New Target For Treating Leukemia Identified
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Med-Chemist : "Quintessential Medicinal Chemistry"
Tuesday, October 13, 2009
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
Saturday, October 10, 2009
Telomerase & Telomerase inhibition.......
When I read about the Nobel prize in Medicine, was really excited because the scientists who discovered the enzyme telomerase got the Nobel prize for the year 2009 and the reason for this is simple and obvious....
When I was working with my previous company (Innovasynth Technologies Limited, Khopoli), I had opportunity to learn lots of things (from Dr. Sergei Gryaznov of Geron Corporation) about the drugs with Telomerase inhibition activity. As for as my knowledge goes, there are many companies working on these class of compounds and hope in the days to come there will be many drugs from this class of compounds and antisense drugs.
About Telomerase :
Telomerase, is an enzyme that adds specific DNA sequence repeats to the 3' end of DNA strands in the telomerase regions, which are found at the ends of eukaryotic chromosomes. The telomeres contain condensed DNA material, giving stability to the chromosomes. The enzyme is a reverse transcriptase that carries its own RNA molecule. Though the existence of a compensatory shortening of telomere (telomerase) mechanism, was first predicted by Soviet biologist Alexey Olovnikov (1973), who also suggested the Telomere hypothesis of ageing and the Telomere relations to cancer. Carol Greider and Elizabeth Blackburn in 1985, discovered telomerase together with Jack Szostak. Greider and Blackburn have been awarded the Nobel Prize in Physiology or Medicine. Congrats for this remarkable achievement.
Telomerase inhibitors :
To safeguard against cancer, adult cells keep track of how many times that they have multiplied, and once they have reached a pre-set limit — often around 80 divisions — they die. Telomerase interferes with this record keeping. So if one can find a drug or gene therapy that interferes with telomerase, it could fight the unchecked growth of cancer cells. As per the claim by lead researcher (Mark Muller), 90% all cancer cells are telomerase rich. Geron corporation, is developing modified DNA molecule (for which Innovasynth, has tie up with Geron to provide the intermediate amidites). The oligonucleotides, which target the template region, or active site, of telomerase. Geron's work has focused oligonucleotides (GRN163 and GRN163L,) and as per the claim by the company, both of them have demonstrated highly potent telomerase inhibitory activity at very low concentrations in biochemical assays, various cellular systems and animal studies. Interestingly these compounds are direct enzyme inhibitors, not antisense compounds and smaller than typical antisense compounds or other oligonucleotide drug candidates. Both compounds use a special thiophosphoramidate chemical backbone and the company is hopeful of convincing clinical trial results. All the best...
Ref : 1. http://nobelprize.org/nobel_prizes/medicine/laureates/2009/press.html
2. http://www.geron.com/products/productinformation/cancerdrug.aspx
When I was working with my previous company (Innovasynth Technologies Limited, Khopoli), I had opportunity to learn lots of things (from Dr. Sergei Gryaznov of Geron Corporation) about the drugs with Telomerase inhibition activity. As for as my knowledge goes, there are many companies working on these class of compounds and hope in the days to come there will be many drugs from this class of compounds and antisense drugs.
About Telomerase :
Telomerase, is an enzyme that adds specific DNA sequence repeats to the 3' end of DNA strands in the telomerase regions, which are found at the ends of eukaryotic chromosomes. The telomeres contain condensed DNA material, giving stability to the chromosomes. The enzyme is a reverse transcriptase that carries its own RNA molecule. Though the existence of a compensatory shortening of telomere (telomerase) mechanism, was first predicted by Soviet biologist Alexey Olovnikov (1973), who also suggested the Telomere hypothesis of ageing and the Telomere relations to cancer. Carol Greider and Elizabeth Blackburn in 1985, discovered telomerase together with Jack Szostak. Greider and Blackburn have been awarded the Nobel Prize in Physiology or Medicine. Congrats for this remarkable achievement.
Telomerase inhibitors :
To safeguard against cancer, adult cells keep track of how many times that they have multiplied, and once they have reached a pre-set limit — often around 80 divisions — they die. Telomerase interferes with this record keeping. So if one can find a drug or gene therapy that interferes with telomerase, it could fight the unchecked growth of cancer cells. As per the claim by lead researcher (Mark Muller), 90% all cancer cells are telomerase rich. Geron corporation, is developing modified DNA molecule (for which Innovasynth, has tie up with Geron to provide the intermediate amidites). The oligonucleotides, which target the template region, or active site, of telomerase. Geron's work has focused oligonucleotides (GRN163 and GRN163L,) and as per the claim by the company, both of them have demonstrated highly potent telomerase inhibitory activity at very low concentrations in biochemical assays, various cellular systems and animal studies. Interestingly these compounds are direct enzyme inhibitors, not antisense compounds and smaller than typical antisense compounds or other oligonucleotide drug candidates. Both compounds use a special thiophosphoramidate chemical backbone and the company is hopeful of convincing clinical trial results. All the best...
