AGTR1 Is Overexpressed in Neuroendocrine Neoplasms, Regulates Secretion and May Serve as a Target for Molecular Imaging and Therapy

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Introduction: Peptide receptor targeting has proven to be a pivotal tool for diagnostic imaging and radioligand therapy of neuroendocrine neoplasms (NENs), which frequently express somatostatin receptors (SSTRs) on their cell surface. However, up to 30 % of NEN patients do not benefit from SSTR-based approaches, others develop a resistance.

Aim(s): Consequently, alternative cell surface targets need to be identified and characterized.

Materials and methods: Cell-based dynamic mass redistribution and calcium mobilization screening using a 998-compound library identified angiotensin II (ATII) as a strong activator of cellular signaling in NEN cells. Expression analyses of the ATII receptor type 1 (AGTR1) revealed upregulation of mRNA (RT-qPCR) and radioligand binding (autoradiography) in pancreatic (n=42) and small-intestinal (n=71) NEN tissues compared to healthy controls (n=25).

Conference: 17th Annual ENETSConcerence (2020)

Presenting Author:

Authors: Grötzinger C, Exner S, Schuldt C, Du J, Sachindra S,

Keywords: receptor, targeting, imaging, prrt, peptide, angiotensin,