Discovery of Small-Molecule Antagonists of the PWWP Domain of NSD2-Reference-Cited by-同舟云学术

Discovery of Small-Molecule Antagonists of the PWWP Domain of NSD2

Published:2021-02-01 Issue:3 Volume:64 Page:1584-1592
ISSN:0022-2623
Container-title:Journal of Medicinal Chemistry
language:en
Short-container-title:J. Med. Chem.

Author:

Ferreira de Freitas Renato¹,Liu Yanli¹,Szewczyk Magdalena M.¹,Mehta Naimee²,Li Fengling¹,McLeod David³,Zepeda-Velázquez Carlos³,Dilworth David¹,Hanley Ronan P.²,Gibson Elisa¹,Brown Peter J.¹,Al-Awar Rima³,James Lindsey I.²^ORCID,Arrowsmith Cheryl H.¹⁴^ORCID,Barsyte-Lovejoy Dalia¹⁵,Min Jinrong¹⁶,Vedadi Masoud¹⁵,Schapira Matthieu¹⁵^ORCID,Allali-Hassani Abdellah¹

Affiliation:

1. Structural Genomics Consortium, University of Toronto, Toronto, Ontario M5G 1L7, Canada

2. Center for Integrative Chemical Biology and Drug Discovery, Division of Chemical Biology and Medicinal Chemistry, UNC Eshelman School of Pharmacy, University of North Carolina at Chapel Hill, Chapel Hill, North Carolina 27599, United States

3. Drug Discovery Program, Ontario Institute for Cancer Research, Toronto, Ontario M5G 0A3, Canada

4. Princess Margaret Cancer Centre and Department of Medical Biophysics, University of Toronto, Toronto, Ontario M5G 2M9, Canada

5. Department of Pharmacology & Toxicology, University of Toronto, Toronto, Ontario M5S 1A8, Canada

6. Department of Physiology, University of Toronto, Toronto, Ontario M5S 1A8, Canada

Funder

National Cancer Institute

Natural Sciences and Engineering Research Council of Canada

Publisher

American Chemical Society (ACS)

Subject

Drug Discovery,Molecular Medicine

Link

https://pubs.acs.org/doi/pdf/10.1021/acs.jmedchem.0c01768

Reference26 articles.

1. NSD2 Links Dimethylation of Histone H3 at Lysine 36 to Oncogenic Programming

2. The NSD family of protein methyltransferases in human cancer

3. In multiple myeloma, t(4;14)(p16;q32) is an adverse prognostic factor irrespective of FGFR3 expression

4. Global chromatin profiling reveals NSD2 mutations in pediatric acute lymphoblastic leukemia

5. Point mutation E1099K in MMSET/NSD2 enhances its methyltranferase activity and leads to altered global chromatin methylation in lymphoid malignancies

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