Daily non-political popular news in brief.

Enzyme structure reveals new drug targets for cancer and other diseases

Researchers now have a clearer understanding of how a key protein controls gene activity and how mutations in the protein may cause disease. The work could provide new avenues to design drugs aimed at cancer, diabetes, HIV, and heart disease.

Read more »

Keywords: enzyme, structure, reveals, drug, targets, cancer, diseases, reveal, target, disease

« Previous | Next »

Similar news on "Enzyme structure reveals new drug targets for cancer and other diseases":

1. Advance in understanding of blood pressure gene could lead to new treatments
   02-04-2007 · EurekAlert!
   Research by scientists at UCL (University College London) has clearly demonstrated for the first time the structure and function of a gene crucial to the regulation of blood pressure. The discovery could be important in the search for new treatments for illnesses such as heart disease, the UK's biggest killer. In a paper published online today in Nature Medicine, the team, led by Professor Patrick Vallance and Dr James Leiper, UCL Department of Medicine, reveal the role of the human gene dimethylarginine dimethylaminohydrolase (DDAH), showing that loss of DDAH activity disrupts nitric oxide (NO) production. NO is critical in the regulation of blood pressure, nervous system functions and the immune system. The role of DDAH is to break down modified amino acids (Asymmetric dimethylarginine (ADMA) and monomethyl arginine (L-NMMA)) that are produced by the body and have been shown to inhibit NO synthase. These molecules accumulate in various disease states including diabetes, renal failure and pulmonary and systemic hypertension, and their concentration in plasma (the fluid component of blood) is strongly predicative of cardiovascular disease and death. In a healthy human body, the majority of ADMA is eliminated through active metabolism by DDAH. Scientists have hypothesised that if DDAH function is impaired, NO production is reduced, and that this could be an important feature of increased cardiovascular risk. To examine this pathway in more detail, the researchers deleted the DDAH gene in mice. These mice went on to develop hypertension, or high blood pressure. They also designed specific inhibitors (small molecules) which bind to the active site of human DDAH. These small molecule inhibitors also induced hypertension in mice, confirming the importance of DDAH in the regulation of blood pressure. Dr Leiper, UCL Medicine, said: “These genetic and chemical approaches to disrupt DDAH showed remarkably consistent results, and provide compelling evidence that loss of DDAH function increases the concentration of ADMA and thereby disrupts vascular NO signalling. “There has been considerable scientific interest in this pathway and the role of ADMA as a novel risk factor, but so far there's been little evidence to support the idea that it's a cause of disease, rather than just a marker. Genes and their pathways are crucial to our understanding of cardiovascular disease and a better understanding of DDAH-1 could lead to important new treatments. “It could help us to establish if genetic variation predisposes certain people to these diseases, or whether environmental factors exert some of their effects through modulation of DDAH activity. “Our research also shows that this pathway could be harnessed therapeutically to limit production of NO in certain situations where too much nitric oxide is a bad thing; for example, hypotension and septic shock. These are some of the biggest problems in intensive care medicine and there is a huge unmet need for drug treatments.” The study, which was carried out at UCL's Rayne Institute, was funded by grants from the British Heart Foundation, the Wellcome Trust and the Medical Research Council. Professor Jeremy Pearson, Associate Medical Director of the British Heart Foundation, said: "The unexpected finding in the 1980s that a simple gas, nitric oxide (NO), is made by cells in the blood vessel wall and is a powerful control of blood vessel relaxation led to the award of the Nobel Prize in 1998 to its discoverers. "More recently, there has been increasing evidence that impairment of NO production is likely to be an important factor in the development of heart and circulatory disease, but the mechanisms responsible are not fully understood. "This study suggests for the first time that the loss of the activity of the enzyme DDAH-1 leads to reduced NO production and may cause heart and circulatory disease. These findings are likely to be important in the search for new ways to optimise the health of our blood vessels." ### Notes for Editors 1. For more information, please contact Ruth Metcalfe in the UCL Media Relations Office on tel: +44 (0)20 7679 9739, mobile: +44 (0)7990 675 947, out of hours: +44 (0)7917 271 364, e-mail: r.metcalfe@ucl.ac.uk2. 'Disruption of methylarginine metabolism impairs vascular homeostasis' is published in the February issue of the journal Nature Medicine. Advance online publication is embargoed to 18.00 GMT (13.00 US Eastern) Sunday 4 February 2007. Journalists can obtain copies of the paper by contacting the UCL Media Relations Office.3. The study was funded by the British Heart Foundation, the Wellcome Trust and the Medical Research Council. About UCL Founded in 1826, UCL was the first English university established after Oxford and Cambridge, the first to admit students regardless of race, class, religion or gender, and the first to provide systematic teaching of law, architecture and medicine. In the government's most recent Research Assessment Exercise, 59 UCL departments achieved top ratings of 5* and 5, indicating research quality of international excellence. UCL is the fourth-ranked UK university in the 2006 league table of the top 500 world universities produced by the Shanghai Jiao Tong University. UCL alumni include Mahatma Gandhi (Laws 1889, Indian political and spiritual leader); Jonathan Dimbleby (Philosophy 1969, writer and television presenter); Junichiro Koizumi (Economics 1969, Prime Minister of Japan); Lord Woolf (Laws 1954, Lord Chief Justice of England & Wales); Alexander Graham Bell (Phonetics 1860s, inventor of the telephone), and members of the band Coldplay.
   Similar news · Read more »
   
