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Marine Ligands of the Pregnane X Receptor (PXR): An Overview

Department of Pharmacology and Toxicology, Faculty of Pharmacy, Charles University, Heyrovského 1203, Hradec Králové 500 05, Czech Republic
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Mar. Drugs 2019, 17(10), 554; https://doi.org/10.3390/md17100554
Received: 10 September 2019 / Revised: 27 September 2019 / Accepted: 27 September 2019 / Published: 28 September 2019
Pregnane X Receptor (PXR) is a ligand-activated transcription factor which binds many structurally different molecules. The receptor is able to regulate the expression of a wide array of genes and is involved in cancer and different key physiological processes such as the metabolism of drugs/xenobiotics and endogenous compounds including lipids and carbohydrates, and inflammation. Algae, sponges, sea squirts, and other marine organisms are some of the species from which structurally new molecules have been isolated that have been subsequently identified in recent decades as ligands for PXR. The therapeutic potential of these natural compounds is promising in different areas and has recently resulted in the registration of trabectedin by the FDA as a novel antineoplastic drug. Apart from being potentially novel drugs, these compounds can also serve as models for the development of new molecules with improved activity. The aim of this review is to succinctly summarize the currently known natural molecules isolated from marine organisms with a proven ability to interact with PXR. View Full-Text
Keywords: natural compound; marine origin; PXR; gene regulation; CYP450; inflammation; cancer natural compound; marine origin; PXR; gene regulation; CYP450; inflammation; cancer
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Carazo, A.; Mladěnka, P.; Pávek, P. Marine Ligands of the Pregnane X Receptor (PXR): An Overview. Mar. Drugs 2019, 17, 554.

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