Target Information

General Information of This Target
Target ID
PATR0ZYOQI
Target Name
Toll-like receptor 7 (TLR7)
Gene Name
TLR7
Gene ID
51284
Sequence
MVFPMWTLKRQILILFNIILISKLLGARWFPKTLPCDVTLDVPKNHVIVDCTDKHLTEIP
GGIPTNTTNLTLTINHIPDISPASFHRLDHLVEIDFRCNCVPIPLGSKNNMCIKRLQIKP
RSFSGLTYLKSLYLDGNQLLEIPQGLPPSLQLLSLEANNIFSIRKENLTELANIEILYLG
QNCYYRNPCYVSYSIEKDAFLNLTKLKVLSLKDNNVTAVPTVLPSTLTELYLYNNMIAKI
QEDDFNNLNQLQILDLSGNCPRCYNAPFPCAPCKNNSPLQIPVNAFDALTELKVLRLHSN
SLQHVPPRWFKNINKLQELDLSQNFLAKEIGDAKFLHFLPSLIQLDLSFNFELQVYRASM
NLSQAFSSLKSLKILRIRGYVFKELKSFNLSPLHNLQNLEVLDLGTNFIKIANLSMFKQF
KRLKVIDLSVNKISPSGDSSEVGFCSNARTSVESYEPQVLEQLHYFRYDKYARSCRFKNK
EASFMSVNESCYKYGQTLDLSKNSIFFVKSSDFQHLSFLKCLNLSGNLISQTLNGSEFQP
LAELRYLDFSNNRLDLLHSTAFEELHKLEVLDISSNSHYFQSEGITHMLNFTKNLKVLQK
LMMNDNDISSSTSRTMESESLRTLEFRGNHLDVLWREGDNRYLQLFKNLLKLEELDISKN
SLSFLPSGVFDGMPPNLKNLSLAKNGLKSFSWKKLQCLKNLETLDLSHNQLTTVPERLSN
CSRSLKNLILKNNQIRSLTKYFLQDAFQLRYLDLSSNKIQMIQKTSFPENVLNNLKMLLL
HHNRFLCTCDAVWFVWWVNHTEVTIPYLATDVTCVGPGAHKGQSVISLDLYTCELDLTNL
ILFSLSISVSLFLMVMMTASHLYFWDVWYIYHFCKAKIKGYQRLISPDCCYDAFIVYDTK
DPAVTEWVLAELVAKLEDPREKHFNLCLEERDWLPGQPVLENLSQSIQLSKKTVFVMTDK
YAKTENFKIAFYLSHQRLMDEKVDVIILIFLEKPFQKSKFLQLRKRLCGSSVLEWPTNPQ
AHPYFWQCLKNALATDNHVAYSQVFKETV

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Family
the Toll-like receptor family
Function
Endosomal receptor that plays a key role in innate and adaptive immunity. Controls host immune response against pathogens through recognition of uridine- containing single strand RNAs (ssRNAs) of viral origin or guanosine analogs. Upon binding to agonists, undergoes dimerization that brings TIR domains from the two molecules into direct contact, leading to the recruitment of TIR-containing downstream adapter MYD88 through homotypic interaction. In turn, the Myddosome signaling complex is formed involving IRAK4, IRAK1, TRAF6, TRAF3 leading to activation of downstream transcription factors NF-kappa-B and IRF7 to induce pro-inflammatory cytokines and interferons, respectively.

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Uniprot Entry
TLR7_HUMAN
HGNC ID
HGNC:15631
KEGG ID
hsa:51284
Full List of The ADC Related to This Target
Phase 1 (discontinued)
Click To Hide/Show 1 ADC Related to This Stage
ADC Info ADC Name Antibody Antigen Payload Linker Ref
ADC Info
NJH395
MIW338
HER2
TLR7 agonist
A non-cleavable linker
Investigative
Click To Hide/Show 3 ADC Related to This Stage
ADC Info ADC Name Antibody Antigen Payload Linker Ref
ADC Info
Anti-HER2_vc-1
Trastuzumab
Receptor tyrosine-protein kinase erbB-2 (ERBB2)
TLR7 agonist-1
Mc-Val-Cit-PABC
 [1]
ADC Info
Anti-HER2_vc-7
Trastuzumab
Receptor tyrosine-protein kinase erbB-2 (ERBB2)
TLR7 agonist-7
Mc-Val-Cit-PABC
 [1]
ADC Info
Anti-HER2_vc-2
Trastuzumab
Receptor tyrosine-protein kinase erbB-2 (ERBB2)
TLR7 agonist-2
Mc-Val-Cit-PABC
 [1]
Phase 1 (discontinued)
Click To Hide/Show 1 ADC Related to This Stage
ADC Info ADC Name Antibody Antigen Payload Linker Ref
ADC Info
PF-08046037
Anti-PD-L1 antibody
PD-L1
Imidazoquinoline-based TLR7 agonist
Mannosidase-cleavable maleimidopropionyl-mannose linker
 [2]
References
Ref 1 Design and Characterization of Immune-Stimulating Imidazo[4,5-c]quinoline Antibody-Drug Conjugates. Mol Pharm. 2022 Sep 5;19(9):3228-3241.
Ref 2 PF-08046037, a PD-L1 targeted TLR7 agonist ISAC, drives innate immune activation and anti-tumor efficacy in preclinical in vitro and in vivo models