle L. Lamb, Jianming Liu, Tom Moss, Daniel O’Neill, Christopher Phillips, Joseph Shaw, Arjan Snijder, Richard Storer, Christopher J. Stubbs, Fujin Han, Chengzhi Li, Jingchuan Qiao, Dongqing Sun, Jingwen Wang, Peng Wang, Wenzhen Yang
Abstract
studies with promising free-brain exposures, paving the way for the design of brain permeable drugs for the treatment of c-MET driven cancers.
Topics & Concepts
ChemistryIn vivoMutantEnzyme inhibitorDrug discoveryPharmacokineticsPharmacologyEnzymeDrugLigand efficiencyKinaseLead compoundBiochemistryLigand (biochemistry)In vitroReceptorMedicineBiotechnologyGeneBiologyEnzyme function and inhibitionPI3K/AKT/mTOR signaling in cancerSynthesis and biological activity