Identification of a High-Affinity Phosphopeptide Inhibitor of Stat3

Autor:	Zhiyong Ren, Larry A. Cabell, Timothy S. Schaefer, John S. McMurray
Rok vydání:	2003
Předmět:	Phosphopeptides STAT3 Transcription Factor Stereochemistry Peptidomimetic Clinical Biochemistry Pharmaceutical Science Antineoplastic Agents Peptide Biochemistry src Homology Domains Inhibitory Concentration 50 Structure-Activity Relationship chemistry.chemical_compound Drug Discovery Peptide synthesis Humans Structure–activity relationship Amino Acid Sequence Molecular Biology Peptide sequence Transcription factor chemistry.chemical_classification Phosphopeptide Organic Chemistry DNA DNA-Binding Proteins chemistry Docking (molecular) Trans-Activators Molecular Medicine Dimerization Protein Binding Transcription Factors
Zdroj:	Bioorganic & Medicinal Chemistry Letters. 13:633-636
ISSN:	0960-894X
DOI:	10.1016/s0960-894x(02)01050-8
Popis:	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.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::546b317e1763f40101cfa69a633851c7 https://doi.org/10.1016/s0960-894x(02)01050-8 Zobrazit plný text záznamu Full Text from ScienceDirect