Yi Liu

TL;DR: A structural analysis of binding modes of known human type II inhibitors are presented and it is demonstrated that they conform to a pharmacophore model that is currently being used to design a new generation of kinase inhibitors.

TL;DR: A highly potent and selective small-molecule ALK inhibitor, NVP-TAE684, which blocked the growth of ALCL-derived and ALK-dependent cell lines with IC50 values between 2 and 10 nM and induced down-regulation of CD30 expression, suggesting that CD30 may be used as a biomarker of therapeutic NPM-ALK kinase activity inhibition.

TL;DR: The discovery of a new class of Bcr-abl inhibitors is reported using an unbiased differential cytotoxicity screen of a combinatorial kinase-directed heterocycle library and it is proposed that this newclass of compounds inhibits BCr-abl kinase activity through an allosteric non-ATP competitive mechanism.

TL;DR: This review surveys the large number of type II inhibitors that have been developed and provides an analysis of their crystallographically determined binding modes, and demonstrates that more than 200 kinases can be targeted.

TL;DR: A general pharmacophore model of type II inhibition is described that enables a rational "hybrid-design" approach whereby a 3-trifluoromethylbenzamide functionality is appended to four distinct type I scaffolds in order to convert them into their corresponding type II counterparts.