Publication
Title
Structural characterization of human urea transporters UT-A and UT-B and their inhibition
Author
Abstract
In this study, we present the structures of human urea transporters UT-A and UT-B to characterize them at molecular level and to detail the mechanism of UT-B inhibition by its selective inhibitor, UTBinh-14. High-resolution structures of both transporters establish the structural basis for the inhibitor's selectivity to UT-B, and the identification of multiple binding sites for the inhibitor will aid with the development of drug lead molecules targeting both transporters. Our study also discovers phospholipids associating with the urea transporters by combining structural observations, native MS, and lipidomics analysis. These insights improve our understanding of urea transporter function at a molecular level and provide a blueprint for a structure-guided design of therapeutics targeting these transporters.
Language
English
Source (journal)
Science Advances
Publication
2023
ISSN
2375-2548
DOI
10.1126/SCIADV.ADG8229
Volume/pages
9 :39 (2023) , p. 1-12
Article Reference
eadg8229
ISI
001142340700008
Pubmed ID
37774028
Full text (Publisher's DOI)
Full text (open access)
UAntwerpen
Faculty/Department
Research group
Publication type
Subject
Affiliation
Publications with a UAntwerp address
External links
Web of Science
Record
Identifier
Creation 04.03.2024
Last edited 07.03.2024
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