Wednesday, November 6, 2013

New drug candidate found for deadly fungal lung infections

Rappleye's team searched a library of commercially-available small molecules used by other investigators to find new antivirals or anticancer drugs. They performed a high-throughput phenotypic screen of 3,600 compounds looking for agents that inhibited fungal, but not human, cells.
To speed the selection process, Rappleye and Edwards engineered Histoplasma cells with a fluorescent protein that made the cells glow red while inside of a living macrophage -- the type of mammalian immune cell that Histoplasma attacks and in which it reproduces.
As the number of fungal cells increased inside the macrophage, so did the fluorescence and consequently, the cells would glow brighter. However, when a macrophage was exposed to an active compound that prevents Histoplasma reproduction, it maintained the same level of brightness. This allowed the scientists to quickly determine efficacy and toxicity of the drug candidate in a natural environment.
"Not only were we able to visually screen thousands of compounds in just a few weeks, but we were also able to measure the compound's impact in a real, live host cell," said Edwards.
The team narrowed down to a primary candidate called 41F5, which is 60 times more toxic to fungal cells than human cells. Their work was published in the September Antimicrobial Agents and Chemotherapy.
The team is currently working with Werner Tjarks, PhD, a medicinal chemist at Ohio State, to see if the selectivity and toxicity profile can be enhanced further for additional testing. Rappleye is also working with the Ohio State's Technology Commercialization Office (TCO) to potentially commercialize the derivatives from 41F5.

Tuesday, November 5, 2013

Metformin could serve as radiosensitizer to treat patients with stage III non-small cell lung cancer

In continuation of my update on metformin

Treating aggressive lung cancer with the diabetes drug metformin along with radiation and chemotherapy may slow tumor growth and recurrence, suggests new preliminary findings from researchers at the Perelman School of Medicine at the University of Pennsylvania being presented during an oral abstract session October 28 at the 15th World Conference on Lung Cancer.

The pre clinical and clinical results, which have set the stage for a first-of-its-kind prospective study, point to metformin as an effective radiosensitizer-a drug that makes tumor cells more sensitive to radiation therapy-to treat stage III non-small cell lung cancer (NSCLC). Because of poor local response and five-year survival rates around 15 percent in late-stage NSCLC patients, well-tolerated, combination therapies are greatly needed.

The abstract is being presented by Ildiko Csiki, MD, PhD, an assistant professor of Radiation Oncology at Penn's Abramson Cancer Center.

Metformin, the most-widely used drug for type-2 diabetes, has been shown to have anti-cancer effects on a number of cancers, including prostate and colon. It activates AMP-related pathways, leading to inactivation of mTOR and suppression of its downstream effectors, a crucial signaling pathway for proliferation and survival of cancer. However, little data exists to support its role in NSCLC. And its role as a radiosensitizer in lung cancer is even less understood.

Two forms of Parkinson's disease identified

A consortium of researchers, headed by a team from the Laboratoire CNRS d'Enzymologie et Biochimie Structurales, is well on the way to providing an explanation. Parkinson’s disease is caused by a protein known as alpha-synuclein, which forms aggregates within neurons, killing them eventually. The researchers have succeeded in characterizing and producing two different types of alpha-synuclein aggregates. Better still, they have shown that one of these two forms is much more toxic than the other and has a greater capacity to invade neurons. This discovery takes account, at the molecular scale, of the existence of alpha-synuclein accumulation profiles that differ from one patient to the next. These results, published on October 10 in Nature Communications, represent a notable advance in our understanding of Parkinson’s disease and pave the way for the development of specific therapies targeting each form of the disease.


Friday, November 1, 2013

New Drug May Someday Battle Obesity and Diabetes - Drugs.com MedNews

New Drug May Someday Battle Obesity and Diabetes - Drugs.com MedNews

New Cholesterol-Lowering Drug, ALN-PCS Shows Early Promise

An experimental drug that lowers LDL "bad" cholesterol by helping sweep it from the bloodstream appears to be both safe and effective in its first human trial.
The drug known as ALN-PCS reduced cholesterol an average of 40 percent in the small, early study, and, if proven to work in large trials, potentially could replace or complement statins, the researchers said.
Currently, statin drugs such as Lipitor, Crestor and Zocor are widely used to control cholesterol. One heart doctor not involved with the new study said another class of drugs might be useful.
"Cardiovascular disease remains the leading cause of death of men and women globally and reduction of LDL cholesterol with statin medications has been demonstrated to substantially reduce the risk of first or recurrent cardiovascular events," said Dr. Gregg Fonarow, a professor of cardiology at the University of California, Los Angeles.

Thursday, October 31, 2013

Popular Morning Sickness Drug Safe in Pregnancy, Study Finds

Metoclopramide (INN  is an antiemetic and gastroprokinetic agent. It belongs to a group of medicines called ´dopaminergic´ blockers. It is commonly used to treat nausea and vomiting, to facilitate gastric emptying in people with gastroparesis, and as a treatment for the gastric stasis often associated with migraine headaches.




Wednesday, October 30, 2013

Overexpressed protein to be culprit in certain thyroid cancers

A specific protein once thought to exist only in the brain may play a crucial role in a deadly form of thyroid cancer, as well as other cancers, and provide a fresh target for researchers seeking ways to stop its progression, UT Southwestern Medical Center researchers report ....

