Old drugs find new target for treating brain tumor

In continuation of erlotinib ................................

Old drugs find new target for treating brain tumor

Researchers discover new class of antimalarial compounds...

Researchers have discovered a group of chemical compounds that might one day be developed into drugs that can treat malaria infection in both the liver and the bloodstream. The study, which appears in the Nov. 18 issue of Science, was led by Elizabeth A. Winzeler, Ph.D., of the Scripps Research Institute in La Jolla, Calif., and was partially funded by the National Institute of Allergy and Infectious Diseases (NIAID), part of the National Institutes of Health.

By screening more than 4,000 chemical compounds that had previously shown activity against blood-stage Plasmodium, the investigators searched for a compound that would also inhibit liver-stage parasites and whose protein structure would allow the modification necessary for future drug development. They found that a group of three related compounds, known collectively as the imidazolopiperazine (IP) cluster, fit these criteria. In addition, strains of Plasmodium that had acquired resistance to other malaria drugs were susceptible to the IP cluster.

Using the IP cluster as a foundation, the researchers designed a drug candidate, GNF179, that reduced levels of one Plasmodium species by 99.7 percent and extended survival by an average of 19 days when tested in malaria-infected mice. By examining infected cells, the researchers confirmed that GNF179 (see the structure) was active in the liver stage of infection. Rresearchers note that while additional studies will be needed to fully understand the drug's mechanism of action and its specific targets within the liver, this study provides a potential starting point for developing new dual-stage antimalarial drugs.....

More : http://www.sciencemag.org/content/early/2011/11/16/science.1211936.abstract

New efficient synthesis for Taxol ?

In continuation of my update on taxol....

Baran's group reports erecting that Rockefeller tree and adding the first few ornaments -- a molecule called taxadiene. A conventional taxadiene synthesis is inefficient and involves 26 steps to produce. The Baran group's method involves just 10 steps to produce many times what has been previously synthesized -- more than sufficient for planned research to find a way to efficiently produce Taxol®.

Innovation Leads to Access.....

The taxadiene synthesis is more than just a midway stop on the way to Taxol®. The current commercial Taxol® production method, which involves culturing cells from the yew tree, is more economical than any new synthesis is likely to be. Instead, Baran and his team are aiming to understand the processes used in nature to produce the compound, which are many times more efficient than those used by scientists to date. "It's my opinion that when there's a huge discrepancy between the efficiency of nature and humans, in the space between, there's innovation.

More specifically, lead researcher Phil Baran believes that, while developing an efficient synthesis for Taxol®, they will gain a fundamentally improved understanding of the chemistry involved and develop more widely applicable techniques. Such innovation could allow production of a whole range of taxanes currently inaccessible for drug discovery research either because the quantities researchers can produce are vanishingly small, or because they can't produce them at all. Control of the taxane oxidation process therefore offers the potential for discovering new and important drugs, perhaps even one or more that is better at fighting specific cancers than Taxol®.

Establishing the remaining steps between taxadiene and Taxol® or other more complex taxanes remains a challenging task that Baran estimates will take years.

"Nature has a choreography in the way she decorates the tree," he said. "It's a precise dance she has worked out over millennia. We have to figure out a way to bring that efficiency to the laboratory setting."

More... : http://www.nature.com/nchem/journal/vaop/ncurrent/full/nchem.1196.html

Janssen receives FDA approval for Xarelto to prevent stroke in people with AF

In continuation of my up date on rivaroxaban.....

Janssen receives FDA approval for Xarelto to prevent stroke in people with AF: The U.S. Food and Drug Administration today approved the anti-clotting drug Xarelto (rivaroxaban) to reduce the risk of stroke in people who have abnormal heart rhythm.

Universitat de Barcelona - A scientific study describes new benefits of nut consumption

In continuation of my update on the benefits of nuts...

Universitat de Barcelona - A scientific study describes new benefits of nut consumption

Crocin for multiple sclerosis?

Medical researchers at the University of Alberta have discovered that an active ingredient in the Persian spice saffron may be a potential treatment for diseases involving neuroinflammation, such as multiple sclerosis. Researchers found there is a compound in saffron, known as crocin (see the structure below), that exerts a protective effect in brain cell cultures and other models of MS. It prevented damage to cells that make myelin in the brain.

Lead researcher  Power said. "Myelin is insulation around nerves. MS is characterized by inflamed brain cells that have lost this protective insulation, which ultimately leads to neurodegeneration.......

More......

Probiotics effective in combating antibiotic-associated diarrhea, studies find; 'Good bugs' look promising as anti-inflammatory agents

Probiotics effective in combating antibiotic-associated diarrhea, studies find; 'Good bugs' look promising as anti-inflammatory agents

Ref : http://www.nature.com/ajg/journal/v106/n10/full/ajg2011201a.html

World's most efficient flexible organic light-emitting diodes created on plastic

World's most efficient flexible organic light-emitting diodes created on plastic

In continuation of my update on usefulness of benzodiazepine derivatives

Lundbeck Inc. presented interim data from its long-term, open-label extension study evaluating ONFI™ (clobazam see structure below) CIV for the adjunctive treatment of drop seizures associated with Lennox-Gastaut syndrome (LGS). Company claims that, these interim results support the reductions in drop seizure rates associated with ONFI when used as add-on therapy for adult and pediatric patients, two years of age or older, with a current or previous diagnosis of LGS. ....

More....

Biogen’s Multiple Sclerosis pill succeeds at a late phase clinical trial

Biogen Idec Inc. has reported success in a late stage clinical trial of its oral multiple sclerosis drug BG-12 (see below structure), a competitor's of Teva Pharmaceutical Industries’ Laquinimod. A 240-milligram dose of BG-12 administered two or three times a day significantly reduced the proportion of patients who relapsed by 49% and 50%, respectively, after two years compared with a placebo....

Company adds that, in addition to significantly reducing ARR, BG-12 met all secondary relapse and MRI endpoints for both dose regimens.....

Ref : http://www.biogenidec.com/PRESS_RELEASE_DETAILS.aspx?ID=5981&ReqId=1621631