| Target Validation Information | |||||
|---|---|---|---|---|---|
| Target ID | T14065 | ||||
| Target Name | Integrin beta-7 | ||||
| Target Type | Successful |
||||
| Drug Potency against Target | TR-14035 | Drug Info | IC50 = 0.75 nM | [526159] | |
| Action against Disease Model | Vedolizmab | Vedoliz uMab inhibited high-affinity adhesion of alpha 4 beta 7-espressing RPMI8866 cells (Mn2+-activated) to MAdCAM-1 with a mean IC50 value of 0.058 ???0.024 ug/ml (0.39 ???0.16 nM; n = 6) | [552949] | Drug Info | |
| The Effect of Target Knockout, Knockdown or Genetic Variations | Wild-type (WT) (beta7+/+) and beta7 gene knockout (beta7-/-) C57BL/6 (H-2(b)) mice and SJL/J (H-2(s)) mice served as donors and recipients of allogeneic skin grafts. An anti-integrin beta7 subunit mAb (FIB504.64) was used to treat WT beta7+/+ C57BL/6 recipients of skin grafts from SJL/J mice.WT C57BL/6 recipients acutely rejected skin from SJL/J mice in 13 days. In contrast,the survival of SJL/J skin on either beta7-/- gene knockout or WT C57BL/6 recipients treated with anti-beta7 subunit mAb, was prolonged by 6 to 7 additional days (P<0.01). The survival of skin allografts from either beta7-/- or beta7+/+ C57BL/6 mice received by SJL/J recipients was not prolonged (P >0.05).Beta7 integrins contribute to skin graft rejection, in accord with their role in mediating the epidermotropism of T-cells during skin inflammation | [526159] | |||
| References | |||||
| Ref 526159 | Bioorg Med Chem Lett. 2001 Oct 22;11(20):2709-13.The discovery of sulfonylated dipeptides as potent VLA-4 antagonists. | ||||
| Ref 552949 | The binding specificity and selective antagonism of vedolizumab, an anti-alpha4beta7 integrin therapeutic antibody in development for inflammatory bowel diseases. J Pharmacol Exp Ther. 2009 Sep;330(3):864-75. doi: 10.1124/jpet.109.153973. Epub 2009 Jun 9. | ||||
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