Peptidyl aldehydes as slow-binding inhibitors of dual-specificity phosphatases.
Peptidyl aldehydes were tested for inhibition of dual-specificity phosphatases VH1 and VHR. The most potent compound, cinnamaldehyde-Gly-Glu-Glu (Cinn-GEE), acted as a slow-binding inhibitor with K(I)* values of 18 and 288 microM against VH1 and VHR, respectively.
Park
Junguk
J
Department of Chemistry, The Ohio State University, 100 West 18th Avenue, Columbus, OH 43210, USA.
Fu
Hua
H
Pei
Dehua
D
D000171:Acrolein / Q000031:analogs & derivatives* / Q000737:chemistry / Q000378:metabolism* / Q000494:pharmacology*; D000972:Antineoplastic Agents, Phytogenic / Q000737:chemistry / Q000378:metabolism* / Q000494:pharmacology*; D001665:Binding Sites; D054640:Dual Specificity Phosphatase 3; D054637:Dual-Specificity Phosphatases; D004791:Enzyme Inhibitors / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology; D006801:Humans; D010446:Peptide Fragments / Q000737:chemistry / Q000378:metabolism* / Q000494:pharmacology*; D017027:Protein Tyrosine Phosphatases / Q000037:antagonists & inhibitors* / Q000378:metabolism
D000972:Antineoplastic Agents, Phytogenic; D004791:Enzyme Inhibitors; D010446:Peptide Fragments; D000171:Acrolein; C489855:dual specificity phosphatase 12; C517025:DUSP3 protein, human; D054640:Dual Specificity Phosphatase 3; D054637:Dual-Specificity Phosphatases; D017027:Protein Tyrosine Phosphatases; C012843:cinnamaldehyde