The use of constitutively active receptors for drug discovery at the g protein-coupled receptor gene pool

Current Opinion in Drug Discovery and Development

Volumn 4, Issue 5, 2001, Pages 548-560

  Behan, D P ^a   Chalmers, D T ^a  

^a ARENA PHARMACEUTICALS   (United States)

Author keywords

Constitutive activity; G protein coupled receptor; Inverse agonist; Melanophores; Screening platforms

Indexed keywords

3 ISOPROPYLAMINO 1 (7 METHYL 4 INDANYLOXY) 2 BUTANOL; ALPRENOLOL; BAY 367620; CIMETIDINE; G PROTEIN COUPLED RECEPTOR; ISOPRENALINE; LIGAND; N (2,3 DIPHENYL 1,2,4 THIADIAZOL 5(2H) YLIDENE)METHANAMINE; RANITIDINE; RESERPINE; SOTALOL; THIOPERAMIDE; UNCLASSIFIED DRUG; CHIMERIC PROTEIN; DRUG RECEPTOR; GTP BINDING PROTEINS; GUANINE NUCLEOTIDE BINDING PROTEIN;

AGONIST; DRUG TARGETING; GENE MUTATION; GENE OVEREXPRESSION; GENE POOL; GENE SEQUENCE; HUMAN; MELANOPHORE; NONHUMAN; REVIEW; SCREENING; SITE DIRECTED MUTAGENESIS; ANIMAL; CHEMISTRY; DRUG DESIGN; DRUG EFFECT; DRUG POTENTIATION; GENETICS; MUTATION; PHARMACOLOGY; UPREGULATION;

ANIMAL; CHIMERIC PROTEINS; DRUG DESIGN; GTP-BINDING PROTEINS; HUMAN; MUTATION; PHARMACOLOGY; RECEPTORS, DRUG; UP-REGULATION;

EID: 0034812072     PISSN: 13676733     EISSN: None     Source Type: Journal    
DOI: None     Document Type: Review

References (54)

1. Antagonists with negative intrinsic activity at δ-opioid receptors coupled to GTP-binding proteins
2. Somatic mutations in the thyrotropin receptor gene cause hyperfunctioning thyroid adenomas
3. Constitutive activation of fibroblast growth factor receptor-2 by a point mutation associated with Crouzon syndrome
4. Hypercalcemia due to constitutive activity of the parathyroid hormone (PTH)/PTH-related peptide receptor: Comparison with primary hyperparathyroidism
5. 2+-sensing receptor (PCAR1) mutation T151M in isolated autosomal dominant hypoparathyroidism
6. A novel mutation of the luteinizing hormone receptor gene causing male gonadotropin-independent precocious puberty
7. Characterization of heterogenous mutations causing constitutive activation of the luteinizing hormone receptor in familial male precocious puberty
8. Genetic heterogeneity of constitutively activating mutations of the human luteinizing hormone receptor in familial male-limited precocious puberty
9. 1-adrenergic receptor involved in coupling to phosphatidylinositol hydrolysis and enhanced sensitivity of biological function
10. 2-adrenergic receptor. Extending the ternary complex model
11. Constitutive activity of receptors coupled to guanine nucleotide regulatory proteins
12. Inverse, protean, and ligand-selective agonism: Matters of receptor conformation
13. 3 receptors regulates histamine neurons in brain
14. 2-adrenoreceptor
15. 2 receptors
16. 2-adrenoreceptor by sustained treatment with inverse agonists but not antagonists
17. Detection of receptor ligands by monitoring selective stabilization of Renilla luciferase-tagged, constitutively active mutant, G-protein-coupled receptor
18. 2-adrenoreceptor-green fluorescent protein fusion proteins
19. BAY36-7620: A potent non-competitive mGlu1 receptor antagonist with inverse agonist activity
20. SCH-202676: An allosteric modulator of both agonist and antagonist binding to G protein-coupled receptors
21. αo protein coexpression: Evidence for inverse agonism
22. Systematic identification of mutations that constitutively activate the angiotensin II type 1A receptor by screening a randomly mutated cDNA library with an original pharmacological bioassay
23. Interaction between transmembrane domains five and six of the α-factor receptor
24. Activation of luteinizing hormone receptor following substitution of Ser-277 with selective hydrophobic residues in the ectodomain hinge region
25. A conserved ASN in transmembrane helix 7 is an on/off switch in the activation of the thyrotropin receptor
26. 2 adrenergic receptor: Constitutive activation, structural instability, and conformational rearrangement of transmembrane segment 6
27. 2 adrenergic receptor involves disruption of an ionic lock between the cytoplasmic ends of transmembrane segments 3 and 6
28. 2 receptor
29. 1b-adrenergic receptor
30. Point mutations causing constitutive signaling of CXCR2 leads to transforming activity similar to Kaposi's sarcoma herpesvirus-G protein-coupled receptor
31. 128 in the third transmembrane domain of the δ-opioid receptor
32. oα protein interactions
33. Characterization of the molecular motions of constitutively active G protein-coupled receptors for parathyroid hormone
34. 1: Precoupling and constitutive activity
35. 2C receptors revealed by heterologous expression
36. 1 protein
37. 1A receptor. Inhibition by anxiolytic partial agonists
38. The human B1 bradykinin receptor exhibits high ligand-independent, constitutive activity. Roles of residues in the fourth intracellular and third transmembrane domains
39. Constitutive signaling by Kaposi's sarcoma-associated herpesvirus G protein-coupled receptor desensitizes calcium mobilization by other receptors
40. Constitutive signaling of the human cytomegalovirus-encoded chemokine receptor US28
41. oα GTPase activity
42. 6 in mammalian cells: Identification of a specific signal transduction species not characteristic of constitutive activation or precoupling
43. 17α
44. oα: Impact on receptor and effector coupling
45. Constitutive activation of tethered-peptide/corticotropin releasing factor receptor chimeras
46. High-throughput quantification of cAMP production mediated by activation of seven transmembrane domain receptors
47. Tools for investigating functional interactions between ligands and G protein-coupled receptors
48. Functional expression and characterization of human D2 and D3 dopamine receptors
49. Use of constitutive G protein-coupled receptor activity for drug discovery
50. A novel system that reports the G-proteins linked to a given receptor: A study of type 3 somatostatin receptor
51. q mutants
52. Functional characterization of a series of mutant G protein αq subunits displaying promiscuous receptor coupling properties
53. 1-coupled receptors
54. The orphan G-protein-coupled receptor ARE113 is a novel receptor target for obesity