Table 1 Inhibition constants for bedaquiline and oligomycin.

From: Bedaquiline inhibits the yeast and human mitochondrial ATP synthases

IC50 (μM) ± SEM

ATP hydrolysis

ATP synthesis

Purified yeast F1Fo

Yeast SMP

Yeast mitochondria

BDQ

Oligomycin A

BDQ

Oligomycin A

BDQ

Oligomycin A

0.027 ± 0.0025

0.107 ± 0.0011

1.28 ± 0.25

1.1 ± 0.04

1.1 ± 0.07

0.1 ± 0.008

    

Human mitoplasts

    

0.66 ± 0.05

0.0054 ± 0.0006

  1. IC50 for ATP hydrolysis and ATP synthesis for BDQ and oligomycin on yeast and human ATP synthase. Cyanide sensitive ATP synthesis for yeast mitochondria was 51.3 ± 2.6 nmoles/ATP/min/mg protein and was inhibited 98% with oligomycin (1 μM). Cyanide sensitive ATP synthesis for human mitoplasts was 9.0 ± 0.6 nmoles/ATP/min/mg protein and was inhibited 98% with oligomycin (1.25 μM). Total ATP synthesis for yeast mitochondria was inhibited by 98.6% with 1.5 mM sodium cyanide and by 59.2% with human mitoplasts.
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