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

European Journal of Medicinal Chemistry
Andrea UnzueCristina Nevado

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Pyr-A1 and Qui-A1) with emphasis on their in depth in vitro and in vivo characterization, together with previously unpublished angiogenesis and fluorescence based assays.

References

Jan 22, 2002·BMC Molecular Biology·S A StephensonJ E Hardingham
Mar 16, 2002·Nature Structural Biology·Christopher PargellisJohn Regan
Apr 24, 2002·Seminars in Cell & Developmental Biology·Ralf H Adams
Jul 18, 2002·Nature Reviews. Drug Discovery·Margaret A Somerville
Dec 10, 2002·Science·G ManningS Sudarsanam
Dec 14, 2002·The International Journal of Biochemistry & Cell Biology·Juha-Pekka Himanen, Dimitar B Nikolov
Feb 4, 2003·Annals of Oncology : Official Journal of the European Society for Medical Oncology·G BerclazA-C Andres
Dec 16, 2003·Biochemical and Biophysical Research Communications·Andrea SturzJens Glienke
Jan 15, 2004·Molecular Pharmacology·Elena Zaks-MakhinaEdwin S Levitan
Jan 27, 2004·Bioorganic & Medicinal Chemistry Letters·Uday R KhireDonald Wolanin
Apr 7, 2004·Proceedings of the National Academy of Sciences of the United States of America·Nicole K NorenElena B Pasquale
Apr 29, 2004·Nature Neuroscience·Elena B Pasquale
May 22, 2004·Neoplasia : an International Journal for Oncology Research·Georg Martiny-BaronHellmut G Augustin
Feb 16, 2005·Cancer Cell·Ellen WeisbergJames D Griffin
Feb 16, 2005·Nature Biotechnology·Miles A FabianDavid J Lockhart
Feb 22, 2005·The Journal of Biological Chemistry·Mitchell KoolpeElena B Pasquale
Jun 3, 2005·Cancer Research·Guangbin XiaParkash S Gill
Jun 17, 2005·Clinical Cancer Research : an Official Journal of the American Association for Cancer Research·Guangbin XiaParkash S Gill
Jun 24, 2005·Nature·Eduard BatlleHans Clevers
Jun 25, 2005·Chemistry & Biology·Zachary A Knight, Kevan M Shokat
Dec 21, 2005·The Journal of Biological Chemistry·Bing WangGuo-Ping Shi
Feb 24, 2006·Proceedings of the National Academy of Sciences of the United States of America·Jonathan S MelnickJeremy S Caldwell
Jun 20, 2006·Nature Chemical Biology·Yi Liu, Nathanael S Gray
Jul 4, 2006·The American Journal of Pathology·S Ram KumarParkash S Gill
Jul 25, 2006·Nature Cell Biology·Nicole K NorenElena B Pasquale
Aug 5, 2006·Nature Reviews. Drug Discovery·Robert A CopelandThomas D Meek
Oct 25, 2006·Journal of Molecular and Cellular Cardiology·Rajesh KumarKenneth M Baker
Nov 11, 2006·Proceedings of the National Academy of Sciences of the United States of America·Alexandr P KornevLynn F Ten Eyck
Jun 19, 2007·Clinical Cancer Research : an Official Journal of the American Association for Cancer Research·Steven B GendreauAlison H Joly
Jun 30, 2007·Bioorganic & Medicinal Chemistry Letters·Paul BamboroughMelanie Washington
Sep 14, 2007·The Biochemical Journal·Jenny BainPhilip Cohen
Sep 22, 2007·Bioorganic & Medicinal Chemistry Letters·R Graham RobinettKaren Lackey
Nov 6, 2007·Bioorganic & Medicinal Chemistry Letters·Richard M AngellMalcolm Willson
Nov 17, 2007·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Craig A Obafemi, Wolfgang Pfleiderer

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Citations

Mar 17, 2016·Journal of Medicinal Chemistry·Andrea UnzueCristina Nevado
Feb 23, 2018·International Journal of Molecular Sciences·Elżbieta PawłowskaJanusz Blasiak
Jul 8, 2020·Pharmaceuticals·Sarah BaudetXavier Nicol
Oct 22, 2018·The International Journal of Biochemistry & Cell Biology·Nayanendu SahaDimitar B Nikolov
Jan 26, 2018·Biochimica Et Biophysica Acta. Reviews on Cancer·Ravi SalgiaPrakash S Gill
Sep 2, 2017·Journal of Chemical Information and Modeling·Jean-Rémy MarchandAmedeo Caflisch

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