antiandrogens/karies

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Structure of human steroid 5α-reductase 2 with anti-androgen drug finasteride

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Human steroid 5α-reductase 2 (SRD5α2) as a critical integral membrane enzyme in steroid metabolism catalyzes testosterone to dihydrotestosterone. Mutations on its gene have been linked to 5α-reductase deficiency and prostate cancer. Finasteride and dutasteride as SRD5α2 inhibitors are widely used

Androgenic Activity of Antiandrogens Predicted by Fit into DNA.

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Computer modeling including graphics and energy calculations were employed for the first time to examine the stereochemical fit of antiandrogens into double-stranded DNA. In this study, we assessed the relative fit of antiandrogens in the cavity between base pairs known to accommodate androgens.

Antiandrogen induced cryptorchidism in the pig is associated with failed gubernacular regression and epididymal malformations.

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OBJECTIVE Can antiandrogens cause cryptorchidism in an animal model with a strip-like gubernaculum? If so, what anatomical abnormalities are associated with cryptorchidism? METHODS Timed pregnant sows received the antiandrogen flutamide during defined gestational intervals. Fetal pigs were evaluated

The biological effect of phthalate esters on transabdominal migration of the testis in fetal rats in comparison with the antiandrogen flutamide.

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Phthalate esters are commonly used as plasticizers for polyvinyl chloride and are known to be hormone-disrupting chemicals. We previously reported that mono-n-butyl phthalate (MBP) administered to rat fetuses induced cryptorchidism postnatally. The aim of this study was to investigate the biological

[Prognostic factors of prostate cancer treated with first-line hormone therapy].

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OBJECTIVE Endocrine therapy of prostate cancer is designed to eliminate the action of androgens to prevent the growth of hormone-sensitive cancer cells. The duration and quality of the response to this treatment vary from one patient to another. The objective of this study was to evaluate the

Androgens in relation to prenatal development and postnatal inversion of the gubernacula in rats.

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Exposure of male rats to the anti-androgen flutamide during fetal life, from day 10 after conception to the day of birth, allowed quantitatively unaltered development of the gubernacula. Apparently, androgens play no important role or no role at all in their growth. Castration of newborn male rats

Targeting alternative sites on the androgen receptor to treat castration-resistant prostate cancer.

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Recurrent, metastatic prostate cancer continues to be a leading cause of cancer-death in men. The androgen receptor (AR) is a modular, ligand-inducible transcription factor that regulates the expression of genes that can drive the progression of this disease, and as a consequence, this receptor is a

Dose-dependent effect of phthalate ester on testicular descent in pre-and post natal rats.

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Mono-n-butyl phthalate (MBP) was administered to pregnant rats from the 15th to the 17th gestational day to investigate the dose-dependent effect of phthalate ester on testicular descent in both pre- and postnatal rats. Thirty pregnant rats (280-330 g) were separated into five groups and

Crystal structure of the T877A human androgen receptor ligand-binding domain complexed to cyproterone acetate provides insight for ligand-induced conformational changes and structure-based drug design.

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Cyproterone acetate (CPA) is a steroidal antiandrogen used clinically in the treatment of prostate cancer. Compared with steroidal agonists for the androgen receptor (AR) (e.g. dihydrotestosterone, R1881), CPA is bulkier in structure and therefore seemingly incompatible with the binding pockets

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