Receptors, Steroid

Publication Title: 
Annual Review of Nutrition

Nutrigenomics refers to the complex effects of the nutritional environment on the genome, epigenome, and proteome of an organism. The diverse tissue- and organ-specific effects of diet include gene expression patterns, organization of the chromatin, and protein post-translational modifications. Long-term effects of diet range from obesity and associated diseases such as diabetes and cardiovascular disease to increased or decreased longevity.

Author(s): 
Ruden, Douglas M.
De Luca, Maria
Garfinkel, Mark D.
Bynum, Kerry L.
Lu, Xiangyi
Publication Title: 
Epigenomics

Sexual differentiation of the brain takes place during a perinatal-sensitive time window as a result of gonadal hormone-induced activational and organizational effects on neuronal substrates. Increasing evidence suggests that epigenetic mechanisms can contribute to the establishment and maintenance of some aspects of these processes, and that these epigenetic mechanisms may themselves be under the control of sex hormones.

Author(s): 
Menger, Yannick
Bettscheider, Marc
Murgatroyd, Chris
Spengler, Dietmar
Publication Title: 
The Journal of Membrane Biology

Soy isoflavone's (genistein and daidzein in particular) biological significance has been thoroughly studied for decades, so we started from the premise that refreshed investigation approach in this field should consider identification of their new molecular targets. In addition to recently described epigenetic aspects of polyphenole action, the cell membrane constituents-mediated effects of soy isoflavones are worthy of special attention.

Author(s): 
Ajdûanovi?, Vladimir
Medigovi?, Ivana
éivanovi?, Jasmina
Moji?, Marija
Miloöevi?, Verica
Publication Title: 
Molecular Pharmacology

Artemisinin drugs are of utmost importance in the treatment of malaria, because they represent the sole class of therapeutically used antimalarial drugs to which malaria parasites have not yet developed resistance. The major disadvantage of these medicines is the comparatively high recrudescence rate, which has been attributed to the remarkable decrease of artemisinin plasma concentrations during multiple dosing. Autoinduction of CYP2B6-mediated metabolism has been implicated as the underlying mechanism. So far, the molecular mechanism of induction by artemisinin has not been resolved.

Author(s): 
Burk, Oliver
Arnold, Katja A.
Nüssler, Andreas K.
Schaeffeler, Elke
Efimova, Ekaterina
Avery, Bonnie A.
Avery, Mitchell A.
Fromm, Martin F.
Eichelbaum, Michel
Publication Title: 
Antimicrobial Agents and Chemotherapy

Artemisinins induce drug metabolism through the activation of the pregnane X receptor (PXR) in vitro. Here, we report the resequencing and genotyping of PXR variants in 75 Vietnamese individuals previously characterized for CYP3A enzyme activity after artemisinin exposure. We identified a total of 31 PXR variants, including 5 novel single nucleotide polymorphisms (SNPs), and we identified significantly different allele frequencies relative to other ethnic groups.

Author(s): 
Piedade, Rita
Schaeffeler, Elke
Winter, Stefan
Asimus, Sara
Schwab, Matthias
Ashton, Michael
Burk, Oliver
Gil, José P.
Publication Title: 
Antimicrobial Agents and Chemotherapy

Malaria patients are frequently coinfected with HIV and mycobacteria causing tuberculosis, which increases the use of coadministered drugs and thereby enhances the risk of pharmacokinetic drug-drug interactions. Activation of the pregnane X receptor (PXR) by xenobiotics, which include many drugs, induces drug metabolism and transport, thereby resulting in possible attenuation or loss of the therapeutic responses to the drugs being coadministered. While several artemisinin-type antimalarial drugs have been shown to activate PXR, data on nonartemisinin-type antimalarials are still missing.

Author(s): 
Piedade, Rita
Traub, Stefanie
Bitter, Andreas
Nüssler, Andreas K.
Gil, José P.
Schwab, Matthias
Burk, Oliver
Publication Title: 
The Journal of Pharmacology and Experimental Therapeutics

An extract of the plant Coleus forskohlii has been used for centuries in Ayurvedic medicine to treat various diseases such as hypothyroidism, heart disease, and respiratory disorders. Additionally, complex herbal mixtures containing this extract are gaining popularity in United States for their putative "fat-burning" properties. The active ingredient in C. forskohlii extract is the diterpene compound forskolin.

Author(s): 
Ding, Xunshan
Staudinger, Jeff L.
Publication Title: 
The Journal of Pharmacology and Experimental Therapeutics

Guggulsterone is the active ingredient in gugulipid, an organic extract of the Commiphora mukul plant. Gugulipid has been used for nearly 3000 years in Ayurvedic medicine, mainly as a treatment for arthritis. Herbal practitioners currently use gugulipid therapy in conditions as diverse as rheumatism, coronary artery disease, arthritis, hyperlipidemia, acne, and obesity. The active ingredient in gugulipid is guggulsterone, a plant sterol compound recently identified as a pregnane X receptor (PXR; NR1I2) ligand.

Author(s): 
Ding, Xunshan
Staudinger, Jeff L.
Publication Title: 
The Journal of Pharmacology and Experimental Therapeutics

An extract of the plant Coleus forskohlii has been used for centuries in Ayurvedic medicine to treat various diseases such as hypothyroidism, heart disease, and respiratory disorders. Additionally, complex herbal mixtures containing this extract are gaining popularity in United States for their putative "fat-burning" properties. The active ingredient in C. forskohlii extract is the diterpene compound forskolin.

Author(s): 
Ding, Xunshan
Staudinger, Jeff L.
Publication Title: 
The Journal of Pharmacology and Experimental Therapeutics

Guggulsterone is the active ingredient in gugulipid, an organic extract of the Commiphora mukul plant. Gugulipid has been used for nearly 3000 years in Ayurvedic medicine, mainly as a treatment for arthritis. Herbal practitioners currently use gugulipid therapy in conditions as diverse as rheumatism, coronary artery disease, arthritis, hyperlipidemia, acne, and obesity. The active ingredient in gugulipid is guggulsterone, a plant sterol compound recently identified as a pregnane X receptor (PXR; NR1I2) ligand.

Author(s): 
Ding, Xunshan
Staudinger, Jeff L.

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