A critical role for a tyrosine residue in the cannabinoid receptors for ligand recognition

Biochemical Pharmacology

Volumn 63, Issue 12, 2002, Pages 2121-2136

  McAllister, Sean D ^a   Tao, Qing ^b   Barnett Norris, Judy ^c   Buehner, Kurt ^c   Hurst, Dow P ^c   Guarnieri, Frank ^d   Reggio, Patricia H ^c   Nowell Harmon, Katharine W ^b   Cabral, Guy A ^b   Abood, Mary E ^a  

^a CALIFORNIA PACIFIC MEDICAL CENTER   (United States)

^b VIRGINIA COMMONWEALTH UNIVERSITY   (United States)

^c KENNESAW STATE UNIVERSITY   (United States)

^d MOUNT SINAI SCHOOL OF MEDICINE   (United States)

Author keywords

cAMP; Cannabinoid receptor; Molecular model; Monte Carlo Stochastic Dynamics; Mutation; Potassium currents

Indexed keywords

2,3 DIHYDRO 5 METHYL 3 (MORPHOLINOMETHYL) 6 (1 NAPHTHOYL)PYRROLO[1,2,3 DE][1,4]BENZOXAZINE; 4 (1,1 DIMETHYLHEPTYL) 1',2',3',4',5',6' HEXAHYDRO 2,3' DIHYDROXY 6' (3 HYDROXYPROPYL)BIPHENYL; AMINO ACID; CANNABINOID 1 RECEPTOR; CANNABINOID 2 RECEPTOR; CANNABINOID RECEPTOR; COMPLEMENTARY DNA; CYCLIC AMP; G PROTEIN COUPLED RECEPTOR; GUANINE NUCLEOTIDE BINDING PROTEIN; ISOLEUCINE; MUTANT PROTEIN; PHENYLALANINE; PROTEIN GIRK1; PROTEIN GIRK4; RADIOLIGAND; RECEPTOR SUBTYPE; TYROSINE; UNCLASSIFIED DRUG;

AMINO ACID SUBSTITUTION; ANIMAL CELL; ARTICLE; BINDING ASSAY; CALCULATION; CONTROLLED STUDY; DRUG POTENCY; GENETIC TRANSFECTION; HUMAN; HUMAN CELL; IMMUNOFLUORESCENCE; LIGAND BINDING; MOLECULAR MODEL; MONTE CARLO METHOD; MUTATION; NONHUMAN; OOCYTE; POTASSIUM CURRENT; PRIORITY JOURNAL; PROTEIN EXPRESSION; SIGNAL TRANSDUCTION; SITE DIRECTED MUTAGENESIS; STOCHASTIC MODEL; WILD TYPE;

AMINO ACID SEQUENCE; COMPUTER SIMULATION; FLUORESCENT ANTIBODY TECHNIQUE; HUMANS; LIGANDS; MODELS, MOLECULAR; MOLECULAR SEQUENCE DATA; MONTE CARLO METHOD; MUTATION; RECEPTORS, CANNABINOID; RECEPTORS, DRUG; RHODOPSIN; SIGNAL TRANSDUCTION; STOCHASTIC PROCESSES; TRYPTOPHAN; TYROSINE;

EID: 0037098239     PISSN: 00062952     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0006-2952(02)01031-6     Document Type: Article

References (53)

