Development and Characterization of Novel and Selective Inhibitors of Cytochrome P450 CYP26A1, the Human Liver Retinoic Acid Hydroxylase
Cytochrome P450 CYP26 enzymes are responsible for all-trans-retinoic acid (atRA) clearance. Inhibition of CYP26 enzymes will increase endogenous atRA concentrations and is an attractive therapeutic target. However, the selectivity and potency of the exist
Diaz, Philippe,Huang, Weize,Keyari, Charles M.,Buttrick, Brian,Price, Lauren,Guilloteau, Nicolas,Tripathy, Sasmita,Sperandio, Vanessa G.,Fronczek, Frank R.,Astruc-Diaz, Fanny,Isoherranen, Nina
Application of the Heck reaction in the synthesis of truncated naphthoic acid retinoids
A series of truncated naphthoic acid retinoids have been prepared using the Heck reaction. These retinoids were evaluated in the RAR transactivation assay in vitro and in the utriculi reduction assay in vivo. It has been found that the naphthalene ring of the retinoids is crucial for their retinoid activity and receptor selectivity.
Yu, Kuo-Long,Chen, Simon,Ostrowski, Jacek,Tramposch, Kenneth M.,Reczek, Peter R.,Mansuri, Muzammil M.,Starrett Jr., John E.
p. 2859 - 2864
(2007/10/03)
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