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[沙利度胺的致畸性及其直接靶点鉴定]

[Thalidomide teratogenicity and its direct target identification].

作者信息

Ito Takumi, Ando Hideki, Handa Hiroshi

出版信息

Nihon Rinsho. 2015 Jan;73(1):143-8.

Abstract

Half a century ago, thalidomide was developed as a sedative drug and was wildly used over 40 countries. However the drug has serious birth defects such as amelia and phocomelia. Now thalidomide is regarded as a clinically effective drug and used for the treatment of multiple myeloma under strict controls. The direct target of thalidomide had been a long-standing question. We identified cereblon as a primary direct target protein for thalidomide teratogenicity using new affinity bead technology in 2010. In this review, we introduce an overview of thalidomide teratogenicity, a story about how we identified cereblon, and recent advances in cereblon studies.

摘要

半个世纪前,沙利度胺作为一种镇静药物被研发出来,并在40多个国家广泛使用。然而,这种药物会导致严重的出生缺陷,如无肢畸形和短肢畸形。如今,沙利度胺被视为一种临床有效药物,在严格管控下用于治疗多发性骨髓瘤。沙利度胺的直接靶点长期以来一直是个问题。2010年,我们使用新的亲和珠技术确定了脑啡肽酶是沙利度胺致畸性的主要直接靶点蛋白。在这篇综述中,我们介绍了沙利度胺致畸性的概述、我们如何确定脑啡肽酶的过程,以及脑啡肽酶研究的最新进展。

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