Ref : 1. http://nobelprize.org/nobel_prizes/medicine/laureates/2009/press.html
2. http://www.geron.com/products/productinformation/cancerdrug.aspx
Friday, October 9, 2009
Wednesday, October 7, 2009
2009 Nobel Prize for Chemistry......
This year's (2009) Nobel Prize in Chemistry is awarded to Venkatraman Ramakrishnan, Thomas A. Steitz and Ada E. Yonath (from left to right respectively) for their studies of the structure and function of the ribosome.
The Nobel Prize in Chemistry for 2009 awards studies of one of life's core processes: the ribosome's translation of DNA information into life. Ribosomes produce proteins, which in turn control the chemistry in all living organisms. As ribosomes are crucial to life, they are also a major target for new antibiotics. Venkatraman Ramakrishnan, Thomas A. Steitz and Ada E. Yonath for having showed what the ribosome looks like and how it functions at the atomic level. All three have used a method called X-ray crystallography to map the position for each and every one of the hundreds of thousands of atoms that make up the ribosome.
This year's three Laureates have all generated 3D models that show how different antibiotics bind to the ribosome. These models are now used by scientists in order to develop new antibiotics, directly assisting the saving of lives and decreasing humanity's suffering. One can read more details with the link.
Congratulations to all of them for this remarkable achievement. Its interesting to note that Dr. Medicinein 1968, its V.Ramakrishnan in the Science field.
Ref : http://nobelprize.org/nobel_prizes/chemistry/laureates/2009/
The Nobel Prize in Chemistry for 2009 awards studies of one of life's core processes: the ribosome's translation of DNA information into life. Ribosomes produce proteins, which in turn control the chemistry in all living organisms. As ribosomes are crucial to life, they are also a major target for new antibiotics. Venkatraman Ramakrishnan, Thomas A. Steitz and Ada E. Yonath for having showed what the ribosome looks like and how it functions at the atomic level. All three have used a method called X-ray crystallography to map the position for each and every one of the hundreds of thousands of atoms that make up the ribosome.
This year's three Laureates have all generated 3D models that show how different antibiotics bind to the ribosome. These models are now used by scientists in order to develop new antibiotics, directly assisting the saving of lives and decreasing humanity's suffering. One can read more details with the link.
Congratulations to all of them for this remarkable achievement. Its interesting to note that Dr. Medicinein 1968, its V.Ramakrishnan in the Science field.
Ref : http://nobelprize.org/nobel_prizes/chemistry/laureates/2009/
Tuesday, October 6, 2009
Minocycline for stroke patients?
Minocycline hydrochloride, also known as minocycline (right structure), is a broad spectrum tetracycline antibiotic, and has a broader spectrum than the other members of the group. It is a bactriostatic antibiotic. As a result of its long half-life it generally has serum levels 2-4 times that of most other tetracyclines (150 mg giving 16 times the activity levels compared to 250 mg of tetracycline at 24–48 hours). It is primarily used to treat acne and other skin infections. Apart from the antibacterial activity, 'minocycline' is recognized as a DMARD (Disease-Modifying Anti-Rheumatic Drug) by the American College of Rheumatology, which recommends its use as a treatment for mild rheumatoid arthritis.
A recent study by the Dr. Cesar V. Borlongan (University of South Florida, USA) has lead to some interesting result, i.e., minocycline can be used to treat the stroke patients !. As per the claim by the researchers this drug might be a better option, when compared with the thrombolytic agent tPA (the only effective drug for acute ischemic stroke) and more over only 2 % of ischemic stroke patients benefit from this treatment due to its limited therapeutic window.
During a stroke, a clot prevents blood flow to parts of the brain, which can have wide ranging short-term and long-term implications. This study recorded the effect of intravenous minocycline in both isolated neurons and animal models after a stroke had been experimentally induced. At low doses it was found to have a neuroprotective effect on neurons by reducing apoptosis of neuronal cells and ameliorating behavioral deficits caused by stroke. The safety and therapeutic efficacy of low dose minocycline and its robust neuroprotective effects during acute ischemic stroke make it an appealing drug candidate for stroke therapy claims the researchers. Congrats for this interesting finding...
Ref : http://www.biomedcentral.com/1471-2202/10/126/abstract
A recent study by the Dr. Cesar V. Borlongan (University of South Florida, USA) has lead to some interesting result, i.e., minocycline can be used to treat the stroke patients !. As per the claim by the researchers this drug might be a better option, when compared with the thrombolytic agent tPA (the only effective drug for acute ischemic stroke) and more over only 2 % of ischemic stroke patients benefit from this treatment due to its limited therapeutic window.
During a stroke, a clot prevents blood flow to parts of the brain, which can have wide ranging short-term and long-term implications. This study recorded the effect of intravenous minocycline in both isolated neurons and animal models after a stroke had been experimentally induced. At low doses it was found to have a neuroprotective effect on neurons by reducing apoptosis of neuronal cells and ameliorating behavioral deficits caused by stroke. The safety and therapeutic efficacy of low dose minocycline and its robust neuroprotective effects during acute ischemic stroke make it an appealing drug candidate for stroke therapy claims the researchers. Congrats for this interesting finding...
Ref : http://www.biomedcentral.com/1471-2202/10/126/abstract
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