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二肽基肽酶-IV抑制剂可通过增强肠促胰岛素来恢复2型糖尿病患者的血糖稳态。

Dipeptidyl peptidase-IV inhibitors can restore glucose homeostasis in type 2 diabetics via incretin enhancement.

作者信息

Mest Hans-Juergen

机构信息

Lilly Forschung GmbH, Lilly Research Laboratories, Essener Bogen 7, 22419 Hamburg, Germany.

出版信息

Curr Opin Investig Drugs. 2006 Apr;7(4):338-43.

PMID:16625820
Abstract

Incretin levels approach normal physiological values following treatment with dipeptidyl peptidase (DPP)-IV inhibitors. This is in contrast to incretin levels resulting from the exogenous administration of glucagon-like peptide (GLP)-1 and its analogs, which can reach super-physiological values. This review describes the role of DPP-IV inhibitors as incretin enhancers in the regulation of glucose homeostasis in type 2 diabetic patients. The roles of incretins and the effect of DPP-IV on their actions are described, as are new therapeutic interventions based on the restoration of impaired incretin secretion in type 2 diabetic patients and obese individuals. In addition, the relevance of DPP-IV inhibition for weight control, its potential influence on beta-cell mass, and possible new indications are discussed, as are the implications of the currently available clinical data.

摘要

使用二肽基肽酶(DPP)-IV抑制剂治疗后,肠促胰岛素水平接近正常生理值。这与外源性给予胰高血糖素样肽(GLP)-1及其类似物所导致的肠促胰岛素水平形成对比,后者可达到超生理值。本综述描述了DPP-IV抑制剂作为肠促胰岛素增强剂在2型糖尿病患者葡萄糖稳态调节中的作用。文中阐述了肠促胰岛素的作用以及DPP-IV对其作用的影响,还介绍了基于恢复2型糖尿病患者和肥胖个体受损肠促胰岛素分泌的新治疗干预措施。此外,还讨论了DPP-IV抑制对体重控制的相关性、其对β细胞量的潜在影响以及可能的新适应症,以及现有临床数据的意义。

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Dipeptidyl peptidase-IV inhibitors can restore glucose homeostasis in type 2 diabetics via incretin enhancement.二肽基肽酶-IV抑制剂可通过增强肠促胰岛素来恢复2型糖尿病患者的血糖稳态。
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Role of the incretin pathway in the pathogenesis of type 2 diabetes mellitus.肠促胰岛素途径在 2 型糖尿病发病机制中的作用。
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Synthesis of (S)-1-(2-chloroacetyl)pyrrolidine-2-carbonitrile: a key intermediate for dipeptidyl peptidase IV inhibitors.
(S)-1-(2-氯乙酰基)吡咯烷-2-甲腈的合成:二肽基肽酶 IV 抑制剂的关键中间体。
Beilstein J Org Chem. 2008;4:20. doi: 10.3762/bjoc.4.20. Epub 2008 Jun 12.
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Dipeptidyl peptidase-4 (DPP-4) inhibitors for type 2 diabetes mellitus.用于2型糖尿病的二肽基肽酶-4(DPP-4)抑制剂。
Cochrane Database Syst Rev. 2008 Apr 16;2008(2):CD006739. doi: 10.1002/14651858.CD006739.pub2.