Description:
Background:
The Wnt
signaling pathway plays essential roles in development and is frequently
hyperactivated in cancer cells as a driving mechanism. Nearly 90% of colon cancers, for
examples are mutated in this pathway. However, direct targeting of this pathway
for cancer drug discovery has been challenging due to receptor redundancy and
complexity. Leucine-rich
repeat containing G-protein coupled receptors 4, 5, and 6 (LGR4-6) functions as
receptors of R-spondins (RSPO) to potentiate the Wnt signaling pathway. Recurrent gene fusions of RSPO2 and RSPO3
were found in ~10% of colorectal cancers.
Inhibition of RSPO-LGR signaling provides a novel approach to the
blockade of Wnt signaling as a potential treatment of cancers with aberrant Wnt
signaling.
Market:
This method could be used in the discovery
of drugs targeted at the Wnt signaling pathway. The multi-billion dollar market size of
drug discovery is growing in the United States, Europe and Asia.
Technology
Highlights:
Scientists at The University of Texas Health Science
Center at Houston (UT Health) have identified methods and compositions that
enable the discovery of agonists and antagonists of RSPO-LGR signaling that can
be used to modulate the Wnt signaling processes. This technology has
the potentials to:
·
Determine if the activity of
LGR4-6 is modulated by measuring Wnt activity in the cell.
·
Identify a composition of a
compound which may be able to bind to LGR4, LGR5 and LGR6
ligands.
IP
Status:
U.S
Patent application filed
Publications:
“R-spondins
function as ligands of the orphan receptors LGR4 and LGR5 to regulate
Wnt/beta-catenin signaling.” PNAS
2011 Jul
12;108(28):11452-7.
http://www.pnas.org/content/early/2011/06/20/1106083108.full.pdf
License
Available:
World-wide; exclusive or non-exclusive
Researchers:
Drs. Qingyun Liu, Kendra Carmon, Xing
Gong