A New Assay Based on Fluorescence Resonance Energy Transfer to Determine the Binding Affinity of Bcl-x_L Inhibitors

Yu FENGDepartment of Molecular Pharmacology, Shanghai Institute of Materia Medica, Chinese Academy of Sciences

Xu SHENDepartment of Molecular Pharmacology, Shanghai Institute of Materia Medica, Chinese Academy of Sciences;School of Pharmacy, East China University of Science and Technology

Kaixian CHENCenter for Drug Design and Discovery, State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences

Hualiang JIANGCenter for Drug Design and Discovery, State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences;School of Pharmacy, East China University of Science and Technology

Dongxiang LIUDepartment of Molecular Pharmacology, Shanghai Institute of Materia Medica, Chinese Academy of Sciences

Abstract

We developed a new assay of Bcl-x_L inhibitors based on fluorescence resonance energy transfer that occurs between an AEDANS-labeled Bak-BH3 peptide and three tryptophans in the BH1 and BH2 domains of Bcl-x_L. The method can tolerate up to 5% DMSO, and it was validated with several Bcl-x_L inhibitors. It can be adapted to screen for compounds targeting other Bcl-2 family proteins.

Keywords

Reprints and Corporate Permissions

Please note: Selecting permissions does not provide access to the full text of the article, please see our help page How do I view content?

To request a reprint or corporate permissions for this article, please click on the relevant link below:

Order Reprints Request Corporate Permissions

Academic Permissions

Please note: Selecting permissions does not provide access to the full text of the article, please see our help page How do I view content?

Obtain permissions instantly via Rightslink by clicking on the button below:

Request Academic Permissions

If you are unable to obtain permissions via Rightslink, please complete and submit this Permissions form. For more information, please visit our Permissions help page.

A New Assay Based on Fluorescence Resonance Energy Transfer to Determine the Binding Affinity of Bcl-x_L Inhibitors

Information for

Open access

Opportunities

Help and information

A New Assay Based on Fluorescence Resonance Energy Transfer to Determine the Binding Affinity of Bcl-xL Inhibitors

Abstract

Reprints and Corporate Permissions

Academic Permissions

Related research

To cite this article:

Download citation

Information for

Open access

Opportunities

Help and information

Keep up to date

Your download is now in progress and you may close this window

Login or register to access this feature

A New Assay Based on Fluorescence Resonance Energy Transfer to Determine the Binding Affinity of Bcl-x_L Inhibitors