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- W2079116818 endingPage "157" @default.
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- W2079116818 abstract "Abstract Dysregulation of the activity of lysine acetyltransferases (KATs) is related to a variety of diseases and/or pathological cellular states; however, their role remains unclear. Therefore, the development of selective modulators of these enzymes is of paramount importance, because these molecules could be invaluable tools for assessing the importance of KATs in several pathologies. We recently found that diethyl pentadecylidenemalonate (SPV106) possesses a previously unobserved inhibitor/activator activity profile against protein acetyltransferases. Herein, we report that manipulation of the carbonyl functions of a series of analogues of SPV106 yielded different activity profiles against KAT2B and KAT3B (pure KAT2B activator, pan‐inhibitor, or mixed KAT2B activator/KAT3B inhibitor). Among the novel compounds, a few derivatives may be useful chemical tools for studying the mechanism of lysine acetylation and its implications in physiological and/or pathological processes." @default.
- W2079116818 created "2016-06-24" @default.
- W2079116818 creator A5012839091 @default.
- W2079116818 creator A5017825556 @default.
- W2079116818 creator A5024040984 @default.
- W2079116818 creator A5040940946 @default.
- W2079116818 creator A5041402506 @default.
- W2079116818 creator A5059757863 @default.
- W2079116818 creator A5062146508 @default.
- W2079116818 creator A5062240357 @default.
- W2079116818 date "2014-10-21" @default.
- W2079116818 modified "2023-10-16" @default.
- W2079116818 title "Identification of Structural Features of 2-Alkylidene-1,3-Dicarbonyl Derivatives that Induce Inhibition and/or Activation of Histone Acetyltransferases KAT3B/p300 and KAT2B/PCAF" @default.
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