| First Author | Lamminen T | Year | 2009 |
| Journal | Mol Cell Endocrinol | Volume | 301 |
| Issue | 1-2 | Pages | 158-62 |
| PubMed ID | 19026716 | Mgi Jnum | J:146969 |
| Mgi Id | MGI:3839040 | Doi | 10.1016/j.mce.2008.10.034 |
| Citation | Lamminen T, et al. (2009) In vivo mouse model for analysis of hydroxysteroid (17beta) dehydrogenase 1 inhibitors. Mol Cell Endocrinol 301(1-2):158-62 |
| abstractText | Hydroxysteroid (17beta) dehydrogenase 1 (HSD17B1) catalyzes the reaction between the low active 17-ketosteroids and the highly active 17beta-hydroxysteroids. In the present study, we have generated transgenic (TG) mice expressing human (h) HSD17B1 under mouse mammary tumor virus (MMTV) promoter (MMTV-hHSD17B1TG mice). The MMTV-hHSD17B1TG mice were used to characterize HSD17B1 enzyme activity and properties of HSD17B1 inhibitor in vivo. Expression of the transgene was detected by enzyme activity and RT-PCR analysis. Increased HSD17B1 activity in the TG mice was detected in vivo by applying estrone as a substrate via an intravenous injection. The developed enzyme activity measurement was then applied to analyze the efficacy of HSD17B1 inhibitor in vivo. The results indicated that the MMTV-hHSD17B1TG mouse model is a valuable novel tool to test human HSD17B1 inhibition by various compounds in vivo. With the potent hHSD17B1 inhibitor compound tested, at highest an 85% and 33% inhibition of the enzyme activity in males and in females, respectively, was observed. |
