An unnatural amino acid that mimics phosphotyrosine.
By replacing the phosphate group in pTyr with an isoxazole carboxylic acid, a novel unnatural amino acid has been successfully synthesized. Subsequently, its incorporation into a known PPI (protein-protein interaction) inhibitor of STAT3 protein (ISS 610) generated I2 which showed reasonable anti-STAT3 activity in both fluorescence polarization and cell-proliferation experiments.
Ge
Jingyan
J
Department of Chemistry, National University of Singapore, 3 Science Drive 3, Singapore 117543.
Wu
Hao
H
Yao
Shao Q
SQ
D000596:Amino Acids / Q000737:chemistry*; D000818:Animals; D002264:Carboxylic Acids / Q000138:chemical synthesis / Q000737:chemistry; D002460:Cell Line; D049109:Cell Proliferation; D005454:Fluorescence Polarization; D006801:Humans; D007555:Isoxazoles / Q000737:chemistry; D051379:Mice; D019000:Phosphotyrosine / Q000737:chemistry*; D011485:Protein Binding; D050796:STAT3 Transcription Factor / Q000037:antagonists & inhibitors / Q000378:metabolism
D000596:Amino Acids; D002264:Carboxylic Acids; D007555:Isoxazoles; D050796:STAT3 Transcription Factor; D019000:Phosphotyrosine