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Ligand Design for Modulation of RXR Functions

Claudio Martínez1, José A Souto1, Angel R de Lera2

  • 1Departamento de Química Orgánica, Facultade de Química, CINBIO and IBIV, Universidade de Vigo, Vigo, Spain.

Methods in Molecular Biology (Clifton, N.J.)
|July 31, 2019
PubMed

Insights

Retinoid X receptors (RXRs) form partnerships with other nuclear receptors. New rexinoids are being designed to target specific receptor surfaces, offering potential therapeutic advancements.

Area of Science:

  • Molecular Biology
  • Endocrinology
  • Drug Discovery

Background:

  • Retinoid X receptors (RXRs) are nuclear receptors known for their versatile heterodimerization capabilities.
  • RXRs interact with various nuclear receptor (NR) superfamily members, influencing gene transcription.
  • RXR ligands, or rexinoids, modulate these interactions, acting as activators or synergists.

Purpose of the Study:

  • To describe the rationale behind the structural diversity in rexinoid design.
  • To highlight new generations of rexinoids targeting specific receptor surfaces.
  • To explore the therapeutic potential of diverse rexinoids, including agonists and selective modulators.

Main Methods:

  • X-ray crystallography of RXR-ligand complexes.
  • High-throughput screening (HTS) for ligand discovery.
  • Molecular modeling and rational drug design.
  • Characterization of novel rexinoids and their interactions.

Main Results:

  • A wide structural diversity of rexinoids has been explored, derived from various sources.
  • New rexinoids are capable of modulating RXR surface structures for targeted regulation.
  • The study outlines a panel of RXR agonists, partial agonists, and selective rexinoids.

Conclusions:

  • Diverse rexinoid design strategies are crucial for exploring RXR's therapeutic landscape.
  • Targeting specific RXR surfaces with novel ligands presents a promising therapeutic avenue.
  • Further exploration of rexinoid potential is needed to overcome current therapeutic limitations.
Keywords:
(Virtual) ligand designAgonistsAntagonistsComputer-assisted RXR ligand discoveryRXRRXR heterodimersRexinoids

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