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神经内分泌肿瘤中的生长抑素 - 多巴胺嵌合分子

Somatostatin-Dopamine Chimeric Molecules in Neuroendocrine Neoplasms.

作者信息

Cantone Maria Celeste, Dicitore Alessandra, Vitale Giovanni

机构信息

Department of Medical Biotechnologies and Translational Medicine, University of Milan, 20129 Milan, Italy.

IRCCS, Laboratory of Geriatric and Oncologic Neuroendocrinology Research, Istituto Auxologico Italiano, 20095 Cusano Milanino, Italy.

出版信息

J Clin Med. 2021 Feb 1;10(3):501. doi: 10.3390/jcm10030501.

Abstract

Neuroendocrine neoplasms (NENs) are a widely heterogeneous family of neoplasms arising from neuroendocrine cells, which are interspersed throughout the body. Despite NENs are relatively rare, their incidence and prevalence are constantly increasing probably due to the improvement in earlier diagnosis and patients' management. When surgery is not curative, particularly for patients with metastatic disease, several medical options are available. Somatostatin analogues (SSA) are the first-line medical therapy for well-differentiated NENs. Interestingly, the heterodimerization of somatostatin receptors (s) with dopamine receptors (DRs) has been discovered in NENs. This phenomenon results in hybrid receptors with enhanced functional activity. On these bases, chimeric molecules embracing somatostatin and dopamine features have been recently developed. The aim of this review is to provide a comprehensive overview of the available preclinical and clinical data regarding chimeric somatostatin-dopamine agonists as a new class of "magic bullet" in the therapy of NENs.

摘要

神经内分泌肿瘤(NENs)是一类广泛的异质性肿瘤家族,起源于散在分布于全身的神经内分泌细胞。尽管NENs相对罕见,但由于早期诊断和患者管理的改善,其发病率和患病率正在不断上升。当手术无法治愈时,特别是对于转移性疾病患者,有几种医学治疗选择。生长抑素类似物(SSA)是高分化NENs的一线药物治疗。有趣的是,在NENs中发现了生长抑素受体(s)与多巴胺受体(DRs)的异源二聚化。这种现象导致具有增强功能活性的杂合受体。基于这些,最近已经开发出具有生长抑素和多巴胺特征的嵌合分子。本综述的目的是全面概述关于嵌合生长抑素 - 多巴胺激动剂作为NENs治疗中一类新型“神奇子弹”的现有临床前和临床数据。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f452/7867079/c142974e65b1/jcm-10-00501-g001.jpg

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