Design, synthesis, and evaluation of sugar amino acid based inhibitors of protein prenyl transferases PFT and PGGT-1.
J Med Chem
; 47(16): 3920-3, 2004 Jul 29.
Article
em En
| MEDLINE
| ID: mdl-15267228
ABSTRACT
Eleven analogues of the C-terminal Ca(1)a(2)X motif found in natural substrates of the prenyl transferases PFT and PGGT-1 were synthesized and evaluated for their inhibition potency and selectivity against PFT and PGGT-1. Replacement of the central dipeptide part a(1)a(2) by a benzylated sugar amino acid resulted in a good and highly selective PFT inhibitor (8, IC(50) = 250 +/- 20 nM). The methyl ester of 8 (13) selectively inhibited protein farnesylation in cultured cells.
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Base de dados:
MEDLINE
Assunto principal:
Açúcares Ácidos
/
Alquil e Aril Transferases
/
Aminoácidos
Idioma:
En
Ano de publicação:
2004
Tipo de documento:
Article