摘要
Eph-ephrin系统是多种疾病包括癌症,糖尿病,神经退行性疾病和炎症的一个潜在的新靶点。过去十年中,在开发Eph受体小分子拮抗剂方面已作出一些努力。天然和合成的化合物被发现,如(聚)苯酚和甾体衍生物,α1激动剂多沙唑嗪,2,5-二甲基吡咯 - 1-苯甲酸及石胆酸和其他氨基酸的结合物。本文为这些化合物提供可用的数据,并讨论其作为药理学工具或领先优化程序的候选者的潜在有效性。
关键词: Eph,肝配蛋白,药物发现,小分子,蛋白质 - 蛋白质,拮抗剂
图形摘要
Current Drug Targets
Title:Targeting the Eph-ephrin System with Protein-Protein Interaction (PPI) Inhibitors
Volume: 16 Issue: 10
Author(s): Massimiliano Tognolini and Alessio Lodola
Affiliation:
关键词: Eph,肝配蛋白,药物发现,小分子,蛋白质 - 蛋白质,拮抗剂
摘要: Eph-ephrin system is emerging as a new potential target in several diseases including cancer, diabetes, neurodegenerative diseases and inflammation. In the last decade, several efforts have been made to develop small molecule antagonists of Eph receptors. Both natural and synthetic compounds were discovered with (poly) phenol and steroidal derivatives on one side and the α1 agonist doxazosin, 2,5-dimethylpyrrol- 1-yl-benzoic acids and amino acid conjugates of lithocholic acid on the other. In the present paper we critically present available data for these compounds and discuss their potential usefulness as pharmacological tools or as candidates for a lead-optimization program.
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Cite this article as:
Massimiliano Tognolini and Alessio Lodola , Targeting the Eph-ephrin System with Protein-Protein Interaction (PPI) Inhibitors, Current Drug Targets 2015; 16 (10) . https://dx.doi.org/10.2174/1389450116666150825144457
DOI https://dx.doi.org/10.2174/1389450116666150825144457 |
Print ISSN 1389-4501 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-5592 |
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