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Identification of Pyridinylpyrimidines as Inhibitors of Human Methionine Aminopeptidases
Author(s) -
Hu Xiaoyi,
Addlagatta Anthony,
Matthews Brian W.,
Liu Jun O.
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.200600757
Subject(s) - methionine , aminopeptidase , identification (biology) , biochemistry , cell culture , chemistry , high throughput screening , cancer cell , biology , amino acid , cancer , leucine , genetics , botany
High‐throughput screening of a library of compounds has led to the identification of a new structural class of human methionine aminopeptidases inhibitors. They inhibited the processing of 14‐3‐3γ in cells and blocked proliferation of both endothelial cells and transformed cancer cell lines. The picture shows the crystal structure of the complex of one inhibitor (yellow) with the type 1 human methionine aminopeptidase (blue Co II , red H 2 O).

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