hCB2 ligand-interaction landscape: cysteine residues critical to biarylpyrazole antagonist binding motif and receptor modulation.

[1]  D. Bylund,et al.  Radioligand binding methods for membrane preparations and intact cells. , 2011, Methods in molecular biology.

[2]  A. Makriyannis,et al.  Mass spectrometry-based GPCR proteomics: comprehensive characterization of the human cannabinoid 1 receptor. , 2010, Journal of proteome research.

[3]  Stephen V Frye,et al.  The art of the chemical probe. , 2010, Nature chemical biology.

[4]  Miles Congreve,et al.  The impact of GPCR structures on pharmacology and structure‐based drug design , 2010, British journal of pharmacology.

[5]  S. Durdağı,et al.  A computational study on cannabinoid receptors and potent bioactive cannabinoid ligands: homology modeling, docking, de novo drug design and molecular dynamics analysis , 2010, Molecular Diversity.

[6]  C. Bass,et al.  Signal transduction via cannabinoid receptors. , 2009, CNS & neurological disorders drug targets.

[7]  R. A. Hall,et al.  Enhancement of the surface expression of G protein-coupled receptors. , 2009, Trends in biotechnology.

[8]  V. Marzo,et al.  The endocannabinoid system: its general strategy of action, tools for its pharmacological manipulation and potential therapeutic exploitation. , 2009, Pharmacological research.

[9]  G. Uhl,et al.  Species differences in cannabinoid receptor 2 (CNR2 gene): identification of novel human and rodent CB2 isoforms, differential tissue expression and regulation by cannabinoid receptor ligands , 2009, Genes, brain, and behavior.

[10]  Sid Topiol,et al.  X-ray structure breakthroughs in the GPCR transmembrane region. , 2009, Biochemical pharmacology.

[11]  Alexandros Makriyannis,et al.  Structural biology of human cannabinoid receptor-2 helix 6 in membrane-mimetic environments. , 2009, Biochemical and biophysical research communications.

[12]  Dynamic conformational responses of a human cannabinoid receptor-1 helix domain to its membrane environment. , 2009, Biochemistry.

[13]  P. Anand,et al.  Targeting CB2 receptors and the endocannabinoid system for the treatment of pain , 2009, Brain Research Reviews.

[14]  A. Makriyannis,et al.  Cannabinoid receptor antagonists: pharmacological opportunities, clinical experience, and translational prognosis , 2009 .

[15]  S. Melmed,et al.  Constitutive somatostatin receptor activity determines tonic pituitary cell response. , 2009, Molecular endocrinology.

[16]  Raymond C Stevens,et al.  Discovery of new GPCR biology: one receptor structure at a time. , 2009, Structure.

[17]  A. Makriyannis,et al.  Pharmacotherapeutic modulation of the endocannabinoid signalling system in psychiatric disorders: Drug-discovery strategies , 2009, International review of psychiatry.

[18]  Alexandros Makriyannis,et al.  Ligand-binding architecture of human CB2 cannabinoid receptor: evidence for receptor subtype-specific binding motif and modeling GPCR activation. , 2008, Chemistry & biology.

[19]  A. Hohmann,et al.  Selective Activation of Cannabinoid CB2 Receptors Suppresses Neuropathic Nociception Induced by Treatment with the Chemotherapeutic Agent Paclitaxel in Rats , 2008, Journal of Pharmacology and Experimental Therapeutics.

[20]  M. Rosenkilde,et al.  Structural Motifs of Importance for the Constitutive Activity of the Orphan 7TM Receptor EBI2: Analysis of Receptor Activation in the Absence of an Agonist , 2008, Molecular Pharmacology.

[21]  A. Makriyannis,et al.  Covalent inhibitors of human monoacylglycerol lipase: ligand-assisted characterization of the catalytic site by mass spectrometry and mutational analysis. , 2008, Chemistry & biology.

[22]  E. Dainese,et al.  Lipid-mediated dimerization of β2-adrenergic receptor reveals important clues for cannabinoid receptors , 2008, Cellular and Molecular Life Sciences.

[23]  N. Stella,et al.  CB2 receptor‐mediated migration of immune cells: it can go either way , 2008, British journal of pharmacology.

[24]  A. Poso,et al.  Targeting the cannabinoid CB2 receptor: modelling and structural determinants of CB2 selective ligands , 2008, British journal of pharmacology.

[25]  C. Lunn,et al.  Biology and therapeutic potential of cannabinoid CB2 receptor inverse agonists , 2008, British journal of pharmacology.

[26]  M. Elphick,et al.  CB1 Cannabinoid Receptor Activity Is Modulated by the Cannabinoid Receptor Interacting Protein CRIP 1a , 2007, Molecular Pharmacology.

