Researchers Find Candidates For New HIV Drugs
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Med-Chemist : "Quintessential Medicinal Chemistry"
Monday, October 19, 2009
Imatinib for the treatment of Scleroderma ?
We know that Imatinib (its mesylate salt, Novartis) is a drug used to treat certain types of cancer. It is used in treating chronic myelogenous leukemia (CML), gastrointestinal stromal tumors (GISTs) and a number of other cancers. It is the first member of a new class of agents that act by inhibiting particular tyrosine kinase enzymes, instead of non-specifically inhibiting rapidly dividing cells.More over the discovery of this compound itself is interesting & its one drug obtained via, High Throughput Screening (HTS). Chemists used a HTS of chemical libraries to identify the molecule 2-phenylaminopyrimidine. This lead compound was then tested and modified by the introduction of methyl and benzamide groups to give it enhanced binding properties, resulting in imatinib. More interesting part of this drug is a recent discovery, i.e., GLEEVEC® (imatinib mesylate) can be used to treat Scleroderma. As per the claim by the researchers, until now no drug has been shown to be effective in treating scleroderma in a clinical trial. Several years ago, a small study provided some evidence that a chemotherapy drug called cyclophosphamide may help scleroderma patients, but the benefit was minimal and this drug causes side effects including infertility and secondary cancers.
The investigators reported an interim analysis of their results, although the study is ongoing. At one year, the investigators saw a 23 percent improvement in skin scores. The researchers also saw an improvement in forced vital capacity scores by 9.6 percent and diffusion capacity scores by 11 percent in the 18 patients who had completed one year of treatment. The lung function data was really exciting,” Dr. Spiera said. “In patients with scleroderma, you usually see lung function tests getting worse over time, and if doctors try a therapy for a year and a patient doesn’t get any worse, we get pretty excited. What is amazing to me in this study is that we actually saw improvements in both lung function tests. Congrats for this remarkable achievement.....
Ref : http://www.hss.edu/newsroom_drug-provide-treatment-scleroderma.asp
The investigators reported an interim analysis of their results, although the study is ongoing. At one year, the investigators saw a 23 percent improvement in skin scores. The researchers also saw an improvement in forced vital capacity scores by 9.6 percent and diffusion capacity scores by 11 percent in the 18 patients who had completed one year of treatment. The lung function data was really exciting,” Dr. Spiera said. “In patients with scleroderma, you usually see lung function tests getting worse over time, and if doctors try a therapy for a year and a patient doesn’t get any worse, we get pretty excited. What is amazing to me in this study is that we actually saw improvements in both lung function tests. Congrats for this remarkable achievement.....
Ref : http://www.hss.edu/newsroom_drug-provide-treatment-scleroderma.asp
Using RNAi-based Technique, Scientists Find New Tumor Suppressor Genes In Lymphoma...
In one of my earlier blog about RNAi, I did mention about the award of USPTO notices to RXi Pharmaceuticals Corporation. But these results are really interesting, the CSHL team’s discovery stems from their use of a powerful technology called RNA interference (RNAi), which suppresses gene activity. The scientists employed RNAi to screen hundreds of candidate tumor-suppressors in living mice, using small hairpin-shaped RNA (shRNA) molecules that attach to specific genes with exquisite specificity and switch them off. In the newly reported experiments, this process revealed more than 10 genes whose deactivation accelerates the development of deadly lymphomas tumors of the immune system in the mice.
The CSHL team’s high-throughput screening strategy to functionally identify cancer genes has thus not only provided insights into cancer development but has also pointed the way toward therapeutic refinements. The team is planning a broader RNAi-based screen that will expand into other tumor models. For details...
Sunday, October 18, 2009
Relationship between H pylori and gastric cancer
In my earlier blogs, I have covered lots of news about the Helicobacter pylori, (H. pylori a gram negative bacterium which infects about 50% of the world population). H. pylori colonization causes a strong systemic immune response. Various tools have been employed to identify the relationship between H pylori and gastric cancer, including c-DNA microarrays. However, most of these methods did not consider the systematic interaction of biological components. While reading science daily, I found this interesting info.
A research team from South Korea studied the complex reaction of gastric inflammation induced by H. pylori in a systematic manner using a protein interaction network.
