Design and synthesis of triazole-based peptidomimetics of a PSD-95 PDZ domain inhibitor

Anders Bach; Thomas B. Pedersen; Kristian Strømgaard

doi:10.1039/C5MD00445D

Design and synthesis of triazole-based peptidomimetics of a PSD-95 PDZ domain inhibitor

Anders Bach, Thomas B. Pedersen, Kristian Strømgaard

4 Citations (Scopus)

73 Downloads (Pure)

Abstract

PSD-95 PDZ domains are biologically important and promising drug targets. Here, we discover a triazole-based peptidomimetic, 10, by ‘click chemistry’. Compound 10 inhibits the PDZ2/GluN2B interaction with affinity similar to tripeptide SAV and better than current small-molecules. Thus, 10 represents a new class of PSD-95 PDZ inhibitors.

Original language	English
Journal	MedChemComm
Volume	7
Issue number	3
Pages (from-to)	531-536
Number of pages	6
ISSN	2040-2503
DOIs	https://doi.org/10.1039/C5MD00445D
Publication status	Published - 1 Mar 2016

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10.1039/C5MD00445DLicence: CC BY

Design and synthesis of triazole-based peptidomimetics of a PSD-95 PDZ domain inhibitorFinal published version, 1.54 MBLicence: CC BY

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title = "Design and synthesis of triazole-based peptidomimetics of a PSD-95 PDZ domain inhibitor",

abstract = "PSD-95 PDZ domains are biologically important and promising drug targets. Here, we discover a triazole-based peptidomimetic, 10, by {\textquoteleft}click chemistry{\textquoteright}. Compound 10 inhibits the PDZ2/GluN2B interaction with affinity similar to tripeptide SAV and better than current small-molecules. Thus, 10 represents a new class of PSD-95 PDZ inhibitors.",

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AU - Pedersen, Thomas B.

AU - Strømgaard, Kristian

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N2 - PSD-95 PDZ domains are biologically important and promising drug targets. Here, we discover a triazole-based peptidomimetic, 10, by ‘click chemistry’. Compound 10 inhibits the PDZ2/GluN2B interaction with affinity similar to tripeptide SAV and better than current small-molecules. Thus, 10 represents a new class of PSD-95 PDZ inhibitors.

AB - PSD-95 PDZ domains are biologically important and promising drug targets. Here, we discover a triazole-based peptidomimetic, 10, by ‘click chemistry’. Compound 10 inhibits the PDZ2/GluN2B interaction with affinity similar to tripeptide SAV and better than current small-molecules. Thus, 10 represents a new class of PSD-95 PDZ inhibitors.

U2 - 10.1039/C5MD00445D

DO - 10.1039/C5MD00445D

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JO - MedChemComm

JF - MedChemComm

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Design and synthesis of triazole-based peptidomimetics of a PSD-95 PDZ domain inhibitor

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