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Modulation of the activity of histone acetyltransferases by long chain alkylidenemalonates (LoCAMs)
- Source :
- Bioorganic & medicinal chemistry, 19 (2011): 3690–3701. doi:10.1016/j.bmc.2011.01.013, info:cnr-pdr/source/autori:Ciro Milite (a), Sabrina Castellano (a), Rosaria Benedetti (b, c),Alessandra Tosco (a),Carmen Ciliberti(a),Caterina Vicidomini (a),Ludovic Boully (a),Gianluigi Franci (b, d), Lucia Altucci (b, d), Antonello Mai (e), Gianluca Sbardella (a)/titolo:Modulation of the activity of histone acetyltransferases by long chain alkylidenemalonates (LoCAMs)/doi:10.1016%2Fj.bmc.2011.01.013/rivista:Bioorganic & medicinal chemistry (Print)/anno:2011/pagina_da:3690/pagina_a:3701/intervallo_pagine:3690–3701/volume:19, Bioorganic & Medicinal Chemistry
- Publication Year :
- 2011
- Publisher :
- Elsevier Science Limited:Oxford Fulfillment Center, PO Box 800, Kidlington Oxford OX5 1DX United Kingdom:011 44 1865 843000, 011 44 1865 843699, EMAIL: asianfo@elsevier.com, tcb@elsevier.co.UK, INTERNET: http://www.elsevier.com, http://www.elsevier.com/locate/shpsa/, Fax: 011 44 1865 843010, 2011.
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Abstract
- A novel class of KAT modulators (long chain alkylidenemalonates, LoCAMs) has been identified. Variations of the alkyl chain length can change the activity profile from inhibition of both KAT3A/KAT2B (as derivative 2a) to the peculiar profile of pentadecylidenemalonate 1b, the first activator/inhibitor of histone acetyltransferases. Together with the powerful apoptotic effect (particularly notable if considering that anacardic acid and other KAT inhibitors are not cell permeable) appoint them as valuable biological tools to understand the mechanisms of lysine acetyltransferases. (C) 2011 Elsevier Ltd. All rights reserved.
- Subjects :
- Lysine Acetyltransferases
Alkylation
Blotting, Western
Clinical Biochemistry
Pharmaceutical Science
Histone acetyltransferases modulators
Biochemistry
03 medical and health sciences
0302 clinical medicine
Cell Line, Tumor
Drug Discovery
Humans
Epigenetics
Enzyme Inhibitors
Molecular Biology
P300/CBP
PCAF activator
KAT
Histone Acetyltransferases
030304 developmental biology
chemistry.chemical_classification
0303 health sciences
biology
Activator (genetics)
Organic Chemistry
Biological activity
U937 Cells
Histone acetyltransferase
Malonates
Enzyme Activation
Enzyme
chemistry
Acyltransferases
030220 oncology & carcinogenesis
biology.protein
Molecular Medicine
p300/CBP
Subjects
Details
- Language :
- English
- Database :
- OpenAIRE
- Journal :
- Bioorganic & medicinal chemistry, 19 (2011): 3690–3701. doi:10.1016/j.bmc.2011.01.013, info:cnr-pdr/source/autori:Ciro Milite (a), Sabrina Castellano (a), Rosaria Benedetti (b, c),Alessandra Tosco (a),Carmen Ciliberti(a),Caterina Vicidomini (a),Ludovic Boully (a),Gianluigi Franci (b, d), Lucia Altucci (b, d), Antonello Mai (e), Gianluca Sbardella (a)/titolo:Modulation of the activity of histone acetyltransferases by long chain alkylidenemalonates (LoCAMs)/doi:10.1016%2Fj.bmc.2011.01.013/rivista:Bioorganic & medicinal chemistry (Print)/anno:2011/pagina_da:3690/pagina_a:3701/intervallo_pagine:3690–3701/volume:19, Bioorganic & Medicinal Chemistry
- Accession number :
- edsair.doi.dedup.....09d1f8d0acf0d1fa73d5f893653ea2e2
- Full Text :
- https://doi.org/10.1016/j.bmc.2011.01.013