Synthesis and biological evaluation of lipophilic Ca(1)a(2)L analogues as potential bisubstrate inhibitors of protein:geranylgeranyl transferase-1.
Bioorg Med Chem
; 13(5): 1463-75, 2005 Mar 01.
Article
em En
| MEDLINE
| ID: mdl-15698762
ABSTRACT
Ca(1)a(2)L analogues, having the central dipeptide a(1)a(2) replaced by a sugar amino acid, were provided at the N-terminal end directly or via a spacer with a lipid. The inhibitory potency toward PGGT-1 of the set of lipophilic Ca(1)a(2)L analogues was improved in comparison with the original analogues, 1 and 2. The most potent inhibitors, 39 and 40, were found to inhibit PGGT-1 with an IC(50)-value of 12.7 and 12.3 microM, respectively, which is a 6-fold improvement over the corresponding analogue 1.
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Base de dados:
MEDLINE
Assunto principal:
Alquil e Aril Transferases
/
Dipeptídeos
/
Inibidores Enzimáticos
Idioma:
En
Ano de publicação:
2005
Tipo de documento:
Article