Title of article
Identification of long chain alkylidenemalonates as novel small molecule modulators of histone acetyltransferases
Author/Authors
Gianluca Sbardella، نويسنده , , Sabrina Castellano، نويسنده , , Caterina Vicidomini، نويسنده , , Dante Rotili، نويسنده , , Angela Nebbioso، نويسنده , , Marco Miceli، نويسنده , , Lucia Altucci، نويسنده , , Antonello Mai، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2008
Pages
5
From page
2788
To page
2792
Abstract
Pentadecylidenemalonate 1b, a simplified analogue of anacardic acid, was identified as the first mixed activator/inhibitor of histone acetyltransferases (HATs). It potentiates PCAF HAT activity while inhibiting those of p300/CBP and recombinant CBP. The remarkable apoptotic effect together with the ability to selectively acetylate histone versus non-histone substrates appoint 1b as a lead for the development of anticancer drugs.
Keywords
Epigenetics , HAT , Histone acetyltransferase modulators , Antitumor agents , Anacardic acid
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2008
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
799447
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