Structure, function and modulation of retinoic acid receptor beta, a tumor suppressor. - Archive ouverte HAL Access content directly
Journal Articles International Journal of Biochemistry and Cell Biology Year : 2007

Structure, function and modulation of retinoic acid receptor beta, a tumor suppressor.

Abstract

Only one of the three-retinoic acid receptors, RARbeta, is frequently deleted or epigenetically silenced at early stages in tumor progression and there is compelling evidence that RARbeta corresponds to a tumor suppressor. Recent discoveries may help to reveal the molecular basis of the tumor suppressive action of this retinoic acid receptor subtype and provide new tools for its analysis and, possibly, therapeutic exploitation. The first concerns the recent elucidation of the crystal structure of the ligand-binding domain of the agonist-bound receptor. The second is the discovery of selective agonists, including isoform selective ligands, which are important tools to facilitate the pharmacological analysis of the tumor suppressor function of this protein in vivo. Lastly, its involvement in a retinoic acid-induced tumor-specific apoptosis program mediated by tumor necrosis factor-related apoptosis-inducing ligand (TRAIL). Herein we describe the structure, function and ligand-dependent transcription mechanism of retinoic acid receptor beta, and use rational drug design to understand the selectivity of these modulators.

Dates and versions

hal-00189381 , version 1 (20-11-2007)

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Susana Alvarez, Pierre Germain, Rosana Alvarez, Fátima Rodríguez-Barrios, Hinrich Gronemeyer, et al.. Structure, function and modulation of retinoic acid receptor beta, a tumor suppressor.. International Journal of Biochemistry and Cell Biology, 2007, 39 (7-8), pp.1406-15. ⟨10.1016/j.biocel.2007.02.010⟩. ⟨hal-00189381⟩
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