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Protein / target

Retinoic acid receptor RXR-gamma

Encoded byRXRGP48443Homo sapiensSwiss-Prot
Clinically validated
Therapeutic maturity
4
Approved medicines
Open Targets target-level
View by indication →
30
Clinical trials
Small-molecule tractable
Druggability
Approved Drug

Protein at a glance

Biological role

Sequence-specific double-stranded DNA binding

Strongest disease association

Neurodegenerative Diseases

Via encoding gene RXRG · Pathway evidence · score 0.52

Therapeutic position

Established drug target

Small molecules

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

Receptor for retinoic acid.

View complete UniProt function annotation

Receptor for retinoic acid. Retinoic acid receptors bind as heterodimers to their target response elements in response to their ligands, all-trans or 9-cis retinoic acid, and regulate gene expression in various biological processes. The RAR/RXR heterodimers bind to the retinoic acid response elements (RARE) composed of tandem 5'-AGGTCA-3' sites known as DR1-DR5. The high affinity ligand for RXRs is 9-cis retinoic acid (By similarity)

Subcellular location

NucleusCytoplasm
Domains and Gene Ontology detail (17)

Domains & features

NR LBD

Gene Ontology

  • Cchromatin
  • Ccytoplasm
  • Cnucleoplasm
  • CRNA polymerase II transcription regulator complex
  • FDNA-binding transcription factor activity, RNA polymerase II-specific
  • Fmolecular condensate scaffold activity
  • Fnuclear receptor activity
  • Fnuclear steroid receptor activity
  • Fretinoic acid-responsive element binding
  • Fsequence-specific double-stranded DNA binding
  • Fzinc ion binding
  • Pcell differentiation

463 aa · 51 kDa

Biological roles

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

Nuclear receptor signallingGOTranscriptional regulationUniProt · GO
View supporting evidence

Nuclear receptor signalling

  • ·nuclear receptor activity

Transcriptional regulation

  • ·Receptor for retinoic acid. Retinoic acid receptors bind as heterodimers to their target…
  • ·RNA polymerase II transcription regulator complex
  • ·DNA-binding transcription factor activity, RNA polymerase II-specific
  • ·DNA-templated transcription

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

Approved medicines with mapped indications

1 medicine · 3 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.

Lymphoma, T-Cell1 medicine
Lymphoma, T-Cell, Cutaneous1 medicine
Broader indication categories (1)
Neoplasms1 medicine

Broad umbrella indications (e.g. “Neoplasms”). Shown here because every medicine also appears under a more specific disease above — kept for completeness, de-emphasised for clarity.

4 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.

bexarotene
ApprovedAgonist

Retinoid X receptor agonist

Indicated for Lymphoma, T-Cell, Lymphoma, T-Cell, Cutaneous, Neoplasms

Acts on a complex — shared with RXRB, RXRA · 1 of 3 recorded protein targets — narrow recorded profile

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 RXRG

Gene-level evidence surfaced through the gene RXRG that 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.

Neoplasms
0.62Moderately supported

Clinical evidence dominant · Open Targets 0.49

Sarcoma, Kaposi
0.59Moderately supported

Clinical evidence dominant · Open Targets 0.48

Alzheimer's Disease
0.37Limited support

Pathway evidence dominant · Open Targets 0.42

Neurodegenerative Diseases
0.34Preliminary

Pathway evidence dominant · Open Targets 0.52 · no direct causal or clinical evidence

Parkinson's Disease
0.30Limited support

Pathway evidence dominant · Open Targets 0.41

View evidence synthesis (5)
NeoplasmsModerately supported
0.62
agreement 0.470.78
Clinical82%Literature18%

Open Targets aggregate 0.49 · 2 independent evidence families

Sarcoma, KaposiModerately supported
0.59
agreement 0.430.74
Clinical100%Literature0%

Open Targets aggregate 0.48 · 2 independent evidence families

Alzheimer's DiseaseLimited support
0.37
agreement 0.240.49
Pathway65%Clinical29%Literature6%

Open Targets aggregate 0.42 · 3 independent evidence families

Neurodegenerative DiseasesPreliminary
0.34
agreement 0.110.57
Pathway100%

Open Targets aggregate 0.52 · 1 independent evidence family · no direct causal or clinical evidence

Parkinson's DiseaseLimited support
0.30
agreement 0.170.42
Pathway85%Clinical15%Literature1%

Open Targets aggregate 0.41 · 3 independent evidence families

This ranking differs from Open Targets' own: re-weighting moves genetically-evidenced diseases above more heavily co-mentioned ones. 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
Neurodegenerative Diseases0.52
Neoplasms0.49
Sarcoma, Kaposi0.48
Alzheimer's Disease0.42
Parkinson's Disease0.41

Drug development

6 compounds recorded · 4 approved · 2 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 (6)
MOFAROTENEPhase 1
ALITRETINOINApproval
IRX-4204Phase 2
BEXAROTENEApproval
ACITRETINApproval
ETRETINATEApproval

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.

Protein degradersEmerging

Feasibility evidence (database ubiquitination and small molecule binder) — no clinical-stage drug of this modality recorded.

View underlying tractability evidence (6)
SM · Approved DrugSM · High-Quality LigandSM · High-Quality PocketSM · Druggable FamilyPR · Database UbiquitinationPR · Small Molecule Binder

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)

TERMINATED · via bexarotene · NCT00615784

UNKNOWN · via bexarotene · NCT00845351

COMPLETED · via bexarotene · NCT00316030

ClinicalTrials.gov via the drug-target graph.

What's happening now

1

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. Regulatory approval2001-03-29

    Approval: Targretin (EMA)

    ema · regulatory · ema · via bexarotene

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.

Related family literature

1

Papers about “Retinoid X Receptors” — a broader family this protein belongs to. Shown as context; not counted as papers specifically about this protein.

mPPAR gamma 2: tissue-specific regulator of an adipocyte enhancer.

Tontonoz P · Genes & development · 1994

via Retinoid X Receptors

Europe PMC literature, reached through curated HGNC family membership. Membership is a taxonomic relationship — it does not imply this protein participates in every mechanism these papers discuss.