Abstract
Rexinoids are selective ligands for the nuclear receptors known as RXRs. They do not bind to the receptors for all-trans-retinoic acid (RARs). Many new rexinoids have been synthesized and then assayed for their ability to suppress proliferation of cancer cells, to inhibit activation of inflammatory cells of the tumor microenvironment, and to prevent carcinogenesis in animal models relevant to human disease. Here we review the literature on the effects of 4 such rexinoids: bexarotene, LG100268, LG101506, and NRX194204. These rexinoids also have potent synergistic effects when used in combination with other active pharmacological agents, and practical clinical applications would benefit from these actions.
Keywords: RXR, Bexarotene, LG100268, Inflammation, Carcinogenesis, Combination therapy.
Graphical Abstract
Current Topics in Medicinal Chemistry
Title:Rexinoids for Prevention and Treatment of Cancer: Opportunities and Challenges
Volume: 17 Issue: 6
Author(s): Karen T. Liby and Michael B. Sporn
Affiliation:
Keywords: RXR, Bexarotene, LG100268, Inflammation, Carcinogenesis, Combination therapy.
Abstract: Rexinoids are selective ligands for the nuclear receptors known as RXRs. They do not bind to the receptors for all-trans-retinoic acid (RARs). Many new rexinoids have been synthesized and then assayed for their ability to suppress proliferation of cancer cells, to inhibit activation of inflammatory cells of the tumor microenvironment, and to prevent carcinogenesis in animal models relevant to human disease. Here we review the literature on the effects of 4 such rexinoids: bexarotene, LG100268, LG101506, and NRX194204. These rexinoids also have potent synergistic effects when used in combination with other active pharmacological agents, and practical clinical applications would benefit from these actions.
Export Options
About this article
Cite this article as:
Liby T. Karen and Sporn B. Michael, Rexinoids for Prevention and Treatment of Cancer: Opportunities and Challenges, Current Topics in Medicinal Chemistry 2017; 17 (6) . https://dx.doi.org/10.2174/1568026616666160617090702
DOI https://dx.doi.org/10.2174/1568026616666160617090702 |
Print ISSN 1568-0266 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4294 |
- Author Guidelines
- Graphical Abstracts
- Fabricating and Stating False Information
- Research Misconduct
- Post Publication Discussions and Corrections
- Publishing Ethics and Rectitude
- Increase Visibility of Your Article
- Archiving Policies
- Peer Review Workflow
- Order Your Article Before Print
- Promote Your Article
- Manuscript Transfer Facility
- Editorial Policies
- Allegations from Whistleblowers
- Announcements
Related Articles
-
The Role of Cellular Plasticity in Cancer Development
Current Medicinal Chemistry Targeted Therapies in Bone Sarcomas
Current Cancer Drug Targets Designing Novel Therapies Against Sarcomas in the Era of Personalized Medicine and Economic Crisis
Current Pharmaceutical Design Case Report of a Large Rhinolith Cast – A Frequently Missed Diagnosis
New Emirates Medical Journal A Systematic Review of Selected Musculoskeletal Late Effects in Survivors of Childhood Cancer
Current Pediatric Reviews Profiling of Enzymatic Activities Using Peptide Arrays
Mini-Reviews in Organic Chemistry Flavonoids in Cancer Prevention
Anti-Cancer Agents in Medicinal Chemistry Mammalian Target of Rapamycin (mTOR) Inhibitors as Anti-Cancer Agents
Current Cancer Drug Targets Understanding Mesenchymal Cancer: The Liposarcoma-Associated t(12;16) (q13;;p11) Chromosomal Translocation as a Model
Current Genomics Primary Cilia in Tumor Biology: The Primary Cilium as a Therapeutic Target in Cholangiocarcinoma
Current Drug Targets Nanosponges Encapsulated Phytochemicals for Targeting Cancer: A Review
Current Drug Targets New Perspectives in the Pharmacological Potential of Naringin in Medicine
Current Medicinal Chemistry EXTraordinary Bones: Functional and Genetic Analysis of the EXT Gene Family
Current Genomics Cyclopamine, a Naturally Occurring Alkaloid, and Its Analogues May Find Wide Applications in Cancer Therapy
Current Topics in Medicinal Chemistry Cancer Metastasis as Disrupted Developmental Phenotype
Current Genomics Development of RGD-Based Radiotracers for Tumor Imaging and Therapy: Translating from Bench to Bedside
Current Molecular Medicine The Efficacy and Mechanism of Proteasome Inhibitors in Solid Tumor Treatment
Recent Patents on Anti-Cancer Drug Discovery The Role of miR-129-5p in Cancer: A Novel Therapeutic Target
Current Molecular Pharmacology Understanding Molecular Pathways and Targets of Brachyury in Epithelial-mesenchymal Transition (EMT) in Human Cancers
Current Cancer Drug Targets The Functional Role of Oncogenic LncRNA BCAR4 for Cancer Outcome
Current Pharmaceutical Design