Binding Site Information of Target
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T18639 | Target Info | |||
| Target Name | Heparin-binding growth factor 1 (FGF1) | ||||
| Synonyms | HBGF-1; Fibroblast growth factor 1; FGFA; FGF-1; Endothelial cell growth factor; ECGF-beta; ECGF; Beta-endothelial cell growth factor; Acidic fibroblast growth factor; AFGF | ||||
| Target Type | Clinical trial Target | ||||
| Gene Name | FGF1 | ||||
| Biochemical Class | Growth factor | ||||
| UniProt ID | |||||
| Drug Binding Sites of Target | Top | |||||
|---|---|---|---|---|---|---|
| Ligand Name: Myo-inositol hexaphosphate | Ligand Info | |||||
| Structure Description | Solution structure of human acidic fibroblast growth factor in complex with anti-angiogenic drug inositol hexaphosphate (IP6) | PDB:2K8R | ||||
| Method | Solution NMR | Resolution | N.A. | Mutation | No | [1] |
| PDB Sequence |
YKKPKLLYCS
10 NGGHFLRILP20 DGTVDGTRDR30 SDQHIQLQLS40 AESVGEVYIK50 STETGQYLAM 60 DTDGLLYGSQ70 TPNEECLFLE80 RLEENHYNTY90 ISKKHAEKNW100 FVGLKKNGSC 110 KRGPRTHYGQ120 KAILFLPLPV130 SSD
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| Ligand Name: Naphthalene Trisulfonate | Ligand Info | |||||
| Structure Description | NMR STUDY OF ACID FIBROBLAST GROWTH FACTOR BOUND TO 1,3,6-NAPHTHALENE TRISULPHONATE, 26 STRUCTURES | PDB:1RML | ||||
| Method | Solution NMR | Resolution | N.A. | Mutation | No | [2] |
| PDB Sequence |
KPKLLYCSNG
33 GHFLRILPDG43 TVDGTRDRSD53 QHIQLQLSAE63 SVGEVYIKST73 ETGQYLAMDT 83 DGLLYGSQTP93 NEECLFLERL103 EENHYNTYIS113 KKHAEKNWFV123 GLKKNGSCKR 133 GPRTHYGQKA143 ILFLPLPVSS153 D
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| Ligand Name: 2,5-Dihydroxybenzenesulfonic Acid | Ligand Info | |||||
| Structure Description | Acidic Fibroblast Growth Factor (FGF-1) complexed with dobesilate | PDB:3K1X | ||||
| Method | X-ray diffraction | Resolution | 1.98 Å | Mutation | No | [3] |
| PDB Sequence |
KKPKLLYCSN
10 GGHFLRILPD20 GTVDGTRDRS30 DQHIQLQLSA40 ESVGEVYIKS50 TETGQYLAMD 60 TDGLLYGSQT70 PNEECLFLER80 LEENHYNTYI90 SKKHAEKNWF100 VGLKKNGSCK 110 RGPRTHYGQK120 AILFLPLPVS130
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Click to Show 3D Structure of This Binding Site
set background white;style ions nothing; color 8e8e8e;style chemicals nothing; select .DBX or .DBX2 or .DBX3 or :3DBX;style chemicals stick;color identity;select .A:10 or .A:103 or .A:104 or .A:105 or .A:110 or .A:118 or .A:119 or .A:120 or .A:121; color #00ffc7; zoom selection;set surface opacity 0.5;set surface Van der Waals surface;set mode all
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| Ligand Name: 2,5-Dihydroxybenzoic acid | Ligand Info | |||||
| Structure Description | Acidic Fibroblast Growth Factor (FGF-1) complexed with gentisic acid | PDB:3JUT | ||||
| Method | X-ray diffraction | Resolution | 2.25 Å | Mutation | No | [3] |
| PDB Sequence |
KKPKLLYCSN
10 GGHFLRILPD20 GTVDGTRDRS30 DQHIQLQLSA40 ESVGEVYIKS50 TETGQYLAMD 60 TDGLLYGSQT70 PNEECLFLER80 LEENHYNTYI90 SKKHAEKNWF100 VGLKKNGSCK 110 RGPRTHYGQK120 AILFLPLPVS130
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Click to Show 3D Structure of This Binding Site
set background white;style ions nothing; color 8e8e8e;style chemicals nothing; select .GTQ or .GTQ2 or .GTQ3 or :3GTQ;style chemicals stick;color identity;select .A:10 or .A:104 or .A:105 or .A:110 or .A:118 or .A:119 or .A:120 or .A:121; color #f3c393; zoom selection;set surface opacity 0.5;set surface Van der Waals surface;set mode all
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| References | Top | ||||
|---|---|---|---|---|---|
| REF 1 | Solution structure of human acidic fibroblast growth factor in complex with anti-angiogenic drug inositol hexaphosphate (IP6) | ||||
| REF 2 | Solution structure of acidic fibroblast growth factor bound to 1,3, 6-naphthalenetrisulfonate: a minimal model for the anti-tumoral action of suramins and suradistas. J Mol Biol. 1998 Sep 4;281(5):899-915. | ||||
| REF 3 | Gentisic acid, a compound associated with plant defense and a metabolite of aspirin, heads a new class of in vivo fibroblast growth factor inhibitors. J Biol Chem. 2010 Apr 9;285(15):11714-29. | ||||
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