Lauryl gallate inhibits the activity of protein tyrosine kinase c-Src purified from human platelets

• Published in: Journal of enzyme inhibition Vol. 16; no. 6; p. 527
• Main Authors: Palacios, C, Cespón, C, Martín De La Vega, C, Roy, G, Serrano, A, Salinas, M, González-Porqué, P
• Format: Journal Article
• Language: English
• Published: Switzerland 01-01-2001
• Subjects: Animals; Blood Platelets - drug effects; Blood Platelets - enzymology; Casein Kinase II; Cyclic AMP-Dependent Protein Kinases - metabolism; Gallic Acid - analogs & derivatives; Gallic Acid - pharmacology; Humans; Intracellular Signaling Peptides and Proteins; Phosphorylation; Protein Tyrosine Phosphatase, Non-Receptor Type 6; Protein Tyrosine Phosphatases - metabolism; Protein-Serine-Threonine Kinases - metabolism; Protein-Tyrosine Kinases - antagonists & inhibitors; Protein-Tyrosine Kinases - isolation & purification; Rats; Rats, Sprague-Dawley; src-Family Kinases
• ISSN: 8755-5093
• DOI: 10.1080/14756360127567

The inhibitory effect of gallic acid (3,4,5-trihydroxybenzoic acid), and its ester derivatives methyl, propyl, octyl and lauryl has been tested on the tyrosine kinase activity of affinity purified c-Src from human platelets, using the artificial substrate Poly (Glu,Na,Tyr) 4:1. When tested as inhibitor of the autophosphorylation of the enzyme and the phosphorylation of the protein tyrosine phosphatase SHP-1 by c-Src, lauryl gallate was found to be a more potent inhibitor than other widely used protein tyrosine kinase (PTK) inhibitors such as genistein and herbimycin A. However, lauryl gallate did not inhibit the activity of the serine threonine kinases protein kinase A (PKA) and casein kinase II (CKII) from rat brain.