Ontology highlight
ABSTRACT:
SUBMITTER: Cumaraswamy AA
PROVIDER: S-EPMC4234445 | biostudies-literature | 2014 Nov
REPOSITORIES: biostudies-literature
Cumaraswamy Abbarna A AA Lewis Andrew M AM Geletu Mulu M Todic Aleksandra A Diaz Diego B DB Cheng Xin Ran XR Brown Carla E CE Laister Rob C RC Muench David D Kerman Kagan K Grimes H Leighton HL Minden Mark D MD Gunning Patrick T PT
ACS medicinal chemistry letters 20140919 11
We herein report the design and synthesis of the first nanomolar binding inhibitor of STAT5 protein. Lead compound <b>13a</b>, possessing a phosphotyrosyl-mimicking salicylic acid group, potently and selectively binds to STAT5 over STAT3, inhibits STAT5-SH2 domain complexation events <i>in vitro</i>, silences activated STAT5 in leukemic cells, as well as STAT5's downstream transcriptional targets, including <i>MYC</i> and <i>MCL1</i>, and, as a result, leads to apoptosis. We believe <b>13a</b> r ...[more]