Tuesday 25 August 2015

Would Nutlin3 be usefull

My molecular report stated that nutlin 3 could be used to improve the action of temodar. Is anybody using it? What do you think about it?

5 comments:

  1. Nutlin-3 is an experimental drug, still in early stage clinical trials for cancer. I have never heard of it being used in human brain tumor patients.

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  2. My brothers molecular report states that he has mdm2 mutation or something like that and that nutlin3 would be usefull. Since nutlin 3 is not available I am looking for something else instead. Here is a study I found about verapamil acting similar to nutlin3.
    What do you think about it?
    http://www.nature.com/bjc/journal/v111/n4/fig_tab/bjc2014325f4.html

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    Replies
    1. Unfortunately this study is not saying that verapamil is an MDM2 antagonist, like nutlin 3. It is saying that verapamil inhibits MDR-1 (also known as P-glycoprotein), which nutlin-3 does as well. So while verapamil may be useful as a P-glycoprotein inhibitor, it can't replace nutlin-3 as an MDM2 antagonist.

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    2. The significance of MDM2 amplification: MDM2 is a negative regulator of p53 (which is a tumor suppressor in its non-mutant form). So the more MDM2, the less p53.

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  3. It looks like telmisartan (an angiotensin II receptor blocker) might be a way to block the MDM2-p53 interaction, similar to nutlin-3.

    http://www.ncbi.nlm.nih.gov/pubmed/24554192

    There has also been retrospective studies showing GBM patients taking this class of drug have improved survival.

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