Target Information
| Target General Information | Top | |||||
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| Target ID |
T31621
(Former ID: TTDR00567)
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| Target Name |
Fibroblast growth factor-2 (FGF2)
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| Synonyms |
bFGF; Heparin-binding growth factor 2; HBGF-2; Fibroblast growth factor 2; FGFB; FGF-2; Basic fibroblast growth factor
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| Gene Name |
FGF2
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| Target Type |
Successful target
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[1] | ||||
| Disease | [+] 1 Target-related Diseases | + | ||||
| 1 | Acne vulgaris [ICD-11: ED80] | |||||
| Function |
Acts as a ligand for FGFR1, FGFR2, FGFR3 and FGFR4. Also acts as an integrin ligand which is required for FGF2 signaling. Binds to integrin ITGAV:ITGB3. Plays an important role in the regulation of cell survival, cell division, cell differentiation and cell migration. Functions as a potent mitogen in vitro. Can induce angiogenesis.
Click to Show/Hide
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| BioChemical Class |
Growth factor
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| UniProt ID | ||||||
| Sequence |
MVGVGGGDVEDVTPRPGGCQISGRGARGCNGIPGAAAWEAALPRRRPRRHPSVNPRSRAA
GSPRTRGRRTEERPSGSRLGDRGRGRALPGGRLGGRGRGRAPERVGGRGRGRGTAAPRAA PAARGSRPGPAGTMAAGSITTLPALPEDGGSGAFPPGHFKDPKRLYCKNGGFFLRIHPDG RVDGVREKSDPHIKLQLQAEERGVVSIKGVCANRYLAMKEDGRLLASKCVTDECFFFERL ESNNYNTYRSRKYTSWYVALKRTGQYKLGSKTGPGQKAILFLPMSAKS Click to Show/Hide
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| 3D Structure | Click to Show 3D Structure of This Target | AlphaFold | ||||
| ADReCS ID | BADD_A01487 | |||||
| HIT2.0 ID | T88QQE | |||||
| Drugs and Modes of Action | Top | |||||
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| Approved Drug(s) | [+] 1 Approved Drugs | + | ||||
| 1 | Sucralfate | Drug Info | Approved | Acne vulgaris | [2], [3], [4] | |
| Clinical Trial Drug(s) | [+] 4 Clinical Trial Drugs | + | ||||
| 1 | Squalamine | Drug Info | Phase 3 | Solid tumour/cancer | [5] | |
| 2 | Bemarituzumab | Drug Info | Phase 2 | Gastric adenocarcinoma | [6] | |
| 3 | DVC1-0101 | Drug Info | Phase 2 | Arteriosclerosis | [7] | |
| 4 | FPA144 | Drug Info | Phase 1 | Bladder cancer | [8] | |
| Discontinued Drug(s) | [+] 2 Discontinued Drugs | + | ||||
| 1 | TGP-580 | Drug Info | Discontinued in Phase 2 | Neurodegenerative disorder | [9] | |
| 2 | RG-8803 | Drug Info | Terminated | Diabetic retinopathy | [10] | |
| Mode of Action | [+] 3 Modes of Action | + | ||||
| Modulator | [+] 4 Modulator drugs | + | ||||
| 1 | Sucralfate | Drug Info | [1], [3] | |||
| 2 | Squalamine | Drug Info | [11] | |||
| 3 | DVC1-0101 | Drug Info | [7] | |||
| 4 | TGP-580 | Drug Info | [13] | |||
| Antagonist | [+] 2 Antagonist drugs | + | ||||
| 1 | Bemarituzumab | Drug Info | [12] | |||
| 2 | FPA144 | Drug Info | [8] | |||
| Inhibitor | [+] 6 Inhibitor drugs | + | ||||
| 1 | RG-8803 | Drug Info | [14] | |||
| 2 | 1,4-Dideoxy-5-Dehydro-O2-Sulfo-Glucuronic Acid | Drug Info | [15] | |||
| 3 | 1,4-Dideoxy-O2-Sulfo-Glucuronic Acid | Drug Info | [15] | |||
| 4 | 2-Sulfhydryl-Ethanol | Drug Info | [15] | |||
| 5 | BIBF100 | Drug Info | [16] | |||
| 6 | N,O6-Disulfo-Glucosamine | Drug Info | [15] | |||
| Chemical Structure based Activity Landscape of Target | Top |
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| Drug Property Profile of Target | Top | |
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| (1) Molecular Weight (mw) based Drug Clustering | (2) Octanol/Water Partition Coefficient (xlogp) based Drug Clustering | |
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| (3) Hydrogen Bond Donor Count (hbonddonor) based Drug Clustering | (4) Hydrogen Bond Acceptor Count (hbondacc) based Drug Clustering | |
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| (5) Rotatable Bond Count (rotbonds) based Drug Clustering | (6) Topological Polar Surface Area (polararea) based Drug Clustering | |
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| "RO5" indicates the cutoff set by lipinski's rule of five; "D123AB" colored in GREEN denotes the no violation of any cutoff in lipinski's rule of five; "D123AB" colored in PURPLE refers to the violation of only one cutoff in lipinski's rule of five; "D123AB" colored in BLACK represents the violation of more than one cutoffs in lipinski's rule of five | ||
| Target Poor or Non Binders | Top | |||||
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| Target Poor or Non Binders | ||||||
| Target Regulators | Top | |||||
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| Target-regulating microRNAs | ||||||
| Target-interacting Proteins | ||||||
| Target Profiles in Patients | Top | |||||
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| Target Expression Profile (TEP) | ||||||
| References | Top | |||||
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| REF 1 | Assessment of sucralfate coating by sequential scintigraphic imaging in radiation-induced esophageal lesions. Gastrointest Endosc. 1995 Feb;41(2):109-14. | |||||
| REF 2 | URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7055). | |||||
| REF 3 | Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015 | |||||
| REF 4 | ClinicalTrials.gov (NCT01284647) A Study to Evaluate the Efficacy of Teprenone On Chinese Patients With Chronic Non-Atrophic Erosive Gastritis. U.S. National Institutes of Health. | |||||
| REF 5 | ClinicalTrials.gov (NCT00139282) A Safety and Efficacy Study of Squalamine Lactate for Injection (MSI-1256F) for "Wet" Age-Related Macular Degeneration. U.S. National Institutes of Health. | |||||
| REF 6 | ClinicalTrials.gov (NCT03694522) A Study of Bemarituzumab (FPA144) Combined With Modified FOLFOX6 (mFOLFOX6) in Gastric/Gastroesophageal Junction Cancer (FIGHT) (FIGHT). U.S. National Institutes of Health. | |||||
| REF 7 | DVC1-0101 to treat peripheral arterial disease: a Phase I/IIa open-label dose-escalation clinical trial. Mol Ther. 2013 Mar;21(3):707-14. | |||||
| REF 8 | Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA) | |||||
| REF 9 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001922) | |||||
| REF 10 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800011158) | |||||
| REF 11 | Clinical pipeline report, company report or official report of Ohr Pharmaceutical. | |||||
| REF 12 | Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA) | |||||
| REF 13 | Expression of fibroblast growth factor-2 transcripts in the healing of acetic acid-induced gastric ulcers. APMIS. 1999 Aug;107(8):767-72. | |||||
| REF 14 | US patent application no. 2010,0278,784, Methods and compositions for treating skin conditions. | |||||
| REF 15 | How many drug targets are there Nat Rev Drug Discov. 2006 Dec;5(12):993-6. | |||||
| REF 16 | Emerging therapies for multiple myeloma. Expert Opin Emerg Drugs. 2009 Mar;14(1):99-127. | |||||
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