Navigation Links
Moving beyond tamoxifen: Drug discovery and the future of selective hormone receptor modulators
Date:2/15/2008

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
gregory.lester@fccc.edu
215-316-8977
Fox Chase Cancer Center
Source:Eurekalert

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 WalkyTalk.com(TM)
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:
*Name:
*Comment:
*Email:
(Date:10/12/2017)... (PRWEB) , ... October 12, 2017 , ... ... Mohebi Hair Restoration, has recently contributed a medical article to the newly revamped ... cosmetictown.com. Dr. Mohebi’s article spotlights the hair transplant procedure known as Follicular ...
(Date:10/12/2017)... D.C. (PRWEB) , ... October 12, 2017 , ... Leading ... their peers in Washington, D.C., for the 49th Congress of the International Society ... ., Vice President of the Center for Cancer and Blood Disorders at ...
(Date:10/12/2017)... RAPIDS, Mich. (PRWEB) , ... October 12, 2017 ... ... Wellness, has been named one of Michigan’s 2017 Best and Brightest in Wellness® ... and Brightest in Wellness® awards program on Friday, Oct. 20 from 7:30 a.m. ...
(Date:10/12/2017)... ... October 12, 2017 , ... In the United States, ... In some states—like New York, New Jersey, Massachusetts, Texas, Virginia, Connecticut, and California—the ... have extremely low property-tax rates, which contributes to the relatively lower cost of ...
(Date:10/12/2017)... ... 2017 , ... Farm Forward joins Bon Appétit ... institutions in announcing the launch of the Leadership Circle , a program ... raised for food. , Founding members of the Leadership Circle also include Airbnb’s ...
Breaking Medicine News(10 mins):
(Date:9/25/2017)... PROVIDENCE, R.I. , Sept. 25, 2017 /PRNewswire/ ... immunogenicity assessment, vaccine design, and immune-engineering today announced ... focused on the development of personalized therapeutic cancer ... and has provided exclusive access to enabling technologies ... MSc Eng., MBA will lead EpiVax Oncology as ...
(Date:9/22/2017)... AVACEN Medical (AVACEN) announced that its CE-Marked ... those with the widespread pain associated with fibromyalgia in ... Essex, England commented, "I had ... no sleep at all, tremendous pain, with every movement ... [the AVACEN 100] enough, how this has and is ...
(Date:9/18/2017)... , Sept. 18, 2017  PMD Healthcare of ... Pharmacy of Kalamazoo, Mich. , have ... service that expedites and streamlines patient and provider access ... 2.0, and wellness management services.  ... used to measure lung function for a variety of ...
Breaking Medicine Technology: