The patent badge is an abbreviated version of the USPTO patent document. The patent badge does contain a link to the full patent document.

The patent badge is an abbreviated version of the USPTO patent document. The patent badge covers the following: Patent number, Date patent was issued, Date patent was filed, Title of the patent, Applicant, Inventor, Assignee, Attorney firm, Primary examiner, Assistant examiner, CPCs, and Abstract. The patent badge does contain a link to the full patent document (in Adobe Acrobat format, aka pdf). To download or print any patent click here.

Date of Patent:
Nov. 10, 2015

Filed:

Feb. 24, 2012
Applicants:

Matthew S. Bogyo, Redwood City, CA (US);

Laura E. Edgington, Melbourne, AU;

Martijn Verdoes, Nijmegen, NL;

Inventors:

Matthew S. Bogyo, Redwood City, CA (US);

Laura E. Edgington, Melbourne, AU;

Martijn Verdoes, Nijmegen, NL;

Attorneys:
Primary Examiner:
Assistant Examiner:
Int. Cl.
CPC ...
C07D 249/12 (2006.01); A61K 49/00 (2006.01); C07D 249/04 (2006.01); C07D 409/12 (2006.01); C07D 409/14 (2006.01); C07F 5/02 (2006.01);
U.S. Cl.
CPC ...
A61K 49/0052 (2013.01); A61K 49/0021 (2013.01); A61K 49/0032 (2013.01); C07D 249/04 (2013.01); C07D 409/12 (2013.01); C07D 409/14 (2013.01); C07F 5/022 (2013.01);
Abstract

Methods and materials for the imaging of cells and tissues containing active proteases such as cathepsin are disclosed. The present materials include activity based probes that bind to an enzyme and are subsequently cleaved. Cleavage results in covalent attachment of a fluorescent signal to a target protease due to removal of a quenching group which, when present on the probe causes altered or no fluorescence. The probes are non-peptidic, small molecule scaffolds linked to a reactive acyloxymethyl ketone group, a fluorophore and a quencher. The probes are cell permeable and may use, for example, a QSY21 (CAS 304014-13-9) quencher and a cyanine dye. The probes form covalent bonds with the active site of cysteine cathepsins, proteases that are upregulated at the tumor boundaries with normal tissue and at sites of inflammation.


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