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Bioorg Med Chem Lett. 2003 Feb 24;13(4):633-6.

Identification of a high-affinity phosphopeptide inhibitor of Stat3.

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  • 1Department of Neuro-Surgery, The University of Texas M. D. Anderson Cancer Center, 1515 Holcombe Boulevard, Houston, TX 77030, USA.


Stat3 is a latent transcription factor that exhibits elevated activity in a variety of human cancers. To find a lead peptide for peptidomimetic drug development we synthesized and tested phosphopeptides derived from known receptor docking sites and found Y(p)LPQTV as the optimal sequence. SAR studies showed that each residue from pY to pY+3 provided binding energy.

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