Target Information

Target General Infomation
Target ID
T48703
Former ID
TTDC00056
Target Name
Toll-like receptor 8
Gene Name
TLR8
Synonyms
CD288 antigen; TLR8
Target Type
Clinical Trial
Disease Autoimmune diabetes [ICD10: E08-E13]
Allergic rhinitis [ICD9: 472.0, 477, 995.3; ICD10: J00, J30, J31.0, T78.4]
Allergy [ICD9: 995.3; ICD10: T78.4]
Diffuse large B-cell lymphoma [ICD9: 200; ICD10: C83.3]
Herpes simplex virus infection [ICD9: 54; ICD10: B00]
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. Acts via MYD88 and TRAF6, leading to NF-kappa-B activation, cytokine secretion and the inflammatory response.
BioChemical Class
Toll-like receptor family
Target Validation
T48703
UniProt ID
Q9NR97
Sequence
MENMFLQSSMLTCIFLLISGSCELCAEENFSRSYPCDEKKQNDSVIAECSNRRLQEVPQT
VGKYVTELDLSDNFITHITNESFQGLQNLTKINLNHNPNVQHQNGNPGIQSNGLNITDGA
FLNLKNLRELLLEDNQLPQIPSGLPESLTELSLIQNNIYNITKEGISRLINLKNLYLAWN
CYFNKVCEKTNIEDGVFETLTNLELLSLSFNSLSHVPPKLPSSLRKLFLSNTQIKYISEE
DFKGLINLTLLDLSGNCPRCFNAPFPCVPCDGGASINIDRFAFQNLTQLRYLNLSSTSLR
KINAAWFKNMPHLKVLDLEFNYLVGEIASGAFLTMLPRLEILDLSFNYIKGSYPQHINIS
RNFSKLLSLRALHLRGYVFQELREDDFQPLMQLPNLSTINLGINFIKQIDFKLFQNFSNL
EIIYLSENRISPLVKDTRQSYANSSSFQRHIRKRRSTDFEFDPHSNFYHFTRPLIKPQCA
AYGKALDLSLNSIFFIGPNQFENLPDIACLNLSANSNAQVLSGTEFSAIPHVKYLDLTNN
RLDFDNASALTELSDLEVLDLSYNSHYFRIAGVTHHLEFIQNFTNLKVLNLSHNNIYTLT
DKYNLESKSLVELVFSGNRLDILWNDDDNRYISIFKGLKNLTRLDLSLNRLKHIPNEAFL
NLPASLTELHINDNMLKFFNWTLLQQFPRLELLDLRGNKLLFLTDSLSDFTSSLRTLLLS
HNRISHLPSGFLSEVSSLKHLDLSSNLLKTINKSALETKTTTKLSMLELHGNPFECTCDI
GDFRRWMDEHLNVKIPRLVDVICASPGDQRGKSIVSLELTTCVSDVTAVILFFFTFFITT
MVMLAALAHHLFYWDVWFIYNVCLAKVKGYRSLSTSQTFYDAYISYDTKDASVTDWVINE
LRYHLEESRDKNVLLCLEERDWDPGLAIIDNLMQSINQSKKTVFVLTKKYAKSWNFKTAF
YLALQRLMDENMDVIIFILLEPVLQHSQYLRLRQRICKSSILQWPDNPKAEGLFWQTLRN
VVLTENDSRYNNMYVDSIKQY
Drugs and Mode of Action
Drug(s) Resiquimod Drug Info Phase 1/2 Herpes simplex virus infection [468141], [546884]
CPG 52364 Drug Info Phase 1 Systemic lupus erythematosus [532501]
VTX-1463 Drug Info Phase 1 Allergic rhinitis [548896]
VTX-2337 Drug Info Discontinued in Phase 2 Allergy [524026]
IM0-8400 Drug Info Discontinued in Phase 1/2 Diffuse large B-cell lymphoma [550999]
Antagonist CPG 52364 Drug Info [551089]
IM0-8400 Drug Info [551000]
VTX-763 Drug Info [543476]
Modulator Resiquimod Drug Info
VTX-2337 Drug Info [550276]
VTX-744 Drug Info [543476]
Agonist VTX-1463 Drug Info [531464]
Pathways
KEGG Pathway Toll-like receptor signaling pathway
NetPath Pathway Leptin Signaling 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 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 524026ClinicalTrials.gov (NCT01666444) VTX-2337 and Pegylated Liposomal Doxorubicin (PLD) in Patients With Recurrent or Persistent Epithelial Ovarian, Fallopian Tube or Primary Peritoneal Cancer. 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 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 548896Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800030038)
Ref 550999Clinical pipeline report, company report or official report of Idera Pharmaceuticals.
Ref 531464VTX-1463, a novel TLR8 agonist for the treatment of allergic rhinitis. Expert Opin Investig Drugs. 2011 Jul;20(7):981-6.
Ref 543476(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: 1758).
Ref 550276Clinical pipeline report, company report or official report of Array BioPharma (Drug: Motolimod / VTX2337).
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.

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