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Protein / target

Toll-like receptor 7

Encoded byTLR7Q9NYK1Homo sapiensSwiss-Prot
Clinically validated
Therapeutic maturity
3
Approved medicines
Open Targets target-level
View by indication →
30
Clinical trials
Small-molecule tractable
Druggability
Approved Drug

Protein at a glance

Biological role

Pattern recognition receptor

Strongest disease association

Systemic lupus erythematosus 17

Via encoding gene TLR7 · Genetic evidence · score 0.76

Therapeutic position

Established drug target

Small molecules

Research activity

Emerging research

4 papers · latest 2021

Derived from structured UniProt, Open Targets and literature data on this page.

Protein profile

UniProt 2026_02

Canonical identity and biological annotation from UniProt.

Function overview

Endosomal receptor that plays a key role in innate and adaptive immunity.

View complete UniProt function annotation

Endosomal receptor that plays a key role in innate and adaptive immunity (PubMed:14976261, PubMed:32433612). Controls host immune response against pathogens through recognition of uridine-containing single strand RNAs (ssRNAs) of viral origin or guanosine analogs (PubMed:12738885, PubMed:27742543, PubMed:31608988, PubMed:32706371, PubMed:35477763). 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 (PubMed:27742543). 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 (PubMed:27742543, PubMed:32706371). In plasmacytoid dendritic cells, RNASET2 endonuclease cooperates with PLD3 or PLD4 5'->3' exonucleases to process RNA and release 2',3'-cyclic guanosine monophosphate (2',3'-cGMP) and cytidine-rich RNA fragments that occupy TLR7 ligand-binding pockets and trigger a signaling-competent state

Subcellular location

Endoplasmic reticulum membraneEndosomeLysosomeCytoplasmic vesicle, phagosome
Domains and Gene Ontology detail (36)

Domains & features

TIR

Gene Ontology

  • Ccytoplasm
  • Cearly phagosome
  • Cendolysosome membrane
  • Cendoplasmic reticulum
  • Cendoplasmic reticulum membrane
  • Cendosome
  • Cendosome membrane
  • CGolgi membrane
  • Clysosome
  • Cplasma membrane
  • Creceptor complex
  • Fdouble-stranded RNA binding

1049 aa · 121 kDa

Biological roles

Reactome v97

What this protein does, drawn together from its UniProt function, Gene Ontology terms and Reactome pathways.

Immune signallingUniProt · GO · ReactomeTranscriptional regulationUniProt · GO
View supporting evidence

Immune signalling

  • ·Endosomal receptor that plays a key role in innate and adaptive immunity (PubMed:1497626…
  • ·inflammatory response
  • ·innate immune response
  • ·positive regulation of inflammatory response

Transcriptional regulation

  • ·Endosomal receptor that plays a key role in innate and adaptive immunity (PubMed:1497626…
  • ·positive regulation of transcription by RNA polymerase II
View underlying pathways (11)

Concepts derived from UniProt GO Reactome — each badge above shows which sources supported that role.

Interaction neighbourhood

STRING v12.0

Proteins with the strongest functional or physical association. Node size and line weight reflect STRING confidence; hover or select a partner to inspect one association.

MYD88TLR8UNC93B1TLR9IRAK1IRAK4TLR3IRF7TLR4TRAF6TLR7

10 strongest partners — larger node and heavier line mean higher confidence

Functional and physical associations from STRING v12.0. Only associations with this protein are drawn — partner-to-partner links are not part of this evidence.

Approved medicines with mapped indications

1 medicine · 2 areas

Approved therapies targeting this protein, grouped by what they are approved to treat — the disease-first view of the medicines below. Relationships come from the canonical approved-indication graph (ChEMBL phase-4), the same source as the drug cards.

Keratosis, Actinic1 medicine
Virus Diseases1 medicine

3 medicines meet Open Targets' target-level approved-medicine definition; the 1 shown here are those on this page with a canonical approved disease indication in the graph. Approved indications from ChEMBL (phase-4), via the canonical drug→disease graph.

