In continuation of my update on tamoxifen
Wednesday, January 2, 2013
Tuesday, January 1, 2013
Scientists design small molecules that recognize myotonic dystrophy-associated RNAs
In continuation of my update on RNAs
Killing the message: An approach to direct the cleavage of RNA targets with small molecules in living cells is described (see scheme). A bifunctional small molecule (purple) that recognizes a specific three nucleotide repeat sequence and cleaves that sequence in response to light was shown to be effective at degrading the myotonic dystrophy type 1 (DM1) extended repeat RNAs, affecting biological functions.
Ref : http://onlinelibrary.wiley.com/doi/10.1002/anie.201206888/abstract
Monday, December 31, 2012
Chinese medicine yields secrets: Atomic mechanism of two-headed molecule derived from Chang Shan, a traditional chinese herb
The mysterious inner workings of Chang Shan a Chinese herbal medicine used for thousands of years to treat fevers associated with malaria have been uncovered thanks to a high-resolution structure solved at The Scripps Research Institute (TSRI). Described in the journal Nature this week, the structure shows in atomic detail how a two-headed compound derived from the active ingredient in Chang Shan works. Scientists have known that this compound, called halofuginone (a derivative of the febrifugine), can suppress parts of the immune system but nobody knew exactly how.
The new structure shows that, like a wrench in the works, halofuginone jams the gears of a molecular machine that carries out "aminoacylation," a crucial biological process that allows organisms to synthesize the proteins they need to live. Chang Shan, also known asDichroa febrifuga Lour, probably helps with malarial fevers because traces of a halofuginone-like chemical in the herb interfere with this same process in malaria parasites, killing them in an infected person's bloodstream.
"Our new results solved a mystery that has puzzled people about the mechanism of action of a medicine that has been used to treat fever from a malaria infection going back probably 2,000 years or more," said Paul Schimmel, PhD, the Ernest and Jean Hahn Professor and Chair of Molecular Biology and Chemistry and member of The Skaggs Institute for Chemical Biology at TSRI. Schimmel led the research with TSRI postdoctoral fellow Huihao Zhou, PhD.
Halofuginone (see structure, below) has been in clinical trials for cancer, but the high-resolution picture of the molecule suggests it has a modularity that would make it useful as a template to create new drugs for numerous other diseases.
Gattex Approved for Short Bowel Syndrome - Drugs.com MedNews
We know that, Gattex (teduglutide) is a recombinant analog of human glucagon-like peptide 2 for the treatment of adults with short bowel syndrome....
Gattex Approved for Short Bowel Syndrome - Drugs.com MedNews
Sunday, December 30, 2012
FDA Approves Adasuve (loxapine) Inhalation Powder for the Acute Treatment of Agitation Associated with Schizophrenia or Bipolar I Disorder in Adults
We know that, Loxapine (Loxapac, Loxitane) is a typical antipsychotic medication, used primarily in the treatment of schizophrenia. It is a member of the dibenzoxazepine class and structurally related to clozapine (which belongs to the chemically akin class of dibenzodiazepines). Several researchers have argued that Loxapine may behave as an atypical antipsychotic. Loxapine may be metabolized by N-demethylation to amoxapine, a tetracyclic antidepressant. ........
Labels:
Adasuve,
antipsychotic,
Drug Discovery,
Loxapine (Loxapac,
Loxitane)
Saturday, December 29, 2012
Dantrolene shows promise for treating DMD
We know that, Dantrolene sodium is a muscle relaxant that acts by abolishing excitation-contraction coupling in muscle cells, probably by action on the ryanodine receptor. It is the only specific and effective treatment for malignant hyperthermia, a rare, life-threatening disorder triggered by general anesthesia. It is also used in the management of neuroleptic malignant syndrome, muscle spasticity (e.g. after strokes, in paraplegia, cerebral palsy, or patients with multiple sclerosis), 3,4-methylenedioxymethamphetamine ("ecstasy") intoxication, serotonin syndrome, and 2,4-dinitrophenol poisoning. It is marketed by JHP Pharmaceuticals LLC as Dantrium (in North America) and Dantrolen (Europe).
Friday, December 28, 2012
Dantrolene shows promise for treating DMD
We know that, Dantrolene sodium is a muscle relaxant that acts by abolishing excitation-contraction coupling in muscle cells, probably by action on the ryanodine receptor. It is the only specific and effective treatment for malignant hyperthermia, a rare, life-threatening disorder triggered by general anesthesia. It is also used in the management of neuroleptic malignant syndrome, muscle spasticity (e.g. after strokes, in paraplegia, cerebral palsy, or patients with multiple sclerosis), 3,4-methylenedioxymethamphetamine ("ecstasy") intoxication, serotonin syndrome, and 2,4-dinitrophenol poisoning. It is marketed by JHP Pharmaceuticals LLC as Dantrium (in North America) and Dantrolen (Europe).
Thursday, December 27, 2012
Lapatinib benefits found for HER2-positive early-stage patients
In continuation of my update on Lapatinib
Wednesday, December 26, 2012
Abiraterone improves outcomes for prostate cancer prior to chemo
In continuation of my update on abiraterone
Vismodegib team wins Drug Discovery of the Year award
In continuation of my update on Vismodegib
Vismodegib team wins Drug Discovery of the Year award: The British Pharmacological Society proudly announces that its first annual Drug Discovery of the Year award has been won by the discovery team developing vismodegib for the treatment of basal cell carcinoma (a type of skin cancer).
Labels:
anticancer activity,
Drug Discovery,
Vismodegib
Monday, December 24, 2012
New low-cost combined therapy shows promise against malaria
Molecular parasitologist Stephen Rich at the University of Massachusetts Amherst has led a research team who report a promising new low-cost combined therapy with a much higher chance of outwitting P. falciparum than current modes. He and plant biochemist Pamela Weathers at the Worcester Polytechnic Institute (WPI), with research physician Doug Golenbock at the UMass Medical School, also in Worcester, have designed an approach for treating malaria based on a new use of Artemisia annua, a plant employed for thousands of years in Asia to treat fever.
"The emergence of resistant parasites has repeatedly curtailed the lifespan of each drug that is developed and deployed," says UMass Amherst graduate student and lead author Mostafa Elfawal. Rich, an expert in the malaria parasite and how it evolves, adds, "We no sooner get the upper hand than the parasite mutates to become drug resistant again. This cycle of resistance to anti-malarial drugs is one of the great health problems facing the world today. We're hoping that our approach may provide an inexpensive, locally grown and processed option for fighting malaria in the developing world."
Currently the most effective malaria treatment uses purified extracts from the Artemisia plant as part of an Artemisinin Combined Therapy (ACT) regime with other drugs such as doxycycline and/or chloroquine, a prescription far too costly for wide use in the developing world. Also, because Artemisia yields low levels of pure artemisinin, there is a persistent worldwide shortage, they add.
The teams's thesis, first proposed by Weathers of WPI, is that locally grown and dried leaves of the whole plant, rich in hundreds of phytochemicals not contained in the purified drug, might be effective against disease at the same time limiting post-production steps, perhaps substantially reducing treatment cost. She says, "Whole-plant Artemisia has hundreds of compounds, some of them not even known yet. These may outsmart the parasites by delivering a more complex drug than the purified form."
Rich adds, "The plant may be its own complex combination therapy. Because of the combination of parasite-killing substances normally present in the plant (artemisinin and flavonoids), a synergism among these constituent compounds might render whole plant consumption as a form of artemisinin-based combination therapy, or what we're calling a 'pACT,' for plant Artemisinin Combination Therapy."
Ref : http://www.plosone.org/article/info%3Adoi%2F10.1371%2Fjournal.pone.0052746
Sunday, December 23, 2012
Research | Research news | Fighting sleeping sickness with X-ray lasers
Using the world’s most powerful X-ray free-electron laser, an international team of researchers, including scientists of the Max Planck Institute for Medical Research in Heidelberg, has obtained new insight into the structure of a medicinally important protein that may serve as a blueprint for the development of drugs to fight sleeping sickness. Science magazine have chosen the experimental study as one of the top ten scientific breakthroughs of the year.
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