Published in J Biol Chem on December 23, 2013
The endocannabinoid system in guarding against fear, anxiety and stress. Nat Rev Neurosci (2015) 0.99
Novel Electrophilic and Photoaffinity Covalent Probes for Mapping the Cannabinoid 1 Receptor Allosteric Site(s). J Med Chem (2015) 0.87
Behavioral effects of the cannabinoid CB1 receptor allosteric modulator ORG27569 in rats. Pharmacol Res Perspect (2014) 0.82
Effects of the cannabinoid CB₁ receptor allosteric modulator ORG 27569 on reinstatement of cocaine- and methamphetamine-seeking behavior in rats. Drug Alcohol Depend (2014) 0.82
Endogenous vs Exogenous Allosteric Modulators in GPCRs: A dispute for shuttling CB1 among different membrane microenvironments. Sci Rep (2015) 0.80
Structural dynamics and energetics underlying allosteric inactivation of the cannabinoid receptor CB1. Proc Natl Acad Sci U S A (2015) 0.79
Diarylureas as allosteric modulators of the cannabinoid CB1 receptor: structure-activity relationship studies on 1-(4-chlorophenyl)-3-{3-[6-(pyrrolidin-1-yl)pyridin-2-yl]phenyl}urea (PSNCBAM-1). J Med Chem (2014) 0.79
Preclinical Studies of Cannabinoid Reward, Treatments for Cannabis Use Disorder, and Addiction-Related Effects of Cannabinoid Exposure. Neuropsychopharmacology (2017) 0.78
New paradigms in chemokine receptor signal transduction: Moving beyond the two-site model. Biochem Pharmacol (2016) 0.77
Structure-activity relationships of substituted 1H-indole-2-carboxamides as CB1 receptor allosteric modulators. Bioorg Med Chem (2015) 0.77
Aiming for allosterism: Evaluation of allosteric modulators of CB1 in a neuronal model. Pharmacol Res (2015) 0.76
Mapping Cannabinoid 1 Receptor Allosteric Site(s): Critical Molecular Determinant and Signaling Profile of GAT100, a Novel, Potent, and Irreversibly Binding Probe. ACS Chem Neurosci (2016) 0.76
Synthesis and biological evaluation of indole-2-carboxamides bearing photoactivatable functionalities as novel allosteric modulators for the cannabinoid CB1 receptor. Eur J Med Chem (2016) 0.76
CB1 allosteric modulator Org27569 is an antagonist/inverse agonist of ERK1/2 signaling. Cannabis Cannabinoid Res (2016) 0.75
Computational Advances for the Development of Allosteric Modulators and Bitopic Ligands in G Protein-Coupled Receptors. AAPS J (2015) 0.75
Allosteric Modulation: An Alternate Approach Targeting the Cannabinoid CB1 Receptor. Med Res Rev (2016) 0.75
Modulation of CB1 cannabinoid receptor by allosteric ligands: Pharmacology and therapeutic opportunities. Neuropharmacology (2017) 0.75
Comparative protein modelling by satisfaction of spatial restraints. J Mol Biol (1993) 64.61
Modeling of loops in protein structures. Protein Sci (2000) 9.68
Allosteric modulators of GPCRs: a novel approach for the treatment of CNS disorders. Nat Rev Drug Discov (2009) 6.69
Structural diversity of G protein-coupled receptors and significance for drug discovery. Nat Rev Drug Discov (2008) 6.18
Allosteric modulation of G protein-coupled receptors. Annu Rev Pharmacol Toxicol (2007) 4.02
Crystal structure of a lipid G protein-coupled receptor. Science (2012) 3.78
Molecular mechanism of 7TM receptor activation--a global toggle switch model. Annu Rev Pharmacol Toxicol (2006) 3.33
Site of G protein binding to rhodopsin mapped with synthetic peptides from the alpha subunit. Science (1988) 2.66
Allosteric modulation of the cannabinoid CB1 receptor. Mol Pharmacol (2005) 2.42
Helix movement is coupled to displacement of the second extracellular loop in rhodopsin activation. Nat Struct Mol Biol (2009) 2.32
Emerging strategies for exploiting cannabinoid receptor agonists as medicines. Br J Pharmacol (2009) 2.23
New concepts in drug discovery: collateral efficacy and permissive antagonism. Nat Rev Drug Discov (2005) 2.14
Allosteric modulation of G protein-coupled receptors: a pharmacological perspective. Neuropharmacology (2010) 1.97
Importance of the extracellular loops in G protein-coupled receptors for ligand recognition and receptor activation. Trends Pharmacol Sci (2011) 1.62
