Document Type
Article
Publication Date
2015
Keywords
Bexarotene, lipids, rexinoids, RXR, thyroid
Digital Object Identifier (DOI)
https://doi.org/10.1002/prp2.122
Abstract
In order to determine the feasibility of utilizing novel rexinoids for chemotherapeutics and as potential treatments for neurological conditions, we undertook an assessment of the side effect profile of select rexinoid X receptor (RXR) analogs that we reported previously. We assessed pharmacokinetic profiles, lipid and thyroid-stimulating hormone (TSH) levels in rats, and cell culture activity of rexinoids in sterol regulatory element-binding protein (SREBP) induction and thyroid hormone inhibition assays. We also performed RNA sequencing of the brain tissues of rats that had been dosed with the compounds. We show here for the first time that potent rexinoid activity can be uncoupled from drastic lipid changes and thyroid axis variations, and we propose that rexinoids can be developed with improved side effect profiles than the parent compound, bexarotene (1).
Rights Information
This work is licensed under a Creative Commons Attribution-Noncommercial-No Derivative Works 4.0 License.
Was this content written or created while at USF?
Yes
Citation / Publisher Attribution
Pharmacology Research & Perspectives, v. 3, issue 2, art. e00122
Scholar Commons Citation
Marshall, Pamela A.; Jurutka, Peter W.; Wagner, Carl E.; van der Vaart, Arjan; Kaneko, Ichiro; Chavez, Pedro I.; Ma, Ning; Bhogal, Jaskaran S.; Shahani, Pritika; Swierski, Johnathon C.; and MacNeill, Mairi, "Analysis of Differential Secondary Effects of Novel Rexinoids: Select Rexinoid X Receptor Ligands Demonstrate Differentiated Side Effect Profiles" (2015). Chemistry Faculty Publications. 117.
https://digitalcommons.usf.edu/chm_facpub/117
