Identification of a high-affinity phosphopeptide inhibitor of Stat3

Z Ren, LA Cabell, TS Schaefer, JS McMurray - Bioorganic & medicinal …, 2003 - Elsevier
Z Ren, LA Cabell, TS Schaefer, JS McMurray
Bioorganic & medicinal chemistry letters, 2003Elsevier
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.
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.
Elsevier