A lipid pathway for ligand binding is necessary for a cannabinoid G protein-coupled receptor. J Biol Chem (2010) 1.59
Allosteric modulator ORG27569 induces CB1 cannabinoid receptor high affinity agonist binding state, receptor internalization, and Gi protein-independent ERK1/2 kinase activation. J Biol Chem (2012) 1.48
An aromatic microdomain at the cannabinoid CB(1) receptor constitutes an agonist/inverse agonist binding region. J Med Chem (2003) 1.43
Molecular characterization of a purified 5-HT4 receptor: a structural basis for drug efficacy. J Biol Chem (2005) 1.41
A lysine residue of the cannabinoid receptor is critical for receptor recognition by several agonists but not WIN55212-2. Mol Pharmacol (1996) 1.35
Allosteric enhancers, allosteric agonists and ago-allosteric modulators: where do they bind and how do they act? Trends Pharmacol Sci (2007) 1.33
Allosteric agonists of 7TM receptors: expanding the pharmacological toolbox. Trends Pharmacol Sci (2006) 1.32
N-(piperidin-1-yl)-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-1H-pyrazole-3-carboxamide (SR141716A) interaction with LYS 3.28(192) is crucial for its inverse agonism at the cannabinoid CB1 receptor. Mol Pharmacol (2002) 1.28
CB(1) receptor allosteric modulators display both agonist and signaling pathway specificity. Mol Pharmacol (2012) 1.26
Structural mimicry in class A G protein-coupled receptor rotamer toggle switches: the importance of the F3.36(201)/W6.48(357) interaction in cannabinoid CB1 receptor activation. J Biol Chem (2004) 1.26
Allosterism and cannabinoid CB(1) receptors: the shape of things to come. Trends Pharmacol Sci (2007) 1.24
Mutation studies of Ser7.39 and Ser2.60 in the human CB1 cannabinoid receptor: evidence for a serine-induced bend in CB1 transmembrane helix 7. Mol Pharmacol (2007) 1.24
Dual role of the second extracellular loop of the cannabinoid receptor 1: ligand binding and receptor localization. Mol Pharmacol (2009) 1.23
Allosteric modulation of muscarinic acetylcholine receptors. Curr Neuropharmacol (2007) 1.21
Heterologous GPCR expression: a bottleneck to obtaining crystal structures. Biotechnol Prog (2007) 1.19
Impact of GPCRs in clinical medicine: monogenic diseases, genetic variants and drug targets. Biochim Biophys Acta (2006) 1.15
Opioid receptor random mutagenesis reveals a mechanism for G protein-coupled receptor activation. Nat Struct Biol (2003) 1.13
Distinct roles of β-arrestin 1 and β-arrestin 2 in ORG27569-induced biased signaling and internalization of the cannabinoid receptor 1 (CB1). J Biol Chem (2013) 1.11
Ligand-specific conformation of extracellular loop-2 in the angiotensin II type 1 receptor. J Biol Chem (2010) 1.10
A key agonist-induced conformational change in the cannabinoid receptor CB1 is blocked by the allosteric ligand Org 27569. J Biol Chem (2012) 1.04
An overview of the metabolic effects of rimonabant in randomized controlled trials: potential for other cannabinoid 1 receptor blockers in obesity. J Clin Pharm Ther (2011) 1.03
Catechol-binding serines of beta(2)-adrenergic receptors control the equilibrium between active and inactive receptor states. Mol Pharmacol (2000) 1.02
Indole-2-carboxamides as allosteric modulators of the cannabinoid CB₁ receptor. J Med Chem (2012) 1.02
Mutational analysis of muscarinic acetylcholine receptors: structural basis of ligand/receptor/G protein interactions. Life Sci (1993) 1.02
Emerging opportunities for allosteric modulation of G-protein coupled receptors. Biochem Pharmacol (2012) 1.01
Identification of the GPR55 agonist binding site using a novel set of high-potency GPR55 selective ligands. Biochemistry (2011) 1.00
Construction of a 3D model of the cannabinoid CB1 receptor: determination of helix ends and helix orientation. Life Sci (1995) 0.99
Biarylpyrazole inverse agonists at the cannabinoid CB1 receptor: importance of the C-3 carboxamide oxygen/lysine3.28(192) interaction. J Med Chem (2006) 0.97
