Target Information
Target General Information | Top | |||||
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Target ID |
T97257
(Former ID: TTDR00511)
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Target Name |
Transforming growth factor beta 1 (TGFB1)
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Synonyms |
Transforming growth factor beta-1 proprotein; Transforming growth factor beta-1; TGFB; TGF-beta1; TGF-beta 1
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Gene Name |
TGFB1
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Target Type |
Successful target
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[1] | ||||
Disease | [+] 1 Target-related Diseases | + | ||||
1 | Idiopathic interstitial pneumonitis [ICD-11: CB03] | |||||
Function |
Transforming growth factor beta-1 proprotein: Precursor of the Latency-associated peptide (LAP) and Transforming growth factor beta-1 (TGF-beta-1) chains, which constitute the regulatory and active subunit of TGF-beta-1, respectively.
Click to Show/Hide
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BioChemical Class |
Growth factor
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UniProt ID | ||||||
Sequence |
MPPSGLRLLLLLLPLLWLLVLTPGRPAAGLSTCKTIDMELVKRKRIEAIRGQILSKLRLA
SPPSQGEVPPGPLPEAVLALYNSTRDRVAGESAEPEPEPEADYYAKEVTRVLMVETHNEI YDKFKQSTHSIYMFFNTSELREAVPEPVLLSRAELRLLRLKLKVEQHVELYQKYSNNSWR YLSNRLLAPSDSPEWLSFDVTGVVRQWLSRGGEIEGFRLSAHCSCDSRDNTLQVDINGFT TGRRGDLATIHGMNRPFLLLMATPLERAQHLQSSRHRRALDTNYCFSSTEKNCCVRQLYI DFRKDLGWKWIHEPKGYHANFCLGPCPYIWSLDTQYSKVLALYNQHNPGASAAPCCVPQA LEPLPIVYYVGRKPKVEQLSNMIVRSCKCS Click to Show/Hide
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3D Structure | Click to Show 3D Structure of This Target | PDB | ||||
ADReCS ID | BADD_A01246 ; BADD_A01249 ; BADD_A03745 ; BADD_A05045 | |||||
HIT2.0 ID | T53AOE |
Drugs and Modes of Action | Top | |||||
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Approved Drug(s) | [+] 1 Approved Drugs | + | ||||
1 | Pirfenidone | Drug Info | Approved | Idiopathic pulmonary fibrosis | [2], [3], [4] | |
Clinical Trial Drug(s) | [+] 5 Clinical Trial Drugs | + | ||||
1 | TG-C | Drug Info | Phase 3 | Arthritis | [5] | |
2 | LY2157299 | Drug Info | Phase 2/3 | Arteriosclerosis | [6], [7] | |
3 | Disitertide | Drug Info | Phase 2 | Macular degeneration | [8] | |
4 | ABBV-151 | Drug Info | Phase 1 | Solid tumour/cancer | [9] | |
5 | SRK-181 | Drug Info | Phase 1 | Solid tumour/cancer | [10] | |
Discontinued Drug(s) | [+] 1 Discontinued Drugs | + | ||||
1 | Mannose phosphate | Drug Info | Discontinued in Phase 2 | Lesion | [11] | |
Mode of Action | [+] 2 Modes of Action | + | ||||
Modulator | [+] 4 Modulator drugs | + | ||||
1 | Pirfenidone | Drug Info | [1] | |||
2 | TG-C | Drug Info | [5], [12] | |||
3 | Mannose phosphate | Drug Info | [17] | |||
4 | ART-144 | Drug Info | [18] | |||
Inhibitor | [+] 4 Inhibitor drugs | + | ||||
1 | LY2157299 | Drug Info | [13], [14] | |||
2 | Disitertide | Drug Info | [8] | |||
3 | ABBV-151 | Drug Info | [15] | |||
4 | SRK-181 | Drug Info | [16] |
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 |
Co-Targets | Top | |||||
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Co-Targets |
Target Regulators | Top | |||||
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Target-regulating microRNAs | ||||||
Target-regulating Transcription Factors | ||||||
Target-interacting Proteins |
Target Profiles in Patients | Top | |||||
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Target Expression Profile (TEP) |
References | Top | |||||
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REF 1 | Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. | |||||
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: 7532). | |||||
REF 3 | 2014 FDA drug approvals. Nat Rev Drug Discov. 2015 Feb;14(2):77-81. | |||||
REF 4 | Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015 | |||||
REF 5 | ClinicalTrials.gov (NCT02072070) Efficacy and Safety Study of TissueGene-C to Degenerative Arthritis. U.S. National Institutes of Health. | |||||
REF 6 | 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: 7797). | |||||
REF 7 | ClinicalTrials.gov (NCT02008318) A Study of LY2157299 in Participants With Myelodysplastic Syndromes. U.S. National Institutes of Health. | |||||
REF 8 | Perspectives of TGF-beta inhibition in pancreatic and hepatocellular carcinomas. Oncotarget. 2014 January; 5(1): 78-94. | |||||
REF 9 | ClinicalTrials.gov (NCT03821935) Study to Determine the Safety, Tolerability, Pharmacokinetics and RP2D of ABBV-151 as a Single Agent and in Combination With ABBV-181 in Participants With Locally Advanced or Metastatic Solid Tumors. U.S. National Institutes of Health. | |||||
REF 10 | ClinicalTrials.gov (NCT04291079) SRK-181 Alone or in Combination With Anti-PD-(L)1 Antibody Therapy in Patients With Locally Advanced or Metastatic Solid Tumors (DRAGON). U.S. National Institutes of Health. | |||||
REF 11 | Mannose phosphate isomerase regulates fibroblast growth factor receptor family signaling and glioma radiosensitivity. PLoS One. 2014 Oct 14;9(10):e110345. | |||||
REF 12 | Clinical pipeline report, company report or official report of Tissue Gene, Inc. | |||||
REF 13 | Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA) | |||||
REF 14 | Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA) | |||||
REF 15 | Clinical pipeline report, company report or official report of AbbVie. | |||||
REF 16 | Clinical pipeline report, company report or official report of Scholar Rock. | |||||
REF 17 | The mannose-6-phosphate analogue, PXS64, inhibits fibrosis via TGF-beta1 pathway in human lung fibroblasts. Immunol Lett. 2015 Jun;165(2):90-101. | |||||
REF 18 | Pharmaceutical products of TORREYA partners. December 2011. |
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