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Inactivation of androgens by UDP-glucuronosyltransferase enzymes in humans


#1

http://www.sciencedirect.com/science?_ob=ArticleURL&_udi=B6T3K-49V9HR1-1&_user=10&_rdoc=1&_fmt=&_orig=search&_sort=d&view=c&_version=1&_urlVersion=0&_userid=10&md5=7d161816f8f78a759dc334be6bfdfb50

Inactivation of androgens by UDP-glucuronosyltransferase enzymes in humans

Alain Bélanger, Georges Pelletier, Fernand Labrie, Olivier Barbier and Sarah Chouinard

Oncology and Molecular Endocrinology Research Center, CHUL Research Center, Laval University, Québec, G1V 4G2, Canada

Available online 23 October 2003.

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Abstract
In humans, 3β-hydroxysteroid dehydrogenase (3β-HSD), 17β-HSD and 5α-reductase activities in androgen target tissues, such as the prostate and skin, convert dehydroepiandrosterone, androstenedione and testosterone into the most potent natural androgen dihydrotestosterone (DHT). This androgen is converted mainly in situ into two phase I metabolites, androsterone (ADT) and androstane-3α,17β-diol (3α-DIOL), which might be back converted to DHT. Here, we discuss the recent findings regarding the characterization of specific UDP-glucuronosyltransferases (UGTs), UGT2B7, B15 and B17, responsible for the glucuronidation of these metabolites. The tissue distribution and cellular localization of the UGT2B transcripts and proteins in humans clearly indicate that these enzymes are synthesized in androgen-sensitive tissues. It is postulated that the conjugating activity of UGT enzymes is the main mechanism for modulating the action of steroids and protecting the androgen-sensitive tissues from deleteriously high concentrations of DHT, ADT and 3α-DIOL.

Article Outline

  1. UGT enzymes
  2. UGT2B7
  3. UGT2B15
  4. UGT2B17
  5. UGT2B enzymes in the human prostate
  6. UGT2B15 and prostate cancer
  7. UGT2B enzymes in the human skin
  8. Conclusions
    References

Figure 1. Enzymes involved in metabolism of androgens in peripheral intracrine tissues [6, 10, 11, 12 and 13]. Dehydroepiandrosterone, its sulfate, androst-5-ene-3β,17β-diol and its sulfate, and androstenedione are secreted by the adrenals, whereas testosterone is produced by the testes. Abbreviations: HSD, hydroxy steroid dehydrogenase; HSE, hydroxysteroid epimerase; RODH, retinoldehydrogenase; 1, the enzyme has not been isolated so far.

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#2

Fighting androgens is not the way


#3

» Fighting androgens is not the way

Depends on whether it can be made into a convenient non-syetemic topical product or not.


#4

» » Fighting androgens is not the way
»
» Depends on whether it can be made into a convenient non-syetemic topical
» product or not.

I believe thats a Dream to have a non systemic topical.if the career can get through the skin then the effects will get systemic with time.


#5

» » » Fighting androgens is not the way
» »
» » Depends on whether it can be made into a convenient non-syetemic
» topical
» » product or not.
»
» I believe thats a Dream to have a non systemic topical.if the career can
» get through the skin then the effects will get systemic with time.

It doesn’t have to be like that, i.e. retinoic acid has no sytemic absorption, and it really works topically :

http://cat.inist.fr/?aModele=afficheN&cpsidt=2648624