Necklace For Long-term And Robust Cardiac Monitoring In Daily Life
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Med-Chemist : "Quintessential Medicinal Chemistry"
Saturday, September 19, 2009
New Antituberculosis Compounds ?
We all know how TB has become a pandemic and several attempts to eradicate the disease have been tried and scientists are still finding new ways. However the most disadvantage part for the scientists lies in the fact that "the disease-causing bacteria have a sophisticated mechanism for surviving dormant in infected cells". i.e., TB bacteria have a sophisticated way to remove the damaged proteins — a protein-cleaving complex known as a proteasome — identified in earlier research by the Nathan lab. By breaking down damaged proteins, the proteasome allows the bacteria to remain dormant, and possibly go on to cause active TB. And hence finding drugs to disable the proteasome would be a new way to fight TB.
In developing proteasome-inhibitor drugs, scientists face several hurdles. A significant one is the fact that human cells also possess proteasomes, which are essential to their survival. To be effective, the drugs would have to specifically target the TB proteasome without adversely affecting the human protein-cleanup complex.
This study represents a shift in strategy for designing antibiotics that treat TB, says Dr. Lin (Assistant Research professor of Microbiology and Immunology at Weill Cornell Medical College). All the groups who tried focused on developing drugs that attacked the bacterium in its active phase, but this group has found a compound that may help to destroy it in its dormant stage.
The Weill Cornell team screened 20,000 compounds for TB proteasome inhibition activity. They identified and synthesized a group of inhibitors, which they then tested for their ability to inhibit the proteasome inside the mycobacteria. They also tested the compounds' effect on monkey epithelial cells and human immune system cells in culture. After reading this article, I could recollect the High Throughput Screening of my compounds (Southern Research Institute, Birmingham). The newly synthesized compounds are specific, less toxic, more active and more over the inhibition of the TB proteasome is irreversible and about 1,000-fold more effective than the minor inhibition observed against human proteasomes.
The Weill Cornell team screened 20,000 compounds for TB proteasome inhibition activity. They identified and synthesized a group of inhibitors, which they then tested for their ability to inhibit the proteasome inside the mycobacteria. They also tested the compounds' effect on monkey epithelial cells and human immune system cells in culture. After reading this article, I could recollect the High Throughput Screening of my compounds (Southern Research Institute, Birmingham). The newly synthesized compounds are specific, less toxic, more active and more over the inhibition of the TB proteasome is irreversible and about 1,000-fold more effective than the minor inhibition observed against human proteasomes.
The structural studies revealed that the inhibitor molecules block the proteasome's ability to degrade proteins in more than one way: by producing a direct chemical change to the proteasome active site, and by altering the conformation of the "pocket" into which protein fragments bind before being degraded. Congrats for this efforts and all the best for their future endeavor.... More....
New Material For Nanoscale Computer Chips
We already use various organic materials for example, flat screens, such as OLED (Organic Light Emitting Diode). The new results show how small and advanced devices made of organic materials can become. I read recently about an article in a blog titled Cell phone TV ? and was amused by the use of OLED and it may overtake the usage of LCDs. I would say the following findings are really interesting and are a step ahead - nanochemists from the Chinese Academy of Sciences and the Nano-Science Center, Department of Chemistry have developed nanoscale electric contacts out of organic and inorganic nanowires. In the contact they have crossed the wires like Mikado sticks and coupled several contacts together in an electric circuit. In this way they have produced prototype computer electronics on the nanoscale and by doing so they have succeeded in placing several transistors consisting of nanowires together on a nano device. Though it is a first step towards realisation of future electronic circuitry based on organic materials – a possible substitute for today’s silicon-based technologies. Hope this step will lead to the possibility of making computers in different ways in the near future...
Ref : http://www.ku.dk/english/news/?content=http://www.ku.dk/english/news/danish_chinese_nano_science.htm
Ref : http://www.ku.dk/english/news/?content=http://www.ku.dk/english/news/danish_chinese_nano_science.htm
New Rabies Vaccine May Require Only A Single Shot... Not 6 !
People were really scared about the number of injections (it used to varies from 12 to 6) rather than the real pain of the dog's bite. Now thanks to Dr. McGettigan according to the researchers, a replication-deficient rabies virus vaccine that lacks a key gene called the matrix (M) gene induced a rapid and efficient anti-rabies immune response in mice and non-human primates.
