Structural basis of selective cannabinoid CB2 receptor activation

[1]  E. El-demerdash,et al.  The Cannabinoid-2 receptor agonist, 1-phenylisatin, protects against cisplatin-induced nephrotoxicity in mice. , 2022, Life sciences.

[2]  N. Grimsey,et al.  Developing the Cannabinoid Receptor 2 (CB2) pharmacopoeia: past, present, and future. , 2022, Trends in pharmacological sciences.

[3]  Lin Cheng,et al.  Molecular mechanism of allosteric modulation for the cannabinoid receptor CB1 , 2022, Nature Chemical Biology.

[4]  F. Park,et al.  Cannabinoid Type 2 Receptor Activation Reduces the Progression of Kidney Fibrosis Using a Mouse Model of Unilateral Ureteral Obstruction. , 2022, Cannabis and cannabinoid research.

[5]  Qing-Rong Liu,et al.  Anti-Inflammatory and Pro-Autophagy Effects of the Cannabinoid Receptor CB2R: Possibility of Modulation in Type 1 Diabetes , 2022, Frontiers in Pharmacology.

[6]  R. Riera,et al.  Efficacy and safety of therapeutic use of cannabis derivatives and their synthetic analogs: Overview of systematic reviews , 2021, Phytotherapy research : PTR.

[7]  G. V. van Westen,et al.  Identification of V6.51L as a selectivity hotspot in stereoselective A2B adenosine receptor antagonist recognition , 2021, Scientific Reports.

[8]  U. Grether,et al.  Cannabinoid receptor type 2 ligands: an analysis of granted patents since 2010. , 2021, Pharmaceutical patent analyst.

[9]  S. Hanauer,et al.  Safety, Pharmacokinetics, and Efficacy of Olorinab, a Peripherally Acting, Highly Selective, Full Agonist of the Cannabinoid Receptor 2, in a Phase 2a Study of Patients With Chronic Abdominal Pain Associated With Crohn’s Disease , 2020, Crohn's & colitis 360.

[10]  S. Vlachou,et al.  A Critical Review of the Role of the Cannabinoid Compounds Δ9-Tetrahydrocannabinol (Δ9-THC) and Cannabidiol (CBD) and their Combination in Multiple Sclerosis Treatment , 2020, Molecules.

[11]  M. Stockler,et al.  Oral THC:CBD cannabis extract for refractory chemotherapy-induced nausea and vomiting (CINV): a randomised, placebo-controlled, phase 2 crossover trial. , 2020, Annals of oncology : official journal of the European Society for Medical Oncology.

[12]  Whitney Mortensen,et al.  Clinical Data for the Use of Cannabis-Based Treatments: A Comprehensive Review of the Literature , 2020, The Annals of pharmacotherapy.

[13]  N. Kaminski,et al.  Targeting Cannabinoid Receptor 2 on Peripheral Leukocytes to Attenuate Inflammatory Mechanisms Implicated in HIV-Associated Neurocognitive Disorder , 2020, Journal of Neuroimmune Pharmacology.

[14]  L. Heitman,et al.  Perspective: Implications of Ligand-Receptor Binding Kinetics for Therapeutic Targeting of G Protein-Coupled Receptors. , 2020, ACS pharmacology & translational science.

[15]  Yong Chen,et al.  Structural basis of ligand recognition and self-activation of orphan GPR52 , 2020, Nature.

[16]  Suwen Zhao,et al.  Activation and Signaling Mechanism Revealed by Cannabinoid Receptor-Gi Complex Structures , 2020, Cell.

[17]  Junmei Wang,et al.  Cryo-EM Structure of the Human Cannabinoid Receptor CB2-Gi Signaling Complex , 2020, Cell.

[18]  K. Erdélyi,et al.  Cannabinoid-2 receptor activation ameliorates hepatorenal syndrome. , 2019, Free radical biology & medicine.

[19]  S. Natesan,et al.  Does the Lipid Bilayer Orchestrate Access and Binding of Ligands to Transmembrane Orthosteric/Allosteric Sites of G Protein-Coupled Receptors? , 2019, Molecular Pharmacology.

[20]  D. Rosenbaum,et al.  Structure of an allosteric modulator bound to the CB1 cannabinoid receptor , 2019, Nature Chemical Biology.

[21]  D. Greaves,et al.  The Impact of Cannabinoid Receptor 2 Deficiency on Neutrophil Recruitment and Inflammation. , 2019, DNA and cell biology.

[22]  M. Çakır,et al.  The protective effect of cannabinoid type 2 receptor activation on renal ischemia–reperfusion injury , 2019, Molecular and Cellular Biochemistry.

