Header

UZH-Logo

Maintenance Infos

Three stories on Eph kinase inhibitors: From in silico discovery to in vivo validation


Unzue, Andrea; Lafleur, Karine; Zhao, Hongtao; Zhou, Ting; Dong, Jing; Kolb, Peter; Liebl, Johanna; Zahler, Stefan; Caflisch, Amedeo; Nevado, Cristina (2016). Three stories on Eph kinase inhibitors: From in silico discovery to in vivo validation. European journal of medicinal chemistry, 112:347-366.

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Pyr-A1 and Qui-A1) with emphasis on their in depth in vitro and in vivo characterization, together with previously unpublished angiogenesis and fluorescence based assays.

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Pyr-A1 and Qui-A1) with emphasis on their in depth in vitro and in vivo characterization, together with previously unpublished angiogenesis and fluorescence based assays.

Statistics

Citations

3 citations in Web of Science®
2 citations in Scopus®
Google Scholar™

Altmetrics

Downloads

0 downloads since deposited on 31 May 2016
0 downloads since 12 months

Additional indexing

Item Type:Journal Article, refereed, original work
Communities & Collections:04 Faculty of Medicine > Department of Biochemistry
07 Faculty of Science > Department of Biochemistry

07 Faculty of Science > Department of Chemistry
Dewey Decimal Classification:540 Chemistry
Language:English
Date:2016
Deposited On:31 May 2016 17:54
Last Modified:31 May 2016 17:54
Publisher:Elsevier
ISSN:0223-5234
Publisher DOI:https://doi.org/10.1016/j.ejmech.2016.01.057
PubMed ID:26907157

Download