Abstract:
:Efforts to interfere with the initiation and promotion of breast and other cancers by endocrine manipulation are not new. It is of obvious benefit to cancer patients to administer substances that combine minimal general toxicity with maximal oestrogen inhibition. Raloxifene is a relatively recent addition to a group of compounds loosely designated as antioestrogens, which implies their ability to antagonize oestrogen effects via competitive binding to the various receptors. This is a reductionist simplification, since their effect varies and ranges from interaction with lipid transduction cascades, covalent binding to proteins and DNA, regulation of growth factors, erbB2, mdr1 and probably p53 expression, complexing with E-cadherin/catenin to active induction of apoptosis and many other effects on the genome. Also, the action of most antioestrogens is not solely antagonistic and different compounds do exert some agonistic effects in various tissues. Apart from some "pure" antioestrogens, the benzothiophene derivative Raloxifene has been found to combine a high degree of selective oestrogen suppression with several other desirable characteristics, such as reduction of bone demineralisation and antiatherogenic effects without endometrial stimulation. It is well tolerated, has been successfully tested as a chemopreventive agent for breast cancer in certain groups of the population and does not prevent ovulation in women with normal menstrual cycles. Certainly, Raloxifene is only another forerunner of upcoming "designer" oestrogen modulators, but it represents a welcome addition to the therapeutic choices available for the control of some menopausal problems as well as for the prevention and treatment of breast cancer, as outlined in the following brief review.
journal_name
Curr Drug Targetsjournal_title
Current drug targetsauthors
Kellen JAdoi
10.2174/1389450013348263keywords:
subject
Has Abstractpub_date
2001-12-01 00:00:00pages
423-5issue
4eissn
1389-4501issn
1873-5592journal_volume
2pub_type
杂志文章,评审abstract::Recent progress in molecular biology has provided application of gene transfer methods in arthritis. Two clinical trails using ex vivo retrovirus mediated delivery of interleukin -1 receptor antagonist gene for rheumatoid arthritis has begun in USA and Germany. However, there are still many issues to be elucidated; on...
journal_title:Current drug targets
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doi:10.2174/1389450033490777
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journal_title:Current drug targets
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journal_title:Current drug targets
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pub_type: 杂志文章,评审
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更新日期:2011-08-01 00:00:00
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journal_title:Current drug targets
pub_type: 杂志文章,评审
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更新日期:2006-03-01 00:00:00
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journal_title:Current drug targets
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pub_type: 杂志文章,评审
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更新日期:2008-10-01 00:00:00
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更新日期:2007-07-01 00:00:00
abstract::There exists an immediate need to develop novel medications for the treatment of mood disorders such as bipolar disorder and depression. Initial interest in glycogen synthase kinase-3 (GSK-3) as a target for the treatment of mood disorders arose from the finding that the mood stabilizing drug lithium directly inhibite...
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