Drugs targeting this protein

1

How approved and investigational drugs engage this protein — mechanism and action type, direct vs complex targeting, and how broadly each acts across other targets. A drug-first view (the section above groups the approved ones disease-first); direct binders with few recorded targets are listed first.

imiquimod
Narrow target profileApprovedAgonist

Toll-like receptor 7 agonist

Indicated for Keratosis, Actinic, Virus Diseases

Direct interaction with this protein · Only this protein recorded as a target

ChEMBL mechanism, action type, target identity and approved indications. Open Targets clinical status.

Translational evidence

Open Targets 26

Why this target matters therapeutically, strongest evidence first. Disease associations are gene-level (via the gene that encodes this protein) and open into the full confidence synthesis; the development universe, tractability and safety annotations are target-level, from Open Targets.

Strongest disease associations · via encoding gene TLR7

Gene-level evidence surfaced through the gene TLR7that encodes this protein — not a direct protein–disease relationship. Ranked by Forefront's causal-directness weighting, so genetically- and clinically-evidenced diseases lead over ones that merely share the literature.

Lupus Erythematosus, Systemic
0.93Well supported

Genetic evidence dominant · Open Targets 0.72

immunodeficiency 74, COVID-19-related, X-linked
0.81Well supported

Genetic evidence dominant · Open Targets 0.61

Systemic lupus erythematosus 17
0.79Well supported

Genetic evidence dominant · Open Targets 0.58

Arthritis, Rheumatoid
0.77Well supported

Clinical evidence dominant · Open Targets 0.62

Actinic keratosis
0.72Moderately supported

Clinical evidence dominant · Open Targets 0.58

View evidence synthesis (5)
Lupus Erythematosus, SystemicWell supported
0.93
agreement 0.831.00
Genetic45%Clinical36%Animal model10%Literature9%Genetic literaturedup

Open Targets aggregate 0.72 · 4 independent evidence families · 1 not counted as duplicate

immunodeficiency 74, COVID-19-related, X-linkedWell supported
0.81
agreement 0.690.93
Genetic69%Animal model31%Genetic literaturedup

Open Targets aggregate 0.61 · 2 independent evidence families · 1 not counted as duplicate

Systemic lupus erythematosus 17Well supported
0.79
agreement 0.670.91
Genetic86%Animal model14%Genetic literaturedup

Open Targets aggregate 0.58 · 2 independent evidence families · 1 not counted as duplicate

Arthritis, RheumatoidWell supported
0.77
agreement 0.640.91
Clinical84%Literature15%RNA expression1%

Open Targets aggregate 0.62 · 3 independent evidence families

Actinic keratosisModerately supported
0.72
agreement 0.560.87
Clinical98%Literature2%

Open Targets aggregate 0.58 · 2 independent evidence families

The evidence agreement range shows how closely the independent evidence families agree — it is not a statistical confidence interval, and nothing here is fitted to outcome data. Derived from Open Targets evidence types under Forefront weighting; the per-type scores above show the calculation.

Show all associations
Lupus Erythematosus, Systemic0.72
Arthritis, Rheumatoid0.62
immunodeficiency 74, COVID-19-related, X-linked0.61
Actinic keratosis0.58
Systemic lupus erythematosus 170.58
Basal cell carcinoma0.57
Malaria0.57
Keratosis0.54
Anogenital human papillomavirus infection0.52
Cutaneous lupus erythematosus0.45

Drug development

12 compounds recorded · 3 approved · 9 in clinical development

Open Targets' development universe — every compound recorded against the target at any stage, not all approved medicines. Distinct from the 1 drug that targets this protein in Forefront's canonical graph (1 with a mapped approved indication, shown above): these count different sets and are not a subset relation.

