التفاصيل البيبلوغرافية
| العنوان: |
GIP receptor: Expression in neuroendocrine tumours, internalization, signalling from endosomes and structure-function relationship studies |
| المؤلفون: |
Jean Claude Reubi, Véronique Gigoux, Irina G. Tikhonova, Daniel Fourmy, Arnau Cordomí |
| المصدر: |
Reubi, J C, Fourmy, D, Cordomi, A, Tikhonova, I G & Gigoux, V 2019, ' GIP receptor : Expression in neuroendocrine tumours, internalization, signalling from endosomes and structure-function relationship studies ', Peptides, pp. 170229 . https://doi.org/10.1016/j.peptides.2019.170229 |
| بيانات النشر: |
Elsevier, 2020. |
| سنة النشر: |
2020 |
| مصطلحات موضوعية: |
endocrine system, Gs alpha subunit, Physiology, Endosome, media_common.quotation_subject, 030209 endocrinology & metabolism, Enteroendocrine cell, Stimulation, Endosomes, Biochemistry, Receptors, Gastrointestinal Hormone, 03 medical and health sciences, Cellular and Molecular Neuroscience, Structure-Activity Relationship, 0302 clinical medicine, Endocrinology, Animals, Humans, Binding site, Internalization, Receptor, 610 Medicine & health, media_common, Chemistry, Endocytosis, Transmembrane domain, Neuroendocrine Tumors, Cancer research, 570 Life sciences, biology, 030217 neurology & neurosurgery, hormones, hormone substitutes, and hormone antagonists, Signal Transduction |
| الوصف: |
GIP is well known as a peptide regulating metabolic functions. In this review paper, we summarize a series of data on GIP receptor (GIPR). First, expression study of GIPR in human neuroendocrine tumours showed a very high incidence (nearly 100%) and a high density in both functional and non functional pancreatic tumours, ileal tumours, bronchial tumours and medullary thyroid carcinomas. Then, data on internalization of GIPR following stimulation by GIP are reported. Rapid and abundant internalization of GIPR also found in tumor pancreatic endocrine cells opens the possibility of tumor imaging and eradication using radiolabeled GIP. Interestingly, internalized GIPR continues to signal in early endosomes stimulating production of cAMP and activation of PKA, thus, supporting the view that GIPR signals from both plasma membrane and vesicles of internalization. At last, we summarize data from studies using in synergy molecular modeling and site-directed mutagenesis, which identified crucial amino acids of transmembrane domains of GIPR involved in GIPR binding site of GIP and/or in its activation and coupling to Gs protein. All together, these last molecular data may help to better understand structure-activity relationship data on GIP and GIPR. |
| وصف الملف: |
application/pdf |
| اللغة: |
English |
| DOI: |
10.7892/boris.138365 |
| DOI: |
10.1016/j.peptides.2019.170229 |
| URL الوصول: |
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ec9391b2c076bd2e61ec8e9d6f7a0fc0 |
| Rights: |
OPEN |
| رقم الانضمام: |
edsair.doi.dedup.....ec9391b2c076bd2e61ec8e9d6f7a0fc0 |
| قاعدة البيانات: |
OpenAIRE |