Allosteric binding sites on muscarinic acetylcholine receptors. Mol Pharmacol (2005) 0.95
Long range effect of mutations on specific conformational changes in the extracellular loop 2 of angiotensin II type 1 receptor. J Biol Chem (2012) 0.89
Structural analysis of the human cannabinoid receptor one carboxyl-terminus identifies two amphipathic helices. Biopolymers (2009) 0.89
Third extracellular loop (EC3)-N terminus interaction is important for seven-transmembrane domain receptor function: implications for an activation microswitch region. J Biol Chem (2010) 0.87
The role of the second and third extracellular loops of the adenosine A1 receptor in activation and allosteric modulation. Biochem Pharmacol (2012) 0.87
Allosteric regulation of muscarinic receptors. Prog Brain Res (1996) 0.86
Ligand Binding Sensitivity of the Extracellular Loop Two of the Cannabinoid Receptor 1. Drug Dev Res (2010) 0.85
Novel insights into CB1 cannabinoid receptor signaling: a key interaction identified between the extracellular-3 loop and transmembrane helix 2. J Pharmacol Exp Ther (2013) 0.78
Allosteric modulation of the cannabinoid CB1 receptor. Mol Pharmacol (2005) 2.42
Hardwiring the brain: endocannabinoids shape neuronal connectivity. Science (2007) 2.21
Structure-activity relationships for 1-alkyl-3-(1-naphthoyl)indoles at the cannabinoid CB(1) and CB(2) receptors: steric and electronic effects of naphthoyl substituents. New highly selective CB(2) receptor agonists. Bioorg Med Chem (2005) 1.93
Targeting of the orphan receptor GPR35 by pamoic acid: a potent activator of extracellular signal-regulated kinase and β-arrestin2 with antinociceptive activity. Mol Pharmacol (2010) 1.86
Pregnenolone can protect the brain from cannabis intoxication. Science (2014) 1.85
The GPR55 ligand L-alpha-lysophosphatidylinositol promotes RhoA-dependent Ca2+ signaling and NFAT activation. FASEB J (2008) 1.83
The putative cannabinoid receptor GPR55 affects osteoclast function in vitro and bone mass in vivo. Proc Natl Acad Sci U S A (2009) 1.63
Evidence that the plant cannabinoid Delta9-tetrahydrocannabivarin is a cannabinoid CB1 and CB2 receptor antagonist. Br J Pharmacol (2005) 1.60
Atypical responsiveness of the orphan receptor GPR55 to cannabinoid ligands. J Biol Chem (2009) 1.60
A lipid pathway for ligand binding is necessary for a cannabinoid G protein-coupled receptor. J Biol Chem (2010) 1.59
Regulation of bone mass, bone loss and osteoclast activity by cannabinoid receptors. Nat Med (2005) 1.56
An aromatic microdomain at the cannabinoid CB(1) receptor constitutes an agonist/inverse agonist binding region. J Med Chem (2003) 1.43
CB2 receptor activation attenuates microcirculatory dysfunction during cerebral ischemic/reperfusion injury. Microvasc Res (2009) 1.38
Inhibition of human neutrophil chemotaxis by endogenous cannabinoids and phytocannabinoids: evidence for a site distinct from CB1 and CB2. Mol Pharmacol (2007) 1.30
N-(piperidin-1-yl)-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-1H-pyrazole-3-carboxamide (SR141716A) interaction with LYS 3.28(192) is crucial for its inverse agonism at the cannabinoid CB1 receptor. Mol Pharmacol (2002) 1.28
CB(1) receptor allosteric modulators display both agonist and signaling pathway specificity. Mol Pharmacol (2012) 1.26
Structural mimicry in class A G protein-coupled receptor rotamer toggle switches: the importance of the F3.36(201)/W6.48(357) interaction in cannabinoid CB1 receptor activation. J Biol Chem (2004) 1.26
(-)-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. Mol Pharmacol (2005) 1.24
Pharmacological characterization of GPR55, a putative cannabinoid receptor. Pharmacol Ther (2010) 1.24
Mutation studies of Ser7.39 and Ser2.60 in the human CB1 cannabinoid receptor: evidence for a serine-induced bend in CB1 transmembrane helix 7. Mol Pharmacol (2007) 1.24
