Inhibitor binding mode and allosteric regulation of Na + -glucose symporters

Paola Bisignano; Chiara Ghezzi; Hyunil Jo; Nicholas F. Polizzi; Thorsten Althoff; Chakrapani Kalyanaraman; Rosmarie Friemann; Matthew P. Jacobson; Ernest M. Wright; Michael Grabe

doi:10.1038/s41467-018-07700-1

Nature Communications (Dec 2018)

Inhibitor binding mode and allosteric regulation of Na + -glucose symporters

Paola Bisignano,
Chiara Ghezzi,
Hyunil Jo,
Nicholas F. Polizzi,
Thorsten Althoff,
Chakrapani Kalyanaraman,
Rosmarie Friemann,
Matthew P. Jacobson,
Ernest M. Wright,
Michael Grabe

Affiliations

Paola Bisignano: Department of Pharmaceutical Chemistry, University of California
Chiara Ghezzi: Department of Physiology, David Geffen School of Medicine at UCLA
Hyunil Jo: Department of Pharmaceutical Chemistry, University of California
Nicholas F. Polizzi: Department of Pharmaceutical Chemistry, University of California
Thorsten Althoff: Department of Physiology, David Geffen School of Medicine at UCLA
Chakrapani Kalyanaraman: Department of Pharmaceutical Chemistry, University of California
Rosmarie Friemann: Department of Chemistry and Molecular Biology, Centre for Antibiotic Resistance (CARe) at University of Gothenburg
Matthew P. Jacobson: Department of Pharmaceutical Chemistry, University of California
Ernest M. Wright: Department of Physiology, David Geffen School of Medicine at UCLA
Michael Grabe: Department of Pharmaceutical Chemistry, University of California

DOI: https://doi.org/10.1038/s41467-018-07700-1
Journal volume & issue: Vol. 9, no. 1
pp. 1 – 10

Abstract

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Sodium-dependent glucose transporters (SGLTs) transport sugars across the plasma membrane and play important roles in renal sugar reabsorption. Here authors develop structural models of human SGLT1/2 (hSGLT1/2) in complex with inhibitors which helps to understand inhibitor subtype selectivity.

Published in Nature Communications

ISSN: 2041-1723 (Online)
Publisher: Nature Portfolio
Country of publisher: United Kingdom
LCC subjects: Science
Website: https://www.nature.com/ncomms/

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