FGFR1 Human, His
Description
Introduction to FGFR1 Human, His
Fibroblast Growth Factor Receptor 1 (FGFR1) with a histidine (His) tag is a recombinant human protein engineered for research and therapeutic applications. The His tag, an 8-amino acid sequence appended to the C-terminus, facilitates purification via metal affinity chromatography. This protein is widely used to study FGFR1 signaling, validate inhibitors, and model FGFR1-related diseases. FGFR1 is a receptor tyrosine kinase critical for cell proliferation, differentiation, and survival, with dysregulation linked to cancers and congenital disorders .
Structure and Function
FGFR1 Human, His retains the canonical structure of native FGFR1:
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Extracellular domain: Three immunoglobulin (Ig)-like subunits (D1, D2, D3) for FGF binding.
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Transmembrane domain: Anchors the receptor to the cell membrane.
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Intracellular kinase domain: Phosphorylates downstream targets (e.g., PLCγ, ERK) upon FGF binding .
The His tag does not interfere with ligand binding or kinase activity. Glycosylation, critical for proper receptor folding and function, is preserved in recombinant FGFR1 produced in Sf9 insect cells .
Production and Purification
| Property | Detail |
|---|---|
| Host System | Sf9 Baculovirus cells |
| Amino Acid Range | 22–376 (363 residues) |
| Molecular Weight | 40.4 kDa (SDS-PAGE: 40–57 kDa due to glycosylation) |
| His Tag | C-terminal, 8-amino acid sequence (e.g., HHHHHHHH) |
| Purification Method | Proprietary chromatography (likely nickel/cobalt affinity) |
Source: Prospec Bio (Catalogue #PKA-100)
Disease Associations
FGFR1 mutations or dysregulation underpin:
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Congenital Disorders:
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Cancers:
Therapeutic Targets
FGFR1 Human, His is used to test inhibitors (e.g., PD166866) that disrupt:
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FGF/FGFR1 Signaling: Blocks ERK/MAPK and PI3K/AKT pathways .
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Cancer Cell Proliferation: Reduces tumor growth in models of rhabdomyosarcoma and breast cancer .
Mechanistic Insights
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FGF8-FGFR1 in GnRH Neurons: Dose- and time-dependent activation of GNRH1 expression in human pluripotent stem cells. FGFR1 localizes to the nucleus during neuronal differentiation, suggesting transcriptional roles .
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Chondrocyte Regulation: FGFR1 inhibition reverses FGF-2-induced MMP-13 upregulation and proteoglycan loss in osteoarthritis models .
Table 1: FGFR1 Amplification in Cancers
Table 2: FGFR1 Mutations and Diseases
Product Specs
FGFR-1, bFGF-R, C-FGR, CD331, fms-related tyrosine kinase 2, Pfeiffer syndrome, CEK, FLG, FLT2, KAL2, BFGFR, FGFBR, HBGFR, FGFR1/FGFR1OP2 FUSION GENE, FGFR1/ZNF198 FUSION GENE, FLG FGFR1/BCR FUSION GENE, FLG protein, FMS-LIKE GENE, N-sam tyrosine kinase, basic fibroblast growth factor receptor 1.
Sf9, Baculovirus cells.
RPSPTLPEQA QPWGAPVEVE SFLVHPGDLL QLRCRLRDDV QSINWLRDGV QLAESNRTRI TGEEVEVQDS VPADSGLYAC VTSSPSGSDT TYFSVNVSDA LPSSEDDDDD DDSSSEEKET DNTKPNRMPV APYWTSPEKM EKKLHAVPAA KTVKFKCPSS GTPNPTLRWL KNGKEFKPDH RIGGYKVRYA TWSIIMDSVV PSDKGNYTCI VENEYGSINH TYQLDVVERS PHRPILQAGL PANKTVALGS NVEFMCKVYS DPQPHIQWLK HIEVNGSKIG PDNLPYVQIL KTAGVNTTDK EMEVLHLRNV SFEDAGEYTC LAGNSIGLSH HSAWLTVLEA LEERPAVMTS PLYLELEHHH HHH.
Product Science Overview
Fibroblast Growth Factor Receptor-1 (FGFR1) is a member of the fibroblast growth factor receptor family, which consists of four membrane-spanning tyrosine kinases (FGFR1-4). These receptors serve as high-affinity receptors for fibroblast growth factors (FGFs), which are involved in various biological processes, including cell growth, differentiation, and tissue repair .
FGFR1 is composed of an extracellular region with three immunoglobulin-like domains, a single hydrophobic membrane-spanning segment, and a cytoplasmic tyrosine kinase domain . The extracellular portion of FGFR1 interacts with FGFs, initiating a cascade of downstream signals that influence mitogenesis and differentiation . FGFR1 binds both acidic and basic fibroblast growth factors and plays a crucial role in limb induction .
The recombinant form of FGFR1, tagged with a polyhistidine (His) sequence, is produced using various expression systems, such as baculovirus . The His tag facilitates the purification of the protein using affinity chromatography, making it easier to isolate and study the receptor . The recombinant FGFR1 is often used in research to understand its role in cellular processes and its involvement in various diseases .
FGFR1 is involved in multiple biological processes, including mesoderm induction, cell growth, migration, organ formation, and bone growth . It is alternatively spliced, generating multiple splice variants that are differentially expressed during embryonic development and in the adult body . Mutations in FGFR1 are associated with several diseases, such as Pfeiffer syndrome, idiopathic hypogonadotropic hypogonadism, Kallmann syndrome type 2, osteoglophonic dysplasia, non-syndromic trigonocephaly, Jackson-Weiss syndrome, and Antley-Bixler syndrome .
