A review of the molecular design and biological activities of RXR agonists

Nathalia Rodrigues de Almeida, Martin Conda-Sheridan

Research output: Contribution to journalReview article

2 Scopus citations

Abstract

An attractive approach to combat disease is to target theregulation of cell function. At the heart of this task are nuclear receptors (NRs); which control functions such as gene transcription. Arguably, the key player in this regulatory machinery is the retinoid X receptor (RXR). This NR associates with a third of the NRs found in humans. Scientists have hypothesized that controlling the activity of RXR is an attractive approach to control cellular functions that modulate diseases such as cancer, diabetes, Alzheimer's disease and Parkinson's disease. In this review, we will describe the key features of the RXR, present a historic perspective of the first RXR agonists, and discuss various templates that have been reported to activate RXR with a focus on their molecular structure, biological activity, and limitations. Finally, we will present an outlook of the field and future directions and considerations to synthesize or modulate RXR agonists to make these compounds a clinical reality.

Original languageEnglish (US)
Pages (from-to)1372-1397
Number of pages26
JournalMedicinal Research Reviews
Volume39
Issue number4
DOIs
StatePublished - Jul 2019

Keywords

  • 9-cis-retinoic acid
  • anticancer agent
  • bexarotene
  • retinoid X receptor
  • rexinoids

ASJC Scopus subject areas

  • Molecular Medicine
  • Pharmacology
  • Drug Discovery

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