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Title:
SUBSTRATES FOR BETA-LACTAMASE AND USES THEREOF SUBSTRATES FOR BETA-LACTAMASE AND USES THEREOF
Document Type and Number:
WIPO Patent Application WO1996030540
Kind Code:
A3
Abstract:
Substrates for beta -lactamase of general formula (I) in which one of X and Y is a fluorescent donor moiety and the other is a quencher (which may or may not re-emit); R' is selected from the group consisting of H, lower (i.e. alkyl of 1 to about 5 carbon atoms) and (CH2)nOH, in which n is 0 or an integer from 1 to 5; R" is selected from the group consisting of H, physiologically acceptable metal and ammonium cations, - CHR<2>OCO(CH2)nCH3, -CHR<2>OCOC(CH3)3, acylthiomethyl, acyloxy-alpha-benzyl, delta-butyrolactonyl, methoxycarbonyloxymethyl, phenyl, methylsulphinylmethyl, beta-morpholinoethyl, dialkylaminoethyl, acyloxyalkyl, dialkylaminocarbonyloxymethyl and aliphatic, in which R<2> is selected from the group consisting of H and lower alkyl; A is selected from the group consisting of S, O, SO, SO2 and CH2; and Z' and Z" are linkers for the fluorescent donor and quencher moieties. Methods of assaying beta -lactamase activity and monitoring expression in systems using beta -lactamase as a reporter gene also are disclosed.

Inventors:
TSIEN ROGER Y (US)
ZLOKARNIK GREGOR (US)
Application Number:
PCT/US1996/004059
Publication Date:
January 09, 1997
Filing Date:
March 20, 1996
Export Citation:
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Assignee:
UNIV CALIFORNIA (US)
TSIEN ROGER Y (US)
ZLOKARNIK GREGOR (US)
International Classes:
C07D463/00; C12N15/09; C07D471/04; C07D501/00; C07D501/20; C07D501/59; C07D505/00; C12N5/02; C12N5/10; C12N9/86; C12N15/55; C12N15/85; C12P17/18; C12P35/00; C12Q1/34; C12Q1/68; (IPC1-7): C12Q/
Foreign References:
EP0354757A21990-02-14
US5162524A1992-11-10
EP0053541A11982-06-09
Other References:
See also references of EP 0817785A2
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