Abstract
Fibroblast growth factor receptors (FGFRs) play an important role in embryonic development, angiogenesis, wound healing, cell proliferation and differentiation. The fibroblast growth factor receptor (FGFR) isoforms have been under intense scrutiny for effective anticancer drug candidates. The fibroblast growth factor (FGF) and its receptor (FGFR) provide another pathway that seems critical to monitoring angiogenesis. Recent findings suggest that FGFR mediates signaling, regulates the PKM2 activity, and plays a crucial role in cancer metabolism. The current review also covers the recent findings on the role of FGFR1 in cancer metabolism. This paper reviews the progress, mechanism, and binding modes of recently known kinase inhibitors such as PD173074, SU series and other inhibitors still under clinical development. Some of the structural classes that will be highlighted in this review include Pyrido[2,3-d]pyrimidines, Indolin- 2-one, Pyrrolo[2,1-f][1,2,4]triazine, Pyrido[2,3-d]pyrimidin-7(8H)-one, and 1,6- Naphthyridin-2(1H)-ones.
Keywords: FGFR receptor, Cancer metabolism, FGFR1 inhibitors, FGFR mediated signaling, cancer
Current Pharmaceutical Design
Title:Fibroblast Growth Factor Receptor Inhibitors
Volume: 19 Issue: 4
Author(s): Suneel Kumar B.V.S, Lakshmi Narasu, Rambabu Gundla, Raveendra Dayam, Sarma J.A.R.P
Affiliation:
Keywords: FGFR receptor, Cancer metabolism, FGFR1 inhibitors, FGFR mediated signaling, cancer
Abstract: Fibroblast growth factor receptors (FGFRs) play an important role in embryonic development, angiogenesis, wound healing, cell proliferation and differentiation. The fibroblast growth factor receptor (FGFR) isoforms have been under intense scrutiny for effective anticancer drug candidates. The fibroblast growth factor (FGF) and its receptor (FGFR) provide another pathway that seems critical to monitoring angiogenesis. Recent findings suggest that FGFR mediates signaling, regulates the PKM2 activity, and plays a crucial role in cancer metabolism. The current review also covers the recent findings on the role of FGFR1 in cancer metabolism. This paper reviews the progress, mechanism, and binding modes of recently known kinase inhibitors such as PD173074, SU series and other inhibitors still under clinical development. Some of the structural classes that will be highlighted in this review include Pyrido[2,3-d]pyrimidines, Indolin- 2-one, Pyrrolo[2,1-f][1,2,4]triazine, Pyrido[2,3-d]pyrimidin-7(8H)-one, and 1,6- Naphthyridin-2(1H)-ones.
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Suneel Kumar B.V.S, Lakshmi Narasu, Rambabu Gundla, Raveendra Dayam, Sarma J.A.R.P , Fibroblast Growth Factor Receptor Inhibitors, Current Pharmaceutical Design 2013; 19 (4) . https://dx.doi.org/10.2174/1381612811306040687
DOI https://dx.doi.org/10.2174/1381612811306040687 |
Print ISSN 1381-6128 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4286 |
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