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Design and Synthesis of Conformationally Constrained Cyclophilin Inhibitors Showing a Cyclosporin-A Phenotype in C. elegans

Dunsmore, Colin J; Malone, Kirk J; Bailey, Kevin R; Wear, Martin A; Florance, Hannah; Shirran, Sally; Barran, Perdita E; Page, Antony P; Walkinshaw, Malcolm D; Turner, Nicholas J

Chembiochem. 2011;12(5):802-810.

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Abstract

Cyclophilin A (CypA) is a member of the immunophilin family of proteins and receptor for the immunosuppressant drug cyclosporin A (CsA). Here we describe the design and synthesis of a new class of small-molecule inhibitors for CypA that are based upon a dimedone template. Electrospray mass spectrometry is utilised as an initial screen to quantify the protein affinity of the ligands. Active inhibitors and fluorescently labelled derivatives are then used as chemical probes for investigating the biological role of cyclophilins in the nematode Caenorhabditis elegans.

Bibliographic metadata

Type of resource:
Content type:
Published date:
Journal title:
ISSN:
Volume:
12
Issue:
5
Start page:
802
End page:
810
Total:
9
Pagination:
802-810
Digital Object Identifier:
10.1002/cbic.201000413
ISI Accession Number:
WOS:000288563000021
Related website(s):
  • Related website <Go to ISI>://WOS:000288563000021
General notes:
  • Times Cited: 0
Access state:
Active

Institutional metadata

University researcher(s):

Record metadata

Manchester eScholar ID:
uk-ac-man-scw:150586
Created by:
Turner, Nicholas
Created:
14th January, 2012, 14:38:12
Last modified by:
Turner, Nicholas
Last modified:
14th January, 2012, 14:38:12

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