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Development of a biological screening system for the evaluation of highly active and selective 17β-HSD1-inhibitors as potential therapeutic agents

17β-Hydroxysteroid dehydrogenase type 1 (17β-HSD1) catalyses the intracellular conversion of oestrone (E1) to oestradiol (E2). E2 is known to be involved in the development and progression of breast cancer and endometriosis. Since 17β-HSD1 is overexpressed in these oestrogen-dependent diseases, inhi... Full description

Journal Title: Molecular and Cellular Endocrinology 2009, Vol.301(1), pp.154-157
Main Author: Kruchten, Patricia
Other Authors: Werth, Ruth , Marchais-Oberwinkler, Sandrine , Frotscher, Martin , Hartmann, Rolf W
Format: Electronic Article Electronic Article
Language: English
Subjects:
E1
E2
Er
Mtt
SAR
ID: ISSN: 0303-7207 ; E-ISSN: 1872-8057 ; DOI: 10.1016/j.mce.2008.09.035
Link: http://dx.doi.org/10.1016/j.mce.2008.09.035
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recordid: elsevier_sdoi_10_1016_j_mce_2008_09_035
title: Development of a biological screening system for the evaluation of highly active and selective 17β-HSD1-inhibitors as potential therapeutic agents
format: Article
creator:
  • Kruchten, Patricia
  • Werth, Ruth
  • Marchais-Oberwinkler, Sandrine
  • Frotscher, Martin
  • Hartmann, Rolf W
subjects:
  • 17β-Hsd1-Inhibitors
  • Drug Development
  • Oestrogen-Dependent Disease
  • Metabolic Stability
  • Screening System
  • Selectivity (17β-Hsd2, Hepatic Cyps, Oestrogen Receptor)
  • 17β-Hsd1
  • 17β-Hsd2
  • E1
  • E2
  • Er
  • Mtt
  • Pampa
  • SAR
  • Teer
  • 17β-Hsd1-Inhibitors
ispartof: Molecular and Cellular Endocrinology, 2009, Vol.301(1), pp.154-157
description: 17β-Hydroxysteroid dehydrogenase type 1 (17β-HSD1) catalyses the intracellular conversion of oestrone (E1) to oestradiol (E2). E2 is known to be involved in the development and progression of breast cancer and endometriosis. Since 17β-HSD1 is overexpressed in these oestrogen-dependent diseases, inhibition of this enzyme may be a more target-directed therapeutical approach compared to established medical treatments. For the identification of highly active and selective 17β-HSD1-inhibitors that are suitable for application as potential therapeutics, there is a need for an appropriate, efficient and reliable screening system. Here, we report the development and application of our screening system using our in house library of potential 17β-HSD1-inhibitors. Four potent and selective compounds with a good first pharmacokinetic profile were identified.
language: eng
source:
identifier: ISSN: 0303-7207 ; E-ISSN: 1872-8057 ; DOI: 10.1016/j.mce.2008.09.035
fulltext: fulltext
issn:
  • 0303-7207
  • 03037207
  • 1872-8057
  • 18728057
url: Link


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titleDevelopment of a biological screening system for the evaluation of highly active and selective 17β-HSD1-inhibitors as potential therapeutic agents
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description17β-Hydroxysteroid dehydrogenase type 1 (17β-HSD1) catalyses the intracellular conversion of oestrone (E1) to oestradiol (E2). E2 is known to be involved in the development and progression of breast cancer and endometriosis. Since 17β-HSD1 is overexpressed in these oestrogen-dependent diseases, inhibition of this enzyme may be a more target-directed therapeutical approach compared to established medical treatments. For the identification of highly active and selective 17β-HSD1-inhibitors that are suitable for application as potential therapeutics, there is a need for an appropriate, efficient and reliable screening system. Here, we report the development and application of our screening system using our in house library of potential 17β-HSD1-inhibitors. Four potent and selective compounds with a good first pharmacokinetic profile were identified.
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17β-Hydroxysteroid dehydrogenase type 1 (17β-HSD1) catalyses the intracellular conversion of oestrone (E1) to oestradiol (E2). E2 is known to be involved in the development and progression of breast cancer and endometriosis. Since 17β-HSD1 is overexpressed in these oestrogen-dependent diseases, inhibition of this enzyme may be a more target-directed therapeutical approach compared to established medical treatments. For the identification of highly active and selective 17β-HSD1-inhibitors that are suitable for application as potential therapeutics, there is a need for an appropriate, efficient and reliable screening system. Here, we report the development and application of our screening system using our in house library of potential 17β-HSD1-inhibitors. Four potent and selective compounds with a good first pharmacokinetic profile were identified.

pubElsevier Ireland Ltd
doi10.1016/j.mce.2008.09.035
lad01Molecular and Cellular Endocrinology