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.
From: Department of Pharmacy, Eberhard Karls University, Auf der Morgenstelle 8, D-72076 Tübingen, Germany. Christian.Peifer@uni-tuebingen.de
Journal of medicinal chemistry
- Publish Date: Dec 2006
- ISSN: 0022-2623
- Volume: 49
- Issue: 25
- Pages: 7549-53
- Medium: Print
- Language: English
- Citation (JAMA): Peifer Christian, Krasowski Agata, Hämmerle Nina, et al. 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.. J. Med. Chem. Dec 2006;49:7549-53
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.
Mesh Headings (Keywords): Amino Acid Sequence, Binding Sites, Crystallography, X-Ray, Hydrophobicity, Indoles, Models, Molecular, Molecular Sequence Data, Pyrroles, Vascular Endothelial Growth Factor Receptor-2, Vascular Endothelial Growth Factor Receptor-3
Check for Full Text / PubMed Unique Identifier (PMID): 17149885
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