Ligand-binding architecture of human CB2 cannabinoid receptor: evidence for receptor subtype-specific binding motif and modeling GPCR activation. Chem Biol (2008) 1.22
A role for L-alpha-lysophosphatidylinositol and GPR55 in the modulation of migration, orientation and polarization of human breast cancer cells. Br J Pharmacol (2010) 1.21
Intracellular cannabinoid type 1 (CB1) receptors are activated by anandamide. J Biol Chem (2011) 1.20
Synthesis and biological evaluation of bivalent ligands for the cannabinoid 1 receptor. J Med Chem (2010) 1.20
HIV-1 infection and alcohol abuse: neurocognitive impairment, mechanisms of neurodegeneration and therapeutic interventions. Brain Behav Immun (2011) 1.18
Inhibitory effect of ethanol on AMPK phosphorylation is mediated in part through elevated ceramide levels. Am J Physiol Gastrointest Liver Physiol (2010) 1.18
Designer drugs: a medicinal chemistry perspective. Ann N Y Acad Sci (2011) 1.17
(-)-Cannabidiol antagonizes cannabinoid receptor agonists and noradrenaline in the mouse vas deferens. Eur J Pharmacol (2002) 1.14
AM1241, a cannabinoid CB2 receptor selective compound, delays disease progression in a mouse model of amyotrophic lateral sclerosis. Eur J Pharmacol (2006) 1.14
Helix 8 Leu in the CB1 cannabinoid receptor contributes to selective signal transduction mechanisms. J Biol Chem (2007) 1.13
Modulation of L-α-lysophosphatidylinositol/GPR55 mitogen-activated protein kinase (MAPK) signaling by cannabinoids. J Biol Chem (2011) 1.11
The endocannabinoid system as a target for the treatment of neurodegenerative disease. Br J Pharmacol (2010) 1.11
Lipids, lipid rafts and caveolae: their importance for GPCR signaling and their centrality to the endocannabinoid system. Life Sci (2005) 1.11
Effect of ethanol on hydrogen peroxide-induced AMPK phosphorylation. Am J Physiol Gastrointest Liver Physiol (2008) 1.10
Palmitoylation and membrane cholesterol stabilize μ-opioid receptor homodimerization and G protein coupling. BMC Cell Biol (2012) 1.10
Adamantyl cannabinoids: a novel class of cannabinergic ligands. J Med Chem (2005) 1.09
6"-Azidohex-2"-yne-cannabidiol: a potential neutral, competitive cannabinoid CB1 receptor antagonist. Eur J Pharmacol (2004) 1.09
Cannabinoid receptor-dependent and -independent anti-proliferative effects of omega-3 ethanolamides in androgen receptor-positive and -negative prostate cancer cell lines. Carcinogenesis (2010) 1.08
Monoacylglycerol lipase regulates 2-arachidonoylglycerol action and arachidonic acid levels. Bioorg Med Chem Lett (2008) 1.07
3-Indolyl-1-naphthylmethanes: new cannabimimetic indoles provide evidence for aromatic stacking interactions with the CB(1) cannabinoid receptor. Bioorg Med Chem (2003) 1.06
The endocannabinoids anandamide and virodhamine modulate the activity of the candidate cannabinoid receptor GPR55. J Neuroimmune Pharmacol (2012) 1.06
Endocannabinoid tone versus constitutive activity of cannabinoid receptors. Br J Pharmacol (2011) 1.05
Cannabinoid receptors: nomenclature and pharmacological principles. Prog Neuropsychopharmacol Biol Psychiatry (2012) 1.03
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. Mol Pharmacol (2005) 1.01
The plant cannabinoid Delta9-tetrahydrocannabivarin can decrease signs of inflammation and inflammatory pain in mice. Br J Pharmacol (2010) 1.01
A role for the putative cannabinoid receptor GPR55 in the islets of Langerhans. J Endocrinol (2011) 1.00
Synthesis and evaluation of Apogossypol atropisomers as potential Bcl-xL antagonists. Cancer Lett (2008) 1.00
Cannabinoid- and lysophosphatidylinositol-sensitive receptor GPR55 boosts neurotransmitter release at central synapses. Proc Natl Acad Sci U S A (2013) 1.00
Identification of the GPR55 agonist binding site using a novel set of high-potency GPR55 selective ligands. Biochemistry (2011) 1.00
Conformationally constrained farnesoid X receptor (FXR) agonists: heteroaryl replacements of the naphthalene. Bioorg Med Chem Lett (2010) 0.99
