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High-throughput fluorescence polarization assay to identify small molecule inhibitors of BRCT domains of breast cancer gene 1 by G.L. Lokesh; Aparna Rachamallu; G.D. Kishore Kumar; Amarnath Natarajan is a Biochemistry, Genetics and Molecular Biology article available to read on EtoBox.

What is High-throughput fluorescence polarization assay to identify small molecule inhibitors of BRCT domains of breast cancer gene 1 about?

The C-terminus region of the 1863 residue early onset of breast cancer gene 1 (BRCA1) nuclear protein contains a tandem globular carboxy terminus domain termed BRCT. The BRCT repeats in BRCA1 are phosphoserine- and/or phosphothreonine-specific binding modules. The interaction of the BRCT(BRCA1) domains with phosphorylated BRCA1-associated carboxyl terminal helicase (BACH1) is cell cycle regulated and is essential for DNA damage-induced checkpoint control during the transition from the G(2) phase to the M phase of the cell cycle. Development of a competitive, homogeneous, high-throughput fluorescence polarization (FP) assay to identify small molecule inhibitors of BRCT(BRCA1)-BACH1 interaction is reported here. The FP assay was used for measuring binding affinities and inhibition constants of BACH1 peptides and small molecule inhibitors of BRCT(BRCA1) domains, respectively. A fluorescently labeled wild-type BACH1 decapeptide (BDP1) containing the critical phosphoserine, a phenylalanine at (P+3), and a GST-BRCT fusion protein were used to establish the FP assay. BDP1 has a dissociation constant (K(d)) of 1.58+/-0.01microM and a dynamic range (DeltamP) of 164.9+/-1.9. The assay tolera

Who reads High-throughput fluorescence polarization assay to identify small molecule inhibitors of BRCT domains of breast cancer gene 1?

Author

G.L. Lokesh; Aparna Rachamallu; G.D. Kishore Kumar; Amarnath Natarajan

Publisher

Elsevier Science; Elsevier ; Elsevier Inc.; Elsevier BV (ISSN 0003-2697)

Published

2006

Language

EN

Field

Biochemistry, Genetics and Molecular Biology (Life Sciences)