Target Information
Target General Infomation | |||||
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Target ID |
T11451
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Former ID |
TTDC00107
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Target Name |
Toll-like receptor 9
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Gene Name |
TLR9
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Synonyms |
TLR-9; TLR9
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Target Type |
Clinical Trial
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Disease | Allergic rhinitis [ICD9: 472.0, 477, 995.3; ICD10: J00, J30, J31.0, T78.4] | ||||
Asthma; Allergy [ICD9: 204.0, 493, 995.3; ICD10: C91.0, J45, T78.4] | |||||
Autoimmune diabetes [ICD10: E08-E13] | |||||
Asthma [ICD10: J45] | |||||
Bacillus anthracis infection [ICD10: A22] | |||||
Chronic lymphocytic leukaemia [ICD10: C91] | |||||
Cancer [ICD9: 140-229; ICD10: C00-C96] | |||||
Colorectal cancer [ICD9: 153, 154; ICD10: C18-C21] | |||||
Diffuse large B-cell lymphoma [ICD9: 200; ICD10: C83.3] | |||||
Glioblastoma multiforme [ICD9: 191; ICD10: C71] | |||||
HBV infection [ICD9: 070.2-070.3; ICD10: B16, B18.0, B18.1] | |||||
HCV infection [ICD9: 070.4, 070.5, 070.70; ICD10: B17.1, B18.2] | |||||
Human immunodeficiency virus infection [ICD9: 279.3; ICD10: B20-B26] | |||||
Infections [ICD9: 001-139; ICD10: A00-B99] | |||||
Inflammatory bowel disease [ICD9: 555, 556; ICD10: K50, K51] | |||||
Influenza virus [ICD10: J11.1] | |||||
Leukemia [ICD9: 208.9; ICD10: C90-C95] | |||||
Lung cancer [ICD9: 162; ICD10: C33-C34] | |||||
Prostate cancer [ICD9: 185; ICD10: C61] | |||||
Renal cell carcinoma; Solid tumours [ICD9: 140-199, 189, 210-229; ICD10: C00-C75, C64, C7A, C7B, D10-D36, D3A] | |||||
Systemic lupus erythematosus [ICD9: 710; ICD10: M32] | |||||
Function |
Participates in the innate immune response to microbial agents. Detects the unmethylated cytidine-phosphate-guanosine (cpg) motivs present in bacterial dna. Acts via myd88 and traf6, leading to nf-kappa-b activation, cytokine secretion andthe inflammatory process.
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BioChemical Class |
Toll-like receptor family
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Target Validation |
T11451
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UniProt ID | |||||
Sequence |
MGFCRSALHPLSLLVQAIMLAMTLALGTLPAFLPCELQPHGLVNCNWLFLKSVPHFSMAA
PRGNVTSLSLSSNRIHHLHDSDFAHLPSLRHLNLKWNCPPVGLSPMHFPCHMTIEPSTFL AVPTLEELNLSYNNIMTVPALPKSLISLSLSHTNILMLDSASLAGLHALRFLFMDGNCYY KNPCRQALEVAPGALLGLGNLTHLSLKYNNLTVVPRNLPSSLEYLLLSYNRIVKLAPEDL ANLTALRVLDVGGNCRRCDHAPNPCMECPRHFPQLHPDTFSHLSRLEGLVLKDSSLSWLN ASWFRGLGNLRVLDLSENFLYKCITKTKAFQGLTQLRKLNLSFNYQKRVSFAHLSLAPSF GSLVALKELDMHGIFFRSLDETTLRPLARLPMLQTLRLQMNFINQAQLGIFRAFPGLRYV DLSDNRISGASELTATMGEADGGEKVWLQPGDLAPAPVDTPSSEDFRPNCSTLNFTLDLS RNNLVTVQPEMFAQLSHLQCLRLSHNCISQAVNGSQFLPLTGLQVLDLSHNKLDLYHEHS FTELPRLEALDLSYNSQPFGMQGVGHNFSFVAHLRTLRHLSLAHNNIHSQVSQQLCSTSL RALDFSGNALGHMWAEGDLYLHFFQGLSGLIWLDLSQNRLHTLLPQTLRNLPKSLQVLRL RDNYLAFFKWWSLHFLPKLEVLDLAGNQLKALTNGSLPAGTRLRRLDVSCNSISFVAPGF FSKAKELRELNLSANALKTVDHSWFGPLASALQILDVSANPLHCACGAAFMDFLLEVQAA VPGLPSRVKCGSPGQLQGLSIFAQDLRLCLDEALSWDCFALSLLAVALGLGVPMLHHLCG WDLWYCFHLCLAWLPWRGRQSGRDEDALPYDAFVVFDKTQSAVADWVYNELRGQLEECRG RWALRLCLEERDWLPGKTLFENLWASVYGSRKTLFVLAHTDRVSGLLRASFLLAQQRLLE DRKDVVVLVILSPDGRRSRYVRLRQRLCRQSVLLWPHQPSGQRSFWAQLGMALTRDNHHF YNRNFCQGPTAE |
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Drugs and Mode of Action | |||||
Drug(s) | Cadi-05 | Drug Info | Phase 3 | Prostate cancer | [522525] |
MGN-1703 | Drug Info | Phase 3 | Colorectal cancer | [524663] | |
SD-101 | Drug Info | Phase 3 | HCV infection | [525113] | |
BL-7040 | Drug Info | Phase 2 | Inflammatory bowel disease | [523753] | |
CpG-10101 | Drug Info | Phase 2 | HCV infection | [521786] | |
CYT003 | Drug Info | Phase 2 | Asthma | [533260] | |
