NCIt definition : An orally bioavailable pyrrolopyridine derivative and Smoothened (Smo) antagonist
with potential antineoplastic activity. Smo antagonist TAK-441 selectively binds to
and inhibits the activity Smo, which is a cell surface co-receptor for ligands in
the Hedgehog (Hh) family. This may result in a suppression of Hh-mediated signaling
pathways, thereby inhibiting the growth of tumor cells in which this pathway is aberrantly
activated. Smo is a G-protein coupled receptor that lies just downstream of the Hh
cell surface receptor Patched-1 in the Hh pathway; in the absence of ligand, Patched-1
(Ptch1) inhibits Smo, and ligand binding to Ptch1 results in increased levels of Smo.
The Hh-mediated signaling pathways play an important role in cellular growth and differentiation,
and tissue repair; constitutive activation of this pathway is associated with uncontrolled
cellular proliferation in a variety of cancers.;
UNII : CY3QT94KWP;
CAS number : 1186231-83-3; a href https://gsrs.ncats.nih.gov/ginas/app/beta/browse-substance?search 1186231-83-3
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G-SRS /a ;
Semantic type(s)