LA JOLLA, Calif., June 6, 2011 – Regulus
Therapeutics Inc., a biopharmaceutical company leading the
discovery and development of innovative medicines targeting
microRNAs, today announced publication
in the Journal of Clinical Investigation of new pre-clinical
data in mice on the antagonism of microRNA-33 (miR-33). The study,
performed with collaborators at NYU Langone Medical Center,
demonstrated that antagonism of
miR-33 with proprietary
chemically modified anti-miR oligonucleotides can promote clearance
of excess cholesterol and statistically significant regression of
atherosclerosis in mice with established atherosclerotic
plaques.

Recent advances in lipid metabolism have identified miR-33 as a
“master switch” of cholesterol transport genes, such as ATP-binding
cassette transporter A1 (ABCA1), a regulator of high density
lipoprotein cholesterol (HDL-C), or ‘good’ cholesterol. Inhibition
of miR-33 results in increased ABCA1 expression and elevations in
HDL-C, suggesting that miR-33 antagonism may be atheroprotective
[Rayneret al. Science 328, 1570 (2010)]. In this new study,
in collaboration with Kathryn Moore, Ph.D., associate professor in
the Department of Medicine at NYU Langone Medical Center, the
impact of miR-33 inhibition was assessed in mice with established
atherosclerotic plaques. Treating mice with anti-miR-33 led to
increased HDL-C, enhanced reverse cholesterol transport to the
plasma, liver and feces, and reductions in plaque size and lipid
content.

“We are encouraged by the continuing progress being made on our
miR-33 program and the ongoing work done in collaboration with Dr.
Moore’s lab at NYU Langone,” said Hubert Chen, M.D., vice president
of translational medi

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