Targeting the Eph-ephrin System with Protein-Protein Interaction (PPI) Inhibitors

被引：11

作者：

Tognolini, Massimiliano ^{[1
]}

Lodola, Alessio ^{[1
]}

机构：

[1] Univ Parma, Dipartimento Farm, I-43124 Parma, Italy

来源：

CURRENT DRUG TARGETS | 2015年 / 16卷 / 10期

关键词：

Eph; ephrin; drug discovery; small molecules; protein-protein; antagonist; RECEPTOR TYROSINE KINASE; SMALL MOLECULES; EPHA2-EPHRINA1; SYSTEM; CANCER THERAPEUTICS; DRUG DISCOVERY; CELL CARCINOMA; BINDING; ANTAGONISTS; ANGIOGENESIS; DISEASE;

D O I：

10.2174/1389450116666150825144457

中图分类号：

R9 [药学];

学科分类号：

1007 ;

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 alpha 1 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.

引用

页码：1048 / 1056

页数：9

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