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Ma A, Yu W, Xiong Y, et al. Structure-activity relationship studies of SETD8 inhibitors. Medchemcomm. 2014;5(12):1892-1898doi: 10.1039/C4MD00317A.
Ma, A., Yu, W., Xiong, Y., Butler, K. V., Brown, P. J., & Jin, J. (2014). Structure-activity relationship studies of SETD8 inhibitors. MedChemComm, 5(12), 1892-1898. https://doi.org/10.1039/C4MD00317A
Ma, Anqi, et al. "Structure-activity relationship studies of SETD8 inhibitors." MedChemComm vol. 5,12 (2014): 1892-1898. doi: https://doi.org/10.1039/C4MD00317A
Ma A, Yu W, Xiong Y, Butler KV, Brown PJ, Jin J. Structure-activity relationship studies of SETD8 inhibitors. Medchemcomm. 2014 Dec;5(12):1892-1898. doi: 10.1039/C4MD00317A. PMID: 25554733; PMCID: PMC4278651.
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Medchemcomm. 2014 Dec;5(12):1892-1898. doi: 10.1039/C4MD00317A.

Structure-activity relationship studies of SETD8 inhibitors.

MedChemComm

Anqi Ma, Wenyu Yu, Yan Xiong, Kyle V Butler, Peter J Brown, Jian Jin

Affiliations

  1. Department of Structural and Chemical Biology, Icahn School of Medicine at Mount Sinai, New York, NY, 10029, United States.
  2. Structural Genomics Consortium, University of Toronto, Toronto, Ontario, M5G 1L7, Canada.
  3. Department of Structural and Chemical Biology, Icahn School of Medicine at Mount Sinai, New York, NY, 10029, United States ; Department of Oncological Sciences, Icahn School of Medicine at Mount Sinai, New York, NY, 10029, United States ; Department of Pharmacology and Systems Therapeutics, Icahn School of Medicine at Mount Sinai, New York, NY, 10029, United States.

PMID: 25554733 PMCID: PMC4278651 DOI: 10.1039/C4MD00317A

Abstract

SETD8 (also known as SET8, PR-SET7, or KMT5A (lysine methyltransferase 5A)) is the only known lysine methyltransferase that catalyzes monomethylation of histone H4 lysine 20 (H4K20). In addition to H4K20, SETD8 monomethylates non-histone substrates such as the tumor suppressor p53 and proliferating cell nuclear antigen (PCNA). Because of its role in regulating diverse biological processes, SETD8 has been pursued as a potential therapeutic target. We recently reported the first substrate-competitive SETD8 inhibitor, UNC0379 (

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