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Synthesis and biological evaluation of lipophilic Ca(1)a(2)L analogues as potential bisubstrate inhibitors of protein:geranylgeranyl transferase-1.
- Source :
-
Bioorganic & medicinal chemistry [Bioorg Med Chem] 2005 Mar 01; Vol. 13 (5), pp. 1463-75. - Publication Year :
- 2005
-
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.
- Subjects :
- Dipeptides chemistry
Enzyme Inhibitors chemistry
Magnetic Resonance Spectroscopy
Mass Spectrometry
Substrate Specificity
Alkyl and Aryl Transferases antagonists & inhibitors
Dipeptides chemical synthesis
Dipeptides pharmacology
Enzyme Inhibitors chemical synthesis
Enzyme Inhibitors pharmacology
Subjects
Details
- Language :
- English
- ISSN :
- 0968-0896
- Volume :
- 13
- Issue :
- 5
- Database :
- MEDLINE
- Journal :
- Bioorganic & medicinal chemistry
- Publication Type :
- Academic Journal
- Accession number :
- 15698762
- Full Text :
- https://doi.org/10.1016/j.bmc.2004.12.035