Target Information
Target General Infomation | |||||
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Target ID |
T46482
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Former ID |
TTDS00311
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Target Name |
Toll-like receptor 7
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Gene Name |
TLR7
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Synonyms |
TLR7
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Target Type |
Successful
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Disease | Autoimmune diabetes [ICD10: E08-E13] | ||||
Allergic rhinitis [ICD9: 472.0, 477, 995.3; ICD10: J00, J30, J31.0, T78.4] | |||||
Asthma [ICD10: J45] | |||||
Bladder cancer [ICD9: 188; ICD10: C67] | |||||
Cancer [ICD9: 140-229; ICD10: C00-C96] | |||||
Diffuse large B-cell lymphoma [ICD9: 200; ICD10: C83.3] | |||||
HCV infection [ICD9: 070.4, 070.5, 070.70; ICD10: B17.1, B18.2] | |||||
HBV infection [ICD9: 070.2-070.3; ICD10: B16, B18.0, B18.1] | |||||
Herpes simplex virus infection [ICD9: 54; ICD10: B00] | |||||
Immuno-modulator [ICD9: 135, 691.8, 692.9, 710-719, 714; ICD10: D86, L20, L20-L30, M00-M25, M05-M06] | |||||
Immuno-stimulant [ICD10: C00-C97] | |||||
Malaria [ICD10: B54] | |||||
Skin cancers [ICD9: 172, 173; ICD10: C43, C44] | |||||
Systemic lupus erythematosus [ICD9: 710; ICD10: M32] | |||||
Function |
Key component of innate and adaptive immunity. TLRs (Toll-like receptors) control host immune response against pathogens through recognition of molecular patterns specific to microorganisms. TLR7 is a nucleotide-sensing TLR which is activated by single-stranded RNA. Acts via MYD88 and TRAF6, leading to NF-kappa-B activation, cytokine secretion and the inflammatory response (By similarity).
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BioChemical Class |
Toll-like receptor family
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Target Validation |
T46482
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UniProt ID | |||||
Sequence |
MVFPMWTLKRQILILFNIILISKLLGARWFPKTLPCDVTLDVPKNHVIVDCTDKHLTEIP
GGIPTNTTNLTLTINHIPDISPASFHRLDHLVEIDFRCNCVPIPLGSKNNMCIKRLQIKP RSFSGLTYLKSLYLDGNQLLEIPQGLPPSLQLLSLEANNIFSIRKENLTELANIEILYLG QNCYYRNPCYVSYSIEKDAFLNLTKLKVLSLKDNNVTAVPTVLPSTLTELYLYNNMIAKI QEDDFNNLNQLQILDLSGNCPRCYNAPFPCAPCKNNSPLQIPVNAFDALTELKVLRLHSN SLQHVPPRWFKNINKLQELDLSQNFLAKEIGDAKFLHFLPSLIQLDLSFNFELQVYRASM NLSQAFSSLKSLKILRIRGYVFKELKSFNLSPLHNLQNLEVLDLGTNFIKIANLSMFKQF KRLKVIDLSVNKISPSGDSSEVGFCSNARTSVESYEPQVLEQLHYFRYDKYARSCRFKNK EASFMSVNESCYKYGQTLDLSKNSIFFVKSSDFQHLSFLKCLNLSGNLISQTLNGSEFQP LAELRYLDFSNNRLDLLHSTAFEELHKLEVLDISSNSHYFQSEGITHMLNFTKNLKVLQK LMMNDNDISSSTSRTMESESLRTLEFRGNHLDVLWREGDNRYLQLFKNLLKLEELDISKN SLSFLPSGVFDGMPPNLKNLSLAKNGLKSFSWKKLQCLKNLETLDLSHNQLTTVPERLSN CSRSLKNLILKNNQIRSLTKYFLQDAFQLRYLDLSSNKIQMIQKTSFPENVLNNLKMLLL HHNRFLCTCDAVWFVWWVNHTEVTIPYLATDVTCVGPGAHKGQSVISLDLYTCELDLTNL ILFSLSISVSLFLMVMMTASHLYFWDVWYIYHFCKAKIKGYQRLISPDCCYDAFIVYDTK DPAVTEWVLAELVAKLEDPREKHFNLCLEERDWLPGQPVLENLSQSIQLSKKTVFVMTDK YAKTENFKIAFYLSHQRLMDEKVDVIILIFLEKPFQKSKFLQLRKRLCGSSVLEWPTNPQ AHPYFWQCLKNALATDNHVAYSQVFKETV |
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Drugs and Mode of Action | |||||
Drug(s) | Hydroxychloroquine | Drug Info | Approved | Malaria | [536651], [542210] |
