[tt] Next Big Future - 2 new articles

Eugen Leitl <eugen at leitl.org> on Wed Aug 20 13:44:02 UTC 2008

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"[2]Next Big Future" - 2 new articles

    1. [3]Aging biomarkers
    2. [4]One dose of RNAi reduces Cholesterol by 60% for three weeks
    3. [5]More Recent Articles
    4. [6]Search Next Big Future

[7]Aging biomarkers

   Scientists have identified biomarkers that indicate telomere
   shortening. CRAMP, stathmin, EF-1a, and chitinase are proteins that
   they found to be secreted from telomere-dysfunctional bone-marrow
   cells of late generation telomerase knockout mice. Their study, which
   was published this week in PNAS, showed an increase in expression of
   these markers in the blood of aging and geriatric people with
   age-related disease; it also allowed them to discriminate between
   young and old and between disease and healthy control groups. Protein
   biomarkers are easier to track with inexpensive blood tests.
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   [14]Proteins induced by telomere dysfunction and DNA damage represent
   biomarkers of human aging and disease

     Telomere dysfunction limits the proliferative capacity of human
     cells by activation of DNA damage responses, inducing senescence or
     apoptosis. In humans, telomere shortening occurs in the vast
     majority of tissues during aging, and telomere shortening is
     accelerated in chronic diseases that increase the rate of cell
     turnover. Yet, the functional role of telomere dysfunction and DNA
     damage in human aging and diseases remains under debate. Here, we
     identified marker proteins (i.e., CRAMP, stathmin, EF-1a, and
     chitinase) that are secreted from telomere-dysfunctional
     bone-marrow cells of late generation telomerase knockout mice
     (G4mTerc -/ -). The expression levels of these proteins increase in
     blood and in various tissues of aging G4mTerc -/ - mice but not in
     aging mice with long telomere reserves. Orthologs of these proteins
     are up-regulated in late-passage presenescent human fibroblasts and
     in early passage human cells in response to g-irradiation. The
     study shows that the expression level of these marker proteins
     increases in the blood plasma of aging humans and shows a further
     increase in geriatric patients with aging-associated diseases.
     Moreover, there was a significant increase in the expression of the
     biomarkers in the blood plasma of patients with chronic diseases
     that are associated with increased rates of cell turnover and
     telomere shortening, such as cirrhosis and myelodysplastic
     syndromes (MDS). Analysis of blinded test samples validated the
     effectiveness of the biomarkers to discriminate between young and
     old, and between disease groups (MDS, cirrhosis) and healthy
     controls. These results support the concept that telomere
     dysfunction and DNA damage are interconnected pathways that are
     activated during human aging and disease.

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[32]One dose of RNAi reduces Cholesterol by 60% for three weeks

   [33]Half of the people do not respond to current cholesterol drugs,
   but one dose of a new RNAi treatment lowers LDL cholesterol by 60% in
   mice and monkeys.
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   The [40]Alnylam Pharmaceuticals drug might one day provide another
   option for patients who are resistant to existing cholesterol-lowering
   drugs due to genetic factors, or it might also be used in combination
   with existing cholesterol-lowering drugs to increase their
   effectiveness.
   The drug employs an approach known as RNA interference, a principle
   that is being studied to develop drugs for many diseases, including
   cancer. With this technique, scientists create short RNA molecules
   that bind to messenger RNA in the cell, causing it to self-destruct.
   That interrupts the process of gene transcription, and thus the
   synthesis of the proteins coded by the gene. Alnylam's new drug
   targets an enzyme called PCSK9, previously shown to affect LDL
   cholesterol levels and risk of heart disease.

     PCSK9 is a hot drug target, says Kevin Fitzgerald, Alnylam's
     director of research. But it's difficult to find small molecules
     that block the enzyme directly because there's no obvious place for
     those molecules to bind. The company's findings demonstrate that
     blocking the production of PCSK9 with RNA interference works in
     nonhuman primates, and that it's effective in a single dose, says
     study coauthor Jay Horton, a professor of internal medicine at UT
     Southwestern who focuses on digestive and liver diseases. The study
     appears online in the Proceedings of the National Academy of
     Sciences (PNAS).
     The Alnylam researchers designed short, double-stranded RNA
     molecules to silence the gene for PCSK9 in rodents, monkeys, and
     humans. They packaged the molecules into lipid-based nanoparticles
     developed by biomedical engineer Robert Langer and his group at
     MIT. The nanoparticles protect the molecules in the bloodstream and
     escort them to liver cells.
     Injecting the drug into mice and rats lowered total cholesterol by
     up to 60 percent, and in monkeys, a single dose cut LDL cholesterol
     by 50 to 60 percent. The reduction lasted about three weeks.
     Although PCSK9's importance was clear from genetic studies in
     rodents and humans, "what was not known was, if you were to acutely
     knock down the level of PCSK9, how long would it take for
     cholesterol to go down," Fitzgerald says. "The answer was, if you
     knock it down today, then your cholesterol is down tomorrow."
     It's not yet clear how well an RNA-interference-based drug that
     requires injections could compete with existing medicines for
     lowering cholesterol. No such drugs have yet been approved by the
     Food and Drug Administration, although several are in clinical
     trials. While there have been some safety concerns with RNA-based
     therapeutics, scientists at Alnylam say that they saw no
     unacceptable side effects in animals given the cholesterol-lowering
     treatment, and people who naturally lack PCSK9 seem healthy.

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Eugen* Leitl <a href="http://leitl.org">leitl</a> http://leitl.org
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