Human Cannabinoid 2 GPCR Ligand-interaction Landscape: Cysteine Residues Critical to Biarylpyrazole Antagonist Binding Motif and Receptor Modulation

The human cannabinoid 2 GPCR (hCB2) is a prime therapeutic target. To define potential cysteine-related binding motifs critical to hCB2-ligand interaction, a library of hCB2 cysteine-substitution mutants and a novel, high-affinity biarylpyrazole hCB2 inverse agonist (AM1336) functionalized to serve...

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Hauptverfasser: Mercier, Richard W., Pei, Ying, Pandarinathan, Lakshmipathi, Janero, David R., Zhang, Jing, Makriyannis, Alexandros
Format: Artigo
Sprache:Inglês
Veröffentlicht: 2010
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Article
Online Zugang:https://ncbi.nlm.nih.gov/pmc/articles/PMC3023919/
https://ncbi.nlm.nih.gov/pubmed/21035736
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1016/j.chembiol.2010.08.010
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