The inside cover picture shows the modulation of lysine acetyltransferase (KAT) activity by SPV106 (yellow). By manipulating the structural features of SPV106, different activity profiles—from pure PCAF (top left) activator, pan inhibitor, or mixed PCAF activator/p300 (bottom right) inhibitor—were obtained. The reported compounds represent useful chemical tools for mechanistic studies of histone H3 (lime) or H4 (orange) acetylation (Ac groups shown as purple spheres) and its implications in physiological and pathological processes. For more details, see the Full Paper by Alessandra Tosco, Gianluca Sbardella et al. on p. 144 ff.
Inside Cover: 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 (ChemMedChem 1/2015)
CASTELLANO, Sabrina;MILITE, CIRO;FEOLI, ALESSANDRA;VIVIANO, MONICA;NOVELLINO, Ettore;TOSCO, ALESSANDRA;SBARDELLA, Gianluca
2015-01-01
Abstract
The inside cover picture shows the modulation of lysine acetyltransferase (KAT) activity by SPV106 (yellow). By manipulating the structural features of SPV106, different activity profiles—from pure PCAF (top left) activator, pan inhibitor, or mixed PCAF activator/p300 (bottom right) inhibitor—were obtained. The reported compounds represent useful chemical tools for mechanistic studies of histone H3 (lime) or H4 (orange) acetylation (Ac groups shown as purple spheres) and its implications in physiological and pathological processes. For more details, see the Full Paper by Alessandra Tosco, Gianluca Sbardella et al. on p. 144 ff.File in questo prodotto:
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