Work

A Small Molecular Scaffold for Selective Inhibition of Wip1 Phosphatase

Year: 2007

Type: article

Abstract: 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.

Source: ChemMedChem

DOI: 10.1002/cmdc.200700281

Authors: Jeong Bang, Hiroshi Yamaguchi, Stewart R. Durell, Ettore Appella, Daniel H. Appella

Institutions: National Cancer Institute, United States Department of Health and Human Services, National Institutes of Health, National Institute of Diabetes and Digestive and Kidney Diseases

Language: English

Topic: Protein Tyrosine Phosphatases

Subfield: Molecular Biology

Field: Biochemistry, Genetics and Molecular Biology

Domain: Life Sciences

Open Access status: green

Funder: National Institutes of Health

Award: G9000236431