2. Enzyme inhibitor produces stable disease in patients with advanced solid cell cancers
   11-08-2006 · EurekAlert!
   Preliminary trials of a MEK enzyme inhibitor have shown that it is capable of producing long-lasting stable disease in patients with advanced solid cancers. Tests showed that the drug inhibited key targets in the patients' tumours, and now it is being tested in phase II clinical trials according to research presented at the 18th EORTC-NCI-AACR Symposium on Molecular Targets and Cancer Therapeutics in Prague.
   Similar news · Read more »
   
3. Alzheimer's enzyme acts as a tumor suppressor
   06-07-2007 · EurekAlert!
   Researchers at Burnham Institute for Medical Research ("Burnham") have provided the first evidence that gamma-secretase, an enzyme key to the progression of Alzheimer's, acts as a tumor suppressor by altering the pathway of epidermal growth factor receptor (EGFR), a potential treatment target for cancer. Expedited to publication online by Proceedings of the National Academy of Sciences, these findings reveal a limitation of targeting gamma-secretase for treatment of Alzheimer's and potentially other diseases.
   Similar news · Read more »
   
4. UIC chemists characterize Alzheimer's neurotoxin structure
   12-03-2007 · EurekAlert!
   A team of UIC chemists has characterized the molecular structure of the intermediate stage of plaque-forming amyloid fibrils, believed to cause Alzheimer's disease. The finding may lead to new drug targets for this and other amyloid diseases, such as Parkinson's and Creutzfeldt-Jakob.
   Similar news · Read more »
   
5. Jefferson scientists uncover key pathway, potential drug targets in autoinflammatory disease
   11-12-2007 · EurekAlert!
   Molecular biologists at Jefferson's Kimmel Cancer Center in Philadelphia have detailed the cascade of cellular events behind some potentially dangerous autoinflammatory diseases. In doing so, they not only have gained a greater understanding of the disease process, but have also identified new potential drug targets for diseases ranging from arthritis to cancer.
   Similar news · Read more »
   
6. Tequila raw ingredient being developed into drug-carrier that targets colon diseases
   03-27-2007 · EurekAlert!
   Compounds derived from the blue agave, a fruit used to make tequila, show promise as a natural, more effective way to deliver drugs to the colon than conventional drug-carriers, according to chemists at the University of Guadalajara in Mexico. The discovery could lead to improved treatments for a variety of colon diseases, including ulcerative colitis, irritable bowel and cancer, they say. The research will be presented in March at the American Chemical Society national meeting.
   Similar news · Read more »
   
7. Telomerase enzyme structure provides significant new target for anti-cancer therapies
   11-13-2007 · EurekAlert!
   Inappropriate activation of a single enzyme, telomerase, is associated with the uncontrollable proliferation of cells seen in as many as 90 percent of all of human cancers. Scientists have long eyed the enzyme as an ideal target for developing broadly effective anti-cancer drugs. Now, researchers working at the Wistar Institute have brought this goal closer by deciphering the 3-D structure of a domain, or region, of the telomerase molecule essential for the enzyme's activity.
   Similar news · Read more »
   
8. Drug that interrupts a key stage of cell division shows promise for advanced solid tumors
   11-08-2006 · EurekAlert!
   One of the first studies to investigate the effects of a new anti-cancer drug in patients with advanced or metastatic solid tumours has shown that it is capable of halting progression of the disease, and the study has provided the first proof of the drug's mechanism of action, the 18th EORTC-NCI-AACR Symposium on Molecular Targets and Cancer Therapeutics in Prague was told on Wednesday.
   Similar news · Read more »
   
9. Researchers reveal genetic secrets of devastating human parasite
   09-20-2007 · EurekAlert!
   An international team of researchers has revealed the genetic secrets of one of the world's most debilitating human parasites, Brugia malayi, which the World Health Organization estimates has seriously incapacitated and disfigured more than 40 million people around the globe. The study reveals dozens of potential new targets for drugs or vaccines and should provide new opportunities for understanding, treating and preventing elephantiasis, the disfiguring disease caused by the Brugia malayi parasite.
   Similar news · Read more »
   
10. A new target for the treatment of breast cancer
    01-11-2007 · EurekAlert!
    The active ingredient in a drug currently being tested to treat rheumatoid arthritis might also one day serve as an effective means of treating one of the deadliest forms of breast cancer. Berkeley Lab researchers have demonstrated that inhibiting the activity of the protease enzyme known as TACE can deprive tumor cells of a key factor needed for their proliferation. TACE is strongly present in a form of breast cancer which responds poorly to current therapies.
    Similar news · Read more »