Lipopeptides for the fragment-based pharmaceutics design

Ziora, Zyta M., Wimmer, Norbert, New, Roger, Skwarczynski, Mariusz and Toth, Istvan (2012) Lipopeptides for the fragment-based pharmaceutics design. International Journal of Organic Chemistry, 2 75-81. doi:10.4236/ijoc.2012.21013

Author Ziora, Zyta M.
Wimmer, Norbert
New, Roger
Skwarczynski, Mariusz
Toth, Istvan
Title Lipopeptides for the fragment-based pharmaceutics design
Journal name International Journal of Organic Chemistry   Check publisher's open access policy
ISSN 2161-4687
Publication date 2012-03
Sub-type Article (original research)
DOI 10.4236/ijoc.2012.21013
Open Access Status DOI
Volume 2
Start page 75
End page 81
Total pages 7
Place of publication Irvine, CA, United States
Publisher Scientific Research Publishing
Collection year 2013
Language eng
Formatted abstract
This paper describes the synthesis of peptide fragments for use in a new type of combinatorial discovery technology, in which the building blocks are brought together by non-covalent interactions, rather than direct chemical bonding. The building blocks of interest—in this case different amino acids—are converted to amphiphiles by attachment to lipid tails. The amphiphiles, when mixed together in aqueous phase, are designed so that they aggregate spontaneously to form micelles. The building blocks form the headgroups of each of the amphiphiles, and these headgroups cover the surface of the micelle in a dynamic close-packed fluid mosaic array. These building blocks come together so closely that two- or three-dimensional structures are created on the surface of the micelles, and these can be screened in biological assays to find out which combination of building blocks is able to elicit a biological response. Lipopeptides consisting of two residues of lipoamino acid and other amino acids moieties have been designed, synthesized, characterized and the abil-ity of these constructs to form supra-molecular assemblies is demonstrated.
Keyword Lipoamino acids
Fragment based design
Supra-molecular assemby
Q-Index Code C1
Q-Index Status Confirmed Code
Institutional Status UQ

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Created: Wed, 20 Jun 2012, 12:06:37 EST by Professor Istvan Toth on behalf of School of Pharmacy