摘要
Eph受体是酪氨酸激酶受体(RTK)中最大的亚家族。Eph受体及其肝配蛋白配体,在细胞间信息介导及其发展过程中发挥着核心作用,也在正常成人的生理保养中占据重要角色。因此,它们发生异常,可以促使人类各种疾病发生。目前,由于Eph受体和其配体的结构已被很好的特征化,并有广泛的最新技术以发展方式来操纵他们,以达到较好的治疗效果。虽然一些试验已进展到临床试验阶段,但到目前为止,显而易见,Eph受体是治疗药物的有效靶点。本文首先研究和总结Eph受体三维结构,其次我们将概述以Ephs为靶点的小分子抑制剂和激活剂的使用情况,同时我们将特别侧重于单克隆抗体或抑制或激活Eph/ephrin信号抗体领域的最新发展。
关键词: 三维结构,药物靶点,Eph受体,单克隆抗体,酪氨酸激酶受体,单链抗体,小分子抑制剂。
图形摘要
Current Drug Targets
Title:Eph Receptors as Drug Targets: Single-Chain Antibodies and Beyond
Volume: 16 Issue: 10
Author(s): Urpo Lamminmaki, Dimitar Nikolov and Juha Himanen
Affiliation:
关键词: 三维结构,药物靶点,Eph受体,单克隆抗体,酪氨酸激酶受体,单链抗体,小分子抑制剂。
摘要: The Eph receptors are the largest sub-family of Receptor Tyrosine Kinases (RTK). They, together with their ephrin ligands, play central roles in cell-cell communication during development, and also in the maintenance of a normal adult physiology. Their malfunction, therefore, can contribute to various human diseases. Since the structures of the Eph receptors and ephrins are by now well characterized, there has been extensive recent work to develop ways to manipulate their action in order to achieve therapeutic benefits. Although few reagents have progressed to clinical trials thus far, it is evident that the Eph receptors are valid targets for therapeutic drugs. In this review we first summarize studies on the three-dimensional structures of Eph receptors. We then give an overview on small molecule inhibitors and activators using Ephs as targets. We put a special focus on the latest developments in the field of monoclonal antibodies and antibody fragments for inhibiting or activating the Eph/ephrin signaling.
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Cite this article as:
Urpo Lamminmaki, Dimitar Nikolov and Juha Himanen , Eph Receptors as Drug Targets: Single-Chain Antibodies and Beyond, Current Drug Targets 2015; 16 (10) . https://dx.doi.org/10.2174/1389450116666150531154619
DOI https://dx.doi.org/10.2174/1389450116666150531154619 |
Print ISSN 1389-4501 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-5592 |
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