From magic bullets to designed multiple ligands

被引：655

作者：

Morphy, R ^{[1
]}

Kay, C ^{[1
]}

Rankovic, Z ^{[1
]}

机构：

[1] Organon Labs, Dept Med Chem, Newhouse ML1 5SH, Lanark, Scotland

来源：

DRUG DISCOVERY TODAY | 2004年 / 9卷 / 15期

关键词：

D O I：

10.1016/S1359-6446(04)03163-0

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

Increasingly, it is being recognised that a balanced modulation of several targets can provide a superior therapeutic effect and side effect profile compared to the action of a selective ligand. Rational approaches in which structural features from selective ligands are combined have produced designed multiple ligands that span a wide variety of targets and target classes. A key challenge in the design of multiple ligands is attaining a balanced activity at each target of interest while simultaneously achieving a wider selectivity and a suitable pharmacokinetic profile. An analysis of literature examples reveals trends and insights that might help medicinal chemists discover the next generation of these types of compounds.

引用

页码：641 / 651

页数：11

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