A novel somatostatin mimic with broad somatotropin release inhibitory factor receptor binding and superior therapeutic potential

被引：106

作者：

Lewis, I ^{[1
]}

Bauer, W ^{[1
]}

Albert, R ^{[1
]}

Chandramouli, N ^{[1
]}

Pless, J ^{[1
]}

Weckbecker, G ^{[1
]}

Bruns, C ^{[1
]}

机构：

[1] Novartis Pharma, Transplantat Res Dept, CH-4002 Basel, Switzerland

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 2003年 / 46卷 / 12期

关键词：

D O I：

10.1021/jm021093t

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A rational drug design approach, capitalizing on structure-activity relationships and involving transposition of functional groups from somatotropin release inhibitory factor (SRIF) into a reduced size cyclohexapeptide template, has led to the discovery of SOM230 (25), a novel, stable cyclohexapeptide somatostatin mimic that exhibits unique high-affinity binding to human somatostatin receptors (subtypes sst1-sst5). SOM230 has potent, long-lasting inhibitory effects on growth hormone and insulin-like growth factor-1 release and is a promising development candidate currently under evaluation in phase I clinical trials.

引用

页码：2334 / 2344

页数：11

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