8BLP

Human Urea Transporter UT-B/UT1 in Complex with Inhibitor UTBinh-14

8BLP の概要

• エントリーDOI: 10.2210/pdb8blp/pdb
• EMDBエントリー: 16110 16111 16112
• 分子名称: Urea transporter 1, PHOSPHATIDYLETHANOLAMINE, DODECYL-BETA-D-MALTOSIDE, ... (6 entities in total)
• 機能のキーワード: slc14a1, ut1, ut-b, urea transporter, inhibitor, solute carrier, transport protein
• 由来する生物種: Homo sapiens (human)
• タンパク質・核酸の鎖数: 3
• 化学式量合計: 155171.46

構造登録者

Chi, G.,Dietz, L.,Pike, A.C.W.,Maclean, E.M.,Mukhopadhyay, S.M.M.,Bohstedt, T.,Wang, D.,Scacioc, A.,McKinley, G.,Arrowsmith, C.H.,Edwards, A.,Bountra, C.,Fernandez-Cid, A.,Burgess-Brown, N.A.,Duerr, K.L. (登録日: 2022-11-10, 公開日: 2023-10-04, 最終更新日: 2023-10-11)

主引用文献

Chi, G.,Dietz, L.,Tang, H.,Snee, M.,Scacioc, A.,Wang, D.,Mckinley, G.,Mukhopadhyay, S.M.M.,Pike, A.C.W.,Chalk, R.,Burgess-Brown, N.A.,Timmermans, J.P.,van Putte, W.,Robinson, C.V.,Durr, K.L.
Structural characterization of human urea transporters UT-A and UT-B and their inhibition.
Sci Adv, 9:eadg8229-eadg8229, 2023

PubMed 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, UTB-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.

PubMed: 37774028
DOI: 10.1126/sciadv.adg8229

実験手法

ELECTRON MICROSCOPY (2.6 Å)