Target intelligence / Profile preview

Retinoic acid receptor RXR (RXR)

Target
RXR
Molecular classification
Nuclear receptor, Transcription factor, Type II nuclear receptor
01

Overview

The Retinoid X receptor (RXR) is a type of nuclear receptor that functions as a transcription factor. It exists as three subtypes (RXR-alpha, RXR-beta, RXR-gamma) and has a modular structure with NTD, DBD, and LBD domains. RXR primarily functions by forming heterodimers with numerous other nuclear receptors (like RAR, VDR, PPAR, etc.) and binding to specific DNA sequences (often DR-1) to regulate gene transcription. Ligand binding to RXR leads to corepressor dissociation and coactivator recruitment, activating transcription. RXRs play crucial roles in development (e.g., axial and limb patterning) and metabolism (e.g., regulating the thyroid pathway). They are considered therapeutic targets; Bexarotene is a clinically used RXR-specific activator. RXRs are described as permissive co-receptors, potentially making them interesting therapeutic targets, though treatment with RXR activators like bexarotene can have side effects such as severe hypothyroidism.

Other names
RXR-alphaRXR-betaRXR-gammaRXRARXRBRXRG
02

Mechanism of action

RXR functions as a nuclear receptor and transcription factor. It is activated by specific ligands (agonists). Upon ligand binding, RXR, primarily as a heterodimer with other nuclear receptors, binds to specific DNA sequences (response elements) in gene promoters. This leads to the dissociation of corepressor proteins, recruitment of coactivator proteins, and promotion of transcription of downstream target genes. Therapeutic activators like Bexarotene bind to and activate RXR.

03

Biological functions

DevelopmentMetabolismTranscriptional regulationHeterodimerization with nuclear receptorsDNA bindingTransmitting retinoid signalsAxial and limb patterningOrgan formationRegulating Thyroid Receptor pathway
04

Safety considerations

Severe hypothyroidism (associated with bexarotene treatment)
05

Interacting drugs

Bexarotene

2 more in the full profile.

Beyond the preview

Go deeper on Retinoic acid receptor RXR (RXR).

Explore the evidence, development activity, and competitive landscape with Gosset’s full data platform.

Drug pipeline

Full profile access

Explore the programs pursuing this target and their development progress.

  • Drug candidates
  • Developers
  • Development stage

Clinical trials

Full profile access

Follow the clinical studies evaluating therapies directed at this target.

  • Trial design
  • Status
  • Readouts

Competitive landscape

Full profile access

Compare approaches across drug candidates, modalities, and indications.

  • Programs
  • Modalities
  • Indications

Literature & evidence

Full profile access

Investigate the research and source evidence behind target biology and development.

  • Publications
  • Sources
  • Analysis

Patents

Full profile access

Explore patent activity around therapies and technologies addressing this target.

  • Patents
  • Assignees
  • Technologies

Research & analysis

Full profile access

Connect target biology, drug development, and emerging evidence in your research.

  • Biology
  • Development news
  • Analysis

Bring the full picture into focus.

See how Gosset can support your research on Retinoic acid receptor RXR (RXR).

Explore the full profile

Gosset Free

Get started with Gosset.

Enter your work email and we’ll be in touch with next steps.

Work email preferred.

Book a call