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Screening and characterization of new histone deacetylase inhibitors (hdaci) using bret based assay

Using BRET technology, we designed a method to measure histone acetylation in living cells. Cells are transfected with a vector coding for a bromodomain fused to renilla luciferase (Rluc-BrD) and with a vector coding for histone H3 fused to yellow fluorescent protein (YFP). In the presence of HDACi, Rluc-BrD and YFP-histone H3 interact and generate an increase of BRET signal.

Interest / Relevance: Since few years, HDACi appear as promising molecules for the treatment of numerous diseases. However, These molecules are toxic and less selective. Development of new compounds will improved these issues as well as their therapeutical efficiency.

Keywords: BRET , screening , HDAC , inhibitors

Scientist's name: Christophe BLANQUART

Publications:

Blanquart C Francois M Charrier C Bertrand P Gregoire M. Pharmacological characterization of histone deacetylase inhibitor and tumor cell-growth inhibition properties of new benzofuranone compounds. Curr Cancer Drug Targets. 2011;11:919?928.

Reference:

RT00422

Type of research tool: Know How

Therapy area(1): Central Nervous System

Therapy area(2): Oncology

Uses(1): Academic Research

Uses(2): Proof of concept in vitro

Uses(3): Industry Research (screening, tox.studies, bioreactor, ...)

Inserm Transfert
Research Tools

Accessible for: Fee-for-service research, Collaboration, Training / Know-How License

Equipment available: Mithras LB 940 Multimode Microplate Reader (Berthold Technologies)

Samples/Models available: Aliquots of expression vectors stored at -20°c.

Rare disease: No

Last update: 12/06/2024

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