Detection of Enzyme Activity and Inhibition during Studies in Solution, In Vitro and In Vivo with CatalyCEST MRI.

ABSTRACT:

Purpose

The detection of enzyme activities and evaluation of enzyme inhibitors have been challenging with magnetic resonance imaging (MRI). To address this need, we have developed a diamagnetic, nonmetallic contrast agent and a protocol known as catalyCEST MRI that uses chemical exchange saturation transfer (CEST) to detect enzyme activity as well as enzyme inhibition.

Procedures

We synthesized a diamagnetic MRI contrast agent that has enzyme responsive and enzyme unresponsive CEST signals. We tested the ability of this agent to detect the activity of kallikrein 6 (KLK6) in biochemical solutions, in vitro and in vivo, with and without a KLK6 inhibitor.

Results

The agent detected KLK6 activity in solution and also detected KLK6 inhibition by antithrombin III. KLK6 acti

SUBMITTER: Sinharay S 

PROVIDER: S-EPMC6010181 | biostudies-literature | 2018 Apr

REPOSITORIES: biostudies-literature