Luna Quest is an emerging
technology company pioneering a new approach to arresting tumor cell
growth through targeted therapies.
| Targeted
therapeutics offer the promise of high efficacy with minimal systemic
toxicity. Most targeted therapeutics are focused on upstream targets
such as epidermal growth factor receptor (EGFR) or mitogen-activated
protein kinase (MAPK). These upstream targets control a broad range
of cellular functions. Thus, inhibition of these upstream kinases
can affect both normal and cancerous tissue, resulting in significant
side effects. |
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RSK, or p90 ribosomal S6 kinase, is a downstream
effector of MAPK. RSK sits at a key regulatory node in which incoming
signals are translated by the cell into changes in gene expression. Remarkably,
there are fundamental differences in the way these signals are interpreted
in normal versus cancer cells.
Luna Quest and our collaborators at
the University of Virginia have identified that the RSK pathway is a key
regulator of cancer cell proliferation. With our discovery of a novel, proprietary
RSK inhibitor, SL0101, we have been able to demonstrate that the inhibition
of RSK proliferation of human cancer lines but does not prevent proliferation
of normal human lines. For example, SL0101 inhibits the growth of the human
breast cancer line MCF-7 but does not affect the normal human breast line
MCF-10A. These discoveries uncovered an unexpected link between RSK activity
and tumor cell proliferation that indicates that RSK is an important new
target for chemotherapeutic agents.
We have successfully developed several
synthetic routes to produce SL0101 and derivatives. Structure-activity
relationships of a series of synthetic derivatives are underway. Additionally,
in vivo ADME studies are ongoing to identify the most promising pre-clinical
candidates.
Luna Quest is actively seeking partners
who have access to new libraries of compounds to screen for additional
leads. Luna Quest has exclusive worldwide use of the patent family that
includes RSK as a novel therapeutic target and SL0101.
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For Further
Information Contact Us:
Email:
Phone: 1(434)972-9951
Fax: 1(434)972-9956
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