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口服活性胰岛素模拟物:我们目前的进展如何?

Orally active insulin mimics: where do we stand now?

作者信息

Balasubramanyam M, Mohan V

机构信息

Madras Diabetes Research Foundation (MDRF), 35 Conran Smith Road, Gopalapuram, Chennai 600 086, India.

出版信息

J Biosci. 2001 Sep;26(3):383-90. doi: 10.1007/BF02703748.

DOI:10.1007/BF02703748
PMID:11568484
Abstract

The war against diabetes through the development of new drugs is an ongoing continuous process to counter the alarming global increase in the prevalence of diabetes and its complications, particularly in developing countries like India. Unfortunately, the speed with which our knowledge of diabetes and its effects is expanding is not matched by the availability of new drugs. Following the identification of the insulin receptor (IR), its intrinsic kinase activity and molecular cloning, many studies have looked at IR as an ideal drug target. This review summarizes in brief the latest advancements in this field with particular reference to the current situation in respect of the development of orally active insulin mimetics in the treatment of type 2 diabetes.

摘要

通过研发新药对抗糖尿病的斗争是一个持续不断的过程,以应对全球糖尿病及其并发症患病率惊人增长的情况,尤其是在印度这样的发展中国家。不幸的是,我们对糖尿病及其影响的认知扩展速度与新药的可获得性并不匹配。在鉴定出胰岛素受体(IR)、其内在激酶活性及分子克隆之后,许多研究将IR视为理想的药物靶点。本综述简要总结了该领域的最新进展,特别提及了口服活性胰岛素模拟物治疗2型糖尿病的研发现状。

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本文引用的文献

1
Design and in vivo evaluation of an oral delivery system for insulin.胰岛素口服给药系统的设计与体内评价
Pharm Res. 2000 Dec;17(12):1468-74. doi: 10.1023/a:1007696723125.
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Molecular basis for the dephosphorylation of the activation segment of the insulin receptor by protein tyrosine phosphatase 1B.蛋白酪氨酸磷酸酶1B使胰岛素受体激活片段去磷酸化的分子基础。
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The molecular mechanism of the insulin-mimetic/sensitizing activity of the antidiabetic sulfonylurea drug Amaryl.
抗糖尿病磺脲类药物亚莫利的胰岛素模拟/增敏活性的分子机制。
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Crystallographic and solution studies of an activation loop mutant of the insulin receptor tyrosine kinase: insights into kinase mechanism.胰岛素受体酪氨酸激酶激活环突变体的晶体学与溶液研究:对激酶机制的见解
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Mechanisms of vanadium action: insulin-mimetic or insulin-enhancing agent?钒的作用机制:胰岛素模拟剂还是胰岛素增强剂?
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Discovery of a potent, highly selective, and orally efficacious small-molecule activator of the insulin receptor.发现一种强效、高度选择性且口服有效的胰岛素受体小分子激活剂。
J Med Chem. 2000 Sep 21;43(19):3487-94. doi: 10.1021/jm000285q.
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Oral hypoglycaemic activity of Ipomoea aquatica.
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Activation of insulin signal transduction pathway and anti-diabetic activity of small molecule insulin receptor activators.小分子胰岛素受体激活剂的胰岛素信号转导通路激活及抗糖尿病活性
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10
Chemistry and insulin-like properties of vanadium(IV) and vanadium(V) compounds.钒(IV)和钒(V)化合物的化学性质及类胰岛素特性。
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