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book (2)


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2008 (2)

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Antitargets : prediction and prevention of drug side effects
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ISBN: 9783527318216 3527318216 Year: 2008 Publisher: Weinheim: Wiley,

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Abstract


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Aromatase inhibitors
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ISBN: 1281242837 9786611242831 3764386932 3764386924 Year: 2008 Publisher: Basel : Birkhauser,

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Abstract

Many breast tumours are dependent upon oestrogen for their development and continued growth. Over the last 25 years hormone therapy has progressed from the irreversible destruction of endocrine glands to the use of drugs that reversibly suppress oestrogen synthesis or action. The inhibition of oestrogen synthesis is most readily achieved by inhibiting the final step in the pathway of oestrogen biosynthesis, the reaction which transforms androgens into oestrogens by creating an aromatic ring in the steroid molecule (hence the enzyme's trivial name, aromatase). Whereas the first aromatase inhibitors to be used therapeutically could be shown to produce drug-induced inhibition of the enzyme and therapeutic benefits in patients with breast cancer, they were not particularly potent and lacked specificity. However, second-generation drugs were developed and most recently third-generation inhibitors have evolved which possess remarkable specificity and potency. Initial results from clinical trials suggest that these agents will become the cornerstones of future endocrine therapy.

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