| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1376540 | Bioorganic & Medicinal Chemistry Letters | 2008 | 5 Pages |
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.
Graphical abstractPentadecylidenemalonate 1b is the first histone acetyltransferases (HAT) modulator able to potentiate PCAF (GNAT family) activity while inhibiting that of CBP (p300/CBP family).Figure optionsDownload full-size imageDownload as PowerPoint slide
Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Gianluca Sbardella, Sabrina Castellano, Caterina Vicidomini, Dante Rotili, Angela Nebbioso, Marco Miceli, Lucia Altucci, Antonello Mai,