Nuclear receptors as drug targets in metabolic diseases: new approaches to therapy

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Updated: Aug 6, 2026

Reverse Yeast Two-hybrid System to Identify Mammalian Nuclear Receptor Residues that Interact with Ligands and/or Antagonists
10:51

Reverse Yeast Two-hybrid System to Identify Mammalian Nuclear Receptor Residues that Interact with Ligands and/or Antagonists

Published on: November 15, 2013

James F Tobin1, Leonard P Freedman

  • 1Department of Cardiovascular and Metabolic Diseases, Wyeth Research, 200 Cambridge Park Drive, Cambridge, MA 02140, USA. jtobin@wyeth.com

Trends in Endocrinology and Metabolism: TEM
|July 28, 2006
PubMed

Insights

Nuclear receptors are key targets for treating metabolic diseases like type 2 diabetes. Understanding selective modulators could lead to safer, more effective therapeutic agents.

Area of Science:

  • Biochemistry
  • Pharmacology
  • Molecular Biology

Background:

  • Nuclear receptors are crucial therapeutic targets for metabolic diseases such as type 2 diabetes, obesity, dyslipidemia, atherosclerosis, and metabolic syndrome.
  • Recent advancements have been made in developing therapeutic agents for specific nuclear receptors, including peroxisome proliferator-activated receptors (PPARs), liver X receptors (LXRs), and farnesoid X receptor (FXR).

Purpose of the Study:

  • To explore the potential of nuclear receptors as therapeutic targets for metabolic diseases.
  • To highlight the need for a deeper understanding of the molecular mechanisms underlying selective receptor modulation.
  • To advocate for the rational design of novel therapeutic agents based on molecular insights.

Main Methods:

  • Review of current literature on nuclear receptor modulators.
  • Analysis of the molecular basis for selective modulation of nuclear receptors.
  • Exploration of new biological insights into nuclear receptor function.

Main Results:

  • The development of selective modulators for nuclear receptors has largely been empirical.
  • A comprehensive understanding of selective modulation is lacking.
  • New biological insights into nuclear receptors are emerging.

Conclusions:

  • Nuclear receptors offer promising therapeutic targets for metabolic syndrome and related conditions.
  • Rational drug design, informed by molecular and biological understanding, is essential for developing next-generation therapeutics.
  • Improved safety and efficacy of treatments for metabolic diseases can be achieved through a deeper understanding of nuclear receptor modulation.

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