Imipramine blocks ethanol-induced ASMase activation, ceramide generation, and PP2A activation, and ameliorates hepatic steatosis in ethanol-fed mice. Am J Physiol Gastrointest Liver Physiol (2011) 0.98
Residues accessible in the binding-site crevice of transmembrane helix 6 of the CB2 cannabinoid receptor. Biochemistry (2008) 0.97
Conformational memories and the endocannabinoid binding site at the cannabinoid CB1 receptor. J Med Chem (2002) 0.97
Synthesis of long-chain amide analogs of the cannabinoid CB1 receptor antagonist N-(piperidinyl)-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-1H-pyrazole-3-carboxamide (SR141716) with unique binding selectivities and pharmacological activities. Bioorg Med Chem (2005) 0.96
Antinociceptive activity of chemical congeners of improgan: optimization of side chain length leads to the discovery of a new, potent, non-opioid analgesic. Neuropharmacology (2006) 0.96
The L-α-lysophosphatidylinositol/GPR55 system and its potential role in human obesity. Diabetes (2011) 0.96
The effect of cannabinoids on capsaicin-evoked calcitonin gene-related peptide (CGRP) release from the isolated paw skin of diabetic and non-diabetic rats. Neuropharmacology (2002) 0.94
Activation of GPR18 by cannabinoid compounds: a tale of biased agonism. Br J Pharmacol (2014) 0.94
Long-range regulatory synergy is required to allow control of the TAC1 locus by MEK/ERK signalling in sensory neurones. Neurosignals (2010) 0.94
Mapping the structural requirements in the CB1 cannabinoid receptor transmembrane helix II for signal transduction. J Pharmacol Exp Ther (2008) 0.94
Multiple actions of anandamide on neonatal rat cultured sensory neurones. Br J Pharmacol (2004) 0.94
Amyotrophic lateral sclerosis: delayed disease progression in mice by treatment with a cannabinoid. Amyotroph Lateral Scler Other Motor Neuron Disord (2004) 0.90
Conformationally constrained farnesoid X receptor (FXR) agonists: Naphthoic acid-based analogs of GW 4064. Bioorg Med Chem Lett (2008) 0.89
A critical role for a tyrosine residue in the cannabinoid receptors for ligand recognition. Biochem Pharmacol (2002) 0.89
Kappa opioid mediation of cannabinoid effects of the potent hallucinogen, salvinorin A, in rodents. Psychopharmacology (Berl) (2010) 0.88
Identification of the GPR55 antagonist binding site using a novel set of high-potency GPR55 selective ligands. Biochemistry (2013) 0.88
Differential activation of cultured neonatal cardiomyocytes by plasmalemmal versus intracellular G protein-coupled receptor 55. J Biol Chem (2013) 0.87
Cannabinoids selectively inhibit proliferation and induce death of cultured human glioblastoma multiforme cells. J Neurooncol (2005) 0.87
Conformational memories with variable bond angles. J Comput Chem (2008) 0.87
In-vivo pharmacological evaluation of the CB1-receptor allosteric modulator Org-27569. Behav Pharmacol (2014) 0.86
GPR55 and GPR35 and their relationship to cannabinoid and lysophospholipid receptors. Life Sci (2012) 0.85
Opioid receptors: toward separation of analgesic from undesirable effects. Trends Biochem Sci (2013) 0.84
GEC1-kappa opioid receptor binding involves hydrophobic interactions: GEC1 has chaperone-like effect. J Biol Chem (2008) 0.84
Endogenous cannabinoids and neutrophil chemotaxis. Vitam Horm (2009) 0.84
Significance of cannabinoid CB1 receptors in improgan antinociception. J Pain (2007) 0.84
Inhibition of striatal dopamine release by CB1 receptor activation requires nonsynaptic communication involving GABA, H2O2, and KATP channels. Neurochem Int (2007) 0.84
FXR agonist activity of conformationally constrained analogs of GW 4064. Bioorg Med Chem Lett (2009) 0.83
Characterization of cannabinoid receptor ligands in tissues natively expressing cannabinoid CB2 receptors. Br J Pharmacol (2013) 0.82
Novel serum biomarkers for detection of excessive alcohol use. Alcohol Clin Exp Res (2015) 0.82
Crucial positively charged residues for ligand activation of the GPR35 receptor. J Biol Chem (2013) 0.82