A new assay based on fluorescence resonance energy transfer to determine the binding affinity of Bcl-xL inhibitors

We developed a new assay of Bcl-xsub(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-xsub(L). The method can tolerate up to 5% DMSO, and it was validated with several Bcl-xsub(...

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Veröffentlicht in:	Bioscience, biotechnology, and biochemistry biotechnology, and biochemistry, 2008-07, Vol.72 (7), p.1936-1939
Hauptverfasser:	Feng, Y.(Chinese Academy of Sciences, Shanghai (China). Shanghai Inst. of Materia Medica), Shen, X, Chen, K, Jiang, H, Liu, D
Format:	Artikel
Sprache:	eng
Schlagworte:	AMINO ACID SEQUENCES APOPTOSE APOPTOSIS Bcl-x bcl-X Protein - antagonists & inhibitors binding assay Binding Sites Biological and medical sciences CHEMICAL COMPOUNDS COMPOSE CHIMIQUE COMPUESTOS QUIMICOS ENZYME INHIBITORS ESPECTROSCOPIA RMN FLUORESCENCE fluorescence resonance energy transfer Fluorescence Resonance Energy Transfer - methods FLUORESCENCIA Fluorescent Dyes Fundamental and applied biological sciences. Psychology INHIBIDORES DE ENZIMAS INHIBITEUR D'ENZYME inhibitor Molecular Probe Techniques NMR SPECTROSCOPY Peptides Protein Binding Protein Structure, Tertiary PROTEINAS PROTEINE PROTEINS SECUENCIAS DE AMINOACIDOS SEQUENCE D'ACIDES AMINES SPECTROSCOPIE RMN TRIPTOFANO TRYPTOPHAN TRYPTOPHANE
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Zusammenfassung:	We developed a new assay of Bcl-xsub(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-xsub(L). The method can tolerate up to 5% DMSO, and it was validated with several Bcl-xsub(L) inhibitors. It can be adapted to screen for compounds targeting other Bcl-2 family proteins.
ISSN:	0916-8451 1347-6947
DOI:	10.1271/bbb.70735