Protein / target

Toll-like receptor 7

TLR7Q9NYK1Homo sapiensSwiss-Prot
Clinically validated
Therapeutic maturity
3
Approved medicines
30
Clinical trials
Small-molecule tractable
Druggability
Approved Drug

Protein at a glance

Biological role

Pattern recognition receptor activity

Primary system

Immune system

Strongest disease association

systemic lupus erythematosus 17

Genetic evidence · score 0.76

Therapeutic maturity

Clinically validated target

3 approved medicines against this target

Druggability

Small molecule

Open Targets tractability · Approved Drug

Clinical development

3 approved · 9 in clinical development

30 linked trials

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

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.

Drugs targeting this protein

1

Whether each drug engages this protein directly or through a complex, and how many other targets are recorded for it. Direct binders with few recorded targets are listed first.

imiquimod
Narrow target profileApprovedAgonist

Toll-like receptor 7 agonist

Appears in clinical studies involving actinic keratosis, keratosis, basal cell carcinoma, anogenital human papillomavirus infection

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

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

Translational evidence

Open Targets 26

Why this target matters therapeutically — disease associations, drugs in development, tractability and safety, from Open Targets.

Strongest genetic associations

Human genetic evidence — the most direct causal link between this target and a disease.

systemic lupus erythematosus 170.76

Genetic · overall 0.58

systemic lupus erythematosus0.75

Genetic · overall 0.72

immunodeficiency 74, COVID-19-related, X-linked0.72

Genetic · overall 0.61

Highest-confidence therapeutic associations

Diseases where a drug acting on this target has already reached clinical development.

rheumatoid arthritis0.98

Clinical · overall 0.62

actinic keratosis0.95

Clinical · overall 0.58

basal cell carcinoma0.93

Clinical · overall 0.57

malaria0.91

Clinical · overall 0.57

keratosis0.89

Clinical · overall 0.54

Highest overall evidence

Remaining associations by Open Targets' aggregated evidence score.

anogenital human papillomavirus infection0.52

Clinical

cutaneous lupus erythematosus0.45

Clinical

Show all associations
systemic lupus erythematosus0.72
rheumatoid arthritis0.62
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

Open Targets ranks 1,226 associations for this target and we store the top 10 by aggregated score. The long tail is largely literature co-mention and RNA-expression evidence, not evidence that this target drives those diseases.

Known drugs · 12 total

CPG-52852Phase 2

melanoma · cutaneous melanoma · hematopoietic and lymphoid cell neoplasm

HYDROXYCHLOROQUINEApproval

malaria · graft versus host disease · temporal arteritis

BAZLITORANPhase 2

rheumatoid arthritis · psoriasis · psoriasis

ENPATORANPhase 3

lupus erythematosus · systemic lupus erythematosus · cutaneous lupus erythematosus

VESATOLIMODPhase 2

hepatitis B virus infection · hepatitis B virus infection · chronic hepatitis B virus infection

HYDROXYCHLOROQUINE SULFATEApproval

rheumatoid arthritis · cutaneous lupus erythematosus · malaria

RESIQUIMODPhase 2

actinic keratosis · primary cutaneous T-cell non-Hodgkin lymphoma · common wart

AFIMETORANPhase 2

systemic lupus erythematosus · cutaneous lupus erythematosus

GSK-2245035Phase 2

asthma · allergic rhinitis · allergic respiratory disease

TELRATOLIMODPhase 1

primary cutaneous T-cell non-Hodgkin lymphoma · neoplasm

Tractability

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

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.

Show remaining trials (24)

WITHDRAWN · via imiquimod · NCT01663558

ClinicalTrials.gov via the drug-target graph.

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.

Forefront confidence

Synthesis

Our own weighting of the evidence behind each disease association. Human genetics and clinical evidence count for most; literature co-mention counts for little, because two entities sharing an abstract is not evidence that one drives the other.

systemic lupus erythematosusWell 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

rheumatoid arthritisWell 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 underlying per-type scores are shown above so the calculation can be checked.

What's happening now

8

Recent activity around this target, drawn from one canonical event stream. Every item is reached through a drug that targets this protein, so each event is news about that drug rather than about the protein directly.

  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.