Molecular Target Synopsis
Overview
Domains and Structures
Drugs and Clinical Candidates
Druggability
Chemistry
Ligand Efficiency Plot
Pathways
Family Cladogram
Interaction Network
Gene Expression
Gene Copy Number Variation
RNAi
Mutations
Germline Genetics

FGF1 (P05230) - Overview - Molecular Target Synopsis

Protein


FGF1, Fibroblast growth factor 1
UniProt P05230

Also Known as FGF1_HUMAN, FGF1, FGFA

Plays an important role in the regulation of cell survival, cell division, angiogenesis, cell differentiation and cell migration. Functions as potent mitogen in vitro. Acts as a ligand for FGFR1 and integrins. Binds to FGFR1 in the presence of heparin leading to FGFR1 dimerization and activation via sequential autophosphorylation on tyrosine residues which act as docking sites for interacting proteins, leading to the activation of several signaling cascades. Binds to integrin ITGAV:ITGB3. Its binding to integrin, subsequent ternary complex formation with integrin and FGFR1, and the recruitment of PTPN11 to the complex are essential for FGF1 signaling. Induces the phosphorylation and activation of FGFR1, FRS2, MAPK3/ERK1, MAPK1/ERK2 and AKT1 (PubMed:18441324, PubMed:20422052). Can induce angiogenesis (PubMed:23469107). Monomer. Homodimer. Interacts with FGFR1, FGFR2, FGFR3 and FGFR4. Affinity between fibroblast growth factors (FGFs) and their receptors is increased by heparan sulfate glycosaminoglycans that function as coreceptors. Found in a complex with FGFBP1, FGF1 and FGF2. Interacts with FGFBP1. Part of a Cu(2+)-dependent multiprotein aggregate containing FGF1, S100A13 and SYT1. Interacts with SYT1. Interacts with S100A13. Interacts with LRRC59. Interacts with CSNKA, CSNKB and FIBP. While binding with LRRC59, CSNKA and FIBP seem mutually exclusive, CSNKB and FIBP may cooperatively interact with FGF1. Forms a ternary complex with FGFR1 and ITGAV:ITGB3 and induces the recruitment of PTPN11 to the complex (PubMed:20422052).

4YOL
HUMAN FIBROBLAST GROWTH FACTOR-1 C16S/A66C/C117A/P134A
RCSB/PDB
Inspect Structure
See all 3D Structures for FGF1

Isoforms / Transcripts (Protein Coding)


Sub-cellular localization


UniProt: FGF1 is active in the following subcellular-locations: cell cortex, cytoplasm, cytosol, nucleus, secreted.
GO terms: FGF1 is active in the following subcellular-locations: cell cortex, cytosol, extracellular matrix, extracellular region, extracellular space, nucleolus.



UniProt
GO terms

Gene Copy Number Variation


In COSMIC - Cell Lines Project FGF1 has gain in 1 cell-lines, loss in 1 cell-lines and no signal in 1003 cell-lines. (see details)

Gene Expression


In NCI60, the highest expressing cell lines are: SF_268, SF_539, SNB_75

In Array Express (RNA-seq of 675 commonly used human cancer cell lines), the highest expressing cell lines are: G61, NCI-H196, NCI-H2052

In Array Express (RNA-seq of long poly adenylated RNA and long non poly adenylated RNA from ENCODE cell lines), the highest expressing cell lines are: BJ, HSMM, A549

(see details)

3D Structures


For FGF1 there are:
96 structures (219 chains) solved
16 are solved in complex with at least one small molecule ligand
1 are solved with an approved drug

FGF1 is solved in complex with the approved drug(s):

DBX/DOBESILIC ACID (3K1X_A, 3K1X_B).

(see details)
Molecular Target 3D Synopsis

Screening and Chemistry


FGF1 has been screened with 130 compounds (150 bioactivities), 47 compounds have bioactivities that show binding affinity of <= 500nM (47 bioactivities). (see details)