Navigation Links
Moving beyond tamoxifen: Drug discovery and the future of selective hormone receptor modulators

How did a failed contraceptive become the first targeted therapy for the treatment of breast cancer" The transformation of tamoxifen, from cast-off to lifesaver, laid the foundation for a new class of therapeutics selective estrogen receptor modulators that could treat or prevent a variety of human diseases, including cancer and osteoporosis, according to V. Craig Jordan, OBE, Ph.D., D.Sc., a researcher at the Fox Chase Cancer Center in Philadelphia.

Today at the 2008 Annual Meeting of the American Association for the Advancement of Science, Jordan reports on efforts to use the lessons learned about tamoxifen to develop new hormone receptor-related drugs for both women and men. His presentation will be part of a symposium, held from 1:45 p.m. to 4:45 p.m., entitled Progress in Cancer Prevention.

As both a preventative and therapeutic agent, tamoxifen has been credited with saving the lives of more than a half million women over the last 30 years, says Jordan, the Alfred G. Knudson Jr., M.D., Ph.D., Chair in Cancer Research at Fox Chase. The process of discovery that made tamoxifen a reality has given us insights into molecular mechanisms that are currently being used to advance the creation and refinement of better drugs.

In the 1970s, Jordans laboratory pioneered the work that turned tamoxifen into a cancer therapy, which then jump-started a field of study into so-called designer estrogens. These drugs, called selective estrogen receptor modulators (SERMS), can have different effects on their targets, estrogen receptors, depending on where the receptor is located within a woman's body. The SERM raloxifene, for example, exhibits an anti-estrogen activity that can prevent cancer in breast tissue, but in other tissue the same drug has an estrogen-like effect that increases bone density. Currently, raloxifene, which was also developed in Jordans laboratory, is approved in post-menopausal women to prevent osteoporosis and treat breast cancer.

The idea that SERMs could act like an estrogen in one place and an anti-estrogen in the other has created a new dimension in drug development, Jordan says. Now we can look at the design of these drugs and see how they can be applied to modulate other receptor sites throughout the body.

According to Jordan, recent studies have shown light on the complex and seemingly contradictory mechanisms behind the activity of receptors for steroids, such as estrogen. These mechanisms include slight structural differences in the estrogen receptors themselves in different tissues, as well as co-regulatory molecules that can influence whether a SERM will turn on or shut down a particular receptor. Of the 48 or so members of the nuclear receptor family, which include the molecules inside cells that bind to estrogen and other hormones, nearly half are able to be regulated in some way.

Our knowledge of how tamoxifen and raloxifene work is now being applied to develop new drugs that are selective male hormone receptor modulators that could be used in men to improve muscle weight during sickness, but without stimulating glands like the prostate, Jordan says. Indeed, a whole variety of nuclear steroid hormone receptor mediated drugs are now possible because of the understanding of SERM action.


Contact: Greg Lester
Fox Chase Cancer Center

Related medicine news :

1. Congressional Budget Includes Earmark to Keep Washingtons Sexual Assault DNA Program Moving Forward
2. AUDIO from Medialink and GlaxoSmithKline: Get Ready to Get Moving to a New You in the New Year
3. After Dropping 162 Pounds, Jodi Davis Inspires Other Michigan Women to Get Moving and Lose Weight Through
4. Growth Needs Space: joimax, Inc. USA, is Moving Into New Premises
5. GPS-like technology helps pinpoint best methods for moving injured players
6. Removing Ovaries Before Menopause Leads to Memory, Movement Troubles
7. Legislative and Regulatory Outlook - 2009 and Beyond for Pharma, Biotech Players
8. Michigan Kidney Patient Goes Above and Beyond to Help His Community - Awarded National DPC Hero Award
9. Fourth Annual James E. Marshall OCD Foundation Beyond Beauty Dinner to Honor E. Scott Beattie, Chairman and CEO, Elizabeth Arden, Inc. and Charles H. Townsend, President and CEO, Conde Nast Publications
10. Ashley Forms Partnership With Roger Burgess and ProCare Rx to Carry Gotham Banner into 2008 and Beyond
11. 10 Cities to Participate in Live Well! Life Beyond Cancer Program Sponsored by The Wellness Community and the Lance Armstrong Foundation
Post Your Comments:
(Date:6/26/2016)... ... June 26, 2016 , ... On June 10-11, 2016, A Forever Recovery, a ... and World’s Longest Breakfast Table in Battle Creek, MI, where the rehabilitation facility is ... to some of the world’s leading providers of cereal and other breakfast foods. Its ...
(Date:6/26/2016)... ... June 26, 2016 , ... ... have been diagnosed with endometriosis. These women need a treatment plan to not ... comprehensive approach that can help for preservation of fertility and ultimately achieving a ...
(Date:6/25/2016)... ... ... "With 30 hand-drawn hand gesture animations, FCPX users can easily customize each ... Film Studios. , ProHand Cartoon’s package transforms over 1,300 hand-drawn pictures into hand ... select a ProHand generator and drag it above media or text in the Final ...
(Date:6/25/2016)... ... June 25, 2016 , ... On Friday, June 10, Van Mitchell, Secretary ... Work award to iHire in recognition of their exemplary accomplishments in worksite health promotion. ... Maryland Workplace Health & Wellness Symposium at the BWI Marriott in Linthicum Heights. iHire ...
(Date:6/24/2016)... ... June 24, 2016 , ... June 19, 2016 is World Sickle Cell ... pain and the benefits of holistic treatments, Serenity Recovery Center of Marne, ... Cell Disease. , Sickle Cell Disease (SCD) is a disorder of the red blood ...
Breaking Medicine News(10 mins):
(Date:6/23/2016)... Roche (SIX: RO, ROG; OTCQX: RHHBY) announced that it ... (procalcitonin) assay as a dedicated testing solution for people ... Roche is the first IVD company in the U.S ... assessment and management. PCT is a sepsis-specific ... blood can aid clinicians in assessing the risk of ...
(Date:6/23/2016)... , , , WHEN: ... , , , , LOCATION: , , , Online, with ... , EXPERT PANELISTS:  , , , Frost & Sullivan,s Global Vice ... Senior Industry Analyst, Divyaa Ravishankar and Unmesh Lal, Program Manager , ... industry is witnessing an exceptional era. Several new demand spaces, such ...
(Date:6/23/2016)... 2016 The vast majority of dialysis patients ... Treatments are usually 3 times a week, with treatment ... travel time, equipment preparation and wait time.  This regimen ... for patients who are elderly and frail.  Many elderly ... rehabilitation centers for some duration of time. ...
Breaking Medicine Technology: