| Target Validation Information | |||||
|---|---|---|---|---|---|
| Target ID | T72835 | ||||
| Target Name | E-selectin | ||||
| Target Type | Clinical Trial |
||||
| Drug Potency against Target | Bimosiamose | Drug Info | IC50 = 70 uMol/L | [552507] | |
| Action against Disease Model | Bimosiamose | An sLex mimetic bimosiamose (TBC-1269) has an IC50 of 70 uMinan HL-60 cell binding assay to P-selectin. | [552754] | Drug Info | |
| The Effect of Target Knockout, Knockdown or Genetic Variations | We examined pulmonary and cutaneous allergic inflammatory responses and silica-induced nonallergic lung inflammation and fibrosis in wild-type and P- and E-selectin-deficient (P/E-/-) double knockout mice. Allergen-sensitized wild-type and P/E-/- double knockout mice were challenged either intradermally or via the airways to induce allergic responses in the skin or lung, respectively. Other animals were subjected to intranasal silica administration to induce a nonallergic lung inflammatory/fibrotic response.The P/E-/- mice exhibited significantly reduced allergic inflammation in the skin and lung. Allergic late-phase ear swelling and allergic lung airway hyperresponsiveness were also significantly attenuated in the P/E-/- mice compared with identically treated wild-type animals. In contrast, pulmonary inflammation and fibrosis induced by intranasal administration of silica particles resulted in a more severe phenotype in the P/E-/- mice. | [552754] | |||
| References | |||||
| Ref 552754 | Characterization of the novel P-selectin inhibitor PSI-697 [2-(4-chlorobenzyl)-3-hydroxy-7,8,9,10-tetrahydrobenzo[h] quinoline-4-carboxylic acid] in vitro and in rodent models of vascular inflammation and thrombosis. J Pharmacol Exp Ther. 2008 Feb;324(2):497-506. Epub 2007 Nov 16. | ||||
| Ref 552507 | Selectin antagonists : therapeutic potential in asthma and COPD. Treat Respir Med. 2005;4(2):85-94. | ||||
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