Target Information

Target General Infomation
Target ID
T46482
Former ID
TTDS00311
Target Name
Toll-like receptor 7
Gene Name
TLR7
Synonyms
TLR7
Target Type
Successful
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]
HBV infection [ICD9: 070.2-070.3; ICD10: B16, B18.0, B18.1]
Herpes simplex virus infection [ICD9: 54; ICD10: B00]
HCV infection [ICD9: 070.4, 070.5, 070.70; ICD10: B17.1, B18.2]
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]
Systemic lupus erythematosus [ICD9: 710; ICD10: M32]
Skin cancers [ICD9: 172, 173; ICD10: C43, C44]
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).
BioChemical Class
Toll-like receptor family
Target Validation
T46482
UniProt ID
Q9NYK1
Sequence
MVFPMWTLKRQILILFNIILISKLLGARWFPKTLPCDVTLDVPKNHVIVDCTDKHLTEIP
GGIPTNTTNLTLTINHIPDISPASFHRLDHLVEIDFRCNCVPIPLGSKNNMCIKRLQIKP
RSFSGLTYLKSLYLDGNQLLEIPQGLPPSLQLLSLEANNIFSIRKENLTELANIEILYLG
QNCYYRNPCYVSYSIEKDAFLNLTKLKVLSLKDNNVTAVPTVLPSTLTELYLYNNMIAKI
QEDDFNNLNQLQILDLSGNCPRCYNAPFPCAPCKNNSPLQIPVNAFDALTELKVLRLHSN
SLQHVPPRWFKNINKLQELDLSQNFLAKEIGDAKFLHFLPSLIQLDLSFNFELQVYRASM
NLSQAFSSLKSLKILRIRGYVFKELKSFNLSPLHNLQNLEVLDLGTNFIKIANLSMFKQF
KRLKVIDLSVNKISPSGDSSEVGFCSNARTSVESYEPQVLEQLHYFRYDKYARSCRFKNK
EASFMSVNESCYKYGQTLDLSKNSIFFVKSSDFQHLSFLKCLNLSGNLISQTLNGSEFQP
LAELRYLDFSNNRLDLLHSTAFEELHKLEVLDISSNSHYFQSEGITHMLNFTKNLKVLQK
LMMNDNDISSSTSRTMESESLRTLEFRGNHLDVLWREGDNRYLQLFKNLLKLEELDISKN
SLSFLPSGVFDGMPPNLKNLSLAKNGLKSFSWKKLQCLKNLETLDLSHNQLTTVPERLSN
CSRSLKNLILKNNQIRSLTKYFLQDAFQLRYLDLSSNKIQMIQKTSFPENVLNNLKMLLL
HHNRFLCTCDAVWFVWWVNHTEVTIPYLATDVTCVGPGAHKGQSVISLDLYTCELDLTNL
ILFSLSISVSLFLMVMMTASHLYFWDVWYIYHFCKAKIKGYQRLISPDCCYDAFIVYDTK
DPAVTEWVLAELVAKLEDPREKHFNLCLEERDWLPGQPVLENLSQSIQLSKKTVFVMTDK
YAKTENFKIAFYLSHQRLMDEKVDVIILIFLEKPFQKSKFLQLRKRLCGSSVLEWPTNPQ
AHPYFWQCLKNALATDNHVAYSQVFKETV
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 522035ClinicalTrials.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 522524ClinicalTrials.gov (NCT00810758) Multiple Oral Dose Study to Evaluate the Safety, Tolerability, Pharmacokinetics and Pharmacodynamics of PF-04878691. U.S. National Institutes of Health.
Ref 523140ClinicalTrials.gov (NCT01185080) Efficacy Study in Allergic Rhinitis Patients After Intranasal Administration of AZD8848. U.S. National Institutes of Health.
Ref 523920ClinicalTrials.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 532501Treatment of systemic lupus erythematosus: new therapeutic avenues and blind alleys. Nat Rev Rheumatol. 2014 Jan;10(1):23-34.
Ref 532515Pharmacokinetic 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 536651Emerging drugs for rheumatoid arthritis. Expert Opin Emerg Drugs. 2008 Mar;13(1):175-96.
Ref 536772New 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 545189Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002417)
Ref 546884Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800010858)
Ref 547967Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800020825)
Ref 548555Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800026574)
Ref 549321Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800035150)
Ref 550256Clinical pipeline report, company report or official report of Anadys Pharmaceuticals (2011).
Ref 550998Clinical pipeline report, company report or official report of Idera Pharmaceuticals (2011).
Ref 550999Clinical pipeline report, company report or official report of Idera Pharmaceuticals.
Ref 526863The 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 531417The 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 531949Repeated intranasal TLR7 stimulation reduces allergen responsiveness in allergic rhinitis. Respir Res. 2012 Jun 22;13:53.
Ref 532515Pharmacokinetic 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 533262Early 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 536564Discovery of ANA975: an oral prodrug of the TLR-7 agonist isatoribine. Nucleosides Nucleotides Nucleic Acids. 2007;26(6-7):635-40.
Ref 536605TLR7/9 antagonists as therapeutics for immune-mediated inflammatory disorders. Inflamm Allergy Drug Targets. 2007 Dec;6(4):223-35.
Ref 537456Imiquimod 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 550256Clinical pipeline report, company report or official report of Anadys Pharmaceuticals (2011).
Ref 551000Clinical pipeline report, company report or official report of Idera Pharmaceuticals.
Ref 551089Coley Pharmaceutical Group Diversifies Pipeline with First-in-Class TLR Antagonist for the Treatment of Systemic Lupus Erythematosus. Lupus Foundation of America, Inc. 2007.
Ref 551871Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015

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