| 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 552876 | Assessment 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 531049 | Bioorg 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. | ||||
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