Novel STAT3 small-molecule inhibitors identified by structure-based virtual ligand screening incorporating SH2 domain flexibility

Efforts to develop STAT3 inhibitors have focused on its SH2 domain starting with short phosphotyrosylated peptides based on STAT3 binding motifs, e.g. pY905LPQTV within gp130. Despite binding to STAT3 with high affinity, issues regarding stability, bioavailability, and membrane permeability of these...

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Veröffentlicht in:	Pharmacological research 2021-07, Vol.169, p.105637-105637, Article 105637
Hauptverfasser:	Kong, Ren, Bharadwaj, Uddalak, Eckols, T. Kris, Kolosov, Mikhail, Wu, Haoyi, Cruz-Pavlovich, Francisco J. Santa, Shaw, Alison, Ifelayo, Oluwatomilona I., Zhao, Hong, Kasembeli, Moses M., Wong, Stephen T.C., Tweardy, David J.
Format:	Artikel
Sprache:	eng
Schlagworte:	Alkylation Binding Sites - drug effects Blotting, Western Cell Line, Tumor - drug effects Drug Evaluation, Preclinical - methods Gas Chromatography-Mass Spectrometry Humans Ligands Molecular Docking Simulation Protein Structure, Tertiary src Homology Domains - drug effects STAT3 Transcription Factor - antagonists & inhibitors STAT3 Transcription Factor - chemistry STAT3 Transcription Factor - genetics Structure-Activity Relationship Surface Plasmon Resonance
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