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Profile and molecular modeling of 3-(indole-3-yl)-4-(3,4,5-trimethoxyphenyl)-1 H-pyrrole-2,5-dione (1) as a highly selective VEGF-R2/3 inhibitor.
- Source :
-
Journal of medicinal chemistry [J Med Chem] 2006 Dec 14; Vol. 49 (25), pp. 7549-53. - Publication Year :
- 2006
-
Abstract
- We report on selectivity profiling of 1 in a panel of 20 protein kinases and molecular modeling indicating 1 to be highly active and selective for VEGF-R2/3. Sequence alignment analysis and detailed insights into the ATP binding pockets of targeted protein kinases from the panel result in a unique structural architecture of VEGF-R2 mainly caused by the hydrophobic pocket I, determining the molecular basis for activity and selectivity of 1.
- Subjects :
- Amino Acid Sequence
Binding Sites
Crystallography, X-Ray
Hydrophobic and Hydrophilic Interactions
Indoles chemistry
Molecular Sequence Data
Pyrroles chemistry
Indoles chemical synthesis
Models, Molecular
Pyrroles chemical synthesis
Vascular Endothelial Growth Factor Receptor-2 chemistry
Vascular Endothelial Growth Factor Receptor-3 chemistry
Subjects
Details
- Language :
- English
- ISSN :
- 0022-2623
- Volume :
- 49
- Issue :
- 25
- Database :
- MEDLINE
- Journal :
- Journal of medicinal chemistry
- Publication Type :
- Academic Journal
- Accession number :
- 17149885
- Full Text :
- https://doi.org/10.1021/jm0609871