Title of article
Crystal structure of human ERK2 complexed with a pyrazolo[3,4-c]pyridazine derivative
Author/Authors
Takayoshi Kinoshita، نويسنده , , Masaichi Warizaya، نويسنده , , Makoto Ohori، نويسنده , , Kentaro Sato، نويسنده , , Masahiro Neya، نويسنده , , Takashi Fujii، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2006
Pages
4
From page
55
To page
58
Abstract
A series of pyrazolopyridazine compounds were briefly investigated as ERK2 inhibitors. The crystal structure of ERK2 complexed with an allyl derivative was determined. The compound induces structural change including movement of the glycine-rich loop and peptide flip between Met108-Glu109. As a result, the newly formed subsite can recognize small hydrophobic substituents but not hydrophilic ones.
Keywords
Structural change , ERK2 , x-ray
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2006
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
796311
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