Design and synthesis of selective, high-affinity inhibitors of human cytochrome P450 2J2 - Université Paris Cité Accéder directement au contenu
Article Dans Une Revue Bioorganic and Medicinal Chemistry Letters Année : 2006

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

Résumé

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.

Mots clés

Dates et versions

hal-00068615 , version 1 (12-05-2006)

Identifiants

Citer

Pierre Lafite, Sylvie Dijols, Didier Buisson, Anne-Christine Macherey, Darryl C. Zeldin, et al.. Design and synthesis of selective, high-affinity inhibitors of human cytochrome P450 2J2. Bioorganic and Medicinal Chemistry Letters, 2006, 16, pp.2777-2780. ⟨10.1016/j.bmcl.2006.02.004⟩. ⟨hal-00068615⟩

Collections

CNRS UP-SCIENCES
94 Consultations
0 Téléchargements

Altmetric

Partager

Gmail Facebook X LinkedIn More