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ARGININE-TERMINATED ANTIMICROBIAL PEPTIDES WITH DENDRIMERIC STRUCTURE |
Jolanta Janiszewska 1, Zofia UrbaĆczyk-Lipkowska 2 |
1. Industrial Chemistry Research Institute (ICRI), Rydygiera 8, Warszawa 01-793, Poland |
Abstract |
Recently, antimicrobial properties of dendrimeric peptides designed as branched analogs of natural linear peptides of various defence systems have been discovered [1]. Biological tests against Gram-positive (S. aureus), Gram-negative (E. coli) and C. albicans as well as cytotoxicity studies showed that better properties have compounds with higher degree of branching ("dendrimeric effect") [2]. In order to follow their interactions with biological membranes a library of dendrimeric peptides including amino acids of L- and D-chirality was synthesized by stepwise solid phase synthesis (AA1: L- or D-Lys, AA2: L- or D-Arg, or Z-L-Arg , Z-D-Arg). Antimicrobial tests showed higher potency of Z-protected derivatives. On the other side, isomeric compounds differ by configuration of amino acids expressed similar activity. This strongly suggested that so called "carpet mechanism" is the dominating interaction between microbial membranes and dendrimeric peptides. This project was supported by grant No. 3T09B 115 28 from the Ministry of Education and Science. 1. Janiszewska J, Swieton J, Lipkowski AW, Urbanczyk-Lipkowska Z., Bioorg. Med. Chem. Lett .2003, 13, 3711-3713. 2. Intern. J. Pharmaceutics, Klajnert B., J. Janiszewska, Urbanczyk-Lipkowska Z, Bryszewska M., Shcharbin D., Labieniec M., 2006, 309, 208-217. |
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Presentation: Poster at V Multidyscyplinarna Konferencja Nauki o Leku, by Jolanta JaniszewskaSee On-line Journal of V Multidyscyplinarna Konferencja Nauki o Leku Submitted: 2006-03-01 07:51 Revised: 2009-06-07 00:44 |