Engineering Peptide Inhibitors To Overcome PDZ Binding Promiscuity

Design of inhibitors: PDZ domains are conserved modules regulating the localization and activity of effector proteins. An integrated approach has been developed that uses peptide‐array screening technologies and fluorescence polarization measurements to analyze five promiscuous PDZ domains. By combi...

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Bibliographic Details
Published in:Angewandte Chemie International Edition 2010-12, Vol.49 (51), p.9912-9916
Main Authors: Vouilleme, Lars, Cushing, Patrick R., Volkmer, Rudolf, Madden, Dean R., Boisguerin, Prisca
Format: Article
Language:English
Subjects:
Amino Acid Sequence
CAL
Carrier Proteins - genetics
Carrier Proteins - metabolism
Cystic Fibrosis
Cystic Fibrosis Transmembrane Conductance Regulator
Drug Design
Humans
Membrane Proteins - genetics
Membrane Proteins - metabolism
PDZ domain
PDZ Domains - drug effects
peptide engineering
Peptide Library
Peptides - chemical synthesis
Peptides - pharmacology
Protein Binding - drug effects
Protein Engineering
SPOT synthesis
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Summary:Design of inhibitors: PDZ domains are conserved modules regulating the localization and activity of effector proteins. An integrated approach has been developed that uses peptide‐array screening technologies and fluorescence polarization measurements to analyze five promiscuous PDZ domains. By combining both methods, a highly specific inhibitor (iCAL3610=ANSRWPTSII) for one of the five PDZ domains was designed.
ISSN:1433-7851
1521-3773
DOI:10.1002/anie.201005575