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Article

Binding Site Characterization of AM1336, a Novel Covalent Inverse Agonist at Human Cannabinoid 2 Receptor, Using Mass Spectrometric Analysis.

Journal of proteome research - 7 Jul 2017

Mallipeddi Srikrishnan, Kreimer Simion, Zvonok Nikolai, Vemuri Kiran, Karger Barry L, Ivanov Alexander R, Makriyannis Alexandros

Abstract excerpt

Cannabinoid 2 receptor (CB2R), a Class-A G-protein coupled receptor (GPCR), is a promising drug target under a wide array of pathological conditions. Rational drug design has been hindered due to our poor understanding of the structural features involved in ligand binding. Binding of a high-affinity biarylpyrazole inverse agonist AM1336 to a library of the human CB2 receptor (hCB2R) cysteine-substituted mutants...

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Source

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Identifiers

PMID: 28374590
DOI: 10.1021/acs.jproteome.7b00023
PMCID: PMC11208095

Provenance

PubMed metadata and Literature Corpus relationships. Corpus snapshot updated 7 Sept 2026. Manifest publication-graph-cohort-2026-09-07.1.

Source receipt: pubmed, retrieved 7 Sept 2026.

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