Dr. Bibb and Dr. Nwariaku teamed up and launched a study of both human and mouse thyroid cancer cells. They discovered that Cdk5 was present in specific cells of the thyroid called C cells, and that the protein could escape normal cellular control and cause the cancer in both humans and mice.
Now, with the help of other UT Southwestern scientists, Dr. Bibb and Dr. Nwariaku, both members of the Harold C. Simmons Cancer Center, are making important progress in their efforts to develop new treatments for this and other more common forms of endocrine cancers. One promising example is the use of high-throughput screening for compounds that block the Cdk5 protein pathway, the researchers said.
"There are currently two FDA-approved drugs for treating neuroendocrine cancers, but neither of them blocks this specific pathway -- one this study has shown to be a crucial vulnerability in the cancer, if appropriately targeted," Dr. Bibb said. "We were surprised, but encouraged, by the finding because they link the human nervous system to disease processes that include the toughest of all foes, cancer."




More read at :Cancer Cell


Tuesday, October 29, 2013

'Peanut butter' test can help diagnose Alzheimer's disease, researchers find

A dollop of peanut butter and a ruler can be used to confirm a diagnosis of early stage Alzheimer's disease, University of Florida Health researchers have found...

Of the 24 patients tested who had mild cognitive impairment, which sometimes signals Alzheimer's disease and sometimes turns out to be something else, about 10 patients showed a left nostril impairment and 14 patients did not. The researchers said more studies must be conducted to fully understand the implications.
"At the moment, we can use this test to confirm diagnosis," Stamps said. "But we plan to study patients with mild cognitive impairment to see if this test might be used to predict which patients are going to get Alzheimer's disease."
Stamps and Heilman point out that this test could be used by clinics that don't have access to the personnel or equipment to run other, more elaborate tests required for a specific diagnosis, which can lead to targeted treatment. At UF Health, the peanut butter test will be one more tool to add to a full suite of clinical tests for neurological function in patients with memory disorders.



Monday, October 28, 2013

Flumazenil reverses stress-triggered anxiety in methamphetamine dependant rats

We know that, Flumazenil (also known as flumazepil, code name Ro 15-1788, trade names Anexate, Lanexat, Mazicon, Romazicon) is abenzodiazepine receptor antagonist primarily available by injection only, and the only benzodiazepine receptor antagonist on the market today.
It was first introduced in 1987 by Hoffmann-La Roche under the trade name Anexate, but only approved by the FDA on December 20, 1991. Some years ago an oral preparation was under development,  though it had low bio-availability and was thus abandoned.

Friday, October 25, 2013

Scientists identify new drug for inherited form of cancer with no known cure

Scientists from the Florida campus of The Scripps Research Institute (TSRI) have identified a new drug candidate for an inherited form of cancer with no known cure.  

The new study showed the drug candidate—known as FRAX97 (see structure) slowed the proliferation and progression of tumor cells in animal models of Neurofibromatosis type 2. This inherited type of cancer, caused by mutations in the anti-tumor gene NF2, leads to tumors of the auditory nerve that connects the inner ear to the brain.


The new compound, originally developed to treat neurodegenerative disease, targets a protein family known as p21-activated kinases or PAKs. These kinases (enzymes that add a phosphate group to other proteins and change their function) play a critical role in the development of Neurofibromatosis type 2. PAK1 has also been implicated in the growth of breast and lung cancers.

"Our study shows that if we inhibit these kinases we can counter the formation of tumors in this brain disease," said Joseph Kissil, a TSRI associate professor who led the study.

Thursday, October 24, 2013

Lundbeck, Otsuka to continue development of Lu AE58054 compound for Alzheimer's disease

We know that, Lu AE58054 is a potent and selective 5-HT6 receptor antagonist under development by Lundbeck as an augmentation therapy for the treatment of cognitive deficits associated with Alzheimer's disease and schizophrenia. As of February 2010 it is in phase II clinical trials...

Tuesday, October 22, 2013

Pfizer reports positive results from two tofacitinib Phase 3 trials for chronic plaque psoriasis

In continuation of my update on Tofacitinib

We know that, Tofacitinib (trade name Xeljanz, formerly tasocitinib, CP-690550) is a drug of the janus kinase (JAK) inhibitor class, discoveredand developed by Pfizer. It is currently approved for the treatment of rheumatoid arthritis (RA) in the United States and is being studied for treatment of psoriasisinflammatory bowel disease, and other immunological diseases, as well as for the prevention of organ transplant rejection. Tofacitinib was not approved by the European regulatory agencies because of concerns over efficacy and safety...


Monday, October 21, 2013

FDA Approves Adempas to Treat Pulmonary Hypertension

In continuation of my update on Adempas (riociguat)....
Food and Drug Administration today approved Adempas (riociguat) to treat adults with two forms of pulmonary hypertension...

Friday, October 18, 2013

Psoriasis Drug May Help Treat Type 1 Diabetes: Report - Drugs.com MedNews

In continuation of my update on alefacept (Amevive)

A drug formerly used to treat the skin condition psoriasis shows promise in treating type 1 diabetes, according to a new study.
Both psoriasis and type 1 diabetes are autoimmune disorders. The drug alefacept (Amevive) is an immune-suppressing drug that was used to treat psoriasis but was withdrawn by its manufacturer in 2011. The drug maker, Astellas Pharma U.S., said at the time that "business needs" led to its decision to pull the drug from the market.
The new study included 49 type 1 diabetes patients at 14 medical centers in the United States. Thirty-three of the patients received weekly injections of alefacept for 12 weeks, followed by a break of 12 weeks and then another 12 weekly doses of the drug. Sixteen patients received a placebo on the same schedule.
The clinical trial's main outcome was a measure of how well the pancreas could secrete insulin in response to food, two hours after eating. Using this measure, the researchers found no significant differences between the two groups of patients. 


Adempas drug gets FDA approval for treatment of pulmonary hypertension

The U.S. Food and Drug Administration today approved Adempas (riociguat) to treat adults with two forms of pulmonary hypertension. Pulmonary hypertension is caused by abnormally high blood pressure in the arteries of the lungs.


Adempas drug gets FDA approval for treatment of pulmonary hypertension