Imiquimod | Drug Info | Approved | Skin cancers | [468123], [536772] | |
ANA773 | Drug Info | Phase 2a | HCV infection | [550256] | |
AZD-8848 | Drug Info | Phase 2 | Allergic rhinitis | [523140] | |
GS-9620 | Drug Info | Phase 2 | HBV infection | [532515] | |
GSK2245035 | Drug Info | Phase 2 | Asthma | [523920] | |
Isatoribine | Drug Info | Phase 2 | HCV infection | [522035] | |
LOXORIBINE | Drug Info | Phase 2 | Immuno-stimulant | [468129], [545189] | |
Resiquimod | Drug Info | Phase 1/2 | Herpes simplex virus infection | [468141], [546884] | |
CPG 52364 | Drug Info | Phase 1 | Systemic lupus erythematosus | [532501] | |
IMO-3100 | Drug Info | Phase 1 | Autoimmune diabetes | [550998] | |
PF-4878691 | Drug Info | Phase 1 | HCV infection | [522524] | |
IM0-8400 | Drug Info | Discontinued in Phase 1/2 | Diffuse large B-cell lymphoma | [550999] | |
ANA-975 | Drug Info | Discontinued in Phase 1 | Immuno-modulator | [547967] | |
DV-1179 | Drug Info | Discontinued in Phase 1 | Systemic lupus erythematosus | [549321] | |
IPH-3201 | Drug Info | Terminated | Cancer | [548555] | |
Agonist | ANA-975 | Drug Info | [536564] | ||
ANA773 | Drug Info | [550256] | |||
AZD-8848 | Drug Info | [531949] | |||
Imiquimod | Drug Info | [537456] | |||
Isatoribine | Drug Info | [536564] | |||
LOXORIBINE | Drug Info | [526863], [551871] | |||
PF-4878691 | Drug Info | [531417] | |||
TMX-202 | Drug Info | [543475] | |||
TMX-30X | Drug Info | [543475] | |||
Antagonist | CPG 52364 | Drug Info | [551089] | ||
Hydroxychloroquine | Drug Info | [536605] | |||
IM0-8400 | Drug Info | [551000] | |||
Modulator | DV-1179 | Drug Info | |||
GS-9620 | Drug Info | [532515] | |||
GSK2245035 | Drug Info | [533262] | |||
IMO-3100 | Drug Info | ||||
IPH-3201 | Drug Info | [543475] | |||
Resiquimod | Drug Info | ||||
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM) | |||||
TEP | EXP Info | ||||
Pathways | |||||
KEGG Pathway | Toll-like receptor signaling pathway | ||||
Measles | |||||
Influenza A | |||||
NetPath Pathway | TCR Signaling Pathway | ||||
PANTHER Pathway | Toll receptor signaling pathway | ||||
Reactome | Trafficking and processing of endosomal TLR | ||||
TRAF6 mediated IRF7 activation in TLR7/8 or 9 signaling | |||||
TRAF6 mediated induction of NFkB and MAP kinases upon TLR7/8 or 9 activation | |||||
MyD88 dependent cascade initiated on endosome | |||||
WikiPathways | Toll-like receptor signaling pathway | ||||
Toll-Like Receptors Cascades | |||||
MyD88 dependent cascade initiated on endosome | |||||
Trafficking and processing of endosomal TLR | |||||
Regulation of toll-like receptor signaling pathway | |||||
References | |||||
Ref 468123 | (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: 5003). | ||||
Ref 468129 | (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: 5018). | ||||
Ref 468141 | (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: 5051). | ||||
Ref 522035 | ClinicalTrials.gov (NCT00480831) A Study of PRO95780 in Patients With Previously Untreated, Advanced-Stage Non-Small Cell Lung Cancer (APM4074g). U.S. National Institutes of Health. | ||||
Ref 522524 | ClinicalTrials.gov (NCT00810758) Multiple Oral Dose Study to Evaluate the Safety, Tolerability, Pharmacokinetics and Pharmacodynamics of PF-04878691. U.S. National Institutes of Health. | ||||
