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Identification of long chain alkylidenemalonates as novel small molecule modulators of histone acetyltransferases.
- Source :
-
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2008 May 01; Vol. 18 (9), pp. 2788-92. Date of Electronic Publication: 2008 Apr 11. - Publication Year :
- 2008
-
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.
- Subjects :
- Acetylation
Apoptosis physiology
Cell Cycle physiology
Humans
Models, Chemical
U937 Cells
p300-CBP Transcription Factors antagonists & inhibitors
Alkadienes chemistry
Antineoplastic Agents chemistry
Antineoplastic Agents pharmacology
Apoptosis drug effects
Cell Cycle drug effects
Enzyme Inhibitors chemistry
Enzyme Inhibitors pharmacology
Histone Acetyltransferases antagonists & inhibitors
Malonates chemistry
Subjects
Details
- Language :
- English
- ISSN :
- 1464-3405
- Volume :
- 18
- Issue :
- 9
- Database :
- MEDLINE
- Journal :
- Bioorganic & medicinal chemistry letters
- Publication Type :
- Academic Journal
- Accession number :
- 18434144
- Full Text :
- https://doi.org/10.1016/j.bmcl.2008.04.017