| Literature DB >> 23810499 |
Sibylle Heidelberger1, Giovanna Zinzalla, Dyeison Antonow, Samantha Essex, B Piku Basu, Jonathan Palmer, Jarmila Husby, Paul J M Jackson, Khondaker M Rahman, Andrew F Wilderspin, Mire Zloh, David E Thurston.
Abstract
STAT3 (Signal Transducer and Activator of Transcription factor 3) is constitutively active in a wide range of human tumours. Stattic is one of the first non-peptidic small molecules reported to inhibit formation of the STAT3:STAT3 protein dimer complex. A mass spectrometry method has been developed to investigate the binding of Stattic to the un-phosphorylated STAT3βtc (U-STAT3) protein. Alkylation of four cysteine residues has been observed with possible reaction at a fifth which could account for the mechanism of action.Entities:
Keywords: Cancer; Mass spectrometry; Protein:protein interaction inhibitor; STAT3
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Year: 2013 PMID： 23810499 DOI： 10.1016/j.bmcl.2013.05.066
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823