Synthesis of a radiolabelled Retinoid X Receptor (RXR) specific ligand

被引:0
|
作者
Held, P
Heck, MP
Iyer, J
Gronemeyer, H
Lebeau, L
Mioskowski, C
机构
[1] CEA SACLAY,SMM,DBCM,F-91191 GIF SUR YVETTE,FRANCE
[2] INST GENET & BIOL MOL & CELLULAIRE,F-67404 ILLKIRCH GRAFFENS,FRANCE
关键词
retinoid; SR11237; tritium; synthesis;
D O I
暂无
中图分类号
Q5 [生物化学];
学科分类号
071010 ; 081704 ;
摘要
Synthesis of 4-[2-(5,5,8,8-tetramethyl-5,6,7,8-tetrahydro-naphthalen- 2-yl)-[1,3]dioxolan-2-yl]-benzoic acid or SR11237, a specific ligand of Retinoid X Receptors, is described in a H-3-labelled version. The labelled retinoid was prepared in 5 steps and tritium was introduced through a final reduction of an aromatic dihalide moiety with H-3(2).
引用
收藏
页码:501 / 507
页数:7
相关论文
共 50 条
  • [1] Novel roles of retinoid X receptor (RXR) and RXR ligand in dynamically modulating the activity of the thyroid hormone receptor/RXR heterodimer
    Li, DS
    Yamada, T
    Wang, F
    Vulin, AI
    Samuels, HH
    JOURNAL OF BIOLOGICAL CHEMISTRY, 2004, 279 (09) : 7427 - 7437
  • [2] Stereoselective synthesis of a retinoid X receptor (RXR) antagonist.
    Lipshutz, BH
    Balls, DB
    Howell, JH
    ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY, 2005, 229 : U414 - U414
  • [3] Retinoid X receptor in retinoic acid receptor retinoid X receptor heterodimers selectively confers an RXR ligand response to target genes in epidermis
    Xiao, JH
    Di, W
    Feng, X
    Peng, ZH
    Li, XY
    Voorhees, JJ
    JOURNAL OF INVESTIGATIVE DERMATOLOGY, 1996, 106 (04) : 80 - 80
  • [4] Alternative retinoid X receptor (RXR) ligands
    Krezel, Wojciech
    Ruhr, Ralph
    de Lera, Angel R.
    MOLECULAR AND CELLULAR ENDOCRINOLOGY, 2019, 491
  • [5] Diarylamines Incorporating Hexahydrophenalene or Octahydrobenzoheptalene as Retinoid X Receptor (RXR)-Specific Agonists
    Amano, Yohei
    Noguchi, Masayuki
    Shudo, Koichi
    CHEMICAL & PHARMACEUTICAL BULLETIN, 2014, 62 (03) : 254 - 259
  • [6] Dual conformation of the ligand induces the partial agonistic activity of retinoid X receptor α (RXRα)
    Miyashita, Yurina
    Numoto, Nobutaka
    Arulmozhiraja, Sundaram
    Nakano, Shogo
    Matsuo, Naoya
    Shimizu, Kanade
    Shibahara, Osamu
    Fujihara, Michiko
    Kakuta, Hiroki
    Ito, Sohei
    Ikura, Teikichi
    Ito, Nobutoshi
    Tokiwa, Hiroaki
    FEBS LETTERS, 2019, 593 (02) : 242 - 250
  • [7] Retinoid X receptor (RXR) within the RXR-retinoic acid receptor heterodimer binds its ligand and enhances retinoid-dependent gene expression
    Minucci, S
    Leid, M
    Toyama, R
    SaintJeannet, JP
    Peterson, VJ
    Horn, V
    Ishmael, JE
    Bhattacharyya, N
    Dey, A
    Dawid, IB
    Ozato, K
    MOLECULAR AND CELLULAR BIOLOGY, 1997, 17 (02) : 644 - 655
  • [8] Retinoid X receptor alpha (RXRα) interaction with sugars
    Soman, Frances L.
    Piva, Camila de Jesus
    Hostetler, Heather A.
    FASEB JOURNAL, 2013, 27
  • [9] Novel retinoid X receptor antagonists: Specific inhibition of retinoid synergism in RXR-RAR heterodimer actions
    Takahashi, B
    Ohta, K
    Kawachi, E
    Fukasawa, H
    Hashimoto, Y
    Kagechika, H
    JOURNAL OF MEDICINAL CHEMISTRY, 2002, 45 (16) : 3327 - 3330
  • [10] Functional evidence for retinoid X receptor (RXR) as a nonsilent partner in the thyroid hormone receptor/RXR heterodimer
    Li, DS
    Li, T
    Wang, F
    Tian, H
    Samuels, HH
    MOLECULAR AND CELLULAR BIOLOGY, 2002, 22 (16) : 5782 - 5792