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Table 1 Screening of 50% inhibitory concentrations of proteasome inhibitors in P. falciparum laboratory strains 3D7, D10 and Dd2

From: Comprehensive study of proteasome inhibitors against Plasmodium falciparum laboratory strains and field isolates from Gabon

 

IC50 (nmol/L)a

Test compounds

3D7

D10

Dd2

1. Peptide proteasome inhibitors

   

   Epoxomicin

6.8

1.7

10.4

   YU101

24.5

17.0

13.8

   YU102

1740

4000

3006

   MG115

97.5

50.0

44.9

   MG132

22.4

33.2

17.3

   Z-L3-VS

16.4

n.d.

4.9

   Ada-Ahx3-L3-VS

300

n.d.

210

   Bortezomib

252

127

561

2. β-lactone

   

   Lactacystin

1490

1211

2553

3. Allosteric inhibitors

   

   Gliotoxin

2171

n.d.

1165

   PR11

n.i.

n.d.

n.i.

   PR39

n.i.

n.d.

n.i.

4. Comparator drugs

   

   Artesunate

0.5

2.5

0.9

   Chloroquine

8.3

5.0

176

  1. aValues are expressed as mean IC50 from two separate determinations against chloroquine-susceptible 3D7 and D10 and chloroquine-resistant Dd2 clones.
  2. n.d.assay not done
  3. n.i.no growth inhibition detectable