Selective inhibition of EZH2 and EZH1 enzymatic activity by a small molecule suppresses MLL-rearranged leukemia

Author:

Xu Bowen12,On Doan M.12,Ma Anqi3,Parton Trevor2,Konze Kyle D.3,Pattenden Samantha G.4,Allison David F.12,Cai Ling12,Rockowitz Shira56,Liu Shichong7,Liu Ying8,Li Fengling9,Vedadi Masoud9,Frye Stephen V.24,Garcia Benjamin A.7,Zheng Deyou56,Jin Jian3,Wang Gang Greg12ORCID

Affiliation:

1. Department of Biochemistry and Biophysics, and

2. Lineberger Comprehensive Cancer Center, University of North Carolina at Chapel Hill, Chapel Hill, NC;

3. Department of Structural and Chemical Biology, Icahn School of Medicine at Mount Sinai, New York, NY;

4. Center for Integrative Chemical Biology and Drug Discovery, University of North Carolina at Chapel Hill, Chapel Hill, NC;

5. Department of Genetics, and

6. Departments of Neurology and Neuroscience, Albert Einstein College of Medicine, Bronx, NY;

7. Epigenetics Program, Department of Biochemistry and Biophysics, Perelman School of Medicine, University of Pennsylvania, Philadelphia, PA;

8. Ansary Stem Cell Institute and Department of Genetic Medicine, Weill Cornell Medical College, New York, NY; and

9. Structural Genomics Consortium, University of Toronto, Toronto, ON, Canada

Abstract

Key Points We characterize active vs inactive analog compounds suitable for inhibition of both PRC2-EZH2 and PRC2-EZH1 ex vivo and in vivo. This study is the first to show oral delivery of an EZH2 and EZH1 dual inhibitor as promising therapeutics for MLL-rearranged leukemia.

Publisher

American Society of Hematology

Subject

Cell Biology,Hematology,Immunology,Biochemistry

全球学者库

1.学者识别学者识别

2.学术分析学术分析

3.人才评估人才评估

"全球学者库"是以全球学者为主线,采集、加工和组织学术论文而形成的新型学术文献查询和分析系统,可以对全球学者进行文献检索和人才价值评估。用户可以通过关注某些学科领域的顶尖人物而持续追踪该领域的学科进展和研究前沿。经过近期的数据扩容,当前全球学者库共收录了国内外主流学术期刊6万余种,收集的期刊论文及会议论文总量共计约1.5亿篇,并以每天添加12000余篇中外论文的速度递增。我们也可以为用户提供个性化、定制化的学者数据。欢迎来电咨询!咨询电话:010-8811{复制后删除}0370

www.globalauthorid.com

TOP

Copyright © 2019-2023 北京同舟云网络信息技术有限公司
京公网安备11010802033243号  京ICP备18003416号-3