Literature DB >> 15501068

Novel retinoid X receptor (RXR) antagonists having a dicarba-closo-dodecaborane as a hydrophobic moiety.

Kiminori Ohta1, Toru Iijima, Emiko Kawachi, Hiroyuki Kagechika, Yasuyuki Endo.   

Abstract

We designed and synthesized novel retinoid X receptor (RXR)-selective antagonists bearing a carborane moiety. Compounds 8a-d or 9a-d themselves have no differentiation-inducing activity toward HL-60 cells and no inhibitory activity towards a retinoic acid receptor (RAR) agonist. However, they inhibit the synergistic activity of an RXR agonist, PA024, in the presence of Am80 on the cell differentiation of HL-60. Transactivation assay using RARs and RXRs suggested that the inhibitory activity of 9b resulted from the selective antagonism at the RXR site of RXR-RAR heterodimers.

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Year:  2004        PMID： 15501068     DOI： 10.1016/j.bmcl.2004.09.035

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN： 0960-894X            Impact factor:   2.823


  6 in total

1.  Genetic and pharmacological evidence that a retinoic acid cannot be the RXR-activating ligand in mouse epidermis keratinocytes.

Authors:  Cécile Calléja; Nadia Messaddeq; Benoit Chapellier; Haiyuan Yang; Wojciech Krezel; Mei Li; Daniel Metzger; Bénédicte Mascrez; Kiminori Ohta; Hiroyuki Kagechika; Yasuyuki Endo; Manuel Mark; Norbert B Ghyselinck; Pierre Chambon
Journal:  Genes Dev       Date:  2006-06-01       Impact factor: 11.361

2.  Modulators of the structural dynamics of the retinoid X receptor to reveal receptor function.

Authors:  Virginie Nahoum; Efrén Pérez; Pierre Germain; Fátima Rodríguez-Barrios; Fabio Manzo; Sabrina Kammerer; Geraldine Lemaire; Oliver Hirsch; Catherine A Royer; Hinrich Gronemeyer; Angel R de Lera; William Bourguet
Journal:  Proc Natl Acad Sci U S A       Date:  2007-10-18       Impact factor: 11.205

3.  Synthesis and evaluation of transthyretin amyloidosis inhibitors containing carborane pharmacophores.

Authors:  Richard L Julius; Omar K Farha; Janet Chiang; L Jeanne Perry; M Frederick Hawthorne
Journal:  Proc Natl Acad Sci U S A       Date:  2007-03-13       Impact factor: 11.205

4.  Design and Synthesis of Novel Breast Cancer Therapeutic Drug Candidates Based upon the Hydrophobic Feedback Approach of Antiestrogens.

Authors:  Kiminori Ohta; Asako Kaise; Fumi Taguchi; Sayaka Aoto; Takumi Ogawa; Yasuyuki Endo
Journal:  Molecules       Date:  2019-11-01       Impact factor: 4.411

Review 5.  Retinoid X Receptor Antagonists.

Authors:  Masaki Watanabe; Hiroki Kakuta
Journal:  Int J Mol Sci       Date:  2018-08-10       Impact factor: 5.923

Review 6.  The Boron Advantage: The Evolution and Diversification of Boron's Applications in Medicinal Chemistry.

Authors:  Katia Messner; Billy Vuong; Geoffrey K Tranmer
Journal:  Pharmaceuticals (Basel)       Date:  2022-02-22
  6 in total

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