[23]  J. Giraldo,et al.  Revealing the Mechanism of Agonist-Mediated Cannabinoid Receptor 1 (CB1) Activation and Phospholipid-Mediated Allosteric Modulation. , 2019, Journal of medicinal chemistry.

[24]  M. R. Iyer,et al.  Crystal Structure of the Human Cannabinoid Receptor CB2 , 2019, Cell.

[25]  Ron O. Dror,et al.  Structure of a Signaling Cannabinoid Receptor 1-G Protein Complex , 2019, Cell.

[26]  C. Lucas,et al.  The pharmacokinetics and the pharmacodynamics of cannabinoids. , 2018, British journal of clinical pharmacology.

[27]  J. Heymann,et al.  Single particle reconstruction and validation using Bsoft for the map challenge. , 2018, Journal of structural biology.

[28]  Mark W. H. Hoorens,et al.  Structure‐kinetic relationship studies of cannabinoid CB2 receptor agonists reveal substituent‐specific lipophilic effects on residence time , 2018, Biochemical pharmacology.

[29]  M. Badowski,et al.  Dronabinol oral solution in the management of anorexia and weight loss in AIDS and cancer , 2018, Therapeutics and clinical risk management.

[30]  S. Steffens,et al.  Cardiovascular effects of marijuana and synthetic cannabinoids: the good, the bad, and the ugly , 2018, Nature Reviews Cardiology.

[31]  R. J. Doerksen,et al.  Selective Cannabinoid 2 Receptor Stimulation Reduces Tubular Epithelial Cell Damage after Renal Ischemia-Reperfusion Injury , 2018, The Journal of Pharmacology and Experimental Therapeutics.

[32]  Albert C. Pan,et al.  Entry from the Lipid Bilayer: A Possible Pathway for Inhibition of a Peptide G Protein-Coupled Receptor by a Lipophilic Small Molecule. , 2015, Biochemistry.

[33]  I. Gaidarov,et al.  Discovery of APD371: Identification of a Highly Potent and Selective CB2 Agonist for the Treatment of Chronic Pain. , 2017, ACS medicinal chemistry letters.

[34]  A. IJzerman,et al.  A Novel Selective Inverse Agonist of the CB2 Receptor as a Radiolabeled Tool Compound for Kinetic Binding Studies , 2017, Molecular Pharmacology.

[35]  Shan Jiang,et al.  Crystal structures of agonist-bound human cannabinoid receptor CB1 , 2017, Nature.

[36]  David J. Fleet,et al.  cryoSPARC: algorithms for rapid unsupervised cryo-EM structure determination , 2017, Nature Methods.

[37]  H. de Vries,et al.  Cannabinoid CB2 receptor ligand profiling reveals biased signalling and off-target activity , 2017, Nature Communications.

[38]  A. Howlett,et al.  CB1 and CB2 Receptor Pharmacology. , 2017, Advances in pharmacology.

[39]  Slawomir Filipek,et al.  Hydrophobic Ligand Entry and Exit Pathways of the CB1 Cannabinoid Receptor , 2016, J. Chem. Inf. Model..

[40]  Jie Yin,et al.  High-resolution crystal structure of the human CB1 cannabinoid receptor , 2016, Nature.

[41]  R. Stevens,et al.  Crystal Structure of the Human Cannabinoid Receptor CB1 , 2016, Cell.

[42]  A. McAinch,et al.  Renal effects of chronic pharmacological manipulation of CB2 receptors in rats with diet‐induced obesity , 2016, British journal of pharmacology.

[43]  L. Pardo,et al.  The pathway of ligand entry from the membrane bilayer to a lipid G protein-coupled receptor , 2016, Scientific Reports.

[44]  L. Heitman,et al.  The novel, orally available and peripherally restricted selective cannabinoid CB2 receptor agonist LEI‐101 prevents cisplatin‐induced nephrotoxicity , 2016, British journal of pharmacology.

[45]  W. Guba,et al.  Novel Triazolopyrimidine‐Derived Cannabinoid Receptor 2 Agonists as Potential Treatment for Inflammatory Kidney Diseases , 2016, ChemMedChem.

[46]  G. Bruno,et al.  Deficiency of cannabinoid receptor of type 2 worsens renal functional and structural abnormalities in streptozotocin-induced diabetic mice. , 2014, Kidney international.

[47]  R. Mechoulam,et al.  Early phytocannabinoid chemistry to endocannabinoids and beyond , 2014, Nature Reviews Neuroscience.

