RAR相关孤儿受体

RAR相关孤儿受体(英語:RAR-related orphan receptorRORs)是核受体的一个家族,是细胞内转录因子的一员[1][2]。有三个ROR家族成员:ROR-α分别由基因RORARORBRORC编码。RORs的不寻常之处在于它们是以单体形式结合到激素反应元件英语hormone response element上的,而其它大部分核受体都是以二聚体形式发挥作用[3]

RAR相关孤儿受体α
識別
符號RORA
替換符號RZRA, ROR1, ROR2, ROR3, NR1F1
Entrez6095
HUGO10258
OMIM600825
PDB1N83
RefSeqNM_002943
UniProtP35398
其他資料
基因座15 q21-q22
RAR相关孤儿受体β
識別
符號RORB
替換符號RZRB, NR1F2, ROR-BETA
Entrez6096
HUGO10259
OMIM601972
PDB1NQ7
RefSeqNM_006914
UniProtQ92753
其他資料
基因座9 q22
RAR相关孤儿受体γ
識別
符號RORC
替換符號RZRG, RORG, NR1F3, TOR
Entrez6097
HUGO10260
OMIM602943
RefSeqNM_005060
UniProtP51449
其他資料
基因座1 q21

配体编辑

目前已有褪黑素是ROR-α内源性配体的报道,而CGP 52608是其人工合成的配体[4]。另外,X-射线晶体衍射(PDB 1n831s0x)数据表明胆固醇或胆固醇衍生物都可能是内源性配体[5]

与之相反,全反式维A酸对ROR-β和-γ有高亲和性,但对ROR-α全无[6]

功能编辑

三种RORs在各个系统中起一些重要角色作用[7],包括:

参考文献编辑

  1. ^ Giguère V, Tini M, Flock G, Ong E, Evans RM, Otulakowski G. Isoform-specific amino-terminal domains dictate DNA-binding properties of ROR alpha, a novel family of orphan hormone nuclear receptors. Genes Dev. 1994, 8 (5): 538–53. PMID 7926749. doi:10.1101/gad.8.5.538. 
  2. ^ Hirose T, Smith RJ, Jetten AM. ROR gamma: the third member of ROR/RZR orphan receptor subfamily that is highly expressed in skeletal muscle. Biochem. Biophys. Res. Commun. 1994, 205 (3): 1976–83. PMID 7811290. doi:10.1006/bbrc.1994.2902. 
  3. ^ Jetten AM, Kurebayashi S, Ueda E. Progress in Nucleic Acid Research and Molecular Biology Volume 69. Prog. Nucleic Acid Res. Mol. Biol. Progress in Nucleic Acid Research and Molecular Biology. 2001, 69: 205–47. ISBN 978-0-12-540069-5. PMID 11550795. doi:10.1016/S0079-6603(01)69048-2.  |chapter=被忽略 (帮助)
  4. ^ Wiesenberg I, Missbach M, Kahlen JP, Schräder M, Carlberg C. Transcriptional activation of the nuclear receptor RZR alpha by the pineal gland hormone melatonin and identification of CGP 52608 as a synthetic ligand. Nucleic Acids Res. 1995, 23 (3): 327–33. PMC 306679 . PMID 7885826. doi:10.1093/nar/23.3.327. 
  5. ^ Kallen JA, Schlaeppi JM, Bitsch F, Geisse S, Geiser M, Delhon I, Fournier B. X-ray structure of the hRORalpha LBD at 1.63 A: structural and functional data that cholesterol or a cholesterol derivative is the natural ligand of RORalpha. Structure. December 2002, 10 (12): 1697–707 [2013-12-01]. PMID 12467577. doi:10.1016/S0969-2126(02)00912-7. (原始内容存档于2019-02-17). 
  6. ^ Stehlin-Gaon C, Willmann D, Zeyer D, Sanglier S, Van Dorsselaer A, Renaud JP, Moras D, Schüle R. All-trans retinoic acid is a ligand for the orphan nuclear receptor ROR beta. Nat. Struct. Biol. 2003, 10 (10): 820–5. PMID 12958591. doi:10.1038/nsb979. 
  7. ^ Jetten AM. Recent advances in the mechanisms of action and physiological functions of the retinoid-related orphan receptors (RORs). Current drug targets. Inflammation and allergy. 2004, 3 (4): 395–412 [2013-12-01]. PMID 15584888. doi:10.2174/1568010042634497. (原始内容存档于2013-12-03). 

外部链接编辑