18F-Labeled PET Probe Targeting Enhancer of Zeste Homologue 2 (EZH2) for Cancer Imaging

Authors

Lihai Yu, London Regional Cancer Program
Nikola Despotovic, Western University
Michael S Kovacs, Western University
Christopher L Pin, Western University
Leonard G Luyt, London Regional Cancer Program

Document Type

Article

Publication Date

3-2019

Journal

ACS Medical Chemistry Letters

Volume

10

Issue

3

First Page

334

Last Page

340

URL with Digital Object Identifier

https://doi.org/10.1021/acsmedchemlett.8b00613

Abstract

The enzyme enhancer of zeste homologue 2 (EZH2) plays a catalytic role in histone methylation (H3K27me3), one of the epigenetic modifications that is dysregulated in cancer. The development of a positron emission tomography (PET) imaging agent targeting EZH2 has the potential to provide a method of stratifying patients for epigenetic therapies. In this study, we designed and synthesized a series of fluoroethyl analogs based upon the structure of EZH2 inhibitors UNC1999 and EPZ6438. Among the candidate compounds,