IMO-2055 | Drug Info | Phase 2 | Renal cell carcinoma; Solid tumours | [550998] | |
JVRS-100 | Drug Info | Phase 2 | Leukemia | [522718] | |
MIS-416 | Drug Info | Phase 2 | Autoimmune diabetes | [549949] | |
Tolamba | Drug Info | Phase 2 | Allergic rhinitis | [522129] | |
Zadaxin/lamivudine | Drug Info | Phase 2 | HBV infection | [549869] | |
AZD1419 | Drug Info | Phase 1 | Asthma | [548372] | |
CPG 52364 | Drug Info | Phase 1 | Systemic lupus erythematosus | [532501] | |
GNKG-168 | Drug Info | Phase 1 | Chronic lymphocytic leukaemia | [524153] | |
IMO-2125 | Drug Info | Phase 1 | HCV infection | [550998] | |
IMO-3100 | Drug Info | Phase 1 | Autoimmune diabetes | [550998] | |
Litenimod | Drug Info | Phase 1 | Glioblastoma multiforme | [551464] | |
MGN-1706 | Drug Info | Phase 1 | Cancer | [525374] | |
N-8295 | Drug Info | Phase 1 | Influenza virus | [549878] | |
SAR-21609 | Drug Info | Phase 1 | Asthma | [530837] | |
IMO-2134 | Drug Info | Preclinical | Asthma; Allergy | [550998] | |
IR-103 | Drug Info | Discontinued in Phase 3 | Human immunodeficiency virus infection | [547777] | |
Agatolimod | Drug Info | Discontinued in Phase 2 | Lung cancer | [547005] | |
IM0-8400 | Drug Info | Discontinued in Phase 1/2 | Diffuse large B-cell lymphoma | [550999] | |
DV-1179 | Drug Info | Discontinued in Phase 1 | Systemic lupus erythematosus | [549321] | |
AVE0675 | Drug Info | Terminated | Asthma | [548655] | |
Agonist | Agatolimod | Drug Info | [536475], [549974] | ||
AVE0675 | Drug Info | [549823] | |||
AZD1419 | Drug Info | [549879] | |||
CpG-10101 | Drug Info | [528995] | |||
CYT003 | Drug Info | [533260] | |||
IMO-2055 | Drug Info | [550998] | |||
IMO-2125 | Drug Info | [550998] | |||
IMO-2134 | Drug Info | [550998] | |||
MGN-1703 | Drug Info | [532775] | |||
MGN-1706 | Drug Info | [543477] | |||
SAR-21609 | Drug Info | [544251] | |||
Activator | BL-7040 | Drug Info | [533251] | ||
Antagonist | CPG 52364 | Drug Info | [551089] | ||
IM0-8400 | Drug Info | [551000] | |||
Modulator | DIMS-9054 | Drug Info | [543477] | ||
DV-1179 | Drug Info | ||||
GNKG-168 | Drug Info | [550450] | |||
IMO-3100 | Drug Info | ||||
Litenimod | Drug Info | [543477] | |||
MIS-416 | Drug Info | ||||
Zadaxin/lamivudine | Drug Info | [527615] | |||
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM) | |||||
TEP | EXP Info | ||||
Pathways | |||||
KEGG Pathway | Toll-like receptor signaling pathway | ||||
Chagas disease (American trypanosomiasis) | |||||
African trypanosomiasis | |||||
Malaria | |||||
Tuberculosis | |||||
Measles | |||||
Herpes simplex infection | |||||
NetPath Pathway | BCR Signaling Pathway | ||||
PANTHER Pathway | Toll receptor signaling pathway | ||||
Reactome | PI3K Cascade | ||||
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 | |||||
Signaling by Type 1 Insulin-like Growth Factor 1 Receptor (IGF1R) | |||||
Regulation of toll-like receptor signaling pathway | |||||
References | |||||
Ref 521786 | ClinicalTrials.gov (NCT00277238) CPG10101 Combination Therapy For The Treatment Of Hepatitis C In Non-Responder (Null And Partial Responder) Hepatitis C Virus (HCV) Genotype 1 Infected Subjects. U.S.National Institutes of Health. | ||||
Ref 522129 | ClinicalTrials.gov (NCT00537355) An Evaluation of the Efficacy and Safety of TOLAMBA for Ragweed-Allergic Rhinitis in an Environmental Exposure Chamber. U.S. National Institutes of Health. | ||||
Ref 522525 | ClinicalTrials.gov (NCT00810849) A Trial of Adjunctive Prednisolone and Mycobacterium w Immunotherapy in Tuberculous Pericarditis. U.S. National Institutes of Health. | ||||
Ref 522718 | ClinicalTrials.gov (NCT00936468) Safety, Tolerability and Immunogenicity of Fluzone With and Without JVRS-100 in Elderly Subjects. U.S. National Institutes of Health. | ||||
Ref 523753 | ClinicalTrials.gov (NCT01506362) Efficacy, Pharmacodynamics, Safety and Tolerability of Oral BL-7040 in Patients With Moderately Active Ulcerative Colitis. U.S. National Institutes of Health. | ||||
