GIP receptor: Expression in neuroendocrine tumours, internalization, signalling from endosomes and structure-function relationship studies.

Reubi, Jean Claude; Fourmy, Daniel; Cordomi, Arnau; Tikhonova, Irina G; Gigoux, Véronique (2020). GIP receptor: Expression in neuroendocrine tumours, internalization, signalling from endosomes and structure-function relationship studies. Peptides, 125, p. 170229. Elsevier 10.1016/j.peptides.2019.170229

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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.

Item Type:

Journal Article (Review Article)

Division/Institute:

04 Faculty of Medicine > Service Sector > Institute of Pathology

UniBE Contributor:

Reubi-Kattenbusch, Jean-Claude

Subjects:

500 Science > 570 Life sciences; biology
600 Technology > 610 Medicine & health

ISSN:

0196-9781

Publisher:

Elsevier

Language:

English

Submitter:

Aurel Perren

Date Deposited:

28 Jan 2020 12:38

Last Modified:

14 Mar 2020 01:33

Publisher DOI:

10.1016/j.peptides.2019.170229

PubMed ID:

31857104

Uncontrolled Keywords:

Activation mechanism Binding site GIP Internalization Neuroendocrine tumours Receptor Signaling

BORIS DOI:

10.7892/boris.138365

URI:

https://boris.unibe.ch/id/eprint/138365

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