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Discovery and SAR of hydrazide antagonists of the pituitary adenylate cyclase-activating polypeptide (PACAP) receptor type 1 (PAC1-R)

Xenia Beebe,Daria Darczak,Rachel A. Davis-Taber,Marie E. Uchic,Victoria E. Scott,Michael F. Jarvis,Andrew O. Stewart

Bioorganic & Medicinal Chemistry Letters（2008）

Cited 28|Views18
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Abstract
Potent small molecule antagonists for the PAC1-R have been discovered. Previously known antagonists for the PAC1-R were slightly truncated peptide ligands. The hydrazides reported here are the first small molecule antagonists ever reported for this class B GPCR.
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Key words
PACAP,Class B GPCR,PAC1-R,Hydrazides
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