Ref 524153 | ClinicalTrials.gov (NCT01743807) Phase I Study of GNKG168 in Acute Lymphoblastic Leukemia and Acute Myelogenous Leukemia. U.S. National Institutes of Health. | ||||
Ref 524663 | ClinicalTrials.gov (NCT02077868) Evaluation of MGN1703 Maintenance Treatment in Patients With mCRC With Tumor Reduction During Induction Treatment. U.S. National Institutes of Health. | ||||
Ref 525113 | ClinicalTrials.gov (NCT02384460) Study of Efficacy and Safety of SD-101 Cream in Patients With Epidermolysis Bullosa. U.S. National Institutes of Health. | ||||
Ref 525374 | Targeting Toll-like receptors: emerging therapeutics? Nat Rev Drug Discov. 2010 Apr;9(4):293-307. doi: 10.1038/nrd3203. | ||||
Ref 530837 | Targeting Toll-like receptors: emerging therapeutics. Nat Rev Drug Discov. 2010 Apr;9(4):293-307. | ||||
Ref 532501 | Treatment of systemic lupus erythematosus: new therapeutic avenues and blind alleys. Nat Rev Rheumatol. 2014 Jan;10(1):23-34. | ||||
Ref 533260 | CYT003, a TLR9 agonist, in persistent allergic asthma - a randomized placebo-controlled Phase 2b study. Allergy. 2015 Sep;70(9):1160-8. | ||||
Ref 547005 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800011959) | ||||
Ref 547777 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800019204) | ||||
Ref 548372 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800025034) | ||||
Ref 548655 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800027402) | ||||
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 549949 | Targeting Innate Receptors with MIS416 Reshapes Th Responses and Suppresses CNS Disease in a Mouse Model of Multiple Sclerosis. PLoS ONE 9(1): e87712. January 31, 2014. | ||||
Ref 527615 | Zadaxin (thymosin alpha1) for the treatment of viral hepatitis. Expert Opin Investig Drugs. 1999 Mar;8(3):281-7. | ||||
Ref 528995 | Safety, pharmacokinetics and immune effects in normal volunteers of CPG 10101 (ACTILON), an investigational synthetic toll-like receptor 9 agonist. Antivir Ther. 2007;12(5):741-51. | ||||
Ref 532775 | Maintenance treatment with the immunomodulator MGN1703, a Toll-like receptor 9 (TLR9) agonist, in patients with metastatic colorectal carcinoma and disease control after chemotherapy: a randomised, double-blind, placebo-controlled trial. J Cancer Res Clin Oncol. 2014 Sep;140(9):1615-24. | ||||
Ref 533251 | Gut feeling: MicroRNA discriminators of the intestinal TLR9-cholinergic links. Int Immunopharmacol. 2015 May 20. pii: S1567-5769(15)00231-3. | ||||
Ref 533260 | CYT003, a TLR9 agonist, in persistent allergic asthma - a randomized placebo-controlled Phase 2b study. Allergy. 2015 Sep;70(9):1160-8. | ||||
Ref 536475 | CPG-7909 (PF-3512676, ProMune): toll-like receptor-9 agonist in cancer therapy. Expert Opin Biol Ther. 2007 Aug;7(8):1257-66. | ||||
Ref 543477 | (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: 1759). | ||||
Ref 544078 | Cationic lipid/DNA complexes (JVRS-100) combined with influenza vaccine (Fluzone?) increases antibody response, cellular immunity, and antigenically drifted protection. Vaccine. 2009 June 12; 27(29):3811-3820. | ||||
Ref 544095 | Phase II study of a TLR-9 agonist (1018 ISS) with rituximab in patients with relapsed or refractory follicular lymphoma. Br J Haematol. 2009 August; 146(3): 282-291. | ||||
Ref 544251 | Trial Watch: Experimental Toll-like receptor agonists for cancer therapy. Oncoimmunology. 2012 August 1; 1(5): 699-716. | ||||
Ref 544459 | Novel drugs targeting Toll-like receptors for antiviral therapy. Future Virol. 2014 September; 9(9): 811-829. | ||||
Ref 547845 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800019871) | ||||
Ref 549949 | Targeting Innate Receptors with MIS416 Reshapes Th Responses and Suppresses CNS Disease in a Mouse Model of Multiple Sclerosis. PLoS ONE 9(1): e87712. January 31, 2014. |
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