Design of antimicrobial compounds based on peptide structures

被引：15

作者：

Appelt, Christian ^{[1
]}

Schrey, Anna K. ^{[1
]}

Soederhaell, J. Arvid ^{[1
]}

Schmieder, Peter ^{[1
]}

机构：

[1] Leibnizinst Mol Pharmakol, FMP, D-13125 Berlin, Germany

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2007年 / 17卷 / 08期

关键词：

antimicrobial peptides; synthesis; design;

D O I：

10.1016/j.bmcl.2007.01.075

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

New antimicrobial compounds are of major importance because of the growing problem of bacterial resistance and antimicrobial peptides have been gaining a lot of interest. Their mechanism of action, however, is often obscure. Here a set of non-peptidic compounds with antimicrobial activity are presented that have been designed based on criteria derived from three-dimensional structures of antimicrobial peptides. Even though only a small set of compounds has been designed, the activity immediately matches that of the original peptides, supporting the proposed criteria for activity, i.e. not the peptidic nature of antimicrobial peptides is responsible for their activity but rather the proper arrangement of the relevant functional groups. (c) 2007 Elsevier Ltd. All rights reserved.

引用

页码：2334 / 2337

页数：4

共 10 条

[1] Interaction of the antimicrobial peptide cyclo(RRWWRF) with membranes by molecular dynamics simulations [J].

Appelt, C ;

Eisenmenger, F ;

Kühne, R ;

Schmieder, P ;

Söderhäll, JA .

BIOPHYSICAL JOURNAL, 2005, 89 (04) :2296-2306

[2] Structure of the antimicrobial, cationic hexapeptide cyclo(RRWWRF) and its analogues in solution and bound to detergent micelles [J].

Appelt, C ;

Wessolowski, A ;

Söderhäll, JA ;

Dathe, M ;

Schmieder, P .

CHEMBIOCHEM, 2005, 6 (09) :1654-1662

[3] 1H-PYRAZOLE-1-CARBOXAMIDINE HYDROCHLORIDE - AN ATTRACTIVE REAGENT FOR GUANYLATION OF AMINES AND ITS APPLICATION TO PEPTIDE-SYNTHESIS [J].

BERNATOWICZ, MS ;

WU, YL ;

MATSUEDA, GR .

JOURNAL OF ORGANIC CHEMISTRY, 1992, 57 (08) :2497-2502

[4] Cyclization increases the antimicrobial activity and selectivity of arginine- and tryptophan-containing hexapeptides [J].

Dathe, M ;

Nikolenko, H ;

Klose, J ;

Bienert, M .

BIOCHEMISTRY, 2004, 43 (28) :9140-9150

[5] Cationic peptides: a new source of antibiotics [J].

Hancock, REW ;

Lehrer, R .

TRENDS IN BIOTECHNOLOGY, 1998, 16 (02) :82-88

[6] Antibiotics at the crossroads [J].

Nathan, C .

NATURE, 2004, 431 (7011) :899-902

[7] Why is big Pharma getting out of antibacterial drug discovery? [J].

Projan, SJ .

CURRENT OPINION IN MICROBIOLOGY, 2003, 6 (05) :427-430

[8] Mechanism of the binding, insertion and destabilization of phospholipid bilayer membranes by α-helical antimicrobial and cell non-selective membrane-lytic peptides [J].

Shai, Y .

BIOCHIMICA ET BIOPHYSICA ACTA-BIOMEMBRANES, 1999, 1462 (1-2) :55-70

[9] Business and medicine - The antibiotic pipeline - Challenges, costs, and values [J].

Wenzel, RP .

NEW ENGLAND JOURNAL OF MEDICINE, 2004, 351 (06) :523-+

[10] Antimicrobial peptides of multicellular organisms [J].

Zasloff, M .

NATURE, 2002, 415 (6870) :389-395

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