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Concept

Steroidogenesis inhibitor

Related publications (13)

Hypothalamic pregnenolone mediates recognition memory in the context of metabolic disorders

Maria del Carmen Sandi Perez, Ioannis Zalachoras

Obesity and type 2 diabetes are associated with cognitive dysfunction. Because the hypothalamus is implicated in energy balance control and memory disorders, we hypothesized that specific neurons in this brain region are at the interface of metabolism and ...

Cell Press2022

Structures of ABCG2 under turnover conditions reveal a key step in the drug transport mechanism

Henning Paul-Julius Stahlberg, Dongchun Ni

ABCG2 is a multidrug transporter that affects drug pharmacokinetics and contributes to multidrug resistance of cancer cells. In previously reported structures, the reaction cycle was halted by the absence of substrates or ATP, mutation of catalytic residue ...

Nature Research2021

Structural basis of drug recognition by the multidrug transporter ABCG2

Henning Paul-Julius Stahlberg, Dongchun Ni

ABCG2 is an ATP-binding cassette (ABC) transporter whose function affects the pharmacokinetics of drugs and contributes to multidrug resistance of cancer cells. While its interaction with the endogenous substrate estrone-3-sulfate (E1S) has been elucidated ...

Elsevier2021

A high resolution LC-MS targeted method for the concomitant analysis of 11 contraceptive progestins and 4 steroids

Cathrin Brisken, Marc Moniatte, Jonathan Paz Montoya, Fabio De Martino, Marie Shamseddin, Csaba Ferenc László

In the context of hormonal contraception and hormone replacement therapy (HRT), many women are exposed to exogenous hormones. Current use of hormonal contraception with combined ethinyl estradiol and different progestins bestows a breast cancer relative ri ...

2019

Increased brain glucocorticoid actions following social defeat in rats facilitates the long-term establishment of social subordination

Maria del Carmen Sandi Perez, Jocelin Grosse, Olivia Zanoletti, Meltem Weger

Social rank is frequently established through aggressive encounters between new conspecifics. Despite increasing evidence suggesting that social rank is critical for the well-being of both humans and animals, knowledge about the factors influencing social ...

2018

Intestinal steroidogenesis controls PPAR expression in the colon and is impaired during ulcerative colitis

Johan Auwerx

Background and aims Immune tolerance breakdown during UC involves the peroxisome proliferator-activated receptor- (PPAR), a key factor in mucosal homoeostasis and the therapeutic target of 5-aminosalycilates, which expression is impaired during UC. Here we ...

Bmj Publishing Group2015

Identification of the Link Between the Hypothalamo-Pituitary Axis and the Testicular Orphan Nuclear Receptor NR0B2 in Adult Male Mice

Kristina Schoonjans

The small heterodimer partner (SHP, nuclear receptor subfamily 0, group B, member 2; NR0B2) is an atypical nuclear receptor known mainly for its role in bile acid homeostasis in the enterohepatic tract. We previously showed that NR0B2 controls testicular f ...

Endocrine Soc2015

The Orphan Nuclear Receptor Nr5a2 Is Essential for Luteinization in the Female Mouse Ovary

Kristina Schoonjans

In the ovary, the follicular granulosa cells express the nuclear receptor Nr5a2 (nuclear receptor subfamily 5 group A member 2), also known as liver receptor homolog-1, and after ovulation, Nr5a2 expression persists in the corpus luteum. Previous studies d ...

Endocrine Soc2014

Liver receptor homolog-1 is essential for pregnancy

Kristina Schoonjans

Successful pregnancy requires coordination of an array of signals and factors from multiple tissues. One such element, liver receptor homolog-1 (Lrh-1), is an orphan nuclear receptor that regulates metabolism and hormone synthesis(1). It is strongly expres ...

Nature Publishing Group2013

A Brain-Permeable Small Molecule Reduces Neuronal Cholesterol by Inhibiting Activity of Sirtuin 2 Deacetylase

Sirtuin 2 (SIRT2) deacetylase-dependent inhibition mediates neuroprotective reduction of cholesterol biosynthesis in an in vitro Huntington's disease model. This study sought to identify the first brain permeable SIRT2 inhibitor and to characterize its cho ...

American Chemical Society2011

SIRT2 inhibition achieves neuroprotection by decreasing sterol biosynthesis

Huntington's disease (HD), an incurable neurodegenerative disorder, has a complex pathogenesis including protein aggregation and the dysregulation of neuronal transcription and metabolism. Here, we demonstrate that inhibition of sirtuin 2 (SIRT2) achieves ...

National Academy of Sciences2010

The orphan nuclear receptor small heterodimer partner mediates male infertility induced by diethylstilbestrol in mice

Johan Auwerx, Kristina Schoonjans

Studies in rodents have shown that male sexual function can be disrupted by fetal or neonatal administration of compounds that alter endocrine homeostasis, such as the synthetic nonsteroidal estrogen diethylstilbestrol (DES). Although the molecular basis f ...

American Society for Clinical Investigation2009

Nonenzymic polycyclisation of analogues of oxidosqualene with a preformed C-ring

Philip Pattison

Some nonenzymic epoxide-initiated polyolefin cyclisations are reported. The presented molecules are partially constrained analogues of (3S)-oxidosqualene, the natural substrate to many important cyclase enzymes. These model compounds feature a preformed C- ...

2008