FGFR

Fibroblast growth factors (FGFs) are mitogenic signaling molecules that have roles in angiogenesis, wound healing, cell migration, neural outgrowth and embryonic development. FGF receptors (FGFRs) are transmembrane catalytic receptors with intracellular tyrosine kinase activity.

Products
Background
Literature
Gene Data

Inhibitors

Cat No Product Name / Activity
4274 AP 24534
Potent multi-kinase and pan-Bcr-Abl inhibitor
4002 FIIN 1 hydrochloride
Potent, irreversible FGFR inhibitor
3724 PD 161570
Selective FGFR inhibitor
3785 PD 166285 dihydrochloride
FGFR, PDGFRβ and Src inhibitor; also inhibits Wee1
3044 PD 173074
FGFR1 and -3 inhibitor
3300 SU 5402
Potent FGFR and VEGFR inhibitor
3335 SU 6668
FGFR, VEGFR and PDGFR inhibitor

Other

Cat No Product Name / Activity
4826 SUN 11602
Basic fibroblast growth factor (bFGF) mimetic; neuroprotective

Fibroblast growth factors (FGFs) (FGF1 - 10 and 16 - 23) are mitogenic signaling molecules that have roles in angiogenesis, wound healing, cell migration, neural outgrowth and embryonic development. FGFs bind heparan sulfate glycosaminoglycans (HSGAGs), which facilitates dimerization (activation) of FGF receptors (FGFRs).

FGFRs are transmembrane catalytic receptors that have intracellular tyrosine kinase activity. There are four human genes encoding FGFRs, which produce seven different receptors (FGFR1b, FGFR1c, FGFR2b, FGFR2c, FGFR3b, FGFR3c and FGFR4) due to alternative splicing events occurring both in the extracellular and intracellular regions. The alternative splice isoforms are generally tissue specific: the b isoform is expressed in epithelial tissue, whereas the c isoform is expressed in mesenchymal tissue. HSGAG-FGF-FGFR binding initiates FGFR dimerization, enabling the cytoplasmic kinase domains to transphosphorylate tyrosine residues and become activated. HSGAGs also function to stabilize FGF-FGFR binding and prevent FGF degradation.

FGFs were first isolated as growth factors for fibroblasts. Since the initial discovery of FGF1 and FGF2, a further 20 structurally related FGFs have been identified, all of which are differentially expressed in many tissues. Of these 22 growth factors, 18 are FGFR ligands. FGFRs couple to the PLCγ, MAPK and PI3-K/Akt intracellular signaling cascades and there is evidence of cross talk with the Notch signaling pathway. In addition, some activated FGF-FGFR complexes are endocytosed and function directly in the cytosol and/or nucleus of the cell.

Mutations in FGFR genes are the cause of several human developmental disorders characterized by skeletal abnormalities such as achondroplasia, and upregulation of FGFR expression may lead to cell transformation and cancer.

Literature for FGFR

Cancer

Cancer Research Product Guide

A collection of over 750 products for cancer research, the guide includes research tools for the study of:

  • Cancer Metabolism
  • Epigenetics in Cancer
  • Receptor Signaling
  • Cell Cycle and DNA Damage Repair
  • Angiogenesis
  • Invasion and Metastasis
Kinases

Kinases Product Listing

A collection of over 400 products for kinase research, the listing includes inhibitors of:

  • Receptor Tyrosine Kinases
  • Protein Kinases A, C, D and G
  • PI-3 Kinase, Akt and mTOR
  • MAPK Signaling
  • Receptor Serine/Threonine Kinases
Stem Cells

Stem Cells Scientific Review

Written by Kirsty E. Clarke, Victoria B. Christie, Andy Whiting and Stefan A. Przyborski, this review provides an overview of the use of small molecules in the control of stem cell growth and differentiation. Key signaling pathways are highlighted, and the regulation of ES cell self-renewal and somatic cell reprogramming is discussed. Compounds available from Tocris are listed.

Angiogenesis in Cancer

Angiogenesis in Cancer Poster

Adapted from the 2015 Cancer Product Guide, Edition 3, this poster summarizes the pathogenesis of angiogenesis in cancer, as well as some of the main angiogenesis therapeutic targets.

Depression

Depression Poster

Major depressive disorder is characterized by depressed mood and a loss of interest and/or pleasure. Updated in 2015 this poster highlights presynaptic and postsynaptic targets for the potential treatment of major depressive disorder, as well as outlining the pharmacology of currently approved antidepressant drugs.

FGFR Gene Data

Gene Species Gene Symbol Gene Accession No. Protein Accession No.
FGFR1 Human FGFR1 NM_023110 Q5BJG2
Mouse Fgfr1 NM_010206 P16092
Rat Fgfr1 NM_024146 O35758
FGFR2 Human FGFR2 NM_022976 Q9UQH7
Mouse Fgfr2 NM_010207 P21803
Rat Fgfr2 NM_012712 Q9R2A0
FGFR3 Human FGFR3 NM_000142 P22607
Mouse Fgfr3 NM_008010 Q61851
Rat Fgfr3 NM_053429 Q9JHX9
FGFR4 Human FGFR4 NM_022963 P22455
Mouse Fgfr4 NM_008011 Q03142
Rat Fgfr4 NM_001109904 Q498D6