Identification of New GPCR Targets in NET Cell Lines Using Ligand Screening

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Introduction: Although somatostatin analogs constitute an important part of current therapeutic strategies, both hypersecretion and proliferation of NETs cannot be controlled efficiently in many patients. Identifying and dissecting new molecular targets and regulatory pathways may help to improve diagnostic and therapeutic options for NET patients.

Aim(s): This study was focused on identifying new G protein-coupled receptor (GPCR) targets on neuroendocrine tumor cells, with special attention to peptide GPCRs and receptors for licenced drugs. Their role in NET cell signaling, secretion and proliferation was studied.

Materials and methods: A ligand screen involving 1,200 peptide and small-molecule ligands was carried out on six permanent cell lines derived from human NETs, among them BON and H727 cells. Dynamic mass redistribution, calcium and cAMP were measured to screen or confirm reactivities of ligands, including specific analogs or antagonists. Proliferation was measured using DAPI HCA or BrDU staining, secretion by ELISA assays.

Conference: 10th Annual ENETSConcerence (2013)

Presenting Author:

Authors: Körner J, Schuldt C, Giesecke Y, Du J, Eichhorn I,

Keywords: secretion, receptor, GPCR, target,