Synthesis and structure-activity relationship of liposomal substrates for phospholipase A(2)

Helene Marie-France Viart, Mads Hartvig Clausen

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Abstract

A recent innovation in the use of liposomes as drug delivery systems consists of covalently attaching an anticancer drug at the sn-2 position of phospholipids. However, some of those lipids could not be hydrolyzed by sPLA2. Steric bulk in the vicinity of the sn-2 position appears to prevent hydrolysis of the substrate. Structurally different lipids have been synthesized and formulated as liposomes, subjected to sPLA2 and the hydrolysis rates have been compared to Molecular Dynamics simulations of the enzyme/substrate complexes.
Original languageEnglish
JournalABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY
Volume242
Pages (from-to)MEDI 344
ISSN0065-7727
Publication statusPublished - 2011
Event242nd National Meeting of the American-Chemical-Society (ACS) - Denver, CO, United States
Duration: 28 Aug 20111 Sep 2011
Conference number: 242
http://cen.acs.org/articles/89/i26/242nd-ACS-National-Meeting.html

Conference

Conference242nd National Meeting of the American-Chemical-Society (ACS)
Number242
Country/TerritoryUnited States
CityDenver, CO
Period28/08/201101/09/2011
Internet address

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