Target intelligence / Profile preview

Retinoic acid receptor alpha and Retinoic acid receptor beta (RAR-α (for alpha), RAR-β (for beta))

Target
RAR-α (for alpha), RAR-β (for beta)
Molecular classification
Nuclear receptor, Ligand-activated transcription factor, Transcription factor, Receptor
01

Overview

Retinoic acid receptor alpha and retinoic acid receptor beta are nuclear hormone receptors that function as ligand-activated transcription factors and mediate the effects of retinoic acid, a vitamin A derivative[1][5][9]. Both are modular proteins composed of domains for DNA binding and ligand (retinoid) binding, and they regulate gene expression by binding to promoter response elements (RAREs) as heterodimers with retinoid X receptors (RXR)[1][5][4]. The RAR-α and RAR-β proteins have critical roles in vertebrate development, cell differentiation, and homeostasis, as well as in certain malignancies and developmental diseases[5][9]. They are considered significant therapeutic targets for retinoid-based drugs, particularly in oncology and dermatology[1][5]. Selectivity among RAR subtypes is relevant for drug design due to differences in tissue distribution and biological function among the alpha, beta, and gamma isoforms[3][9].

Other names
Nuclear receptor subfamily 1 group B member 1 (NR1B1) for RAR-αNuclear receptor subfamily 1 group B member 2 (NR1B2) for RAR-βRARA for retinoic acid receptor alphaRARB for retinoic acid receptor betaRetinoic acid receptor alpha1, alpha2 (isoforms)RAR alpha, RAR beta
02

Mechanism of action

Modulation of gene expression by binding to retinoic acid response elements (RARE) on DNA, altering transcription of downstream genes Heterodimerization with retinoid X receptors (RXR) to mediate gene regulation Recruitment or displacement of corepressors/coactivators to influence chromatin structure and transcription

03

Biological functions

Regulation of gene transcription in response to retinoic acidCell growth and differentiationEmbryonic development and organogenesisCell cycleApoptosisCellular morphogenesis
04

Disease associations

Cancer (notably acute promyelocytic leukemia for RAR-α)Neurodegenerative diseaseDevelopmental disordersOther retinoid-related disease states
05

Safety considerations

Teratogenicity of retinoid drugs (birth defects)Retinoic acid syndrome (differentiation syndrome) in leukemia therapy with retinoidsHypervitaminosis A/toxicityMucocutaneous and hepatic side effects with retinoid drugs
06

Interacting drugs

All-trans retinoic acid (tretinoin)

4 more in the full profile.

07

Biomarkers

PML-RARA fusion (for diagnosis and therapy in acute promyelocytic leukemia)RARβ promoter methylation (in some cancers)Expression levels of RAR isoforms in tumors

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