Constitutive activation of the neurotensin receptor 1 by mutation of Phe358 in helix seven

British Journal of Pharmacology

Volumn 135, Issue 4, 2002, Pages 997-1002

  Barroso, Séverine ^a   Richard, Françoise ^a   Nicolas Ethève, Delphine ^a   Kitabgi, Patrick ^a   Labbé Jullié, Catherine ^a  

^a INSTITUT DE PHARMACOLOGIE MOLÉCULAIRE ET CELLULAIRE   (France)

Author keywords

Constitutive activity; G protein coupled receptor; Mutation; Neurotensin; NTS1

Indexed keywords

CYCLIC AMP; G PROTEIN COUPLED RECEPTOR; INOSITOL PHOSPHATE; NEUROTENSIN; NEUROTENSIN RECEPTOR; PHENYLALANINE;

ANIMAL CELL; ARTICLE; CELL STRAIN COS1; CONCENTRATION RESPONSE; MUTATION; NONHUMAN; PRIORITY JOURNAL;

ANIMALS; BINDING SITES; COS CELLS; CYCLIC AMP; GTP-BINDING PROTEINS; INOSITOL PHOSPHATES; PHENYLALANINE; POINT MUTATION; PROTEIN STRUCTURE, SECONDARY; PYRAZOLES; QUINOLINES; RATS; RECEPTORS, NEUROTENSIN;

EID: 0036185646     PISSN: 00071188     EISSN: None     Source Type: Journal    
DOI: 10.1038/sj.bjp.0704546     Document Type: Article

References (31)

1. Identification of residues involved in neurotensin binding and modeling of the agonist binding site in neurotensin receptor 1
2. Constitutive activation of the delta opioid receptor by mutations in transmembrane domains III and VII
3. Immunological and biochemical characterization of processing products from the neurotensin/neuromedin N precursor in the rat medullary thyroid carcinoma 6-23 cell line
4. Pharmacology of muscarinic receptor subtypes constitutively activated by G proteins
5. Inverse agonist activity of beta-adrenergic antagonists
6. Human calcitonin receptors exhibit agonist-independent (constitutive) signaling activity
7. Mechanism of activation and inactivation of opsin: Role of Glu113 and Lys296
8. Requirement of rigid-body motion of transmembrane helices for light activation of rhodopsin
9. Constitutive activation of the human vasoactive intestinal peptide 1 receptor, a member of the new class II family of G protein-coupled receptors
10. G protein-coupled receptors. II. Mechanism of agonist activation
11. Agonists induce conformational changes in transmembrane domains III and VI of the beta2 adrenoceptor
12. Mutation of Asn111 in third transmembrane domain of the AT1A angiotensin II receptor induces its constitutive activation
13. Biochemical and pharmacological profile of a potent and selective nonpeptide antagonist of the neurotensin receptor
14. Mutagenesis and modeling of the neurotensin receptor NTR1. Identification of residues that are critical for binding SR 48692, a nonpeptide neurotensin antagonist
15. Ligand: A versatile computerized approach for characterization of ligand-binding systems
16. Thrombin receptor activating mutations. Alteration of an extracellular agonist recognition domain causes constitutive signaling
17. Somatic mutations causing constitutive activity of the thyrotropin receptor are the major cause of hyperfunctioning thyroid adenomas: Identification of additional mutations activating both the cyclic adenosine 3′,5′-monophosphate and inositol phosphate-Ca2+cascades
18. Review: Amino acid domains involved in constitutive activation of G- protein-coupled receptors
19. Activation of the alphalb-adrenergic receptor is initiated by disruption of an interhelical salt bridge constraint
20. Characteristics for a salt-bridge switch mutation of the alpha(1b) adrenergic receptor. Altered pharmacology and rescue of constitutive activity
21. Impaired G protein coupling of the neurotensin receptor by mutations in extracellular loop 3
22. Constitutively active mutants of rhodopsin
23. Potency of ligands correlates with affinity measured against agonist and inverse agonists but not against neutral ligand in constitutively active chemokine receptor
24. Neurotensin and neuroendocrine regulation
25. Use of nonpeptide antagonists to explore the physiological roles of neurotensin. Focus on brain neurotensin/dopamine interactions
26. Constitutively active G protein-coupled receptors: Potential mechanisms of receptor activation
27. Inverse agonists and neutral antagonists of recombinant human Al adenosine receptors stably expressed in Chinese hamster ovary cells
28. Involvement of Trp-284, Val-296, and Val297 of the human delta-opioid receptor in binding of delta-selective ligands
29. Neurotensin and neurotensin receptors
30. Neurotensin receptors: Binding properties, transduction pathways, and structure
31. Deletion mutation in the putative third intracellular loop of the rat neurotensin receptor abolishes polyphosphoinositide hydrolysis but not cyclic AMP formation in CHO-K1 cells