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.
John Easton | EurekAlert!
Microscope measures muscle weakness
16.11.2018 | Friedrich-Alexander-Universität Erlangen-Nürnberg
Good preparation is half the digestion
16.11.2018 | Max-Planck-Institut für Stoffwechselforschung
Researchers at the University of New Hampshire have captured a difficult-to-view singular event involving "magnetic reconnection"--the process by which sparse particles and energy around Earth collide producing a quick but mighty explosion--in the Earth's magnetotail, the magnetic environment that trails behind the planet.
Magnetic reconnection has remained a bit of a mystery to scientists. They know it exists and have documented the effects that the energy explosions can...
Biochips have been developed at TU Wien (Vienna), on which tissue can be produced and examined. This allows supplying the tissue with different substances in a very controlled way.
Cultivating human cells in the Petri dish is not a big challenge today. Producing artificial tissue, however, permeated by fine blood vessels, is a much more...
Faster and secure data communication: This is the goal of a new joint project involving physicists from the University of Würzburg. The German Federal Ministry of Education and Research funds the project with 14.8 million euro.
In our digital world data security and secure communication are becoming more and more important. Quantum communication is a promising approach to achieve...
On Saturday, 10 November 2018, the research icebreaker Polarstern will leave its homeport of Bremerhaven, bound for Cape Town, South Africa.
When choosing materials to make something, trade-offs need to be made between a host of properties, such as thickness, stiffness and weight. Depending on the application in question, finding just the right balance is the difference between success and failure
Now, a team of Penn Engineers has demonstrated a new material they call "nanocardboard," an ultrathin equivalent of corrugated paper cardboard. A square...
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16.11.2018 | Life Sciences
16.11.2018 | Life Sciences