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Impact of the Recent Mouse P-Glycoprotein Structure for Structure-Based Ligand Design.

ABSTRACT: P-Glycoprotein (P-gp), a transmembrane, ATP-dependent drug efflux transporter, has attracted considerable interest both with respect to its role in tumour cell multidrug resistance and in absorption-distribution and elimination of drugs. Although known since more than 30 years, the understanding of the molecular basis of drug/transporter interaction is still limited, which is mainly due to the lack of structural information available. However, within the past decade X-ray structures of several bacterial homologues as well as very recently also of mouse P-gp have become available. Within this review we give an overview on the current status of structural information available and on its impact for structure-based drug design.

SUBMITTER: Klepsch F

PROVIDER: S-EPMC6422301 | biostudies-literature | 2010 Apr

REPOSITORIES: biostudies-literature

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Impact of the Recent Mouse P-Glycoprotein Structure for Structure-Based Ligand Design.

Klepsch Freya F Ecker Gerhard F GF

Molecular informatics 20100420 4

P-Glycoprotein (P-gp), a transmembrane, ATP-dependent drug efflux transporter, has attracted considerable interest both with respect to its role in tumour cell multidrug resistance and in absorption-distribution and elimination of drugs. Although known since more than 30 years, the understanding of the molecular basis of drug/transporter interaction is still limited, which is mainly due to the lack of structural information available. However, within the past decade X-ray structures of several b ...[more]

PMID: 27463054

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