| dc.contributor.author |
Nicolaou, A |
en |
| dc.contributor.author |
Kokotos, G |
en |
| dc.contributor.author |
Constantinou-Kokotou, V |
en |
| dc.contributor.author |
Charitos, C |
en |
| dc.contributor.author |
Noula, C |
en |
| dc.contributor.author |
Verger, R |
en |
| dc.contributor.author |
Gibbons, WA |
en |
| dc.date.accessioned |
2014-06-06T06:43:25Z |
|
| dc.date.available |
2014-06-06T06:43:25Z |
|
| dc.date.issued |
1997 |
en |
| dc.identifier.issn |
10752617 |
en |
| dc.identifier.uri |
http://62.217.125.90/xmlui/handle/123456789/1261 |
|
| dc.relation.uri |
http://www.scopus.com/inward/record.url?eid=2-s2.0-0031181702&partnerID=40&md5=93d79035be1a1b2003c3f28f2cc51b17 |
en |
| dc.subject |
Inhibition |
en |
| dc.subject |
Lipid mimettcs |
en |
| dc.subject |
Lipopeptides |
en |
| dc.subject |
Monolayer |
en |
| dc.subject |
Phospholipase A2 |
en |
| dc.subject |
Synthesis |
en |
| dc.subject.other |
enzyme inhibitor |
en |
| dc.subject.other |
lipid |
en |
| dc.subject.other |
lipoprotein |
en |
| dc.subject.other |
peptide |
en |
| dc.subject.other |
phospholipase A |
en |
| dc.subject.other |
animal |
en |
| dc.subject.other |
article |
en |
| dc.subject.other |
chemistry |
en |
| dc.subject.other |
drug antagonism |
en |
| dc.subject.other |
enzymology |
en |
| dc.subject.other |
fast atom bombardment mass spectrometry |
en |
| dc.subject.other |
molecular mimicry |
en |
| dc.subject.other |
nuclear magnetic resonance spectroscopy |
en |
| dc.subject.other |
pancreas |
en |
| dc.subject.other |
swine |
en |
| dc.subject.other |
synthesis |
en |
| dc.subject.other |
Animals |
en |
| dc.subject.other |
Enzyme Inhibitors |
en |
| dc.subject.other |
Lipids |
en |
| dc.subject.other |
Lipoproteins |
en |
| dc.subject.other |
Magnetic Resonance Spectroscopy |
en |
| dc.subject.other |
Molecular Mimicry |
en |
| dc.subject.other |
Pancreas |
en |
| dc.subject.other |
Peptides |
en |
| dc.subject.other |
Phospholipases A |
en |
| dc.subject.other |
Spectrometry, Mass, Fast Atom Bombardment |
en |
| dc.subject.other |
Swine |
en |
| dc.title |
Synthesis and properties of novel lipopeptides and lipid mimetics |
en |
| heal.type |
journalArticle |
en |
| heal.publicationDate |
1997 |
en |
| heal.abstract |
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 μM and inhibitory power Z= 13 in the monolayer assay. © 1997 European Peptide Society and John Wiley & Sons, Ltd. |
en |
| heal.journalName |
Journal of Peptide Science |
en |
| dc.identifier.issue |
4 |
en |
| dc.identifier.volume |
3 |
en |
| dc.identifier.spage |
291 |
en |
| dc.identifier.epage |
298 |
en |