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

Potent small molecule antagonists for the PAC 1-R have been discovered. Previously known antagonists for the PAC 1-R were slightly truncated peptide ligands. The hydrazides reported here are the first small molecule antagonists ever reported for this class B GPCR. Potent small molecule antagonists f...

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Bibliographic Details
Published inBioorganic & medicinal chemistry letters Vol. 18; no. 6; pp. 2162 - 2166
Main Authors Beebe, Xenia, Darczak, Daria, Davis-Taber, Rachel A., Uchic, Marie E., Scott, Victoria E., Jarvis, Michael F., Stewart, Andrew O.
Format Journal Article
LanguageEnglish
Published Oxford Elsevier Ltd 15.03.2008
Elsevier
Subjects
Biological and medical sciences
Calcium - metabolism
Cells, Cultured
Class B GPCR
Humans
Hydrazides
Hydrazines - chemistry
Magnetic Resonance Spectroscopy
Medical sciences
Molecular Structure
Neuropharmacology
Neurotransmitters. Neurotransmission. Receptors
PAC 1-R
PACAP
Peptidergic system (neuropeptide, opioid peptide, opiates...). Adenosinergic and purinergic systems
Pharmacology. Drug treatments
Pituitary Adenylate Cyclase-Activating Polypeptide - metabolism
Radioligand Assay
Receptors, Pituitary Adenylate Cyclase-Activating Polypeptide, Type I - antagonists & inhibitors
Receptors, Pituitary Adenylate Cyclase-Activating Polypeptide, Type I - metabolism
Structure-Activity Relationship
Class B GPCR
Hydrazides
PACAP
PAC 1-R
Organic hydrazide
In vitro
PAC1 receptor
PAC1-R
Structure activity relation
G protein coupled receptor
Antagonist
Small molecule
Chemical synthesis
Pituitary adenylate cyclase activating peptide
Biological receptor
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Summary:Potent small molecule antagonists for the PAC 1-R have been discovered. Previously known antagonists for the PAC 1-R were slightly truncated peptide ligands. The hydrazides reported here are the first small molecule antagonists ever reported for this class B GPCR. Potent small molecule antagonists for the PAC 1-R have been discovered. Previously known antagonists for the PAC 1-R were slightly truncated peptide ligands. The hydrazides reported here are the first small molecule antagonists ever reported for this class B GPCR.
Bibliography:ObjectType-Article-1
SourceType-Scholarly Journals-1
ObjectType-Feature-2
content type line 23
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2008.01.052