HOME >> BIOLOGY >> NEWS
Tamoxifen-like drug suggests new ways to selectively block estrogen

The ability of an experimental drug known as GW5638 to change the shape of the estrogen receptor is helping researchers understand why drugs like tamoxifen and raloxifene behave the way they do, simulating the effects of estrogen in some tissues and blocking it in others. The finding indicates that this little-known drug may play an important role in preventing, as well as treating, breast cancer and suggests ways to design new drugs with even more specific effects.

In the May 13, 2005, issue of Molecular Cell, researchers from the University of Chicago, Renz Research, Inc., Duke University and GlaxoSmithKline show how GW5638 fits into a pocket in the estrogen receptor in a way that differs slightly, but importantly, from how tamoxifen fits. The slight difference changes the shape of the receptor in ways that alter its effects on the numerous coregulatory proteins that interact with it.

"We found a small, but significant, change in conformation that goes a long way towards explaining why these drugs have different effects in different tissues," said Geoffrey Greene, Ph.D., professor in the Ben May Institute for Cancer Research at the University of Chicago.

"This type of information should help us design drugs that produce even more specific outcomes. In particular, we could design new small molecules that would be more effective than tamoxifen or raloxifene at preventing breast cancer, heart disease and bone loss without increasing the risk of endometrial cancer."

Tamoxifen and raloxifene are the best-known members of a class of drugs known as specific estrogen receptor modulators or SERMs. These drugs mimic some effects of estrogen and block others. For example, tamoxifen blocks the effects of estrogen in the breast and thus is widely used to treat and prevent breast cancers that depend on estrogen. But it has the opposite effect in the uterus, acting like estrogen to stimulate tissue growth and increasing the risk of uterine
'"/>

Contact: John Easton
John.Easton@uchospitals.edu
773-702-6241
University of Chicago Medical Center
12-May-2005


Page: 1 2 3

Related biology news :

1. New study suggests Concord grape juice may provide protection against breast cancer
2. Study suggests estrogen deficiency can lead to obesity-induced high blood pressure after menopause
3. Experiment suggests limitations to carbon dioxide tree banking
4. Immunity in social amoeba suggests ancient beginnings
5. New model for autism suggests women carry the disorder and explains age as a risk factor
6. Pediatric ritalin use may affect developing brain, new study suggests
7. Oldest DNA ever recovered suggests earth was warmer than previously believed
8. Tick-related disease thrives on cholesterol, study suggests
9. Study suggests other causes for childhood brain aneurysms
10. New study suggests potential for a broadly-protective HIV vaccine
11. DNA analysis suggests under-reported kills of threatened whales

Post Your Comments:
*Name:
*Comment:
*Email:


(Date:11/19/2019)... ... November 19, 2019 , ... ... preparation, and Bio-Rad Laboratories, Inc. (NYSE: BIO and BIOb), a global leader in ... Diagenode will offer Single-Cell ATAC-Seq (scATAC-Seq) Services, featuring Bio-Rad’s Droplet Digital PCR technology, ...
(Date:11/19/2019)... ... November 19, 2019 , ... Hosted at the Las ... MJBizCon 2019 is the largest gathering of MJBiz business professionals in the ... programming to benefit every sector, there is no show quite like it. Atlantic Ultraviolet ...
(Date:11/14/2019)... POWAY, Calif. (PRWEB) , ... November 13, 2019 , ... ... successfully enrolled the first patients in an FDA approved clinical trial for stem ... anniversary of the formation of the company as a subsidiary of VetStem Biopharma. , ...
Breaking Biology News(10 mins):
(Date:1/7/2020)... ... January 06, 2020 , ... ... announced its expansion into whole-home smart lighting with two new products: the Brilliant ... the ability for homeowners and homebuilders to affordably add high-end smart lighting to ...
(Date:12/31/2019)... ... 2019 , ... At this year's SLAS conference, Visikol will present several talks ... 3D cell culture , advanced imaging and multiplex analysis . Specifically, ... steatosis , inflammation and fibrosis as well as a 2D cell culture ...
(Date:12/27/2019)... ... December 27, 2019 , ... Vici Health Sciences is ... pipeline that offers patients and healthcare providers options in the treatment of ... collaboration with doctors and managed care professionals and developed at Vici’s R&D ...
(Date:12/18/2019)... ... December 17, 2019 , ... Philadelphia ... to announce that it has hired Dr. Alia Orbin, Ph.D., J.D., an experienced ... in the preparation, filing and prosecution of patent applications related to pharmaceutical sciences, ...
Breaking Biology Technology:
Cached News: