Unversität Zürich

Polyphor Ltd.

Universitaet Zuerich

Sergio Locurio

Daniel Obrecht

Frank Gombert

Christian Ludin

Jan Wim Vrijbloed

Françoise Jung

John Anthony Robinson

Alexander Lederer

Francoise Jung

Shivaprasad Shankaramma

Frank Otto Gombert

A method of screening for template-fixed &#x3b2;-hairpin mimetics and libraries including a plurality of these mimetics is provided. The template-fixed &#x3b2;-hairpin mimetics are of the following general formula:R-Cys-Z-Cys-R&#x2003;&#x2003;Iwherein the two cysteine residues are bridged by a disulfide bond, thereby forming a cyclic peptide; Rand Rare di- or tripeptide moieties of certain types, as defined herein; and Z is a chain of n amino acid residues with n being an integer from 4 to 20 and with each of these n amino acid residues being, independently, derived from any naturally occurring L-&#x3b1;-amino acid.

Template fixed beta-hairpin loop mimetics and their use in phage display

Template-fixed &#x3b2;-hairpin mimetics and libraries including a plurality of these mimetics are provided. The template-fixed &#x3b2;-hairpin mimetics are of the following general formula:R-Cys-Z-Cys-R&#x2003;&#x2003;Iwherein the two cysteine residues are bridged by a disulfide bond, thereby forming a cyclic peptide; Rand Rare di- or tripeptide moieties of certain types, as defined herein; and Z is a chain of n amino acid residues with n being an integer from 4 to 20 and with each of these n amino acid residues being, independently, derived from any naturally occurring L-&#x3b1;-amino acid.

Template fixed &#x3b2;-hairpin loop mimetics and their use in phage display

Template-fixed &#x3b2;-hairpin mimetics and libraries including a plurality of these mimetics are provided. The template-fixed &#x3b2;-hairpin mimetics are of the following general formula:R-Cys-Z-Cys-R&#x2003;&#x2003;(I)wherein the two cysteine residues are bridged by a disulfide bond, thereby forming a cyclic peptide; Rand Rare di- or tripeptide moieties of certain types, as defined herein; and Z is a chain of n amino acid residues with n being an integer from 4 to 20 and with each of these n amino acid residues being, independently, derived from any naturally occurring L-&#x3b1;-amino acid.

Template-fixed &#x3b2;-hairpin peptidomimetics of the general formula (I), wherein Z is a template-fixed chain of 12 &#x3b1;-amino acid residues which, depending on their positions in the chain (counted starting from the N-terminal amino acid) are Gly or Pro, or of certain types, at least one of these residues being of the type of N-substituted glycines, which types, as the remaining symbols in the above formula, are defined in the description and the claims, and salts thereof, have the property to inhibit the growth of or to kill microorganisms. They can be used as disinfectants for foodstuffs, cosmetics, medicaments or other nutrient-containing materials or as medicaments to treat or prevent infections. These &#x3b2;-hairpin peptidomimetics can be manufactured by processes which are based on a mixed solid- and solution phase synthetic strategy. 

Template-fixed peptidomimetics with antimicrobial activity

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Sergio Locurio