Navigation Links
Tamoxifen-like drug suggests new ways to selectively block estrogen

/p>

A newer group of drugs, known as selective estrogen receptor down-regulators, or SERDs, have a more potent anti-estrogen effect, involving destabilization of the estrogen receptor, which leads to its degradation.

GW5638 fits somewhere in the middle, acting like a SERM in some tissues and more like a SERD in others, including mammary tissue, where it is a powerful estrogen antagonist. As a consequence, GW 5638 can inhibit the growth of breast cancers that have become resistant to tamoxifen. It may also be more effective than tamoxifen at preventing cancer in women at high risk.

Equally important was learning how the very slight difference between tamoxifen and GW5638 altered the interactions between the estrogen receptor and other molecules that are regulated by the estrogen receptor.

Estrogen, tamoxifen and GW5638 all bind to the estrogen receptor in the same "pocket," but after binding they change the shape, or conformation, of the receptor in different ways. GW5638 pushes one small part of the estrogen receptor, a peptide spiral called helix 12, out of place. By shifting helix 12 to an odd spot, GW5638 disrupts the ways in which several other molecules that normally interact with the estrogen receptor go about their jobs.

These molecules, called coactivators or corepressors, can enhance or repress the effects of estrogen. They are present at different levels in different tissues.

"H12 positioning is essential for these interactions," Greene said. "By changing the conformation of the estrogen receptor, this drug changes the way it interacts with a whole series of related downstream molecules. And those interactions explain why these drugs have different effects in different locations, such as breast, bone or uterus."

This finding opens a new arena for drug design, suggests Greene. Nuclear receptors, such as the estrogen receptor, are major drug targets, accounting for more than 20 percent of all drugs. This fi
'"/>

Source:University of Chicago Medical Center


Page: 1 2 3

Related biology news :

1. Insight into natural cholesterol control suggests novel cholesterol-lowering therapy
2. Light therapy may combat fungal infections, new evidence suggests
3. Major new UNC-based drinking water study suggests pregnancy fears may be overstated
4. Community MRSA is re-emergence of 1950s pandemic, study suggests
5. Neandertal femur suggests competition with hyenas and a shift in landscape use
6. Discovery suggests why stem cells run through stop signs
7. Research suggests fitness of Florida panthers improved by limited breeding with Texas animals
8. Preventing a pandemic: Study suggests strategies for containing a flu outbreak
9. Logging doubles threat to the Amazon, rivaling clear-cutting, study suggests
10. Storing carbon to combat global warming may cause other environmental problems, study suggests
11. Same-sex mating by fungi spawned infection outbreak, evidence suggests
Post Your Comments:
*Name:
*Comment:
*Email:
TAG: Tamoxifen like drug suggests new ways selectively block estrogen

