Method for measuring aromatase activity

C - Chemistry – Metallurgy – 09 – B

Patent

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C09B 48/00 (2006.01) C07J 1/00 (2006.01) C07J 9/00 (2006.01) C09B 15/00 (2006.01) C09B 62/00 (2006.01) C12Q 1/26 (2006.01) G01N 33/52 (2006.01)

Patent

CA 2529669

The present invention relates to compounds useful for measuring aromatase activity. The invention further provides methods for measuring aromatase activity and for screening test agents which modulate aromatase activity. A kit is also provided for use in such screening methods. The compounds are of the general Formula (I): R-L-S. R is a fluorescent dye molecule, which is either an acridone dye of general Formula (II): (see formula II) or a quinacridone dye of general Formula (III): (see formula III) L is an optional linker group containing from 1 to 40 linked atoms which are carbon atoms which may optionally include one or more groups selected from the group consisting of -NR'-, -O-, -S-, -CH=CH-, -C.ident.C-, -CONH- and phenylenyl groups, wherein R' is H or C1 to C4 alkyl; and S is a substrate group of the enzyme aromatase of Formula (IX): (see formula IX).

L'invention concerne des composés utilisés pour mesurer l'activité de l'aromatase. L'invention concerne en outre des procédés permettant de mesurer l'activité de l'aromatase et de trier des agents de référence qui modulent l'activité de l'aromatase. L'invention concerne également un nécessaire permettant de mettre lesdits procédés en oeuvre.

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