Nature Communications (Dec 2019)
Discovery of a chemical probe for PRDM9
- Abdellah Allali-Hassani,
- Magdalena M. Szewczyk,
- Danton Ivanochko,
- Shawna L. Organ,
- Jabez Bok,
- Jessica Sook Yuin Ho,
- Florence P. H. Gay,
- Fengling Li,
- Levi Blazer,
- Mohammad S. Eram,
- Levon Halabelian,
- David Dilworth,
- Genna M. Luciani,
- Evelyne Lima-Fernandes,
- Qin Wu,
- Peter Loppnau,
- Nathan Palmer,
- S. Zakiah A. Talib,
- Peter J. Brown,
- Matthieu Schapira,
- Philipp Kaldis,
- Ronan C. O’Hagan,
- Ernesto Guccione,
- Dalia Barsyte-Lovejoy,
- Cheryl H. Arrowsmith,
- John M. Sanders,
- Solomon D. Kattar,
- D. Jonathan Bennett,
- Benjamin Nicholson,
- Masoud Vedadi
Affiliations
- Abdellah Allali-Hassani
- Structural Genomics Consortium, University of Toronto
- Magdalena M. Szewczyk
- Structural Genomics Consortium, University of Toronto
- Danton Ivanochko
- Structural Genomics Consortium, University of Toronto
- Shawna L. Organ
- Structural Genomics Consortium, University of Toronto
- Jabez Bok
- Institute of Molecular and Cell Biology (IMCB), Agency for Science, Technology and Research (A*STAR)
- Jessica Sook Yuin Ho
- Institute of Molecular and Cell Biology (IMCB), Agency for Science, Technology and Research (A*STAR)
- Florence P. H. Gay
- Institute of Molecular and Cell Biology (IMCB), Agency for Science, Technology and Research (A*STAR)
- Fengling Li
- Structural Genomics Consortium, University of Toronto
- Levi Blazer
- Structural Genomics Consortium, University of Toronto
- Mohammad S. Eram
- Structural Genomics Consortium, University of Toronto
- Levon Halabelian
- Structural Genomics Consortium, University of Toronto
- David Dilworth
- Structural Genomics Consortium, University of Toronto
- Genna M. Luciani
- Structural Genomics Consortium, University of Toronto
- Evelyne Lima-Fernandes
- Structural Genomics Consortium, University of Toronto
- Qin Wu
- Structural Genomics Consortium, University of Toronto
- Peter Loppnau
- Structural Genomics Consortium, University of Toronto
- Nathan Palmer
- Institute of Molecular and Cell Biology (IMCB), Agency for Science, Technology and Research (A*STAR)
- S. Zakiah A. Talib
- Institute of Molecular and Cell Biology (IMCB), Agency for Science, Technology and Research (A*STAR)
- Peter J. Brown
- Structural Genomics Consortium, University of Toronto
- Matthieu Schapira
- Structural Genomics Consortium, University of Toronto
- Philipp Kaldis
- Institute of Molecular and Cell Biology (IMCB), Agency for Science, Technology and Research (A*STAR)
- Ronan C. O’Hagan
- Merck & Co., Inc.
- Ernesto Guccione
- Institute of Molecular and Cell Biology (IMCB), Agency for Science, Technology and Research (A*STAR)
- Dalia Barsyte-Lovejoy
- Structural Genomics Consortium, University of Toronto
- Cheryl H. Arrowsmith
- Structural Genomics Consortium, University of Toronto
- John M. Sanders
- Merck & Co., Inc.
- Solomon D. Kattar
- Merck & Co., Inc.
- D. Jonathan Bennett
- Merck & Co., Inc.
- Benjamin Nicholson
- Merck & Co., Inc.
- Masoud Vedadi
- Structural Genomics Consortium, University of Toronto
- DOI
- https://doi.org/10.1038/s41467-019-13652-x
- Journal volume & issue
-
Vol. 10,
no. 1
pp. 1 – 11
Abstract
PRDM9 is a PR domain containing histone methyl transferase which expression is normally restricted to the germline that has also been linked to a number of somatic cancers. Here the authors describe the identification of a small molecule that selectivity inhibits the methyltransferase activity of PRDM9 in biochemical and cellular assays
