Discovery of 3-(2,6-Dichloro-3,5-dimethoxy-phenyl)-1-{6-[4-(4-ethyl-piperazin-1-yl)-phenylamino]-pyrimidin-4-yl}-1-methyl-urea (NVP-BGJ398), A Potent and Selective Inhibitor of the Fibroblast Growth Factor Receptor Family of Receptor Tyrosine Kinase

Vito Guagnano; Pascal Furet; Carsten Spanka; Vincent Bordas; Mickaël Le Douget; Christelle Stamm; Josef Brueggen; Michael R. Jensen; Christian Schnell; Herbert Schmid; Markus Wartmann; Joerg Berghausen; Peter Drueckes; Alfred Zimmerlin; Dirksen Bussiere; Jeremy Murray; Diana Graus Porta

doi:10.1021/jm2006222

Discovery of 3-(2,6-Dichloro-3,5-dimethoxy-phenyl)-1-{6-[4-(4-ethyl-piperazin-1-yl)-phenylamino]-pyrimidin-4-yl}-1-methyl-urea (NVP-BGJ398), A Potent and Selective Inhibitor of the Fibroblast Growth Factor Receptor Family of Receptor Tyrosine Kinase

Journal of Medicinal Chemistry ◽

10.1021/jm2006222 ◽

2011 ◽

Vol 54 (20) ◽

pp. 7066-7083 ◽

Cited By ~ 258

Author(s):

Vito Guagnano ◽

Pascal Furet ◽

Carsten Spanka ◽

Vincent Bordas ◽

Mickaël Le Douget ◽

...

Keyword(s):

Growth Factor ◽

Tyrosine Kinase ◽

Fibroblast Growth Factor ◽

Receptor Tyrosine Kinase ◽

Fibroblast Growth Factor Receptor ◽

Growth Factor Receptor ◽

Selective Inhibitor ◽

Fibroblast Growth ◽

Receptor Family

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AZD4547: An Orally Bioavailable, Potent, and Selective Inhibitor of the Fibroblast Growth Factor Receptor Tyrosine Kinase Family

Cancer Research ◽

10.1158/0008-5472.can-11-3034 ◽

2012 ◽

Vol 72 (8) ◽

pp. 2045-2056 ◽

Cited By ~ 316

Author(s):

Paul R. Gavine ◽

Lorraine Mooney ◽

Elaine Kilgour ◽

Andrew P. Thomas ◽

Katherine Al-Kadhimi ◽

...

Keyword(s):

Growth Factor ◽

Tyrosine Kinase ◽

Fibroblast Growth Factor ◽

Receptor Tyrosine Kinase ◽

Fibroblast Growth Factor Receptor ◽

Growth Factor Receptor ◽

Selective Inhibitor ◽

Fibroblast Growth ◽

Orally Bioavailable ◽

Receptor Tyrosine Kinase Family

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Proteomic analyses of signalling complexes associated with receptor tyrosine kinase identify novel members of fibroblast growth factor receptor 3 interactome

Cellular Signalling ◽

10.1016/j.cellsig.2017.10.003 ◽

2018 ◽

Vol 42 ◽

pp. 144-154 ◽

Cited By ~ 7

Author(s):

Lukas Balek ◽

Pavel Nemec ◽

Peter Konik ◽

Michaela Kunova Bosakova ◽

Miroslav Varecha ◽

...

Keyword(s):

Growth Factor ◽

Tyrosine Kinase ◽

Fibroblast Growth Factor ◽

Receptor Tyrosine Kinase ◽

Fibroblast Growth Factor Receptor ◽

Growth Factor Receptor ◽

Fibroblast Growth ◽

Proteomic Analyses

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Abstract B246: NVP-BGJ398: A potent and selective inhibitor of the fibroblast growth factor receptor family.

10.1158/1535-7163.targ-11-b246 ◽

2011 ◽

Author(s):

Vito Guagnano ◽

Diana Graus Porta ◽

Vincent Bordas ◽

Mickael Le Douget ◽

Christelle Stamm ◽

...

Keyword(s):

Growth Factor ◽

Fibroblast Growth Factor ◽

Fibroblast Growth Factor Receptor ◽

Growth Factor Receptor ◽

Selective Inhibitor ◽

Fibroblast Growth ◽

Receptor Family

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Novel inhibitor for fibroblast growth factor receptor tyrosine kinase

Bioorganic & Medicinal Chemistry Letters ◽

10.1016/j.bmcl.2007.06.058 ◽

2007 ◽

Vol 17 (17) ◽

pp. 4812-4818 ◽

Cited By ~ 19

Author(s):

Naparat Kammasud ◽

Chantana Boonyarat ◽

Satoshi Tsunoda ◽

Hiroaki Sakurai ◽

Ikuo Saiki ◽

...

