doi: 10.1016/j.bmcl.2013.05.066.
Epub 2013 May 29.
Investigation of the protein alkylation sites of the STAT3:STAT3 inhibitor Stattic by mass spectrometry
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- PMID: 23810499
- DOI: 10.1016/j.bmcl.2013.05.066
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Investigation of the protein alkylation sites of the STAT3:STAT3 inhibitor Stattic by mass spectrometry
Bioorg Med Chem Lett.
.
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.
Keywords: Cancer; Mass spectrometry; Protein:protein interaction inhibitor; STAT3.
Copyright © 2013. Published by Elsevier Ltd.
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