Title: Differences in motilin receptor desensitization after stimulation with motilin or motilides are due to alternative receptor trafficking
Authors: Mitselos, Anna ×
Vanden Berghe, Pieter
Peeters, Theo
Depoortere, Inge #
Issue Date: 2008
Publisher: Pergamon-elsevier science ltd
Series Title: Biochemical Pharmacology vol:75 issue:5 pages:1115-1128
Abstract: Backgrounds & aims: The motilin receptor (MTLR) is an important therapeutic target for treatment of hypomotility disorders. The negative outcome in clinical trials with the motilin agonist, ABT-229, indicated that desensitization may limit the therapeutic usefulness of motilides. We therefore compared the mechanisms involved in the intracellular trafficking of the MTLR after stimulation with motilin, erythromycin-A (EM-A) or ABT-229. Methods: Desensitization was studied by measuring changes in Ca2(+) rises and by receptor binding studies in CHO cells co-expressing the Ca2+ indicator apoaequorin and the MTLR, Cterminally tagged with EGFP. Receptor phosphorylation was studied by immunoprecipitation. MTLR-EGFP trafficking to organelles and translocation of beta-arrestins were visualized by fluorescence microscopy.
ISSN: 0006-2952
Publication status: published
KU Leuven publication type: IT
Appears in Collections:Translational Research in GastroIntestinal Disorders
× corresponding author
# (joint) last author

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