View all recorded compounds (10)
CPG-52852Phase 2
HYDROXYCHLOROQUINEApproval
BAZLITORANPhase 2
ENPATORANPhase 3
VESATOLIMODPhase 2
HYDROXYCHLOROQUINE SULFATEApproval
RESIQUIMODPhase 2
AFIMETORANPhase 2
GSK-2245035Phase 2
TELRATOLIMODPhase 1

Open Targets known-drugs universe. Drug name and highest clinical stage only — the disease relationship is NOT read from this slice (it carries trial-context noise); approved indications come from the canonical graph above.

Tractability

Small moleculesStrong

Approved Drug and High-Quality Ligand support this modality.

AntibodiesEmerging

Feasibility evidence (go cc high conf and uniprot sigp or tmhmm) — no clinical-stage drug of this modality recorded.

Protein degradersEmerging

Feasibility evidence (database ubiquitination and half-life data) — no clinical-stage drug of this modality recorded.

Other modalitiesStrong

Advanced Clinical support this modality.

View underlying tractability evidence (9)
SM · Approved DrugSM · High-Quality LigandSM · Druggable FamilyAB · GO CC high confAB · UniProt SigP or TMHMMPR · Database UbiquitinationPR · Half-life DataPR · Small Molecule BinderOC · Advanced Clinical

Raw Open Targets tractability assessment buckets, by modality.

Clinical trials

30

Trials of drugs that target this protein — reached indirectly through those drugs, so a trial listed here studies the drug, not the protein. Ranked by active status, then clinical phase and recency, and spread across the targeting drugs.

View all trials (26)

WITHDRAWN · via imiquimod · NCT01663558

COMPLETED · via imiquimod · NCT01161888

COMPLETED · via imiquimod · NCT02135419

ClinicalTrials.gov via the drug-target graph.

What's happening now

8

Recent therapeutic activity around this target — regulatory actions, clinical trials and safety signals for a drug that targets this protein, plus publications where such a drug is a genuine subject. Every item is reached indirectly through the drug, not the protein itself; incidental mentions (a paper that merely measures a drug) and press items are excluded.

  1. Label change2026-06-24

    Label change: IMIQUIMOD (ANDA091308)

    fda · regulatory · fda · via imiquimod

  2. Regulatory approval2012-08-23

    Approval: Zyclara (EMA)

    ema · regulatory · ema · via imiquimod

  3. New publication2012-07-05
    Topical TLR7 agonist imiquimod can induce immune-mediated rejection of skin metastases in patients with breast cancer.

    Clinical cancer research : an official journal of the American Association for Cancer Research · 2012 · 176 citations · Europe PMC · via imiquimod

  4. Regulatory approval2012-04-06

    Approval: IMIQUIMOD (ANDA091308)

    fda · regulatory · fda · via imiquimod

  5. New publication2012-01-14
    Enhanced port-wine stain lightening achieved with combined treatment of selective photothermolysis and imiquimod.

    Journal of the American Academy of Dermatology · 2012 · 46 citations · Europe PMC · via imiquimod

  6. New publication2009-05-01
    Imiquimod-induced psoriasis-like skin inflammation in mice is mediated via the IL-23/IL-17 axis.

    Journal of immunology (Baltimore, Md. : 1950) · 2009 · 1,628 citations · Europe PMC · via imiquimod

  7. New publication2008-07-01
    Immunization of malignant melanoma patients with full-length NY-ESO-1 protein using TLR7 agonist imiquimod as vaccine adjuvant.

    Journal of immunology (Baltimore, Md. : 1950) · 2008 · 182 citations · Europe PMC · via imiquimod

  8. Regulatory approval1998-09-18

    Approval: Aldara (EMA)

    ema · regulatory · ema · via imiquimod

Objective event titles are shown unmodified; the event kind and significance line are derived from structured fields. Forefront AttentionEvent stream aggregating Europe PMC Regulatory filings ClinicalTrials.gov.

Research activity

4 papers · to 2021

Papers linked directly to this protein. This is the protein's own literature — descriptor-derived papers are kept separate below.

Most cited

Recent

Europe PMC papers linked directly to this protein.