Navigation Links
A new mechanism for reversible proteasome inhibition
Date:12/13/2010

. While healthy cells survive by building up a new proteasome, the fast-growing cancer cells suffocate in their own waste and end up in apoptosis.

The trick of both of these proteasome blockers is a two-step reaction. The tiny molecule fits a specific site on the proteasome like a key going into a lock. However, the reversible docking at the binding site is followed by an irreversible ring formation that prevents the key from being pulled back out. By choosing another head group, Professor Michael Groll und Dr. Melissa Graewert were able to achieve a reversible ring formation. The new head group contains an aldehyde and a keto group in immediate proximity. They also react with the binding sites on the proteasome by forming a ring. However, the reaction of these two groups is reversible: The key can be removed from the lock and the proteasome can resume its work.

Within the framework of their work supported by the Cluster of Excellence Center for Integrated Protein Science Munich (CIPSM), the TUM scientists succeeded in confirming the assumed mechanism using X-ray structure analysis of inhibited proteasome crystals. It also became clear how this binding mechanism could be developed into a drug with fewer side effects. In addition to the head group, the binding mechanism contains a short chain of amino acids that can be designed to fit into the binding pockets of the proteasome. By varying the amino acids, the binding can be optimized to specifically attack immuno-proteasomes.

"The reversible two-step binding mechanism shown here is unique to proteasomes," says Michael Groll, who holds the Chair of Biochemistry at the Department of Chemistry of the Technische Universitaet Mnchen. "This explains the high selectivity and leads us to expect relatively minor side effects. The reversible reaction opens up a much wider field of application. We can now develop these binding mechanisms further in the direction of immunosuppressive agents." It is pre
'/>"/>

Contact: Andreas Battenberg
battenberg@zv.tum.de
49-892-891-0510
Technische Universitaet Muenchen
Source:Eurekalert  

Page: 1 2 3

Related medicine news :

