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生长抑素受体选择性非肽配体发现方面的最新进展。

Recent progress in the discovery of selective, non-peptide ligands of somatostatin receptors.

作者信息

Wolkenberg Scott E, Thut Catherine J

机构信息

Merck and Co Inc, PO Box 4, WP14-1, West Point, PA 19486, USA.

出版信息

Curr Opin Drug Discov Devel. 2008 Jul;11(4):446-57.

Abstract

Over the past 5 years, researchers in industry and academia have reported the design, synthesis and evaluation of many non-peptide ligands for somatostatin receptors. Structurally diverse agonists and antagonists that, in some cases, exhibit selectivity among the somatostatin receptor subtypes have been published. These agents represent research tools for the clarification of individual receptor pharmacology and are also promising leads for the development of orally active therapeutics for endocrine disorders, proliferative diseases and mood disorders. This review summarizes recent developments in the identification of non-peptide ligands of somatostatin receptors.

摘要

在过去5年里,工业界和学术界的研究人员报告了许多用于生长抑素受体的非肽配体的设计、合成和评估。已经发表了结构多样的激动剂和拮抗剂,在某些情况下,它们在生长抑素受体亚型中表现出选择性。这些药物是用于阐明个体受体药理学的研究工具,也是开发用于治疗内分泌疾病、增殖性疾病和情绪障碍的口服活性疗法的有前景的先导物。这篇综述总结了生长抑素受体非肽配体鉴定方面的最新进展。

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