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A Small Molecular Scaffold for Selective Inhibition of Wip1 Phosphatase
Author(s) -
Bang Jeong,
Yamaguchi Hiroshi,
Durell Stewart R.,
Appella Ettore,
Appella Daniel H.
Publication year - 2008
Publication title -
chemmedchem
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.817
H-Index - 100
eISSN - 1860-7187
pISSN - 1860-7179
DOI - 10.1002/cmdc.200700281
Subject(s) - chemistry , microbiology and biotechnology , library science , biology , computer science
Inhibiting Wip1. Using a pyrrole‐based scaffold, we developed a series of small molecules that mimic the three‐dimensional arrangement of the polar and hydrophobic functional groups of the best cyclic peptide inhibitor. Iterative optimization cycles of design, synthesis, and kinetic testing has lead to a selective inhibitor of Wip1. The picture shows the structure of the best inhibitor bound to the active site of the enzyme.