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Comment
. 2020 Jun 8;37(6):764-766.
doi: 10.1016/j.ccell.2020.05.016.

Selective Targeting of Different Bromodomains by Small Molecules

Jun Qi  1 , Yang Shi  2
Affiliations
Free article
Comment

Selective Targeting of Different Bromodomains by Small Molecules

Jun Qi et al. Cancer Cell. .
Free article

Abstract

Two papers, published in Science and Nature, report inhibitiors selectively targeting distinct bromodomains of BET proteins. These advanced chemical tools facilitate functional understanding of epigenetic regulators in normal and disease states and enable development of new medicine potentially with lower toxicity.

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Conflict of interest statement

Declaration of Interests J.Q. is a scientific co-founder and consultant for Epiphanes and is a shareholder of Zentalis. Y.S. is a scientific co-founder and equity holder of Constellation Pharmaceuticals and Athelas Therapeutics, an equity holder of Imago Biosciences, and a consultant for Active Motif.

Comment on

  • Selective inhibition of the BD2 bromodomain of BET proteins in prostate cancer.
    Faivre EJ, McDaniel KF, Albert DH, Mantena SR, Plotnik JP, Wilcox D, Zhang L, Bui MH, Sheppard GS, Wang L, Sehgal V, Lin X, Huang X, Lu X, Uziel T, Hessler P, Lam LT, Bellin RJ, Mehta G, Fidanze S, Pratt JK, Liu D, Hasvold LA, Sun C, Panchal SC, Nicolette JJ, Fossey SL, Park CH, Longenecker K, Bigelow L, Torrent M, Rosenberg SH, Kati WM, Shen Y. Faivre EJ, et al. Nature. 2020 Feb;578(7794):306-310. doi: 10.1038/s41586-020-1930-8. Epub 2020 Jan 22. Nature. 2020. PMID: 31969702
  • Selective targeting of BD1 and BD2 of the BET proteins in cancer and immunoinflammation.
    Gilan O, Rioja I, Knezevic K, Bell MJ, Yeung MM, Harker NR, Lam EYN, Chung CW, Bamborough P, Petretich M, Urh M, Atkinson SJ, Bassil AK, Roberts EJ, Vassiliadis D, Burr ML, Preston AGS, Wellaway C, Werner T, Gray JR, Michon AM, Gobbetti T, Kumar V, Soden PE, Haynes A, Vappiani J, Tough DF, Taylor S, Dawson SJ, Bantscheff M, Lindon M, Drewes G, Demont EH, Daniels DL, Grandi P, Prinjha RK, Dawson MA. Gilan O, et al. Science. 2020 Apr 24;368(6489):387-394. doi: 10.1126/science.aaz8455. Epub 2020 Mar 19. Science. 2020. PMID: 32193360 Free PMC article.

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