[27]  W. Hagmann,et al.  F200A substitution in the third transmembrane helix of human cannabinoid CB1 receptor converts AM2233 from receptor agonist to inverse agonist. , 2006, European journal of pharmacology.

[28]  Qian Liu,et al.  3D-QSAR studies of arylpyrazole antagonists of cannabinoid receptor subtypes CB1 and CB2. A combined NMR and CoMFA approach. , 2006, Journal of medicinal chemistry.

[29]  A. Makriyannis,et al.  (-)-7′-Isothiocyanato-11-hydroxy-1′,1′-dimethylheptylhexahydrocannabinol (AM841), a High-Affinity Electrophilic Ligand, Interacts Covalently with a Cysteine in Helix Six and Activates the CB1 Cannabinoid Receptor , 2005, Molecular Pharmacology.

[30]  W. Pierce,et al.  Purification and mass spectroscopic analysis of human CB1 cannabinoid receptor functionally expressed using the baculovirus system. , 2005, The journal of peptide research : official journal of the American Peptide Society.

[31]  D. Hurst,et al.  Cysteine 2.59(89) in the Second Transmembrane Domain of Human CB2 Receptor Is Accessible within the Ligand Binding Crevice: Evidence for Possible CB2 Deviation from a Rhodopsin Template , 2005, Molecular Pharmacology.

[32]  M. Scheinin,et al.  Uneven cellular expression of recombinant alpha2A-adrenoceptors in transfected CHO cells results in loss of response in adenylyl cyclase inhibition. , 2005, Biochimica et biophysica acta.

[33]  T. Kokkola,et al.  S-Nitrosothiols modulate G protein-coupled receptor signaling in a reversible and highly receptor-specific manner , 2005, BMC Cell Biology.

[34]  K. Kage,et al.  Species comparison and pharmacological characterization of rat and human CB2 cannabinoid receptors. , 2004, European journal of pharmacology.

[35]  Leonardo Pardo,et al.  Ser and Thr Residues Modulate the Conformation of Pro-Kinked Transmembrane α-Helices , 2004 .

[36]  Z. H. Song,et al.  Effects of D3.49A, R3.50A, and A6.34E mutations on ligand binding and activation of the cannabinoid-2 (CB2) receptor. , 2003, Biochemical pharmacology.

[37]  T. Lovenberg,et al.  Constitutive activity of histamine h(3) receptors stably expressed in SK-N-MC cells: display of agonism and inverse agonism by H(3) antagonists. , 2001, The Journal of pharmacology and experimental therapeutics.

[38]  P Ferrara,et al.  Mutational analysis and molecular modelling of the antagonist SR 144528 binding site on the human cannabinoid CB(2) receptor. , 2000, European journal of pharmacology.

[39]  P. Casellas,et al.  Cannabinoid receptor interactions with the antagonists SR 141716A and SR 144528. , 1999, Life sciences.

[40]  J. Andreassi,et al.  Role of a conserved lysine residue in the peripheral cannabinoid receptor (CB2): evidence for subtype specificity. , 1999, Molecular pharmacology.

[41]  A. Makriyannis,et al.  Structure-activity relationships of pyrazole derivatives as cannabinoid receptor antagonists. , 1999, Journal of medicinal chemistry.

[42]  P. Casellas,et al.  SR 144528, an antagonist for the peripheral cannabinoid receptor that behaves as an inverse agonist. , 1999, The Journal of pharmacology and experimental therapeutics.

[43]  J. Kukkonen,et al.  Protean agonism at alpha2A-adrenoceptors. , 1998, Molecular pharmacology.

[44]  J. Shryock,et al.  Inverse agonists and neutral antagonists of recombinant human A1 adenosine receptors stably expressed in Chinese hamster ovary cells. , 1998, Molecular pharmacology.

[45]  P. Casellas,et al.  SR 144528, the first potent and selective antagonist of the CB2 cannabinoid receptor. , 1998, The Journal of pharmacology and experimental therapeutics.

[46]  K. Neve,et al.  Constitutive activity of a chimeric D2/D1 dopamine receptor. , 1997, Molecular pharmacology.

[47]  J. Harrison,et al.  Agonist-independent effect of an allosteric enhancer of the A1 adenosine receptor in CHO cells stably expressing the recombinant human A1 receptor. , 1997, The Journal of pharmacology and experimental therapeutics.

[48]  Z. Vogel,et al.  The peripheral cannabinoid receptor: adenylate cyclase inhibition and G protein coupling , 1995, FEBS letters.

[49]  J. Ballesteros,et al.  [19] Integrated methods for the construction of three-dimensional models and computational probing of structure-function relations in G protein-coupled receptors , 1995 .

[50]  P. Conn.  Methods in neurosciences , 1991 .