Ref 523140 | ClinicalTrials.gov (NCT01185080) Efficacy Study in Allergic Rhinitis Patients After Intranasal Administration of AZD8848. U.S. National Institutes of Health. | ||||
Ref 523920 | ClinicalTrials.gov (NCT01607372) A Study to Investigate the Safety, Pharmacodynamics and Efficacy Against Allergic Reactivity of Repeat Intranasal Administration of the TLR7 Agonist GSK2245035 in Subjects With Respiratory Allergies. U.S. National Institutes of Health. | ||||
Ref 532501 | Treatment of systemic lupus erythematosus: new therapeutic avenues and blind alleys. Nat Rev Rheumatol. 2014 Jan;10(1):23-34. | ||||
Ref 532515 | Pharmacokinetic and pharmacodynamic properties of GS-9620, a novel Toll-like receptor 7 agonist, demonstrate interferon-stimulated gene induction without detectable serum interferon at low oral doses. J Pharmacol Exp Ther. 2014 Jan;348(1):96-105. | ||||
Ref 536772 | New drugs in development for the treatment of endometriosis. Expert Opin Investig Drugs. 2008 Aug;17(8):1187-202. | ||||
Ref 542210 | (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: 7198). | ||||
Ref 545189 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002417) | ||||
Ref 546884 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800010858) | ||||
Ref 547967 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800020825) | ||||
Ref 548555 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800026574) | ||||
Ref 549321 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800035150) | ||||
Ref 550256 | Clinical pipeline report, company report or official report of Anadys Pharmaceuticals (2011). | ||||
Ref 526863 | The Toll-like receptor 7 (TLR7)-specific stimulus loxoribine uncovers a strong relationship within the TLR7, 8 and 9 subfamily. Eur J Immunol. 2003 Nov;33(11):2987-97. | ||||
Ref 531417 | The innate immune response, clinical outcomes, and ex vivo HCV antiviral efficacy of a TLR7 agonist (PF-4878691). Clin Pharmacol Ther. 2011 Jun;89(6):821-9. | ||||
Ref 531949 | Repeated intranasal TLR7 stimulation reduces allergen responsiveness in allergic rhinitis. Respir Res. 2012 Jun 22;13:53. | ||||
Ref 532515 | Pharmacokinetic and pharmacodynamic properties of GS-9620, a novel Toll-like receptor 7 agonist, demonstrate interferon-stimulated gene induction without detectable serum interferon at low oral doses. J Pharmacol Exp Ther. 2014 Jan;348(1):96-105. | ||||
Ref 533262 | Early clinical evaluation of the intranasal TLR7 agonist GSK2245035: Use of translational biomarkers to guide dosing and confirm target engagement. Clin Pharmacol Ther. 2015 Oct;98(4):369-80. | ||||
Ref 536564 | Discovery of ANA975: an oral prodrug of the TLR-7 agonist isatoribine. Nucleosides Nucleotides Nucleic Acids. 2007;26(6-7):635-40. | ||||
Ref 536605 | TLR7/9 antagonists as therapeutics for immune-mediated inflammatory disorders. Inflamm Allergy Drug Targets. 2007 Dec;6(4):223-35. | ||||
Ref 537456 | Imiquimod Enhances IFN-gamma Production and Effector Function of T Cells Infiltrating Human Squamous Cell Carcinomas of the Skin. J Invest Dermatol. 2009 Jun 11. | ||||
Ref 543475 | (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. (Target id: 1757). | ||||
Ref 550256 | Clinical pipeline report, company report or official report of Anadys Pharmaceuticals (2011). |
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