+検索条件
-Structure paper
| タイトル | Structural characterization of human urea transporters UT-A and UT-B and their inhibition. |
|---|---|
| ジャーナル・号・ページ | Sci Adv, Vol. 9, Issue 39, Page eadg8229, Year 2023 |
| 掲載日 | 2023年9月29日 |
著者 | Gamma Chi / Larissa Dietz / Haiping Tang / Matthew Snee / Andreea Scacioc / Dong Wang / Gavin Mckinley / Shubhashish M M Mukhopadhyay / Ashley C W Pike / Rod Chalk / Nicola A Burgess-Brown / Jean-Pierre Timmermans / Wouter van Putte / Carol V Robinson / Katharina L Dürr / ![]() |
| PubMed 要旨 | 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, ...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. |
リンク | Sci Adv / PubMed:37774028 / PubMed Central |
| 手法 | EM (単粒子) |
| 解像度 | 2.6 - 3.0 Å |
| 構造データ | EMDB-16110, PDB-8blo: ![]() EMDB-16111: Map of Human Urea Transporter UT-A Collected with 0 and 30 Degree Tilts EMDB-16112, PDB-8blp: |
| 化合物 | ![]() ChemComp-PLD: ![]() ChemComp-LMN: ![]() ChemComp-HOH: ![]() ChemComp-PTY: ![]() ChemComp-LMT: ![]() ChemComp-5D3: ![]() ChemComp-Y01: |
| 由来 |
|
キーワード | TRANSPORT PROTEIN / SLC14A2 / UT2 / UT-A / Urea Transporter / Inhibitor / Solute Carrier / SLC14A1 / UT1 / UT-B |
ムービー
コントローラー
構造ビューア
万見文献について



著者

リンク











homo sapiens (ヒト)
キーワード