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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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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cited_by cdi_FETCH-LOGICAL-c4775-d47e38ba258d3f72c28dc29214947892bce8daa66b1c210691e72fd5f941598b3
cites cdi_FETCH-LOGICAL-c4775-d47e38ba258d3f72c28dc29214947892bce8daa66b1c210691e72fd5f941598b3
container_end_page 9916
container_issue 51
container_start_page 9912
container_title Angewandte Chemie International Edition
container_volume 49
creator Vouilleme, Lars
Cushing, Patrick R.
Volkmer, Rudolf
Madden, Dean R.
Boisguerin, Prisca
description 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.
doi_str_mv 10.1002/anie.201005575
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identifier ISSN: 1433-7851
ispartof Angewandte Chemie International Edition, 2010-12, Vol.49 (51), p.9912-9916
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source Wiley
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
title Engineering Peptide Inhibitors To Overcome PDZ Binding Promiscuity
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