Eugene R. Hickey

TL;DR: A new allosteric binding site for a diaryl urea class of highly potent and selective inhibitors against human p38 MAP kinase is reported, requiring a large conformational change not observed previously for any of the protein Ser/Thr kinases.

TL;DR: In this article, the authors identify a biologically active HMTase inhibitor that allows for the transient modulation of H3K9me2 marks in mammalian chromatin and demonstrate that transient incubation of several cell lines with BIX-01294 lowers bulk H3 K 9me2 levels that are restored upon removal of the inhibitor.

TL;DR: A key binding domain that is distinct from the adenosine 5'-triphoshate (ATP) binding site is exposed when the conserved activation loop adopts a conformation permitting lipophilic and hydrogen bonding interactions between this class of inhibitors and the protein.

TL;DR: Analysis of the reported Pim-1 kinase-domain structures leads to a hypothesis as to how Pim kinase activity might be regulated in vivo.

TL;DR: In this article, novel aromatic heterocyclic compounds of formula (I) wherein Ar1,Ar2,L,Q and X are described are described. And processes of making such compounds are also disclosed.