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Drug Discov Today. 2004 Aug 1;9(15):641-51.

From magic bullets to designed multiple ligands.

Author information

1
Medicinal Chemistry Department, Organon Laboratories, Newhouse, Lanarkshire ML1 5SH, UK. r.morphy@organon.co.uk

Abstract

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.

PMID:
15279847
DOI:
10.1016/S1359-6446(04)03163-0
[Indexed for MEDLINE]
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