ECE2018 Poster Presentations: Pituitary and Neuroendocrinology Neuroendocrinology (28 abstracts)
Desensitization of the human motilin receptor by motilin and motilides
Bunzo Matsuura , Akiko Takano , Tomoe Kawamura , Shin Yamamoto , Hidenori Senba , Teruki Miyake , Shinya Furukawa , Masanori Abe & Yoichi Hiasa
Ehime University, Toon, Japan.
The motilin receptor (MLNR) belongs to a family of Class I G protein-coupled receptors, and is an important endogenous regulator of gastrointestinal motor function. Motilin and erythromycin (EM), two chemically distinct full agonists of the motilin receptor, bind to distinct regions of this receptor, while the action of these different chemical classes of agonists likely yields a common activation state of the cytosolic face of this receptor that is responsible for interaction with its G protein. In the current work, we studied the desensitization of the MLNR by motilin and motilides in CHO cell line stably expressing the cloned Halo-tagged MLNR. We also studied receptor internalization following application of motilin and motilides visualized by using Halo-tagged MLNR. Desensitization of the MLNR was induced by prestimulation of CHO cells expressing Halo-tagged MLNR with concentration of over 10−8 M of motilin, while was not induced by prestimulation with any concentration of EM or other macrolides. Halo-tagged MLNR was trafficking into the cytosol after motilin and EM stimulation and was recycling to cell surface more slowly with motilin stimulation than with EM stimulation. These data supported that it should be possible to develop motilides with high potency and less desensitizing ability.
Volume 56
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Endocrine Abstracts
ISSN 1470-3947 (print) | ISSN 1479-6848 (online)
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