Keyword(s):

Growth Factor ◽

Tyrosine Kinase ◽

Fibroblast Growth Factor ◽

Receptor Tyrosine Kinase ◽

Fibroblast Growth Factor Receptor ◽

Growth Factor Receptor ◽

Fibroblast Growth

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Identification of tyrosines 154 and 307 in the extracellular domain and 653 and 766 in the intracellular domain as phosphorylation sites in the heparin-binding fibroblast growth factor receptor tyrosine kinase (flg )

Protein Science ◽

10.1002/pro.5560020109 ◽

1993 ◽

Vol 2 (1) ◽

pp. 86-92 ◽

Cited By ~ 29

Author(s):

Jinzhao Hou ◽

Kerstin Mckeehan ◽

Mikio Kan ◽

John W. Crabb ◽

Wallace L. Mckeehan ◽

...

Keyword(s):

Growth Factor ◽

Tyrosine Kinase ◽

Fibroblast Growth Factor ◽

Receptor Tyrosine Kinase ◽

Fibroblast Growth Factor Receptor ◽

Growth Factor Receptor ◽

Phosphorylation Sites ◽

Fibroblast Growth ◽

Heparin Binding ◽

Intracellular Domain

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Incisor Degeneration in Rats Induced by Vascular Endothelial Growth Factor/Fibroblast Growth Factor Receptor Tyrosine Kinase Inhibition

Toxicologic Pathology ◽

10.1177/0192623309357950 ◽

2010 ◽

Vol 38 (2) ◽

pp. 267-279 ◽

Cited By ~ 11

Author(s):

Anthony M. Fletcher ◽

Carla L. Bregman ◽

Jochen Woicke ◽

Theodora W. Salcedo ◽

Robert H. Zidell ◽

...

Keyword(s):

Vascular Endothelial Growth Factor ◽

Growth Factor ◽

Tyrosine Kinase ◽

Fibroblast Growth Factor ◽

Receptor Tyrosine Kinase ◽

Fibroblast Growth Factor Receptor ◽

Growth Factor Receptor ◽

Vascular Endothelial ◽

Fibroblast Growth ◽

Endothelial Growth Factor

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Ocular Adverse Effects of Infigratinib, a New Fibroblast Growth Factor Receptor Tyrosine Kinase Inhibitor

Ophthalmology ◽

10.1016/j.ophtha.2020.08.026 ◽

2020 ◽

Author(s):

M. Teresa Magone ◽

Iris R. Hartley ◽

Edmond Fitzgibbon ◽

Rachel Bishop ◽

Mike Arango ◽

...

Keyword(s):

Growth Factor ◽

Adverse Effects ◽

Tyrosine Kinase ◽

Tyrosine Kinase Inhibitor ◽

Fibroblast Growth Factor ◽

Receptor Tyrosine Kinase ◽

Fibroblast Growth Factor Receptor ◽

Kinase Inhibitor ◽

Growth Factor Receptor ◽

Fibroblast Growth

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Re: Magone et al.: Ocular adverse effects of infigratinib, a new fibroblast growth factor receptor tyrosine kinase inhibitor (Ophthalmology. 2021;128:624–626)

Ophthalmology ◽

10.1016/j.ophtha.2021.05.012 ◽

2021 ◽

Author(s):

Jasmine H. Francis ◽

Julia Canestraro ◽

David H. Abramson

Keyword(s):

Growth Factor ◽

Adverse Effects ◽

Tyrosine Kinase ◽

Tyrosine Kinase Inhibitor ◽

Fibroblast Growth Factor ◽

Receptor Tyrosine Kinase ◽

Fibroblast Growth Factor Receptor ◽

Kinase Inhibitor ◽

Growth Factor Receptor ◽

Fibroblast Growth

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Activation Mechanism of Fibroblast Growth Factor Receptor Tyrosine Kinase Revealed by Crystal Structure of Fibroblast Growth Factor Receptor Ectodomain Bound to Fibroblast Growth Factor and Heparin

Insulin & Related Proteins - Structure to Function and Pharmacology ◽

10.1007/0-306-47582-0_15 ◽

2002 ◽

pp. 189-200

Author(s):

L. Pellegrini ◽

D. F. Burke ◽

T. L. Blundell

Keyword(s):

Crystal Structure ◽

Growth Factor ◽

Tyrosine Kinase ◽

Fibroblast Growth Factor ◽

Receptor Tyrosine Kinase ◽

Fibroblast Growth Factor Receptor ◽

Growth Factor Receptor ◽

Activation Mechanism ◽

Fibroblast Growth

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Chronic activity of ectopic type 1 fibroblast growth factor receptor tyrosine kinase in prostate epithelium results in hyperplasia accompanied by intraepithelial neoplasia

The Prostate ◽

10.1002/pros.10311 ◽

2004 ◽

Vol 58 (1) ◽

pp. 1-12 ◽

Cited By ~ 18

Author(s):

Fen Wang ◽

Kerstin McKeehan ◽

Chundong Yu ◽

Michael Ittmann ◽

Wallace L. McKeehan

Keyword(s):

Growth Factor ◽

Tyrosine Kinase ◽

Fibroblast Growth Factor ◽

Receptor Tyrosine Kinase ◽

Fibroblast Growth Factor Receptor ◽

Growth Factor Receptor ◽

Intraepithelial Neoplasia ◽

Fibroblast Growth ◽

Prostate Epithelium

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