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:7/10/2014)...  Pomerantz LLP has filed a class action ... "Company")(NYSE-MKT: PVCT) and certain of its officers.  The ... Middle District of Tennessee , ... consisting of all persons or entities who purchased ... 2013 and May 22, 2014, both dates inclusive ...
(Date:7/10/2014)... SHELTON, Conn. , July 2, 2014 NXT-ID, Inc., ... market, reports that CEO Mr. Gino Pereira was ... radio show in Tampa Florida . Mr. ... radio host Cedric Harris and how the Wocket™ ... secure alternative.  Cedric Harris tells ...
(Date:7/10/2014)... 8, 2014 Fingerprint Cards, ... design win (DW). An Asian OEM has selected FPC1021 for ... start in August 2014.   FPC is proud ... has a planned date for start of mass production in ... of SEK 5M, for delivery in the first half of ...
Breaking Biology News(10 mins):SHAREHOLDER ALERT: Pomerantz Law Firm Announces the Filing of a Class Action against Provectus Biopharmaceuticals, Inc. and Certain Officers - PVCT 2SHAREHOLDER ALERT: Pomerantz Law Firm Announces the Filing of a Class Action against Provectus Biopharmaceuticals, Inc. and Certain Officers - PVCT 3Security and Your Money: Tampa Bay Radio Host Cedric Harris Talks to NXT-ID CEO Mr. Gino Pereira about the Wocket Smart Wallet 2Security and Your Money: Tampa Bay Radio Host Cedric Harris Talks to NXT-ID CEO Mr. Gino Pereira about the Wocket Smart Wallet 3Security and Your Money: Tampa Bay Radio Host Cedric Harris Talks to NXT-ID CEO Mr. Gino Pereira about the Wocket Smart Wallet 4FPC Wins DW and Initial Ramp Order for FPC1021 Touch Sensor for Flagship Smartphone from Asian OEM 2
... an effective vaccine for hepatitis B and public health officials ... for the infectious liver disease, tens of thousands of people ... to a new study by researchers at Brown University, missed ... why infections persist. "This is a really simple thing ...
... - A comprehensive multi-disciplinary synthesis just published in ... investigation and policy development to address significant environmental, social ... climate change. "Effects of climate change on the ... synthesis of range change prediction in a warming world" ...
... Mass. Geoscientists at the University of Massachusetts Amherst ... first evidence that warm-cold climate oscillations well known in ... also appear as tropical rainfall variations in the Amazon ... expression of these cycles in the Southern Hemisphere. ...
Cached Biology News:Many high-risk Americans don't get hepatitis B vaccine 2Many high-risk Americans don't get hepatitis B vaccine 3Climate change invites alien invaders - Is Canada ready? 2Evidence of past Southern hemisphere rainfall cycles related to Antarctic temperatures 2
(Date:7/10/2014)... UK (PRWEB) July 10, 2014 ... 21st Century Medicine Forum on ‘Commercialising Longevity Research’ ... and entrepreneurs to the London Bioscience Innovation Center ... Research Foundation and Aging Analytics Ltd. The meeting ... investment in translational research for age-related disease, as ...
(Date:7/10/2014)... Terascala, the industry leader in ... a former vice president of product management for Flexera ... of marketing. Terascala’s software when combined with leading compute ... highest performance and most reliable solutions for processing big ... channel expansion and broaden its product portfolio. His leadership ...
(Date:7/10/2014)... Robert Harman, DVM, Founder and CEO of Vet-Stem, ... announce the relaunch of his highly informative blog, now named ... “ What are Stem Cells ?” Dr. Harman’s purpose ... in the basics of stem cell therapy so that pet ... of treatment when considering regenerative medicine. , A veterinarian by ...
(Date:7/10/2014)... EvoDerma ’s NOOME Anti-Aging Motion has been upgraded ... with a second treatment cup to help prevent and smooth ... is thinner on the edges for a softer contact with ... uneven surfaces on the face, neck and décolleté. Choose to ... areas such as the cheeks and neck, or opt for ...
Breaking Biology Technology:DKV Sponsors Forum on Commercialising Longevity Research; Brings Together Scientists, Investors, Entrepreneurs and Celebrities 2DKV Sponsors Forum on Commercialising Longevity Research; Brings Together Scientists, Investors, Entrepreneurs and Celebrities 3DKV Sponsors Forum on Commercialising Longevity Research; Brings Together Scientists, Investors, Entrepreneurs and Celebrities 4DKV Sponsors Forum on Commercialising Longevity Research; Brings Together Scientists, Investors, Entrepreneurs and Celebrities 5DKV Sponsors Forum on Commercialising Longevity Research; Brings Together Scientists, Investors, Entrepreneurs and Celebrities 6Terascala Expands Executive Team 2Terascala Expands Executive Team 3Robert Harman, DVM Talks About What Stem Cells are in His Latest Blog Series for Vet-Stem, Inc. 2Robert Harman, DVM Talks About What Stem Cells are in His Latest Blog Series for Vet-Stem, Inc. 3Introducing a New Bonus Treatment Cup for EvoDerma’s NOOME Anti-Aging Motion 2
... , , , ... when revenues aren,t growing, many organizations are looking for ways to ... these things by better managing processes and the documents that go ... applications ( http://onbase.com/English/Products ). But here,s the roadblock: budgets ...
... , THE WOODLANDS, Texas, Sept. 9 Lexicon ... focused on discovering and developing breakthrough treatments for human disease, announced today ... and chief executive officer, will present at the Morgan Stanley Global Healthcare ... on Tuesday, September 15, 2009 at 1:35 p.m. Eastern Time. ...
... England, September 9 Clinical Therapeutics,(, http://www.clinicaltherapeutics.com/ ) ... the addition of Michael G. Spigarelli, MD, PhD,to ... As section editor for the Pediatric, Adolescent, ... Research section), Dr. Spigarelli brings a wealth of ...
Cached Biology Technology:Hyland Software Provides Grant Assistance to Kick-Start Technology Projects 2Hyland Software Provides Grant Assistance to Kick-Start Technology Projects 3Hyland Software Provides Grant Assistance to Kick-Start Technology Projects 4Lexicon Pharmaceuticals to Present at the Morgan Stanley Global Healthcare Unplugged Conference 2Clinical Therapeutics Announces the Addition of Michael G. Spigarelli, MD, PhD, as Editor for a Refocused Pediatric, Adolescent, & Maternal Therapeutics Section 2
Sheep polyclonal to Salmonella Thomasville ( Abpromise for all tested applications). Antigen: Native Salmonella thomasville...
anti-achaete...
... for all tested applications). ... from within residues 1 - 100 of Mouse ... proprietary) (Peptide available as ... 5453 Swiss Protein ID: ...
... Capture high-resolution chemiluminescent and bioluminescent ... High-sensitivity camera is cooled to subzero ... dynamic range for high quality images ... light-tight cabinet provides optimum conditions for ...
Biology Products: