Literature DB >> 1323296

Identification of synthetic retinoids with selectivity for human nuclear retinoic acid receptor gamma.

B A Bernard1, J M Bernardon, C Delescluse, B Martin, M C Lenoir, J Maignan, B Charpentier, W R Pilgrim, U Reichert, B Shroot.   

Abstract

The action of retinoids on gene regulation is mediated by three distinct nuclear retinoic acid receptor (RAR) subtypes called RAR alpha, beta and gamma. Since RAR gamma is predominantly expressed in adult skin, specific ligands for this subtype could (i) represent valuable tools to evaluate the biological role of RAR gamma in skin and (ii) provide therapeutic entities with a higher therapeutic index at lower teratogenic risk. Using in vitro binding studies and a functional transactivation assay, we have identified three compounds with high RAR gamma selectivity.

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Year:  1992        PMID: 1323296     DOI: 10.1016/0006-291x(92)90842-9

Source DB:  PubMed          Journal:  Biochem Biophys Res Commun        ISSN: 0006-291X            Impact factor:   3.575


  25 in total

1.  Mass-spectrometric analysis of agonist-induced retinoic acid receptor gamma conformational change.

Authors:  Valerie J Peterson; Elisabeth Barofsky; Max L Deinzer; Marcia I Dawson; Kai-Chia Feng; Xiao-kun Zhang; Machender R Madduru; Mark Leid
Journal:  Biochem J       Date:  2002-02-15       Impact factor: 3.857

2.  An in vitro model for the pro-fibrotic effects of retinoids: mechanisms of action.

Authors:  A C Rankin; B M Hendry; J P Corcoran; Q Xu
Journal:  Br J Pharmacol       Date:  2013-11       Impact factor: 8.739

3.  Retinoid-induced apoptosis and Sp1 cleavage occur independently of transcription and require caspase activation.

Authors:  F J Piedrafita; M Pfahl
Journal:  Mol Cell Biol       Date:  1997-11       Impact factor: 4.272

4.  Cell-type and promoter-context dependent retinoic acid receptor (RAR) redundancies for RAR beta 2 and Hoxa-1 activation in F9 and P19 cells can be artefactually generated by gene knockouts.

Authors:  R Taneja; B Roy; J L Plassat; C F Zusi; J Ostrowski; P R Reczek; P Chambon
Journal:  Proc Natl Acad Sci U S A       Date:  1996-06-11       Impact factor: 11.205

5.  Highly twisted adamantyl arotinoids: synthesis, antiproliferative effects and RXR transactivation profiles.

Authors:  Santiago Pérez-Rodríguez; Maria A Ortiz; Raquel Pereira; Fátima Rodríguez-Barrios; Angel R de Lera; F Javier Piedrafita
Journal:  Eur J Med Chem       Date:  2009-01-20       Impact factor: 6.514

Review 6.  The lipophilic bullet hits the targets: medicinal chemistry of adamantane derivatives.

Authors:  Lukas Wanka; Khalid Iqbal; Peter R Schreiner
Journal:  Chem Rev       Date:  2013-02-25       Impact factor: 60.622

7.  Adamantyl arotinoids that inhibit IκB kinase α and IκB kinase β.

Authors:  Paula Lorenzo; María A Ortiz; Rosana Alvarez; F Javier Piedrafita; Angel R de Lera
Journal:  ChemMedChem       Date:  2013-05-07       Impact factor: 3.466

8.  Inhibition of activation-induced apoptosis of thymocytes by all-trans- and 9-cis-retinoic acid is mediated via retinoic acid receptor alpha.

Authors:  Z Szondy; U Reichert; J M Bernardon; S Michel; R Tóth; E Karászi; L Fésüs
Journal:  Biochem J       Date:  1998-05-01       Impact factor: 3.857

9.  p38 MAPK signaling mediates retinoic acid-induced CD103 expression in human dendritic cells.

Authors:  Mandi M Roe; Marziah Hashimi; Steve Swain; Krista M Woo; Diane Bimczok
Journal:  Immunology       Date:  2020-09-14       Impact factor: 7.397

10.  A retinoic acid receptor beta agonist (CD2019) overcomes inhibition of axonal outgrowth via phosphoinositide 3-kinase signalling in the injured adult spinal cord.

Authors:  Marta Agudo; Ping Yip; Meirion Davies; Elizabeth Bradbury; Patrick Doherty; Stephen McMahon; Malcolm Maden; Jonathan P T Corcoran
Journal:  Neurobiol Dis       Date:  2009-10-02       Impact factor: 5.996

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