Target Validation Information
Target ID T57011
Target Name mRNA of Intercellularadhesion molecule-1
Target Type
Successful
Drug Potency against Target A-286982 Drug Info IC50 = 44 nM [531049]
Action against Disease Model Alicaforsen Immunotoxicity studies were performed in mice to elucidate the nature of effects of ISIS 2302 on mammalian immune function. ISIS 2302 (1, 5, 20, or 50 mg/kg/dose) was administered intravenously every other day for 27 days. The pro-inflammatory properties of the drug were observed at doses > or = 20 mg/kg. A dose-dependent increase in spleen weight was associated with increased absolute splenocyte and B-lymphocyte counts after the 50 mg/kg/dose regimen. The mitogenic response of B-lymphocytes to bacterial lipopolysaccharide was increased after the 20 and 50 mg/kg/doses but antibody-forming cell activities remained unchanged. Total ser uM IgG concentration was decreased after the 20 and 50 mg/kg/dose regimens but IgM titers were unchanged. Increases in IL-6, IL-12, andMCP-1 as well as NK cell activity were observed after administration of 20 and 50 mg/kg/dose. Cytotoxic T-lymphocyte activity was decreased by the 50 mg/kg/dose regimen. Other changes in immune function were not observed in ISIS 2302-dosed mice [552876] Drug Info
The Effect of Target Knockout, Knockdown or Genetic Variations Genetic de?ciency of ICAM-1 signi?cantly attenuated myocardial necrosis in mice in association with reductions in myocardial neutrophil in?ltration, following both brief and extended periods of reperfusion. [552876]
References
Ref 552876Assessment of the effects of ISIS 2302, an anti-sense inhibitor of human ICAM-1, on cellular and humoral immunity in mice. J Immunotoxicol. 2006 Dec 1;3(4):199-211. doi: 10.1080/15476910601046538.
Ref 531049Bioorg Med Chem Lett. 2010 Sep 1;20(17):5269-73. Epub 2010 Jul 23.Discovery of tetrahydroisoquinoline (THIQ) derivatives as potent and orally bioavailable LFA-1/ICAM-1 antagonists.

If You Find Any Error in Data or Bug in Web Service, Please Kindly Report It to Dr. Zhou and Dr. Zhang.