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Table 1 Binding affinities of different BH3 peptides to the three major anti-apoptotic Bcl-2 family proteins

From: Optimization and validation of mitochondria-based functional assay as a useful tool to identify BH3-like molecules selectively targeting anti-apoptotic Bcl-2 proteins

 

SPR

FP assay

BH3 peptide

Bcl-2

Bcl-xL

Mcl-1

Bcl-2

Bcl-xL

Mcl-1

IC50[nM] ± SD

IC50[nM] ± SD

IC50[nM] ± SD

Ki[nM] ± SD

Ki[nM] ± SD

Ki[nM] ± SD

Bid

51.21 ± 0.42

5.86 ± 1.81

60.11 ± 16.8

11.2 ± 1.4

8.8 ± 1.5

6.0 ± 3.3

Bad

4.37 ± 0.4

8.64 ± 7.49

>30000

7.1 ± 0.7

3.2 ± 0.4

>20000

Bim

1.26 ± 0.09

1.42 ± 0.07

1.33 ± 0.06

≤1

≤1

≤1

Noxa

>30000

>30000

51.0 ± 13.6

>10000

>10000

97 ± 7.7

  1. BH3 peptides were screened for their binding affinities to the three anti-apoptotic Bcl-2 family proteins using surface plasmon resonance and fluorescence polarization methods, as described in the Methods. Results are representative of at least three independent experiments.
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BMC Biotechnology

ISSN: 1472-6750

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