Ontology highlight
ABSTRACT:
SUBMITTER: Morlacchi P
PROVIDER: S-EPMC4027771 | biostudies-literature | 2014 Jan
REPOSITORIES: biostudies-literature
Morlacchi Pietro P Mandal Pijus K PK McMurray John S JS
ACS medicinal chemistry letters 20131204 1
An improved synthesis of a phosphopeptidomimetic prodrug targeting the Src Homology 2 (SH2) domain of signal transducer and activator of transcription 6 (STAT6) is reported. In our convergent methodology, we employed a phosphotyrosine surrogate active ester harboring pivaloyloxymethyl groups, which efficiently coupled to tert-butylglycinyl proline diarylamide. Biological evaluation of 1 has not been reported. We show that it inhibits STAT6 phosphorylation in intact human bronchial epithelial cel ...[more]