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Novel Activity-Based Probes for TET Enzymatic Activity

Description:

Method and probes for detecting and quantifying epigenetic regulator TET enzymatic activity; this method can be used for high throughput screening of TET inhibitors or activators.

 

Inventor

Rahul Kohli, M.D., Ph.D.

 

Problem

Ten eleven translocation (TET) enzymes are important epigenetic regulators.  TETs catalyze the step-wise oxidation of 5-methylcytosine (5mC) to 5-hydroxymethylcytosine (5hmC), 5-formylcytosine (5fC) and 5-carboxylcytosine (5caC) in genomic DNA, promoting DNA demethylation and gene expression changes.  TET enzymes are therefore critical in normal development and in cancer, however, assessing TET activity remains experimentally challenging.  Currently available commercial kits are indirect assays of TET activity, limited in scope, laborious, and cannot be used in vivo

 

Solution

Dr. Kohli and his team at Penn have developed an improved enzyme assay for TET.  Dr. Kohli has engineered specific probes for TETs that yield unique reaction intermediates; these intermediates can be easily detected and their abundance is a direct measurement of TET activity.  This method presents a novel, facile, and valuable tool for evaluating TET activity.

 

Applications

•       Measure TET enzymatic activity directly in vitro or in vivo

•       High throughput screen for TET modulators, inhibitors or activators

 

Advantages

•       Direct measurement of TET enzymatic activity

•       Straightforward methodology

•       Can be used to detect TET1, TET2, and TET3 activity

•       Can be used to determine when and where specific TET enzymes are active in particular cellular niches

 

Stage of Development

•       In vitro data

 

Desired Partnerships

1.       License

2.       Co-development

 

Docket #: 18-8629


Patent Information:
For Information, Contact:
Jessica Casciano
University of Pennsylvania
casciano@upenn.edu
Inventors:
Rahul Kohli
Keywords: