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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.