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:
Sep. 17, 2019

Filed:

Nov. 30, 2017
Applicant:

The University of Chicago, Chicago, IL (US);

Inventors:

Bryan C. Dickinson, Chicago, IL (US);

Rahul S. Kathayat, Chicago, IL (US);

Michael W. Beck, Chicago, IL (US);

Assignee:

The University of Chicago, Chicago, IL (US);

Attorney:
Primary Examiner:
Int. Cl.
CPC ...
C07D 493/10 (2006.01); A61K 38/05 (2006.01); A61K 31/35 (2006.01); A61K 31/365 (2006.01); C07K 5/062 (2006.01); A61K 31/4375 (2006.01); C07K 5/068 (2006.01); A61K 31/498 (2006.01);
U.S. Cl.
CPC ...
A61K 38/05 (2013.01); A61K 31/35 (2013.01); A61K 31/365 (2013.01); A61K 31/4375 (2013.01); A61K 31/498 (2013.01); C07D 493/10 (2013.01); C07K 5/0606 (2013.01); C07K 5/06086 (2013.01);
Abstract

Synthetic probes for detecting the activity of enzymes that catalyze reactions of post-translationally modified cysteine residues are described. The probes include 'turn-on' probes that include a carbamate linkage that is cleaved via an intramolecular reaction with a free thiol produced by an enzyme catalyzed activity. The probes also include ratiometric, Michael addition-based probes that respond to enzymatic activity by a change in structure that results in a change in fluorescence properties. Methods of using the probes to detect enzymatic activity and disease are described. For example, the probes can be used to detect enzymatic activity in a variety of samples, including live cells and heterogeneous tissues. In addition, prodrugs that can be activated by enzymes that catalyze reactions of post-translationally modified cysteine residues and methods of using the prodrugs to treat disease are described.


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