In summary, in an HTS campaign against human recombinant
SIRT1 using a library comprising 147,000 compounds,
we have successfully identified 2 classes of compounds, activators
and inhibitors. We confirmed a set of quinoxalins with
strong activating potential on recombinant SIRT1. Compounds,
such as the SIRT1 activators 1 to 3 and the tetrahydrocarbazolebased
SIRT1 inhibitor compound 4 presented here, have the
ability to modulate the activity of SIR proteins such as SIRT1.
I'm an attorney, not a biologist, so reading the attached study is about as useful to me as reading a technical treatise on fee tails and the rule against perpetuities would be for a non-attorney.
With that said, this snippet from the study caught my eye:
"Resveratrol is a weak activator of SIRT1 function, thereby
providing a precedented standard for comparative studies with
these more potent activators. These compounds are at least
10-fold more potent in the in vitro suppression of TNF-α release
compared to resveratrol."
Edited by TianZi, 23 April 2008 - 04:45 AM.