Peptidomimetic Inhibitors of Extracellular Aspartic Proteinases of Candida albicans and Candida tropicalis

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Title:Peptidomimetic Inhibitors of Extracellular Aspartic Proteinases of Candida albicans and Candida tropicalis
Creators:
Brožková, Kateřina
Křížová, Ivana
Pavlíčková, Libuše
Hradilek, Martin
Fusek, Martin
Ruml, Tomáš
Souček, Milan
Pichová, Iva
Journal or Publication Title:
Collection of Czechoslovak Chemical Communications, 64, 1, pp. 130-137
Uncontrolled Keywords:Peptides, Peptide inhibitors, Secreted aspartic proteinases, <i>Candida</i> <i>tropicalis</i>, Subsite specificity, <i>Candida</i> <i>albicans</i>, Peptide bond isosteres, Peptidomimetics

Abstract

In an attempt to develop effective inhibitors of <i>Candida</i> secreted aspartic proteinases, we have prepared a series of <i>N</i>-protected peptides varying in the type of scissile bond replacement, in the P and P' side chains as well as in the N- and C-terminal modifications. The compounds were tested <i>in vitro</i> with the chromogenic peptide substrate using purified secreted proteinases of <i>C. albicans</i> and <i>C. tropicalis</i>. Our results have confirmed that the binding of inhibitors and their effectiveness is influenced by a number of enzyme-inhibitor interactions. Moreover, factors like solvation/desolvation contribute to the optimal binding energy of the inhibitors. <p>

Title:Peptidomimetic Inhibitors of Extracellular Aspartic Proteinases of Candida albicans and Candida tropicalis
Creators:
Brožková, Kateřina
Křížová, Ivana
Pavlíčková, Libuše
Hradilek, Martin
Fusek, Martin
Ruml, Tomáš
Souček, Milan
Pichová, Iva
Uncontrolled Keywords:Peptides, Peptide inhibitors, Secreted aspartic proteinases, <i>Candida</i> <i>tropicalis</i>, Subsite specificity, <i>Candida</i> <i>albicans</i>, Peptide bond isosteres, Peptidomimetics
Divisions:Life and Chemical Sciences > Institute of Organic Chemistry and Biochemistry > Collection of Czechoslovak Chemical Communications
Journal or Publication Title:Collection of Czechoslovak Chemical Communications
Volume:64
Number:1
Page Range:pp. 130-137
ISSN:0010-0765
E-ISSN:1212-6950
Publisher:Institute of Organic Chemistry and Biochemistry
Related URLs:
URLURL Type
http://dx.doi.org/10.1135/cccc19990130UNSPECIFIED
ID Code:1463
Item Type:Article
Deposited On:06 Feb 2009 17:09
Last Modified:06 Feb 2009 16:09

Citation

Brožková, Kateřina; Křížová, Ivana; Pavlíčková, Libuše; Hradilek, Martin; Fusek, Martin; Ruml, Tomáš; Souček, Milan; Pichová, Iva (1999) Peptidomimetic Inhibitors of Extracellular Aspartic Proteinases of Candida albicans and Candida tropicalis. Collection of Czechoslovak Chemical Communications, 64 (1). pp. 130-137. ISSN 0010-0765

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