Receptor Nomenclature NR2B1
Receptor code 4.1:RX:2:B1
Molecular information Hs:462aa, P19793, chr. 9q34.313
Rn:467aa, P287004
Mm: 467aa, Q05343, chr. 258
DNA binding
   Structure Homodimer, heterodimer, RXR partner
   HRE core sequence AGGTCA (DR-1, DR-2, DR-3, DR-4, DR-5)
Partners TR2 and TR4 (physical, functional): DNA binding7,9,10 ; VDR (physical, functional): DNA binding9,10; RARα, RARβ, and RARγ (physical, functional): DNA binding7,914; PPARα, PPARβ, and PPARγ (physical, functional): DNA binding15,16; LXRα and LXRβ (physical, functional): DNA binding1720; FXR (physical, functional): DNA binding21; PXR (physical, functional): DNA binding2225; CAR (physical, functional): DNA binding26,27; NGFI-B (physical, functional): DNA binding28,29; NURR1 (physical, functional): DNA binding29
Agonists CD3254 (3 nM), LG100268 (3.2 nM), LGD1069 (36 nM),* 9-cis-retinoic acid (6.7–73 nM),* methoprenic acid (2 μM) [IC50]8,12,3039; AGN194204 (0.4 nM) [Kd]40; SR11237, docosahexaenoic acid, phytanic acid4144
Antagonists LG100754 (3.4 nM) [IC50]36,45,46; PA451, UVI300347,48
Coactivators NCOA1, NCOA2, NCOA3, PGC-1α, PPARBP, TBP, TAFII110, TAFII28, CREBBP, p30036,4959
Biologically important isoforms RXRα1 {Mm}: differs from RXRα2 in the A/B domain60; RXRα2 {Mm}: specifically expressed in testis60
Tissue distribution Liver, lung, muscle, kidney, epidermis, and intestine; major isotype in the skin {Hs, Mm, Rn} [Northern blot, in situ hybridization, Western blot]3,8,61
Functional assays Differentiation of 3T3-L1 cells to adipocytes measured by the accumulation of triglyceride produced within the cytoplasm of the adipocyte {Mm}33,62,63 ; induction of apoptosis (associated with RARα activation) in leukemia cell lines {Hs}38,64; primitive endodermal differentiation and morphological differentiation in F9 murine embryonal carcinoma cell line {Mm}65,66
Mutant phenotype Knockout mice have hypoplasia of the myocardium, which leads to animal death due to cardiac failure at around embryonic day 14.5; animals also have ocular malformation {Mm} [knockout]51,6773
  • aa, amino acid; chr, chromosome; HRE, hormone response element; NGFI-B, nerve growth factor-induced clone B; PGC-1α, PPAR coactivator-1α; PPARBP, PPAR-binding protein; TBP, TATA-box binding protein; CREBBP, cAMP response element-binding protein-binding protein

  • * Radioligand

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