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Retinoic acid receptor alpha; Retinoic acid receptor beta; Retinoic acid receptor gamma (RAR-α, RAR-β, RAR-γ)
- Target
- RAR-α, RAR-β, RAR-γ
- Molecular classification
- Nuclear receptor, Transcription factor, Ligand-activated receptor
01
Overview
Retinoic acid receptors (RARα, RARβ, RARγ) are nuclear hormone receptors and transcription factors that bind retinoic acid and regulate the expression of numerous genes involved in cell differentiation, proliferation, apoptosis, and morphogenesis. They heterodimerize with retinoid X receptors (RXRs) and, upon ligand binding, modulate chromatin and transcriptional activity. RARs play redundant and unique physiological roles, notably in embryonic development and skin homeostasis, and are key targets for therapies in dermatology and oncology
- Other names
- RAR-alphaRAR-betaRAR-gammaNR1B1NR1B2NR1B3
02
Mechanism of action
Agonists: bind to receptors, induce conformational change, recruit coactivators, and activate transcription of target genes. Antagonists: block activation, maintain repression of target genes
03
Biological functions
Regulation of gene expressionSignal transductionCell growth and differentiationEmbryonic developmentModulation of skin homeostasis (including pigmentation, collagen synthesis, and sebum production)
04
Disease associations
Cancer (notably acute promyelocytic leukemia via RAR-alpha)Dermatological diseases (e.g., acne, psoriasis, hyperpigmentation)Developmental disordersOther (e.g. inflammation, vitamin A deficiency syndromes)
05
Safety considerations
Teratogenicity (especially relevant in pregnancy)Skin irritation (erythema, peeling, sensitivity with topical retinoids)Systemic toxicity with oral retinoids (e.g., hypervitaminosis A, liver dysfunction)
06
Interacting drugs
Tretinoin
5 more in the full profile.
07
Biomarkers
Expression levels of RARA, RARB, RARG mRNA/protein in tumor or skin samplesPML-RARα fusion protein in acute promyelocytic leukemia
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