Using structural and mechanistic information to design novel inhibitors/substrates of P-glycoprotein

Design of inhibitors of P-glycoprotein still represents a challenging task for medicinal chemists. The polyspecificity of the transporter combined with the limited structural information renders rational drug design approaches rather ineffective. Within this article we will exemplify how recent insi...

Full description

Saved in:

Bibliographic Details
Published in:	Current topics in medicinal chemistry Vol. 10; no. 17; p. 1769
Main Authors:	Klepsch, Freya, Stockner, Thomas, Erker, Thomas, Müller, Markus, Chiba, Peter, Ecker, Gerhard F
Format:	Journal Article
Language:	English
Published:	United Arab Emirates 01-12-2010
Subjects:	Antineoplastic Agents - chemical synthesis Antineoplastic Agents - chemistry Antineoplastic Agents - pharmacology ATP Binding Cassette Transporter, Subfamily B, Member 1 - antagonists & inhibitors ATP Binding Cassette Transporter, Subfamily B, Member 1 - metabolism Binding Sites - drug effects Biological Transport - drug effects Drug Design Humans Molecular Structure
Online Access:	Get more information
Tags:	Add Tag No Tags, Be the first to tag this record!

Description
Summary:	Design of inhibitors of P-glycoprotein still represents a challenging task for medicinal chemists. The polyspecificity of the transporter combined with the limited structural information renders rational drug design approaches rather ineffective. Within this article we will exemplify how recent insights into structure and mechanism of P-glycoprotein may aid in design of potent inhibitors.
ISSN:	1873-4294
DOI:	10.2174/156802610792928004