The M gene is one of the central genes of the rabies virus, and its absence inhibits the virus from completing its life cycle. The virus in the vaccine infects cells and induces an immune response, but the virus is deficient in spreading. The immune response induced with this process is so substantial that only one inoculation may be sufficient enough both pre-exposure and post-exposure settings. The details will be published in the forth coming journal of infectious disease (J Infect Dis.).
Congrats, Dr.McGettigan and co-workers.
Congrats, Dr.McGettigan and co-workers.
Thursday, September 17, 2009
Survey Concludes Telaprevir a Winner for HCV Genotype 1 | Hepatitis Central News, Updates and Commentary
I did mention in my earlier blog about this drug and one person did (Dawn - Blog Name) mention she was happy about the info. I am sure the following update will help her. All the best...(Dawn, U can mail me at dr.umesh1969@gmail.com-if u find this info useful). I am happy something I did blog and that helped a needy & this encourages me to do spend more time with my blog.....
Survey Concludes Telaprevir a Winner for HCV Genotype 1 | Hepatitis Central News, Updates and Commentary
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FDA Okays Vaccines for 2009 H1N1 Influenza Virus !
At last one can breathe a sigh of relief from the H1N1 pandemic.....
FDA's approval of the Vaccine for H1N1.........
News: FDA Okays Vaccines for 2009 H1N1 Influenza Virus.
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FDA's approval of the Vaccine for H1N1.........
News: FDA Okays Vaccines for 2009 H1N1 Influenza Virus.
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Tuesday, September 15, 2009
Tuberculosis Patients Can Reduce Transmissability By Inhaling Interferon Through A Nebulizer
As for as my knowledge goes "Interferons" - (glycoproteins - natural cell-signaling proteins produced by the cells of the immune system of most vertebrates in response to challenges such as viruses, parasites and tumor cells).
1. assist the immune response by inhibiting viral replication within host cells, activating natural killer cells and macrophages, increasing antigen presentation to T lymphocytes.
2. increasing the resistance of host cells to viral infection.
And are said to possess the antiviral and antitumour activity.
1. assist the immune response by inhibiting viral replication within host cells, activating natural killer cells and macrophages, increasing antigen presentation to T lymphocytes.
2. increasing the resistance of host cells to viral infection.
And are said to possess the antiviral and antitumour activity.
But this finding is really interesting.................."Tuberculosis Patients Can Reduce Transmissability By Inhaling Interferon Through A Nebulizer"
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Tigecycline- as antimalarial drug ?
As for my knowledge goes, 'Tigecycline' is being used as drug for the antibiotic resistant strain 'Staphylococcus aureus'. And this drug belongs to the class of "glycylcyclines" (similar to tetracyclines : central four-ring carbocyclic skeleton). The broad spectrum activity is attributed to the D-9 position substitution. It is a bacteriostatic and acts by the inhibition of protein synthesis. It has been found to be active against both Gram positive and Gram negative bacterii.
Now thanx to the researchers from the Medical University of Vienna, Austria, who have achieved something interesting feat, i.e., Tigecycline has significant antimalarial activity on its own and may also be effective against multi drug-resistant malaria when administered in combination with traditional antimalarial drugs.
Increasing resistance of Plasmodium falciparum to existing drugs has resulted in the search for new antimalarial therapies and I congratulate the team for this important achievement. More interestingly the drug is 6 times more active against P. falciparum than doxycycline. As the drug itself is an established one, its one more addition to the serendepity list. Congrats the team...
Ref : http://www.asm.org/index.php?option=com_content&view=article&id=91042
Monday, September 14, 2009
Lurasidone - positive results from phase 3 clinical trials !
I read about this compound few months back, that it is one of "atypical antipsychotic" drugs that are being tried and this drug has shown promising results in the phase II and is being studied clinically for phase III by a Japanese company.
As per the claims by the company 'Lurasidone, blocks D2- and 5-HT2A-receptors and the advantage is it causes less extrapyramidal side effects than current antipsychotics.
Yes the phase 3 results are really interesting, with Lurasidone 40 and 120 mg, taken once-daily, demonstrated significantly greater improvement versus placebo on the primary efficacy measure. A total of 53% of patients on lurasidone 40 mg/day and 47% of patients on lurasidone 120 mg/day demonstrated a 30% or more improvement on the PANSS total score from baseline versus 38% on placebo. Lurasidone was also well-tolerated with an overall discontinuation rate similar to placebo (40% vs. 39% placebo) and few adverse event-related discontinuations (9% for both the overall lurasidone group and placebo). Adverse events seen in the trial were generally mild.
Congrats for this achievement.
Ref : http://dsp-america.com/pdf/news/LurasidonePh3Results.pdf
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