Design and synthesis of phosphotyrosine mimetics.
Selective inhibitors of protein tyrosine phosphatases (PTPases) are of great interest as therapeutic agents and research tools. Several phenylalanine derivatives (1, 2) designed as phosphotyrosine mimetics or irreversible active site inhibitors were successfully synthesized, then incorporated into a combinatorial library based on a peptidomimetic beta-strand template.
Yan
Zheng
Z
Molecumetics Ltd., 2023 120th Ave. N.E., Bellevue, WA 98005-2199, USA.
Kahn
Michael
M
Qabar
Maher
M
Urban
Jan
J
Kim
Hwa-Ok
HO
Blaskovich
Mark A
MA
D040761:Biomimetic Materials / Q000138:chemical synthesis; D020650:Combinatorial Chemistry Techniques / Q000379:methods; D015195:Drug Design; D004791:Enzyme Inhibitors / Q000138:chemical synthesis / Q000494:pharmacology; D019151:Peptide Library; D010649:Phenylalanine / Q000031:analogs & derivatives / Q000494:pharmacology; D019000:Phosphotyrosine / Q000031:analogs & derivatives* / Q000138:chemical synthesis*; D017433:Protein Structure, Secondary; D017027:Protein Tyrosine Phosphatases / Q000037:antagonists & inhibitors; D013329:Structure-Activity Relationship
D004791:Enzyme Inhibitors; D019151:Peptide Library; D019000:Phosphotyrosine; D010649:Phenylalanine; D017027:Protein Tyrosine Phosphatases