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Table 1 In vitro activity of AVX001, AVX002, and DHA in the mixed micelle cPLA2α enzyme assay

From: Cytosolic group IVA phospholipase A2 inhibitors, AVX001 and AVX002, ameliorate collagen-induced arthritis

Name

Structure

In vitro enzyme activity

GIVA cPLA2

GVIA iPLA2

GV sPLA2

GIVA cPLA2

vesicle assay

% Inhibita

XI(50)

% Inhibita

% Inhibita

IC50 (nM)b

AVX001

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90

0.0072 ± 0.0007

68

62

120 ± 58

AVX002

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93

0.0057 ± 0.001

88

68

126 ± 37

DHA

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8.9

ND

38

32

ND

  1. DHA Docosahexaenic acid, cPLA cytosolic phospholipase A2 protein, IC50 half maximal inhibitory concentration, ND not determined
  2. aMixed micelle enzyme in vitro assay: % inhibition at a 0.091 mol fraction of each inhibitor
  3. bVesicle enzyme in vitro data included for reference. Inhibitors were tested in the 0–3 μM range [11]
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Arthritis Research & Therapy

ISSN: 1478-6362

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