Related Experiment Video

Updated: Aug 20, 2026

Prediction and Validation of Gene Regulatory Elements Activated During Retinoic Acid Induced Embryonic Stem Cell Differentiation
09:07

Prediction and Validation of Gene Regulatory Elements Activated During Retinoic Acid Induced Embryonic Stem Cell Differentiation

Published on: June 21, 2016

Selective retinoic acid receptor ligands for rheumatoid arthritis

Blake C Beehler1, Constance E Brinckerhoff, Jacek Ostrowski

  • 1Bristol-Myers Squibb Company, Pharmaceutical Research Institute, Route 206 and Provinceline Road, E1355 Mail Stop 13-08, Princeton, NJ 08543, USA. blake.beehler@bms.com

Current Opinion in Investigational Drugs (London, England : 2000)
|December 3, 2004
PubMed

Insights

Retinoids, which modulate retinoic acid receptors (RARs), show renewed promise for rheumatoid arthritis (RA) treatment. Newer synthetic RAR-selective retinoids offer improved efficacy and reduced toxicity compared to earlier agents.

Area of Science:

  • Immunology
  • Pharmacology
  • Rheumatology

Background:

  • Retinoids, modulators of retinoic acid receptors (RARs), have been investigated for rheumatoid arthritis (RA) therapy for over two decades.
  • Initial in vitro and in vivo studies showed promise, but clinical trials were hampered by poor efficacy and significant side effects.
  • Advances in understanding retinoid biology have spurred the development of novel synthetic retinoids.

Purpose of the Study:

  • To explore the potential of novel synthetic retinoids in treating rheumatoid arthritis.
  • To evaluate the improved pharmacological profiles and reduced toxicity of RAR-selective retinoids.
  • To re-evaluate the therapeutic utility of retinoids in the context of RA management.

Main Methods:

  • Development of synthetic retinoids with selective modulation of RAR isotypes.
  • Preclinical and clinical evaluation of these novel agents for RA treatment.
  • Assessment of efficacy, side effect profiles, and pharmacokinetic properties.

Main Results:

  • Synthetic retinoids demonstrate selective modulation of RAR isotypes.
  • These agents exhibit potential for enhanced pharmacological activity.
  • Reduced toxicity profiles are anticipated compared to earlier retinoid therapies.

Conclusions:

  • RAR-selective retinoids represent a promising advancement in retinoid-based RA therapy.
  • These compounds offer a renewed therapeutic avenue for rheumatoid arthritis due to improved safety and efficacy.
  • Further research and clinical trials are warranted to fully establish the role of these agents in RA treatment.

More Related Videos

Methodology for Studying Interactions of Vitamin A Membrane Receptors and Opsin Protein with their Ligands in Generating the Retinylidene Protein08:18

Methodology for Studying Interactions of Vitamin A Membrane Receptors and Opsin Protein with their Ligands in Generating the Retinylidene Protein

Published on: October 4, 2024

Related Concept Videos

Transducer Mechanism: Nuclear Receptors01:31

Transducer Mechanism: Nuclear Receptors

Nuclear receptors, or NRs, are unique transcription factors that regulate gene transcription and affect the cellular pathways involved in reproduction, development, or metabolism. Their ability to be stimulated by small lipophilic ligands and control vital cellular processes makes them ideal drug targets. Nearly 10-15% of currently prescribed drugs target these receptors.
About 48 different soluble family members of nuclear receptors are identified that can be divided into two main classes:
The JAK-STAT Signaling Pathway01:20

The JAK-STAT Signaling Pathway

Several cytokine receptors have tightly bound Janus kinase or JAK proteins attached at their cytosolic tail. Small signaling molecules such as cytokines, growth hormones, or prolactins bind to the cytokine receptors and initiate their dimerization. The dimerization brings the cytosolic JAKs together that trans-phosphorylate and activates each other. The activated JAKs now phosphorylate cytosolic tails of the cytokine receptors, which serve as binding sites for adaptor proteins such as  SH2...
Connective Tissue Cell Types01:22

Connective Tissue Cell Types

Connective tissue develops from the mesoderm of a developing embryo and consists of cells, fibers, and ground substance: a gel-like material containing large complexes of carbohydrates and proteins. Connective tissue was first identified as a separate tissue family in the 18th century, and Johannes Peter Muller coined the term connective tissue.
Fat cells (adipocytes), smooth muscle cells (myoblasts), and bone cells (osteoblasts) are some connective tissue cell types. Some immune system cells...