Abstract 1361: Fragment based drug discovery of selective inhibitors of Fibroblast Growth Factor Receptor (FGFR)

Abstract 1361: Fragment based drug discovery of selective inhibitors of Fibroblast Growth Factor Receptor (FGFR)

Recent data in a number of tumour types has implicated Fibroblast Growth Factor (FGF) and Fibroblast Growth Factor receptor (FGFR) signalling as being key to the molecular pathology of cancer. A fragment screening campaign was conducted against the tyrosine kinase domain of FGFR1 to detect low molec...

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Veröffentlicht in:Cancer research (Chicago, Ill.) Ill.), 2011-04, Vol.71 (8_Supplement), p.1361-1361
Hauptverfasser: Saxty, Gordon, Akkari, R, Angibaud, P, Arts, J, Benderitter, P, Berdini, V, Bonnet, P, Cleasby, A, Embrechts, W, Freyne, E, Gilissen, R, King, P, Lacrampe, J, Ligny, Y, Madin, A, Mcclue, S, Mevellec, L, Murray, C W., Newell, H, Page, M, Papanikos, A, Perera, T, Querolle, O, Rees, D C., Rich, S J., Saalau-Bethell, S M., Sement, E, Simmonet, Y, Squires, M, Tronel, V, Ward, G A., Willems, M, B, Wroblowski, Thompson, N T.
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Sprache:eng
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Zusammenfassung:Recent data in a number of tumour types has implicated Fibroblast Growth Factor (FGF) and Fibroblast Growth Factor receptor (FGFR) signalling as being key to the molecular pathology of cancer. A fragment screening campaign was conducted against the tyrosine kinase domain of FGFR1 to detect low molecular weight compounds that bound to the hinge region of the kinase. The screening produced several fragment inhibitors (molecular weight
ISSN:0008-5472
1538-7445
DOI:10.1158/1538-7445.AM2011-1361