78287-71-5Relevant academic research and scientific papers
Thiazole- and imidazole-containing peptidomimetic inhibitors of protein farnesyltransferase
Bolchi, Cristiano,Pallavicini, Marco,Bernini, Sergio K.,Chiodini, Giuseppe,Corsini, Alberto,Ferri, Nicola,Fumagalli, Laura,Straniero, Valentina,Valoti, Ermanno
experimental part, p. 5408 - 5412 (2011/10/12)
Mimetics of the C-terminal CAAX tetrapeptide of Ras protein were designed replacing internal dipeptide AA with 4-amino-2-phenylbenzoic acid and cysteine (C) with 2-amino-4-thiazolyl-, 2-mercapto-4-thiazolyl-, 2-mercapto-4-imidazolyl- and 2-methylmercapto-4-thiazolyl-acetic or propionic acid. The compound in which C is replaced by 2-amino-4-thiazolylacetic acid inhibited FTase activity in the low nanomolar range and showed antiproliferative effect on rat aortic smooth muscle cells interfering with Ras farnesylation. On the basis of these results, 2-aminothiazole can be considered as an alternative to heterocycles, such as pyridine and imidazole, normally used in FTase inhibitors designed as non-thiol CAAX mimetics.
