| Target Validation Information | |||||
|---|---|---|---|---|---|
| Target ID | T25703 | ||||
| Target Name | Heme oxygenase | ||||
| Target Type | Clinical Trial |
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| Drug Potency against Target | AZALANSTAT | Drug Info | IC50 = 5300 nM | [528712] | |
| Action against Disease Model | Stannsoporfin | Studies in vitro, in animal models, and in adult and newborn h uMans have demonstrated that certain tin(Sn)-porphyrins competitively inhibit the activity of heme oxygenase (the rate-limiting enzyme in heme catabolism), reduce production of bilirubin and can thereby substantially diminish plasma levels of the bile pigment | [553220] | Drug Info | |
| The Effect of Target Knockout, Knockdown or Genetic Variations | A link between HO-1 and iron homeostasis has been demonstrated in HO-1 knockout mice, which develop major hemosiderosis in solid organs such as liver and kidney. Moreover, genetic HO-1 deficiency causes a chronic inflammatory condition in these animals. As the liver plays a crucial role for the body's iron homeostasis (eg. via secretion of the iron regulatory hormone hepcidin) and also for systemic inflammation, hepatic HO-1 may be important for the regulation of both systems. In particular, cell-specific functions of HO-1 in liver tissue macrophages (Kupffer cells) might be of major significance, because these cells play a key role in iron recycling during erythrophagocytosis and also in the control of hepatic and systemic inflammatory responses. This review discussthe current knowledge on interactions of the HO-1 with iron metabolism in the context of systemic as well as hepatic inflammatory disorders. Recent advances in the understanding of the functional role of HO-1 in inflammatory liver diseases, namely viral hepatitis, alcoholic liver disease and non-alcoholic steatohepatitis are s uMmarized. Finally, it is highlighted how targeted modulation of HO-1 may provide specific protection in these inflammatory disorders. | [528712] | |||
| References | |||||
| Ref 528712 | Bioorg Med Chem. 2007 May 1;15(9):3225-34. Epub 2007 Feb 22.Heme oxygenase inhibition by 2-oxy-substituted 1-(1H-imidazol-1-yl)-4-phenylbutanes: effect of halogen substitution in the phenyl ring. | ||||
| Ref 553220 | Control of jaundice in preterm newborns by an inhibitor of bilirubin production: studies with tin-mesoporphyrin. Pediatrics. 1994 Jan;93(1):1-11. | ||||
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