2,4-Diaminopyrimidines derivatives were developed as a novel class of SNSR4 antagonists. Structure activity relationship of the diamino pyrimidine core was explored and a tool compound suitable for target validation was identified.
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Development of 2,4-diaminopyrimidine derivatives as novel SNSR4 antagonists.
Bioorg Med Chem Lett
April 2011
Department of Medicinal Chemistry, AstraZeneca R&D Montreal, 7171 Frederick-Banting, Montréal, Québec, Canada H4S 1Z9.
2,4-Diaminopyrimidines derivatives were developed as a novel class of SNSR4 antagonists. Structure activity relationship of the diamino pyrimidine core was explored and a tool compound suitable for target validation was identified.
View Article and Find Full Text PDFCyclic dimers of C-terminal gamma2-MSH analogs as selective antagonists of the human sensory nerve-specific receptor (SNSR-4).
Adv Exp Med Biol
June 2009
Department of Medicinal Chemistry, AstraZeneca R&D Montreal, 7171 Frederick Banting, St. Laurent, QC, Canada H4S 1Z9.
Simultaneous activation of the delta opioid receptor (deltaOR)/sensory neuron-specific receptor-4 (SNSR-4) hetero-oligomer by the mixed bivalent agonist bovine adrenal medulla peptide 22 activates SNSR-4 but inhibits deltaOR signaling.
Mol Pharmacol
August 2006
Département de Biochimie, Université de Montréal, H3C 3J7 Montréal, QC, Canada.
Hetero-oligomerization among G protein-coupled receptors has been proposed to contribute to signal integration. Because sensory neuron-specific receptors (SNSRs) and the opioid receptors (OR) share a common ligand, the bovine adrenal medulla peptide (BAM) 22, and have opposite effects on pain modulation, we investigated the possible consequences of deltaOR/SNSR-4 hetero-oligomerization on the signaling properties of both receptor subtypes. Bioluminescence resonance energy transfer revealed that the human deltaOR has similar propensity to homo-oligomerize and to form hetero-oligomers with human SNSR-4 when coexpressed in human embryonic kidney 293 cells.
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