title: Fibroblast growth factor receptor inhibitors.
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.
authors.affiliation: GVK Biosciences Pvt. Ltd., Phase-1, Technocrats Industrial Estate, Balanagar 500037, Andhra Pradesh, India. suneelkumar.bvs@gmail.com
authors.forename: Suneel B V S
authors.initials: SB
authors.lastname: Kumar
authors.forename: Lakshmi
authors.initials: L
authors.lastname: Narasu
authors.forename: Rambabu
authors.initials: R
authors.lastname: Gundla
authors.forename: Raveendra
authors.initials: R
authors.lastname: Dayam
authors.forename: Sarma
authors.initials: S
authors.lastname: J A R P
mesh_terms: D020533:Angiogenesis Inhibitors / Q000494:pharmacology; D000818:Animals; D000970:Antineoplastic Agents / Q000494:pharmacology*; D015195:Drug Design; D006801:Humans; D009369:Neoplasms / Q000098:blood supply / Q000188:drug therapy / Q000378:metabolism; D009389:Neovascularization, Pathologic / Q000188:drug therapy; D018919:Neovascularization, Physiologic; D020033:Protein Isoforms; D011743:Pyrimidines / Q000494:pharmacology; D051496:Receptor, Fibroblast Growth Factor, Type 1 / Q000037:antagonists & inhibitors / Q000378:metabolism; D017468:Receptors, Fibroblast Growth Factor / Q000037:antagonists & inhibitors* / Q000378:metabolism; D015398:Signal Transduction
chemical_list: D020533:Angiogenesis Inhibitors; D000970:Antineoplastic Agents; C115711:PD 173074; D020033:Protein Isoforms; D011743:Pyrimidines; D017468:Receptors, Fibroblast Growth Factor; C496348:FGFR1 protein, human; D051496:Receptor, Fibroblast Growth Factor, Type 1