Abstract
Several selective and potent EphB4 inhibitors have been discovered, optimized and biophysically characterized by our groups over the past years. On the outset of these discoveries high throughput docking techniques were applied. Herein, we review the optimization campaigns started from three of these hits (Xan-A1, Pyr-A1 and Qui-A1) with emphasis on their in depth in vitro and in vivo characterization, together with previously unpublished angiogenesis and fluorescence based assays.
Keywords:
Drug discovery; EphB4; In silico; Kinase; Potency; Selectivity.
Copyright © 2016 Elsevier Masson SAS. All rights reserved.
Publication types
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Research Support, Non-U.S. Gov't
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Review
MeSH terms
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Animals
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Computer Simulation
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Drug Design*
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Humans
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Isoquinolines / chemistry
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Isoquinolines / pharmacology
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Neoplasms / drug therapy
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Neoplasms / enzymology
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Protein Kinase Inhibitors / chemistry*
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Protein Kinase Inhibitors / pharmacology*
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Quinoxalines / chemistry
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Quinoxalines / pharmacology
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Receptor, EphB2 / antagonists & inhibitors*
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Receptor, EphB2 / metabolism
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Structure-Activity Relationship
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Xanthine / chemistry
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Xanthine / pharmacology
Substances
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Isoquinolines
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Protein Kinase Inhibitors
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Quinoxalines
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pyrrolo(2,3-b)quinoxaline
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Xanthine
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Receptor, EphB2