Discovery of Low‐Molecular‐Weight Ligands for the AF6 PDZ Domain | Zendy

Joshi Mangesh | Zendy; Vargas Carolyn | Zendy; Boisguerin Prisca | Zendy; Diehl Annette | Zendy; Krause Gerd | Zendy; Schmieder Peter | Zendy; Moelling Karin | Zendy; Hagen Volker | Zendy; Schade Markus | Zendy; Oschkinat Hartmut | Zendy

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Discovery of Low‐Molecular‐Weight Ligands for the AF6 PDZ Domain

Author(s) -

Joshi Mangesh,

Vargas Carolyn,

Boisguerin Prisca,

Diehl Annette,

Krause Gerd,

Schmieder Peter,

Moelling Karin,

Hagen Volker,

Schade Markus,

Oschkinat Hartmut

Publication year - 2006

Publication title -

angewandte chemie international edition

Language(s) - English

Resource type - Journals

SCImago Journal Rank - 5.831

H-Index - 550

eISSN - 1521-3773

pISSN - 1433-7851

DOI - 10.1002/anie.200503965

Subject(s) - pdz domain , domain (mathematical analysis) , ligand (biochemistry) , block (permutation group theory) , chemistry , groove (engineering) , template , computer science , computational biology , nanotechnology , biology , materials science , biochemistry , mathematics , combinatorics , metallurgy , mathematical analysis , receptor

In the groove : The “drugability” of protein–protein interaction domains is still a matter of debate. The 3D structure of a complex of a small organic ligand and the AF6 PDZ domain revealed the creation of a binding pocket by the ligand (see picture). The derived compound is able to compete with a natural peptide ligand of the domain and represents a basic building block for the generation of selective PDZ inhibitors.

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