1. Molecular cloning of a human cannabinoid receptor which is also expressed in testis
2. Molecular characterization of a peripheral receptor for cannabinoids
3. 2 receptors
4. 2): Identification of cannabinoid receptor subtype-selective ligands
5. Pharmacology of cannabinoid receptors
6. 2 receptors
7. 2 cannabinoid receptor
8. Cannabinoid inhibition of adenylate cyclase. Pharmacology of the response in neuroblastoma cell membranes
9. Activation of the human peripheral cannabinoid receptor results in inhibition of adenylyl cyclase
10. Cannabinoids inhibit N-type calcium channels in neuroblastoma-glioma cells
11. Cannabinoid receptors can activate and inhibit G-protein-coupled inwardly rectifying potassium channels in a Xenopus oocyte expression system
12. 1 antagonist SR141716A
13. Cannabinoid receptor interactions with the antagonists SR141716A and SR144528
14. 2
15. 2): Evidence for subtype specificity
16. Computational studies of Helix 5 residues of the CB receptors that are important for ligand interaction, subtype selectivity and activation
17. A refined model of the thyrotropin-releasing hormone (TRH) receptor binding pocket. Novel mixed mode Monte Carlo/Stochastic Dynamics simulations of the complex between TRH and TRH receptor
18. Crystal structure of rhodopsin: A G-protein-coupled receptor
19. Integrated methods for the construction of three-dimensional models and computational probing of structure function relations in G-protein-coupled receptors
20. 1 receptor: Determination of helix ends and helix orientation
21. Analysis and refinement of criteria for predicting the structure and relative orientations of transmembranal helical domains
22. A proposed structure for transmembrane segment 7 of G-protein-coupled receptors incorporating an Asn-Pro/Asp-Pro motif
23. A reciprocal mutation supports Helix 2 and Helix 7 proximity in the gonadotropin-releasing hormone receptor
24. Conformational memories and the exploration of biologically relevant peptide conformations: An illustration for the gonadotropin-releasing hormone
25. 1 receptor V6.43/I6.46 groove induces a Helix 6 active conformation
26. Functional microdomains in G-protein-coupled receptors. The conserved arginine-cage motif in the gonadotropin-releasing hormone receptor
27. 2 adrenoceptor
28. MacroModel - An integrated software system for modeling organic and bioorganic molecules using molecular mechanics
29. Analysis of the relationship between side-chain conformation and secondary structure in globular proteins
30. Aromatic-aromatic interaction: A mechanism of protein structure stabilization
31. Cannabinoid structure-activity relationships: Correlation of receptor binding and in vivo activities
32. 2, disrupts G-protein coupling
33. 50) of an enzymatic reaction
34. A simple direct assay for cyclic AMP in plasma and other biological samples using an improved competitive protein binding technique
35. Expression of a cannabinoid receptor in baculovirus infected insect cells
36. Residues in the fifth membrane-spanning segment of the dopamine D2 receptor exposed in the binding-site crevice
37. Complex salt bridges in proteins: Statistical analysis of structure and function
38. π-π interactions: The geometry and energetics of phenylalanine-phenylalanine interactions in proteins
39. 2 receptor
40. 2-adrenegic receptor involves disruption of an ionic lock between the cytoplasmic ends of transmembrane segments 3 and 6
41. 2-adrenergic receptor alters the orientation of its sixth membrane-spanning segment
42. SR141716A, a potent and selective antagonist of the brain cannabinoid receptor
43. Activation of inwardly rectifying potassium channels (GIRK1) by co-expressed rat brain cannabinoid receptors in Xenopus oocytes
44. 3H]β-funaltrexamine covalent binding in the cloned rat μ opioid receptor
45. A hydrophobic cluster between transmembrane Helices 5 and 6 constrains the thyrotropin-releasing hormone receptor in an inactive conformation
46. A cluster of aromatic residues in the sixth membrane-spanning segment of the dopamine D2 receptor is accessible in the binding-site crevice
47. Electrostatic and aromatic microdomains within the binding-site crevice of the D2 receptor: Contributions of the second membrane-spanning segment
48. Dopamine D4/D2 receptor selectivity is determined by a divergent aromatic microdomain contained within the second, third, and seventh membrane-spanning segments
49. 2 receptors: Achievements and challenges
50. Relationships between apparent binding energies measured in site-directed mutagenesis experiments and energetics of binding and catalysis
51. A lysine residue of the cannabinoid receptor is critical for receptor recognition by several agonists but not WIN 55212-2
52. Ligand binding and modulation of cyclic AMP levels depend on the chemical nature of residue 192 of the human cannabinoid receptor 1