The researchers drew a conclusion that immune-related proteins activated by H. pylori infection interact with proto-oncogene proteins. The hub and bottleneck proteins are potential drug targets for gastric inflammation and cancer.
A research team from South Korea studied the complex reaction of gastric inflammation induced by H. pylori in a systematic manner using a protein interaction network.
The researchers drew a conclusion that immune-related proteins activated by H. pylori infection interact with proto-oncogene proteins. The hub and bottleneck proteins are potential drug targets for gastric inflammation and cancer.
Their study showed how a systematic approach such as the network construction produces meaningful information. It also offered a relatively easy and simple framework to understand the complexity of cellular interactions having functional importance. Therefore, the application of this tool may be an alternative to find important genes and drug targets in other diseases and in complex biological systems....
Ref : http://www.wjgnet.com/1007-9327/15/4518.asp
Glucokinase activators, new class of drugs for the treatment of type 2 diabetes .....
Glucokinase activators (GKAs) represent a promising new class of drugs for the treatment of type 2 diabetes that act directly on both the pancreas and the liver. Glucokinase (GK) is a key enzyme in glucose-sensing tissues that regulates glucose homeostatasis. GKAs lower glucose levels by enhancing the ability of pancreatic beta cells to “sense glucose” and increase insulin secretion in a glucose-dependent manner. Simultaneously, GKAs increase the uptake and disposal of glucose in the liver, while simultaneously reducing the amount it produces.
For more details, read the link
Drug Pipeline
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For more details, read the link
Drug Pipeline
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Friday, October 16, 2009
Thursday, October 15, 2009
Small amounts of funding can produce big results !
I agree with the author if planned and executed his ideas in a systematic manner, one could achieve miracles. Though, Southern Research Institute, Birmingham (for its High Throughput Studies for drug resistant TB) tried the same idea (by paying some money for the newly synthesized chemicals), the approach suggested by the author is far relevant now than it was in those days.....
Read more :Big banks, big pharma, big problems - opinion - 12 October 2009 - New Scientist
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Tuesday, October 13, 2009
Human milk oligosaccharides protect infants against infection
An innovative process developed by Jennewein Biotechnologie GmbH allows for the first time ever the production of these scarce sugar molecules (Human milk oligosaccharides) for use as an ingredient in baby food and in additional food products. For details, read the link..
Human milk oligosaccharides protect infants against infection
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A special protien in the stomach against Helicobacter pylori ....
In my earlier blogs, I did mention with the help of Broccoli and Glutamine how one can avoid the stomach ulcer caused by H. pylori infection (which in turn lead to gastric adenocarcinoma and MALT lymphoma). But this is something interesting a special protein in the lining of the stomach has been shown to be an important part of the body’s defence against the stomach ulcer bacterium Helicobacter pylori in a new study from the Sahlgrenska Academy at the University of Gothenburg. The discovery may explain why the bacterium makes some people more ill than others.
The research team has shown that a protein called MUC1 found in the lining of the stomach is important for the body’s defence against the bacterium. Greatly magnified, MUC1 looks like a tree growing out of low bushes on the surface of the stomach. As MUC1 is taller than the other structures on the cell surface, Helicobacter pylori readily becomes attached to the protein and then rarely gets to infect the cell. As per the claim by the researchers MUC1 acts as a decoy which prevents the bacterium from coming into close contact with the cell surface. Genetic variations between people mean that MUC1 molecules vary in length, and this may be part of the reason why Helicobacter pylori makes some people more ill than others. Congrats for this improtant achievement..
Ref : http://www.plospathogens.org/article/info%3Adoi%2F10.1371%2Fjournal.ppat.1000617
The research team has shown that a protein called MUC1 found in the lining of the stomach is important for the body’s defence against the bacterium. Greatly magnified, MUC1 looks like a tree growing out of low bushes on the surface of the stomach. As MUC1 is taller than the other structures on the cell surface, Helicobacter pylori readily becomes attached to the protein and then rarely gets to infect the cell. As per the claim by the researchers MUC1 acts as a decoy which prevents the bacterium from coming into close contact with the cell surface. Genetic variations between people mean that MUC1 molecules vary in length, and this may be part of the reason why Helicobacter pylori makes some people more ill than others. Congrats for this improtant achievement..
Ref : http://www.plospathogens.org/article/info%3Adoi%2F10.1371%2Fjournal.ppat.1000617
Monday, October 12, 2009
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