Modulation of Retinoic Acid Receptor Subtypes by 5- and 8-Substituted (Naphthalen-2-yl)-based Arotinoids

ChemMedChem ◽  
2015 ◽  
Vol 10 (8) ◽  
pp. 1378-1391
Author(s):  
Susana Álvarez ◽  
Michele Lieb ◽  
Claudio Martínez ◽  
Harshal Khanwalkar ◽  
Fátima Rodríguez-Barrios ◽  
...  
Keyword(s):  
Retinoic Acid ◽  
Retinoic Acid Receptor ◽  
Receptor Subtypes ◽  
Acid Receptor

Characterization of the differential coregulator binding signatures of the Retinoic Acid Receptor subtypes upon (ant)agonist action

2017 ◽  
Vol 1865 (9) ◽  
pp. 1195-1206 ◽  
Author(s):  
Ignacio Miro Estruch ◽  
Diana Melchers ◽  
René Houtman ◽  
Laura H.J. de Haan ◽  
John P. Groten ◽  
...  
Keyword(s):  
Retinoic Acid ◽  
Retinoic Acid Receptor ◽  
Receptor Subtypes ◽  
Acid Receptor ◽  
Agonist Action

scholarly journals An RPE cell line as a useful in vitro model for studying retinoic acid receptor β: expression and affinity

2008 ◽  
Vol 28 (6) ◽  
pp. 327-334 ◽  
Author(s):  
Barbara Pavan ◽  
Alessandro Dalpiaz ◽  
Carla Biondi ◽  
Marzia Nieddu ◽  
Antonella De Luca ◽  
...  
Keyword(s):  
Retinoic Acid ◽  
Retinoic Acid Receptor ◽  
Retinal Pigment ◽  
Nuclear Extract ◽  
Retinal Pigment Epithelial Cells ◽  
Receptor Subtypes ◽  
Ligand Interaction ◽  
Acid Receptor ◽  
Nuclear Extracts

Retinoids mediate their biological effect by interacting with specific nuclear receptors. Of the several known RAR (retinoic acid receptor) subtypes, RAR-β is of particular interest, since its expression is silenced in many cancers and it is believed to be a tumour suppressor. Specific ligands of RAR-β can potentially be used in anti-cancer therapy. In the present study, we have investigated the feasibility of using HRPE cells (human retinal pigment epithelial cells) as an experimental model for characterizing RAR-β–ligand interaction. RT–PCR (reverse transcription–PCR) and Western blot analyses show that HRPE cells specifically express only RAR-β and none of the other receptor subtypes. In addition, we show that the expression of RAR-β increases with increasing passage number of the cells. Interestingly, the increase in RAR-β expression is not associated with telomere shortening, a typical biomarker of cellular senescence. In the present study, we also describe a protocol for characterizing RAR-β–ligand interactions using nuclear extract from late passage HRPE cells as a source of endogenous RAR-β. Using [3H]CD367 as the ligand, RAR-β in HRPE cells showed an affinity of 9.6±0.6 nM and a Bmax of 780±14 fmol/mg of protein. We have confirmed the feasibility of using this assay to detect the interaction of ligands with RAR-β by investigating the ability of certain flavonoids to inhibit the binding of [3H]CD367 to nuclear extracts from HRPE cells. The inhibition constant of the flavonoids for RAR-β was between approx. 1–30 μM, showing that the flavonoids interact with RAR-β with low affinity.

Synthesis, Structure-Affinity Relationships, and Biological Activities of Ligands Binding to Retinoic Acid Receptor Subtypes

1995 ◽  
Vol 38 (26) ◽  
pp. 4993-5006 ◽  
Author(s):  
Bruno Charpentier ◽  
Jean-Michel Bernardon ◽  
Jacques Eustache ◽  
Corinne Millois ◽  
Bernard Martin ◽  
...  
Keyword(s):  
Retinoic Acid ◽  
Retinoic Acid Receptor ◽  
Biological Activities ◽  
Receptor Subtypes ◽  
Acid Receptor

Effect of age and retinoic acid supplementation on retinoic acid receptor subtypes expression in human lymphocytes

2004 ◽  
Vol 2004 (Spring) ◽  
Author(s):  
Dana MACEJOVA ◽  
Olga KRIZANOVA ◽  
Elena TIBENSKA ◽  
Marie-Chantal FARGES ◽  
Marie-Paule VASSON ◽  
...  
Keyword(s):  
Retinoic Acid ◽  
Retinoic Acid Receptor ◽  
Human Lymphocytes ◽  
Receptor Subtypes ◽  
Acid Supplementation ◽  
Acid Receptor ◽  
Effect Of Age

scholarly journals Serine 232 and Methionine 272 Define the Ligand Binding Pocket in Retinoic Acid Receptor Subtypes

1998 ◽  
Vol 273 (6) ◽  
pp. 3490-3495 ◽  
Author(s):  
Jacek Ostrowski ◽  
Thor Roalsvig ◽  
Laura Hammer ◽  
Anne Marinier ◽  
John E. Starrett ◽  
...  
Keyword(s):  
Retinoic Acid ◽  
Ligand Binding ◽  
Retinoic Acid Receptor ◽  
Binding Pocket ◽  
Receptor Subtypes ◽  
Ligand Binding Pocket ◽  
Acid Receptor

Contribution of retinoic acid receptor signalling to adrenal cortex morphology and functional zonation through modulation of WNT/[beta]-catenin pathway

2017 ◽  
Author(s):  
Zein Rami El ◽  
Amanda J Rickard ◽  
Golib Dzib Jose Felipe ◽  
Benoit Samson-Couterie ◽  
Angelique Rocha ◽  
...  
Keyword(s):  
Retinoic Acid ◽  
Adrenal Cortex ◽  
Retinoic Acid Receptor ◽  
Beta Catenin ◽  
Acid Receptor ◽  
Receptor Signalling
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