Crystallographic Analysis of MATE-Type Multidrug Exporter with Its Inhibitors View Full Text


Ontology type: schema:Chapter     


Chapter Info

DATE

2018

AUTHORS

Tsukasa Kusakizako , Yoshiki Tanaka , Christopher J. Hipolito , Hiroaki Suga , Osamu Nureki

ABSTRACT

Multidrug exporters expressed in pathogens efflux substrate drugs such as antibiotics, and thus, the development of inhibitors against them has eagerly been anticipated. Furthermore, the crystal structures of multidrug exporters with their inhibitors provide novel insights into the inhibitory mechanism and the development of more specific and effective inhibitors. We previously reported the complex structures of the Multidrug And Toxic compound Extrusion (MATE)-type multidrug exporter with the macrocyclic peptides, which inhibit the efflux of substrates by the MATE-type multidrug exporter (Tanaka et al., Nature 496:247-251, 2013). In this chapter, we describe methodologies of the screening and synthesis of macrocyclic peptides as inhibitors, as well as the purification, crystallization, and structure determination of the complexes of the MATE-type multidrug exporter with its inhibitors. More... »

PAGES

37-57

Identifiers

URI

http://scigraph.springernature.com/pub.10.1007/978-1-4939-7454-2_3

DOI

http://dx.doi.org/10.1007/978-1-4939-7454-2_3

DIMENSIONS

https://app.dimensions.ai/details/publication/pub.1092971001

PUBMED

https://www.ncbi.nlm.nih.gov/pubmed/29177824


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