(Date:8/27/2014)... Aug. 27, 2014  WaferGen Bio-systems, Inc. (NASDAQ: WGBS) ... underwritten public offering of units of common stock and ... gross proceeds of $20 million, prior to deducting underwriting ... Company.  The shares and warrants are immediately separable and ... sold in the offering consists of 2,000 shares of ...
(Date:8/27/2014)... 2014 Reportlinker.com announces that a new ... Law Enforcement Biometrics Market in North ... About Biometrics Biometrics is a technology ... of their physical or behavioral patterns. It involves ... such as fingerprints, face recognition, DNA, palm print, ...
(Date:8/27/2014)... it only requires nerve cells to rearrange existing patterns ... generate new patterns, a study of monkeys has found. ... recordings of electrical activity of brain cell networks. The ... Health. , "We looked into the brain and may ... the box," said Aaron Batista, Ph.D., an assistant professor ...
Breaking Biology News(10 mins):WaferGen Bio-Systems Announces Successful Completion of Public Offering Raising $20 Million 2WaferGen Bio-Systems Announces Successful Completion of Public Offering Raising $20 Million 3Law Enforcement Biometrics Market in North America 2014-2018 2Law Enforcement Biometrics Market in North America 2014-2018 3Law Enforcement Biometrics Market in North America 2014-2018 4Law Enforcement Biometrics Market in North America 2014-2018 5Scientists plug into a learning brain 2Scientists plug into a learning brain 3
... have developed a new type of miniature endoscope that ... application of minimally invasive diagnostic and therapeutic procedures. ... from the Wellman Center for Photomedicine at MGH describes ... in a mouse model. , "This new ...
... botulism following cosmetic injections to the face indicates that ... resulted in toxin levels up to 40 times the ... the November 22/29 issue of JAMA. , Botulism ... of the spore-forming bacterium Clostridium botulinum and toxin-producing strains ...
... from Indiana University Bloomington and eight collaborating institutions ... of bacteria that live in rocks 2.8 kilometers ... rely on radioactive uranium to convert water molecules ... a confirmed expansion of Earth's biosphere, the three-dimensional ...
Cached Biology News:Three-dimensional, miniature endoscope opens new diagnostic possibilities 2Highly concentrated botulinum preparation for cosmetic injections can result in severe illness 2Highly concentrated botulinum preparation for cosmetic injections can result in severe illness 3Bacteria that use radiated water as food 2Bacteria that use radiated water as food 3
(Date:8/27/2014)... YORK , Aug. 27, 2014 ... is available in its catalogue: Global ... http://www.reportlinker.com/p02316662/Global-Chelating-Agents-Market-2014-2018.html About Chelating Agent A ... form covalent bonds with metal ions, thereby forming ... that some metal-ions have on chemical processes, formulations, ...
(Date:8/27/2014)... 27, 2014 Guggenheim Securities, the investment banking ... the hiring of veteran equity analyst Charles "Tony" Butler ... Butler will focus on the biotech/biopharma sector. ... of experience and a broad network of relationships in ... Director and Head of Equities at Guggenheim Securities. "His ...
(Date:8/27/2014)... 2014  ARCH Venture Partners, one of the ... development of seed and early-stage advanced technology companies, ... with more than $400 million in subscriptions. ARCH ... target by more than $150 million. ... and potential of our approach to finding and ...
(Date:8/27/2014)... OR (PRWEB) August 27, 2014 According ... “Consolidation continues to reshape the look and feel of ... Consumer demand for higher-quality ingredients will push for more ... American market have experienced strong market growth in the ... attributes in their food and cosmetics to fit a ...
Breaking Biology Technology:Global Chelating Agents Market 2014-2018 2Global Chelating Agents Market 2014-2018 3Global Chelating Agents Market 2014-2018 4Guggenheim Securities Hires Analyst Charles "Tony" Butler to Expand Healthcare Coverage 2Latest ARCH Venture Partners Fund Closes Above $400 Million 2Latest ARCH Venture Partners Fund Closes Above $400 Million 3Daring to be Different Raw Materials & Ingredient Supply Shortage Fuels Vital Force™ Technology New Ingredient Enhancements 2Daring to be Different Raw Materials & Ingredient Supply Shortage Fuels Vital Force™ Technology New Ingredient Enhancements 3
... Networks Corporation s recent acquisition of Network Engineering ... brings NEAs strength in the key technology of voice ... announced it bought the Wausau-based IT firm last week ... keep all of NEAs 22 employees. , ,"The combination ...
... interested in achieving greater efficiencies in product development and ... the University of Wisconsin-Madisons Center for Quick Response ... in Biotech briefing, co-hosted by the center and ... held Wednesday, Aug. 18 from 9 a.m. to noon ...
... aimed at protecting businesses , ,MADISON, Wis. ... with MasterCard to help battle online identity ... , ,Under the arrangement, NameProtect will use its technology ... other forms of payment fraud. Phishing describes the act ...
Cached Biology Technology:Berbee acquisition could expand VoIP in Wisconsin 2NameProtect and MasterCard unite to combat online fraud, phishing 2
... technology, SilenceMag is the most efficient ... and easy to use, SilenceMag is ... designed for siRNA delivery, SilenceMag allows ... doses of siRNA.,SilenceMag formulation gives reliable ...
... between the various commercial and lab-prepared glass ... the length and GC content of the ... protocol employed all influence the optimal hybridization ... all the different variables to consider, it ...
... Feature Extraction Software reads and ... to prepare microarray data for ... * one 2-year license ... NFP/Academic accounts , * ...
... The DMW143 taken from the SMZ line ... environments of production and testing. It is available ... base (FBGG) or a space-saving compact base (N2GG). ... computer, TV and a projector all at the ...
Biology Products: