Syn-Med-Chemist-"Quintessential Synthetic Chemistry"---A Synthetic Chemist's Perception......
Saturday, December 27, 2014
Friday, December 26, 2014
Monday, December 22, 2014
Friday, December 19, 2014
New study reveals how COX-2 inhibitors can increase risk of heart attack in arthritis patients
In continuation of my update COX-2
A class of drug for treating arthritis - all but shelved over fears about side effects - may be given a new lease of life, following the discovery of a possible way to identify which patients should avoid using it.
The new study, led by Imperial College London and published in the journal Circulation, sheds new light on the 10-year-old question of how COX-2 inhibitors - a type of non-steroidal anti-inflammatory drug (NSAID) - can increase the risk of heart attack in some people.
NSAIDs - which include very familiar drugs such as ibuprofen, diclofenac and aspirin - are widely-used treatments for debilitating inflammatory conditions such as arthritis as well as being used for general pain relief worldwide. NSAIDs are also being investigated for their potential to prevent cancer. COX-2 inhibitors, which include Vioxx and Celebrex, were developed in the 1990s to avoid the risk of stomach ulcers caused by some NSAIDs, but after they were linked to an increased risk of heart attacks, they rapidly fell out of favour and some brands, including Vioxx, were withdrawn.
The new study, in mice and human volunteers, was led by Professor Jane Mitchell and Dr James Leiper. Professor Mitchell, from the National Heart and Lung Institute at Imperial, said:
Thursday, December 18, 2014
Drugs delay disease progression for women with hormone-receptor-positive metastatic breast cancer
A new combination of cancer drugs delayed disease progression for patients with hormone-receptor-positive metastatic breast cancer, according to a multi-center phase II trial. The findings of the randomized study (S6-03) were presented at the 2014 San Antonio Breast Cancer Symposium, held Dec. 6-9, by Kerin Adelson, M.D., assistant professor of medical oncology at Yale Cancer Center and chief quality officer at Smilow Cancer Hospital at Yale-New Haven.
The trial enrolled 118 post-menopausal women with metastatic hormone-receptor-positive breast cancer whose cancer continued to progress after being treated with an aromatase inhibitor. The study, based on work done by Doris Germain of Mt. Sinai Hospital, found that the combination of the drugs bortezomib and fulvestrant — versus fulvestrant alone — doubled the rate of survival at 12 months and reduced the chance of cancer progression overall.
Bortezomib, used most commonly in treating multiple myeloma, is a proteasome inhibitor that prevents cancer cells from clearing toxic material. Fulvestrant causes clumping of the estrogen-receptor protein. When bortezomib blocks the ability of the cell to clear these protein clumps, they grow larger and become toxic to the cancer cells. This, in turn, amplifies the effectiveness of fulvestrant, a drug commonly used in this subset of patients.
Wednesday, December 17, 2014
Tuesday, December 16, 2014
Monday, December 15, 2014
Sunday, December 14, 2014
Friday, December 12, 2014
Spinach chlorophyll activates polymer production line
Inspired by nature, scientists in Australia have united light and chlorophyll to generate a range of polymers that have biomedical applications.
During photosynthesis, chlorophyll is activated by visible light, and an electron is promoted from its ground state to an excited state. In plants, this excited electron goes on to react with carbon dioxide and water, via photoinduced electron transfer (PET). However, in the system devised by Cyrille Boyer and colleagues at the University of New South Wales, the excited electron is donated to a monomer, generating a radical, which then goes on to further react and generate polymers through a process known as living radical polymerisation.
One of the challenges in polymer synthesis is achieving control over the length and structure of the polymers generated. Boyer’s team has addressed this using a form of living polymerisation called reversible addition fragmentation chain transfer, or RAFT, polymerisation, which incorporates an agent, normally a thiocarbonlythio compound, as a mediating species. The RAFT agent is capable of accepting and donating radicals, thus ‘sharing’ the radicals around evenly between the species present, ensuring each polymer chain has the opportunity to grow at an equal rate. This leads to a narrow range of polymer lengths and molecular weights (a low polydispersity index), and a high degree of control over the reaction. Various architectures, including star-shaped, comb-shaped and ring-shaped polymers can be synthesised in this way.
Thursday, December 11, 2014
Wednesday, December 10, 2014
Monday, December 8, 2014
Experimental Cholesterol-Lowering Drug Effective, Study Reports
An experimental antibody drug, alirocumab could prove effective at lowering LDL ("bad") cholesterol levels for patients who have side effects with cholesterol-lowering statin medications.
That's the conclusion of a clinical trial presented Monday at the American Heart Association annual meeting in Chicago.
Sunday, December 7, 2014
Saturday, December 6, 2014
Monday, December 1, 2014
Researchers discover why advanced melanoma patients respond to pembrolizumab drug
Work supported by the Stand Up To Cancer (SU2C) - Cancer Research Institute (CRI) - Immunology Translational Research Dream Team, launched in 2012 to focus on how the patient's own immune system can be harnessed to treat some cancers have pioneered an approach to predict why advanced melanoma patients respond to a new life-saving melanoma drug. This new drug, pembrolizumab (Keytruda), was recently approved by the FDA. These findings are reported in Nature online November 26, 2014, ahead of print in the journal.
Over a two-year study, researchers including Dr. Antoni Ribas of UCLA Jonsson Cancer Center and co-leader of the CRI-SU2C Immunology Dream studied 46 patients with advanced melanoma treated with pembrolizumab. These patients had tumor biopsies before and during treatment. The researchers analyzed those biopsies and classified them according to whether the patient responded or not to pembrolizumab. The study then used the biopsy findings to predict the likelihood whether patients would likely to respond to this treatment
Friday, November 28, 2014
TET1 enzyme may be important target for cancer diagnostics, treatment
Mutations in the KRAS gene have long been known to cause cancer, and about one third of solid tumors have KRAS mutations or mutations in the KRAS pathway. KRAS promotes cancer formation not only by driving cell growth and division, but also by turning off protective tumor suppressor genes, which normally limit uncontrolled cell growth and cause damaged cells to self-destruct.
A new University of Iowa study provided a deeper understanding of how KRAS turns off tumor suppressor genes and identifies a key enzyme in the process. The findings, published online Nov. 26 in the journal Cell Reports, suggest that this enzyme, known as TET1, may be an important target for cancer diagnostics and treatment.
In KRAS-driven cancers, tumor suppressor genes are turned off, or silenced, because the DNA that controls their expression is modified by methylation. The UI study shows that KRAS promotes this methylation-associated gene silencing by turning off the TET1 enzyme, which can remove methyl marks from DNA.
Thursday, November 27, 2014
Wednesday, November 26, 2014
Tuesday, November 25, 2014
Monday, November 17, 2014
Sunday, November 9, 2014
Friday, October 24, 2014
Sunday, October 12, 2014
Friday, October 10, 2014
Grapefruit juice stems weight gain in mice fed a high-fat diet, study finds
Mice fed a high-fat diet gained 18 percent less weight when they drank clarified, no-pulp grapefruit juice compared with a control group of mice that drank water, a new study demonstrated. Juice-drinking mice also showed improved levels of glucose, insulin and a type of fat called triacylglycerol compared with their water-drinking counterparts.
Ref : http://www.plosone.org/article/info%3Adoi%2F10.1371%2Fjournal.pone.0108408
Saturday, October 4, 2014
Friday, October 3, 2014
Australian researchers use hookworms to reduce symptoms of celiac disease
Australian researchers have achieved groundbreaking results in a clinical trial using hookworms to reduce the symptoms of celiac disease.
The results are also good news for sufferers of other inflammatory conditions such as asthma and Crohn's disease.
In the small trial run over a year, 12 participants were each experimentally infected with 20 Necator americanus (hookworm) larvae.
They were then given gradually increasing doses of gluten - beginning with just one-tenth of a gram per day (the equivalent of less than a one-inch segment of spaghetti) and increasing in two further stages to a final daily dose of three grams (75 spaghetti straws).
"By the end of the trial, with worms onboard, the trial subjects were eating the equivalent of a medium-sized bowl of spaghetti, with no ill effects," James Cook University (JCU) immunologist Paul Giacomin said.
