Target Validation Information
Target ID T85616
Target Name Thioredoxin
Target Type
Clinical Trial
Drug Potency against Target PX-12 Drug Info Ki = 0.5 nM [552866]
Action against Disease Model PX-12 The disulfides inhibited the thioredoxin dependent proliferation of MCF-7 breast cancer cells with ICso values of 1.2 pM, respectively Based on previous studies PX-12 has IC50 value of about 1.2FM. Drug Info
The Effect of Target Knockout, Knockdown or Genetic Variations Mesangial cell apoptosis contributes to the pathogenesis of diabetic nephropathy. Here we show that thioredoxin interacting protein (TXNIP) is involved in high glucose (HG)-induced mouse mesangial cell (MMC) apoptosis. HG induced activation of apoptosis signal regulating kinase-1 (ASK1) in a time-dependent manner in MMCs. Treatment with antioxidant, tempol, or knockdown of TXNIP in MMCs reduced HG-mediated apoptosis, expression of cleaved caspase-3, Bax/Bcl-2 ratio and activation of ASK1. These data suggest that knockdown of TXNIP prevented HG-induced cell apoptosis and activation of ASK1 may be via reduction of oxidative stress in MMCs [552866]
References
Ref 552866Dopamine D5 receptors: a challenge to medicinal chemists. Mini Rev Med Chem. 2008 Sep;8(10):976-95.

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