3-[6-(2-Dimethylamino-1-imidazol-1-yl-butyl)-naphthalen-2-yloxy]-2,2-dimethyl-propionic Acid As a Highly Potent and Selective Retinoic Acid Metabolic Blocking Agent
Overview
Authors
Affiliations
3-[6-(2-Dimethylamino-1-imidazol-1-yl-butyl)-naphthalen-2-yloxy]-2,2-dimethyl-propionic acid and analogs were designed and synthesized as highly potent and selective CYP26 inhibitors, serving as retinoic acid metabolic blocking agents (RAMBAs), with demonstrated in vivo efficacy to increase the half-life of exogenous atRA.
Retinoid signaling in skeletal development: Scoping the system for predictive toxicology.
Knudsen T, Pierro J, Baker N Reprod Toxicol. 2020; 99:109-130.
PMID: 33202217 PMC: 11451096. DOI: 10.1016/j.reprotox.2020.10.014.
Nelson C, Buttrick B, Isoherranen N Curr Top Med Chem. 2013; 13(12):1402-28.
PMID: 23688132 PMC: 4366427. DOI: 10.2174/1568026611313120004.
The role of CYP26 enzymes in retinoic acid clearance.
Thatcher J, Isoherranen N Expert Opin Drug Metab Toxicol. 2009; 5(8):875-86.
PMID: 19519282 PMC: 2730205. DOI: 10.1517/17425250903032681.