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Updated: Jun 22, 2026

Development and Maintenance of a Preclinical Patient Derived Tumor Xenograft Model for the Investigation of Novel Anti-Cancer Therapies
Published on: September 30, 2016
Therapeutic potential of "rexinoids" in cancer prevention and treatment
Takemi Tanaka1, Luigi M De Luca
1University of Texas Health Science Center, Institute of Molecular Medicine, Houston, Texas 77030, USA. Takemi.Tanaka@uth.tmc.edu
Abstract:
Retinoid X receptor (RXR) is a combinatorial partner for one third of the 48 human nuclear receptor superfamily members and acts as a master coordinator of nuclear receptor signaling pathways involved in the control of cell growth and differentiation. Thus, ligand-dependent simultaneous activation of multiple pathways is an attractive strategy for molecular-targeted therapy of neoplastic disease. However, clinical trials in RXR-targeted molecular therapy with the RXR ligand (rexinoid) have yielded disappointing outcomes. In this review, we discuss a possible mechanism underlying the loss of sensitivity to rexinoid therapy.
Insights
Retinoid X receptor (RXR) ligands, or rexinoids, are promising for cancer therapy by activating multiple pathways. However, clinical trials show disappointing outcomes, suggesting a loss of sensitivity to rexinoid therapy.
Area of Science:
- Molecular biology
- Oncology
- Pharmacology
Background:
- Retinoid X receptor (RXR) is a key regulator of nuclear receptor signaling, controlling cell growth and differentiation.
- RXR partners with numerous nuclear receptors, making it a target for simultaneous pathway activation.
- Targeting RXR offers a potential strategy for molecular-targeted cancer therapy.
Purpose of the Study:
- To explore the reasons behind the disappointing outcomes of clinical trials using RXR-targeted therapy.
- To investigate the mechanisms contributing to the loss of sensitivity to rexinoid therapy.
Main Methods:
- This review synthesizes current research on RXR signaling and rexinoid therapy.
- Analysis of clinical trial data and preclinical studies investigating RXR function.
Main Results:
- Simultaneous activation of multiple pathways via RXR ligands (rexinoids) is a theoretically attractive cancer therapy approach.
- Clinical trials targeting RXR have shown limited success, indicating a loss of therapeutic sensitivity.
Conclusions:
- Understanding the mechanisms of rexinoid resistance is crucial for developing effective RXR-targeted cancer therapies.
- Further research is needed to overcome the challenges observed in clinical applications of rexinoid therapy.
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