Design and synthesis of selective, high-affinity inhibitors of human cytochrome P450 2J2.

Article Details

Citation

Copy to clipboard

Lafite P, Dijols S, Buisson D, Macherey AC, Zeldin DC, Dansette PM, Mansuy D

Design and synthesis of selective, high-affinity inhibitors of human cytochrome P450 2J2.

Bioorg Med Chem Lett. 2006 May 15;16(10):2777-80. Epub 2006 Feb 21.

PubMed ID

16495056 [ View in PubMed

]

Abstract

The active site topology, substrate specificity, and biological roles of the human cytochrome P450 CYP2J2, which is mainly expressed in the cardiovascular system, are poorly known even though recent data suggest that it could be a novel biomarker and potential target for therapy of human cancer. This paper reports a first series of high-affinity, selective CYP2J2 inhibitors that are related to terfenadine, with K(i) values as low as 160nM, that should be useful tools to determine the biological roles of CYP2J2.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Terfenadine	Cytochrome P450 2J2	IC 50 (nM)	8100	N/A	N/A	Details