1. IU research team discovers TB disease mechanism and molecule to block it
2. UCR researcher identifies mechanism malaria parasite uses to spread in red blood cells
3. Tumor mechanism identified
4. Multiple sclerosis, Italian researchers discover a possible onset mechanism for the disease
5. Pancreatic Cancer Study Reveals Mechanism Initiating Disease, In Mice
6. Pancreatic cancer study reveals mechanism initiating disease, in mice
7. Study identifies 1 of the mechanisms behind breast cancer metastasis
8. Mechanism that may trigger degenerative disease identified
9. A key mechanism links virgin olive oil to protection against breast cancer
10. Scripps Research scientists uncover previously unknown natural mechanism that controls cocaine use
11. Study makes exciting progress in elucidating the mechanisms of bortezomib in lymphoma
Post Your Comments:
*Name:
*Comment:
*Email:
Related Image:
A new mechanism for reversible proteasome inhibition
(Date:1/22/2015)... Gabe’s Chemo Duck Program is pleased to announce the release of ... kids with cancer. The Chemo Duck App, available on iTunes for ... games to help children of all ages living with cancer adjust ... kids entertained, educated and at ease while waiting for clinic visits ...
(Date:1/22/2015)... Angelweddingdress is a famous wedding dress company ... to follow it on Facebook, Twitter, and Pinterest. The fans ... Angelweddingdress draws a lottery every week. , Moreover, the company ... 2015. Click Angelweddingdress homepage for more information. ...
(Date:1/22/2015)... 2015 Juvent Sports ( http://www.juventsports.com ) ... PGA Merchandise Show to bestow a Juvent Sports Achievement ... golfer, Arlene McKitrick. The award commemorated and congratulated McKitrick ... win. She won her first amateur tournament in 1979 ...
(Date:1/22/2015)... 2015 For over 20 years, Dr. David Cruz ... Vista area has treated just about every type of injury ... And for those same twenty-plus years, the team at ... injuries with the best possible doctor. With the combined ...
(Date:1/22/2015)... La Jolla, Calif. (PRWEB) January 22, 2015 ... and Assemblymembers Susan Bonilla (D-Concord) and Kristin Olsen ... (CHI) for their leadership in advancing biotechnology, biomedical ... Mitchell, Bonilla and Olsen each received the “2014 ...
Breaking Medicine News(10 mins):Health News:Chemo Duck Launches First App Ever Created for Kids with Cancer 2Health News:Chemo Duck Launches First App Ever Created for Kids with Cancer 3Health News:Angelweddingdress Invites Its Customers To Follow It On Facebook, Twitter, And Pinterest 2Health News:All-Time Leading Female Amateur Golfer Arlene McKitrick Receives Juvent Sports Achievement Award at 2015 PGA Show 2Health News:All-Time Leading Female Amateur Golfer Arlene McKitrick Receives Juvent Sports Achievement Award at 2015 PGA Show 3Health News:Industry Leading Chiropractor in Oceanside Joins the Doctors on Liens Network 2Health News:California Biomedical Community Honors Senator Holly Mitchell, Assemblymembers Susan Bonilla & Kristin Olsen 2Health News:California Biomedical Community Honors Senator Holly Mitchell, Assemblymembers Susan Bonilla & Kristin Olsen 3
... than 20% of men in western cultures are affected ... suffer from OSA experience more harmful //psychological symptoms than ... in Journal of Forensic Sciences. ,Sex ... Continuous Positive Airway Pressure(CPAP), whereby compressed air is applied ...
... tooth whitening product found to have no negative health ... by Dr. Ian Monroe, entitled, "Use of Hydrogen Peroxide-Based ... ,The article was published in Journal ... including unpublished clinical studies of over 4000 human subjects. ...
... Diabetes Center, global leader in diabetes research, care ... Health, Inc. as an independent company. //The first ... Veraxa will market the Joslin Vision NetworkTM (JVN), ... developed by Joslin to address a significant patient ...
... multi-tasking and walking the tightrope to make a success of ... can chew! Though, such qualities //are the epitome of the ... pat on the back for such back-breaking endeavors. Today’s ... due to the build up of stress and over work ...
... replacement therapy for men with low testosterone levels appears ... to some reports that this therapy may be harmful, ... of JAMA, a theme issue on men's health. ... Research Foundation and University of California, Los Angeles, presented ...
... President, Dr Mukesh Haikerwal, today congratulated the Government on ... consultation // with the AMA, and which delivers for ... pleased that the draconian conditions and red tape associated ... ,'The Government has agreed that the expertise in ...
Cached Medicine News:Health News:Joslin Diabetes Center Launches Veraxa Health 2Health News:Joslin Diabetes Center Launches Veraxa Health 3Health News:Joslin Diabetes Center Launches Veraxa Health 4Health News:Joslin Diabetes Center Launches Veraxa Health 5Health News:Testosterone Replacement Therapy Appears Safe for Prostate 2Health News:Government Strikes Right Balance with PBS Reform 2
(Date:1/22/2015)... Jan. 22, 2015 /PRNewswire/ - Pivotal Therapeutics Inc. (OTCQX:PVTTF; CSE:PVO), ("Pivotal" ... on Omega-3 therapies for cardiovascular disease and overall health is ... accomplishments in 2014 and its outlook for 2015 from the ... Shareholders, We would like to take this opportunity ...
(Date:1/22/2015)... 22, 2015  Profil Institute for Clinical Research, Inc., a ... announced today a new textbook,  Translational Research Methods for ... a leading global scientific publisher. The textbook ... for use in early phase clinical studies of new ...
(Date:1/22/2015)... , Jan. 22, 2015 Research and Markets ... of the "Microbiology Testing/Clinical Microbiology Market by ... Forecast to 2019" report to their offering. ... array of techniques for the detection of infectious ...
Breaking Medicine Technology:Pivotal Therapeutics: Year in Review and CEO Update 2Pivotal Therapeutics: Year in Review and CEO Update 3Pivotal Therapeutics: Year in Review and CEO Update 4Pivotal Therapeutics: Year in Review and CEO Update 5Pivotal Therapeutics: Year in Review and CEO Update 6Pivotal Therapeutics: Year in Review and CEO Update 7New Textbook "Translational Research Methods for Diabetes, Obesity and Cardiometabolic Drug Development" Provides Critical Review Of Current And Emerging Clinical Investigation Methods 2New Textbook "Translational Research Methods for Diabetes, Obesity and Cardiometabolic Drug Development" Provides Critical Review Of Current And Emerging Clinical Investigation Methods 3Global Microbiology Testing/Clinical Microbiology (Instrument, Analyzer, Incubator, Kit, Microscope, Molecular Diagnostics) Market - Forecast to 2019 2Global Microbiology Testing/Clinical Microbiology (Instrument, Analyzer, Incubator, Kit, Microscope, Molecular Diagnostics) Market - Forecast to 2019 3
... BOSTON, Dec. 7 The Epilepsy Research Foundation (ERF), a ... Family Foundation, a private philanthropic foundation, today announced two new ... in funding. The grant awards were announced by the ... the Milken Family Foundation, during the 7th Judith Hoyer Lecture ...
... , ENGLEWOOD, Colo., Dec. 7 Baxa ... during this week,s ASHP Midyear Clinical Meeting (MCM). DoseEdge ... and pharmacy efficiency through the management of IV and ... current pharmacy practice and techniques, while providing a framework ...
Cached Medicine Technology:The Epilepsy Research Foundation and Milken Family Foundation Announce Prestigious Translational Research Grants for Two Pioneering Epilepsy Therapies 2The Epilepsy Research Foundation and Milken Family Foundation Announce Prestigious Translational Research Grants for Two Pioneering Epilepsy Therapies 3The Epilepsy Research Foundation and Milken Family Foundation Announce Prestigious Translational Research Grants for Two Pioneering Epilepsy Therapies 4The Epilepsy Research Foundation and Milken Family Foundation Announce Prestigious Translational Research Grants for Two Pioneering Epilepsy Therapies 5Baxa Features DoseEdge(TM) Pharmacy Workflow Manager at the ASHP Midyear Clinical Meeting 2Baxa Features DoseEdge(TM) Pharmacy Workflow Manager at the ASHP Midyear Clinical Meeting 3
... Bowman Perfusion Monitor runs continuously and displays ... In the automatic (autopilot) mode, the monitor ... a pre-determined set of rules. The rules ... tissue perfusion, as well as tissue temperature, ...
... Laserflo BPM2 is designed to give ... data in neurosurgical intensive care, trauma, ... is safe and easy to use, ... hemodynamics. The built-in audible alarm alerts ...
... Clinitemp Perfusion Monitor Strips are non-invasive and ... or maintain. Clinitemp Perfusion Monitor Strips are ... are accurate and reliable. The advanced liquid ... in a wide range of applications including ...
... highly featured laser doppler system for ... from multiple tissue sites. This latest ... Signal Processing (DSP) and laser Doppler ... simple to use, multi-channel monitor, setting ...
Medicine Products: