Crystal structure of human ERK2 complexed with a pyrazolo[3,4-c]pyridazine derivative.
Article Details
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Kinoshita T, Warizaya M, Ohori M, Sato K, Neya M, Fujii T
Crystal structure of human ERK2 complexed with a pyrazolo[3,4-c]pyridazine derivative.
Bioorg Med Chem Lett. 2006 Jan 1;16(1):55-8. Epub 2005 Oct 18.
- PubMed ID
- 16242327 [ View in PubMed]
- 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.
DrugBank Data that Cites this Article
- Polypeptides
Name UniProt ID Mitogen-activated protein kinase 1 P28482 Details - Binding Properties
Drug Target Property Measurement pH Temperature (°C) 5-(2-PHENYLPYRAZOLO[1,5-A]PYRIDIN-3-YL)-1H-PYRAZOLO[3,4-C]PYRIDAZIN-3-AMINE Mitogen-activated protein kinase 1 IC 50 (nM) 1900 N/A N/A Details