ISSN:
1075-2617
Keywords:
lipopeptides
;
lipid mimetics
;
synthesis
;
phospholipase A2
;
inhibition
;
monolayer
;
Chemistry
;
Biochemistry and Biotechnology
Source:
Wiley InterScience Backfile Collection 1832-2000
Topics:
Chemistry and Pharmacology
Notes:
Lipid mimetics, synthetic molecules that resemble natural lipids either structurally or functionally, have been developed as potential medicinal substances. They have been successfully applied in the development of drug and peptide delivery systems and for the development of inhibitors or lipid metabolizing enzymes. Phospholipase A2 is considered to be involved as the rate-limiting step in the production of lipid mediators of inflammatory responses and, as such, it has been a target for drug design. A series of lipid mimetics including lipopeptides, amides and alcohols of lipidic α-amino acids, have been tested by bulk and monolayer assay techniques. The findings suggested the direct interaction of the tested compounds with porcine pancreatic phospholipase A2. The inactivation of the enzyme occurred in a competitive manner. The most active compound 1 (2-amino-N-hexadecyl-L-hexanamide) showed an apparent IC50 of 12 μ M and inhibitory power Z=13 in the monolayer assay. © 1997 European Peptide Society and John Wiley & Sons, Ltd.
Additional Material:
2 Tab.
Type of Medium:
Electronic Resource
