Martin Frotscher

ORCID: 0000-0003-1777-8890 · 19 papers in corpus · active 2008-2023

Study types

  • other 15
  • article 3
  • review 1

Condition tags

  • endometriosis 19
article 2023
Journal of medicinal chemistry ·doi:10.1021/acs.jmedchem.3c00571

Treating estrogen-dependent diseases like endometriosis with drugs suppressing local estrogen activation may be superior to existing endocrine therapies. Steroid sulfatase (STS) and 17β-hydroxysteroid dehydrogenase type 1 (17β-HSD1) are key…

article 2022
Journal of medicinal chemistry ·doi:10.1021/acs.jmedchem.2c00589

A novel approach for the dual inhibition of steroid sulfatase (STS) and 17β-hydroxysteroid dehydrogenase type 1(17β HSD1) by a single drug was explored, starting from in-house 17β HSD1 inhibitors via masking their phenolic OH group with a s…

other 2019
European journal of medicinal chemistry ·doi:10.1016/j.ejmech.2019.05.084

Estrogens are the major female sex steroid hormones, estradiol (E2) being the most potent form in humans. Disturbing the balance between E2 and its weakly active oxidized form estrone (E1) leads to diverse types of estrogen-dependent diseas…

other 2017
Journal of medicinal chemistry ·doi:10.1021/acs.jmedchem.7b00062

STS and 17β-HSD1 are attractive targets for the treatment of estrogen-dependent diseases like endometriosis and breast cancer. The simultaneous inhibition of both enzymes appears more promising than blockage of either protein alone. We desc…

other 2017
European journal of medicinal chemistry ·doi:10.1016/j.ejmech.2016.11.004

Current endocrine therapeutics for the estrogen-dependent disease endometriosis often lead to considerable side-effects as they act by reducing estrogen action systemically. A more recent approach takes advantage of the fact that the weak e…

other 2015
European journal of medicinal chemistry ·doi:10.1016/j.ejmech.2015.08.030

17β-Estradiol (E2), the most potent human estrogen, is known to be involved in the etiology of estrogen-dependent diseases (EDD) like breast cancer and endometriosis. 17β-Hydroxysteroid dehydrogenase type 1 (17β-HSD1) catalyses the last ste…

other 2014
European journal of medicinal chemistry ·doi:10.1016/j.ejmech.2014.05.074

Estradiol is the most potent estrogen in humans. It is known to be involved in the development and proliferation of estrogen dependent diseases such as breast cancer and endometriosis. The last step of its biosynthesis is catalyzed by 17β-h…

other 2012
PloS one ·doi:10.1371/journal.pone.0029252

17β-estradiol (E2), the most potent estrogen in humans, known to be involved in the development and progession of estrogen-dependent diseases (EDD) like breast cancer and endometriosis. 17β-HSD1, which catalyses the reduction of the weak es…

article 2012
Journal of medicinal chemistry ·doi:10.1021/jm201735j

The reduction of estrone to estradiol, the most potent estrogen in human, is catalyzed by 17β-hydroxysteroid dehydrogenase type 1 (17β-HSD1). A promising approach for the treatment of estrogen-dependent diseases is the reduction of intracel…

review 2011
The Journal of steroid biochemistry and molecular biology ·doi:10.1016/j.jsbmb.2010.12.013

17β-Hydroxysteroid dehydrogenases (17β-HSDs) are oxidoreductases, which play a key role in estrogen and androgen steroid metabolism by catalyzing final steps of the steroid biosynthesis. Up to now, 14 different subtypes have been identified…

other 2011
ChemMedChem ·doi:10.1002/cmdc.201000457

An attractive target that has still to be explored for the treatment of estrogen-dependent diseases, such as breast cancer and endometriosis, is the enzyme responsible for the last step in the biosynthesis of estradiol (E2): 17β-hydroxyster…

other 2011
Journal of medicinal chemistry ·doi:10.1021/jm1009082

Inhibition of 17β-hydroxysteroid dehydrogenase type 1 (17β-HSD1) is a novel and attractive approach to reduce the local levels of the active estrogen 17β-estradiol in patients with estrogen-dependent diseases like breast cancer or endometri…

other 2010
Journal of medicinal chemistry ·doi:10.1021/jm101073q

Estradiol (E2), the most important estrogen in humans, is involved in the initiation and progression of estrogen-dependent diseases such as breast cancer and endometriosis. Its local production in the target cell is regulated by 17β-hydroxy…

other 2010
Bioorganic & medicinal chemistry ·doi:10.1016/j.bmc.2010.03.065

17Beta-hydroxysteroid dehydrogenase type 1 (17beta-HSD1) catalyzes the reduction of estrone into estradiol, which is the most potent estrogen in humans. Lowering intracellular estradiol concentration by inhibition of this enzyme is a promis…

other 2009
Molecular and cellular endocrinology ·doi:10.1016/j.mce.2008.09.035

17beta-Hydroxysteroid dehydrogenase type 1 (17beta-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 17b…

other 2009
The Journal of steroid biochemistry and molecular biology ·doi:10.1016/j.jsbmb.2009.02.006

The most potent estrogen estradiol (E2) plays a pivotal role in the initiation and progression of estrogen dependent diseases. 17beta-Hydroxysteroid dehydrogenase type 1 (17betaHSD1) catalyses the NADPH-dependent E2-formation from estrone (…

other 2009
Molecular and cellular endocrinology ·doi:10.1016/j.mce.2008.09.024

17beta-Hydroxysteroid dehydrogenase type 1 (17beta-HSD1) catalyzes the transformation of estrone (E1) into the most potent estrogen, estradiol (E2), which stimulates cell proliferation and decreases apoptosis. 17beta-HSD1 is often strongly …

other 2009
Molecular and cellular endocrinology ·doi:10.1016/j.mce.2008.09.012

17beta-Hydroxysteroid dehydrogenase type 1 (17beta-HSD1) is responsible for the catalytic reduction of the weak estrogen estrone (E1) into the highly potent 17beta-estradiol (E2). As 17beta-HSD1 is often overexpressed in mammary tumors and …

other 2008
Journal of medicinal chemistry ·doi:10.1021/jm8006917

17beta-Estradiol (E2), the most potent female sex hormone, stimulates the growth of mammary tumors and endometriosis via activation of the estrogen receptor alpha (ERalpha). 17beta-Hydroxysteroid dehydrogenase type 1 (17beta-HSD1), which is…