title: Role of the carboxyl-terminal region, di-leucine motif and cysteine residues in signalling and internalization of vasopressin V1a receptor.
abstract: The structural requirements for internalization and signalling of the vasopressin V1a receptor were investigated in stably transfected HEK-293 cells. Removal of the 51 C-terminal amino acids did not affect vasopressin binding, calcium signalling, heterologous desensitization or internalization of the receptor. Deletion of 14 additional amino acids reduced vasopressin-dependent calcium increase and impaired receptor internalization. Substitution of cysteines 371-372 did not affect intracellular signalling, but decreased endocytosis by 26%. Substitution of the 361-362 leucine by alanine residues reduced by 56% V1a receptor sequestration without affecting calcium signalling. These results indicate that di-cysteine and mostly di-leucine motifs present in the C-terminal region of the V1a receptor are involved in its internalization.
authors.affiliation: Service de Biologie Cellulaire, CEA/Saclay, Gif-sur-Yvette, France.
authors.forename: L
authors.initials: L
authors.lastname: Preisser
authors.forename: N
authors.initials: N
authors.lastname: Ancellin
authors.forename: L
authors.initials: L
authors.lastname: Michaelis
authors.forename: C
authors.initials: C
authors.lastname: Creminon
authors.forename: A
authors.initials: A
authors.lastname: Morel
authors.forename: B
authors.initials: B
authors.lastname: Corman
mesh_terms: D002118:Calcium / Q000378:metabolism; D002460:Cell Line; D003545:Cysteine / Q000502:physiology*; D004305:Dose-Response Relationship, Drug; D004797:Enzyme-Linked Immunosorbent Assay; D005455:Fluorescent Antibody Technique; D006801:Humans; D007700:Kinetics; D007930:Leucine / Q000502:physiology*; D008954:Models, Biological; D016296:Mutagenesis; D011485:Protein Binding; D017483:Receptors, Vasopressin / Q000737:chemistry / Q000378:metabolism*; D015398:Signal Transduction; D013997:Time Factors; D014162:Transfection; D014667:Vasopressins / Q000494:pharmacology
chemical_list: D017483:Receptors, Vasopressin; D014667:Vasopressins; D007930:Leucine; D003545:Cysteine; D002118:Calcium