"That's a meal that would usually trigger a debilitating inflammatory response, leaving a celiac patient suffering symptoms like diarrhea, cramps and vomiting."
Thursday, October 2, 2014
Scientists discover new clues about drug used in treating blood cancer
Keck Medicine of USC scientists have discovered new clues about a drug instrumental in treating a certain blood cancer that may provide important targets for researchers searching for cures.
The team investigated whether demethylation of gene bodies induced by the drug 5-Aza-CdR (decitabine), which is used to treat pre-leukemia, could alter gene expression and possibly be a therapeutic target in cancer.
"When we put the drug in cancer cells, we found it not only reactivated some tumor suppressor genes, but it down-regulated the overexpressed oncogene (cancer gene)," said Gangning Liang, Ph.D., associate professor of research, Keck School of Medicine of USC Department of Urology, who is corresponding author on the research. "Overexpression is what turns cancer 'on.' The mechanism by which the drug accomplishes this dual action is by removing DNA methylation in the gene body, which we didn't expect."
Wednesday, October 1, 2014
MIT researchers use disarmed version of anthrax toxin to deliver cancer drugs
Bacillus anthracis bacteria have very efficient machinery for injecting toxic proteins into cells, leading to the potentially deadly infection known as anthrax. A team of MIT researchers has now hijacked that delivery system for a different purpose: administering cancer drugs.
"Anthrax toxin is a professional at delivering large enzymes into cells," says Bradley Pentelute, the Pfizer-Laubauch Career Development Assistant Professor of Chemistry at MIT. "We wondered if we could render anthrax toxin nontoxic, and use it as a platform to deliver antibody drugs into cells."
In a paper appearing in the journal ChemBioChem, Pentelute and colleagues showed that they could use this disarmed version of the anthrax toxin to deliver two proteins known as antibody mimics, which can kill cancer cells by disrupting specific proteins inside the cells. This is the first demonstration of effective delivery of antibody mimics into cells, which could allow researchers to develop new drugs for cancer and many other diseases, says Pentelute, the senior author of the paper.
Tuesday, September 30, 2014
New findings could pave way for treating autoimmune diseases
Scientists from A*STAR's Bioprocessing Technology Institute (BTI) have established a clearer relationship between two cells which serve our body's natural defence mechanisms against diseases and infections. Their findings, published in the prestigious journal CELL REPORTS, will help the medical community better understand autoimmunity and could pave the way for treatment of autoimmune diseases.
Natural killer T (NKT) cells and B cells are two of many immune cell types that work in tandem to help the body fight against foreign infectious agents. NKT cells have very potent functions and are crucial to the immune system despite making up only a small percentage of white blood cells. While scientists have established that NKT cells can promote the production of antibodies by B cells to combat infection, little is known about the effect of B cells on NKT cells until now.
Monday, September 29, 2014
Thursday, September 18, 2014
Thursday, September 11, 2014
Now, women experiencing morning sickness can benefit from Diclegis drug
Up to 85 percent of pregnant women are affected by nausea and vomiting of pregnancy (NVP), more commonly known as morning sickness. Many turn to conservative management such as diet and lifestyle changes, however if this does not provide relief, women should speak with their healthcare professional about prescription treatment options.
Diclegis (see structure) is the only FDA-approved prescription NVP treatment for women who do not respond to conservative management. Approved in April 2013, the FDA granted Diclegis Pregnancy Category A status, its highest rating.
Duchesnay USA, the maker of Diclegis, is dedicated to providing pregnant women with safe and effective pharmacological treatments.
Tuesday, September 9, 2014
Actavis Announces FDA Acceptance for Filing of NDA for Eluxadoline
Actavis plc (NYSE: ACT) today announced that the U.S. Food and Drug Administration (FDA) has accepted for filing Actavis' New Drug Application (NDA) for eluxadoline, an investigational drug for the treatment of diarrhea and abdominal pain in men and women with diarrhea predominant Irritable Bowel Syndrome (IBS-D). Actavis' NDA for eluxadoline has been granted priority review status by the FDA.
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