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Target identification for a Hedgehog pathway inhibitor reveals the receptor GPR39

Frederic Bassilana,Adam Carlson,Jennifer A DaSilva,Bianka Grosshans,Solange Vidal,Valerie Beck,Barbara Wilmeringwetter,Luis A Llamas, Todd B Showalter,Pascal Rigollier,Aaron Bourret,Arun Ramamurthy, Xu Wu,Fred Harbinski,Samantha Plonsky, Lac Lee,Heinz Ruffner,Paola Grandi,Markus Schirle,Jeremy Jenkins,Andreas W Sailer,Tewis Bouwmeester,Jeffrey A Porter,Vic Myer,Peter M Finan,John A Tallarico,Joseph F Kelleher III,Klaus Seuwen,Rishi K Jain,Sarah J Luchansky

NATURE CHEMICAL BIOLOGY（2014）

Cited 48|Views34
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Abstract
new small-molecule inhibitor of the Hedgehog signaling pathway acts independently of Smoothened (Smo). Rather than acting through Smo, which is a GPCR-like protein of the pathway, the compound acts through the orphan GPCR GPR39, with the level of GPR39 activation correlating with Hh pathway inhibition.
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nature chemical biology, science
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