[48]  John Reilly,et al.  Observed Drug-Receptor Association Rates Are Governed by Membrane Affinity: The Importance of Establishing “Micro-Pharmacokinetic/Pharmacodynamic Relationships” at the β2-Adrenoceptor , 2014, Molecular Pharmacology.

[49]  Hugh Rosen,et al.  Crystal Structure of a Lipid G Protein–Coupled Receptor , 2012, Science.

[50]  S. Boyce,et al.  Discovery and optimization of 1-(4-(pyridin-2-yl)benzyl)imidazolidine-2,4-dione derivatives as a novel class of selective cannabinoid CB2 receptor agonists. , 2011, Journal of medicinal chemistry.

[51]  P Pacher,et al.  Is lipid signaling through cannabinoid 2 receptors part of a protective system? , 2011, Progress in lipid research.

[52]  Stephen P. H. Alexander,et al.  International Union of Basic and Clinical Pharmacology. LXXIX. Cannabinoid Receptors and Their Ligands: Beyond CB1 and CB2 , 2010, Pharmacological Reviews.

[53]  A. Howlett,et al.  CB(1) cannabinoid receptors and their associated proteins. , 2010, Current medicinal chemistry.

[54]  P. Emsley,et al.  Features and development of Coot , 2010, Acta crystallographica. Section D, Biological crystallography.

[55]  H. Pan,et al.  Cannabinoid-2 receptor limits inflammation, oxidative/nitrosative stress, and cell death in nephropathy. , 2010, Free radical biology & medicine.

[56]  Randy J. Read,et al.  Acta Crystallographica Section D Biological , 2003 .

[57]  Vincent B. Chen,et al.  Correspondence e-mail: , 2000 .

[58]  A. Hohmann,et al.  Cannabinoid CB2 receptors: a therapeutic target for the treatment of inflammatory and neuropathic pain , 2008, British journal of pharmacology.

[59]  H. Pan,et al.  Cannabinoid‐2 receptor mediates protection against hepatic ischemia/reperfusion injury , 2007, FASEB journal : official publication of the Federation of American Societies for Experimental Biology.

[60]  Daniel Fleischer,et al.  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 , 2007, Molecular Pharmacology.

[61]  R. Copeland,et al.  Drug–target residence time and its implications for lead optimization , 2006, Nature Reviews Drug Discovery.

[62]  P. Pacher,et al.  The Endocannabinoid System as an Emerging Target of Pharmacotherapy , 2006, Pharmacological Reviews.

[63]  David N Mastronarde,et al.  Automated electron microscope tomography using robust prediction of specimen movements. , 2005, Journal of structural biology.

[64]  Conrad C. Huang,et al.  UCSF Chimera—A visualization system for exploratory research and analysis , 2004, J. Comput. Chem..

[65]  M. Herkenham,et al.  International Union of Pharmacology. XXVII. Classification of Cannabinoid Receptors , 2002, Pharmacological Reviews.

[66]  H. Weinstein,et al.  Comparison of the amino acid residues in the sixth transmembrane domains accessible in the binding-site crevices of mu, delta, and kappa opioid receptors. , 2001, Biochemistry.

[67]  R. Mechoulam,et al.  HU-308: a specific agonist for CB(2), a peripheral cannabinoid receptor. , 1999, Proceedings of the National Academy of Sciences of the United States of America.

[68]  J. Ballesteros,et al.  A cluster of aromatic residues in the sixth membrane-spanning segment of the dopamine D2 receptor is accessible in the binding-site crevice. , 1998, Biochemistry.

[69]  B. Martin,et al.  Cannabis: pharmacology and toxicology in animals and humans. , 1996, Addiction.

[70]  M. Krečmerová,et al.  Lipases as Tools in the Synthesis of Prodrugs from Racemic 9-(2,3-Dihydroxypropyl)adenine , 2012, Molecules.

[71]  S. Galiègue,et al.  Expression of central and peripheral cannabinoid receptors in human immune tissues and leukocyte subpopulations. , 1995, European journal of biochemistry.

[72]  S. Munro,et al.  Molecular characterization of a peripheral receptor for cannabinoids , 1993, Nature.

[73]  H. Okayama,et al.  High-efficiency transformation of mammalian cells by plasmid DNA. , 1987, Molecular and cellular biology.

[74]  P. K. Smith,et al.  Measurement of protein using bicinchoninic acid. , 1985, Analytical biochemistry.

[75]  Y. Cheng,et al.  Relationship between the inhibition constant (K1) and the concentration of inhibitor which causes 50 per cent inhibition (I50) of an enzymatic reaction. , 1973, Biochemical pharmacology.

[76]  O. Mock [Animals and humans]. , 1967, Therapie der Gegenwart.