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