Design and synthesis of triazole-based peptidomimetics of a PSD-95 PDZ domain inhibitor
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Design and synthesis of triazole-based peptidomimetics of a PSD-95 PDZ domain inhibitor. / Bach, Anders; Pedersen, Thomas B.; Strømgaard, Kristian.
In: MedChemComm, Vol. 7, No. 3, 2016, p. 531-536.Research output: Contribution to journal › Journal article › Research › peer-review
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TY - JOUR
T1 - Design and synthesis of triazole-based peptidomimetics of a PSD-95 PDZ domain inhibitor
AU - Bach, Anders
AU - Pedersen, Thomas B.
AU - Strømgaard, Kristian
PY - 2016
Y1 - 2016
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
M3 - Journal article
VL - 7
SP - 531
EP - 536
JO - MedChemComm
JF - MedChemComm
SN - 2040-2503
IS - 3
ER -
ID: 154053805