Discovery of a Potent and Selective Targeted NSD2 Degrader for the Reduction of H3K36me2

Author:

Hanley Ronan P.1,Nie David Y.234,Tabor John R.1,Li Fengling2,Sobh Amin5,Xu Chenxi67,Barker Natalie K.8,Dilworth David2,Hajian Taraneh2,Gibson Elisa2ORCID,Szewczyk Magdalena M.2,Brown Peter J.2ORCID,Barsyte-Lovejoy Dalia29,Herring Laura E.8ORCID,Wang Gang Greg6710ORCID,Licht Jonathan D.5,Vedadi Masoud29ORCID,Arrowsmith Cheryl H.234ORCID,James Lindsey I.16ORCID

Affiliation:

1. 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

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

3. Princess Margaret Cancer Centre, University Health Network, Toronto, Ontario M5G 1L7, Canada

4. Department of Medical Biophysics, University of Toronto, Toronto, Ontario M5G 1L7, Canada

5. University of Florida Health Cancer Center, The University of Florida Cancer and Genetics Research Complex, Gainesville, Florida 32610, United States

6. Lineberger Comprehensive Cancer Center, University of North Carolina at Chapel Hill School of Medicine, Chapel Hill, North Carolina 27599, United States

7. Department of Biochemistry and Biophysics, University of North Carolina at Chapel Hill School of Medicine, Chapel Hill, North Carolina 27599, United States

8. UNC Proteomics Core Facility, Department of Pharmacology, University of North Carolina at Chapel Hill, Chapel Hill, North Carolina 27599, United States

9. Department of Pharmacology and Toxicology, University of Toronto, Toronto, Ontario M5S 1A8, Canada

10. Department of Pharmacology, University of North Carolina at Chapel Hill School of Medicine, Chapel Hill, North Carolina 27599, United States

Funder

National Science Foundation

Government of Canada

U.S. Department of Health and Human Services

American Cancer Society

Leukemia and Lymphoma Society

Princess Margaret Cancer Foundation

Structural Genomics Consortium

Publisher

American Chemical Society (ACS)

Subject

Colloid and Surface Chemistry,Biochemistry,General Chemistry,Catalysis

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