INHIBITION OF FARNESYL-PROTEIN TRANSFERASE BY NEW FARNESYL PHOSPHONATE DERIVATIVES OF PHENYLALANINE

Authors
LAMOTHE M PERRIN D BLOTIERES D LEBORGNE M GRAS S BONNET D HILL BT HALAZY S
Citation
M. Lamothe et al., INHIBITION OF FARNESYL-PROTEIN TRANSFERASE BY NEW FARNESYL PHOSPHONATE DERIVATIVES OF PHENYLALANINE, Bioorganic & medicinal chemistry letters, 6(12), 1996, pp. 1291-1296
Citations number
35
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
6
Issue
12
Year of publication
1996
Pages
1291 - 1296
Database
ISI
SICI code
0960-894X(1996)6:12<1291:IOFTBN>2.0.ZU;2-I
Abstract
New farnesyl phosphonate derivatives of phenylalanine have been prepar ed as inhibitors of farnesyl-protein transferase (FPT). Enzyme inhibit ion studies with bovine brain FPT and rat liver squalene synthase show that compound <(3a)under bar> is a new, potent and selective FPT inhi bitor. Moreover, structural modifications from <(3a)under bar> have pr ovided some useful information concerning the key structural subunits necessary for optimum and selective FPT inhibition. Copyright (C) 1996 Elsevier Science Ltd