8ste | pdb_00008ste

Cryo-EM structure of NKCC1 Fu_CTD

spinqualitylabelsall models 8ste, resolution 3.34Å Show:Asymmetric Unit Biological Assembly Drag the structure with the mouse to rotate   Export Animated Image   Print3D Structural highlights 8ste is a 2 chain structure with sequence from Homo sapiens. Full crystallographic information is available from OCA. For a guided tour on the structure components use FirstGlance. Ligands: FUN Resources: FirstGlance, OCA, PDBe, RCSB, PDBsum, ProSAT Function A0A8C9GPS0_9PRIM Publication Abstract from PubMed The Na-K-2Cl cotransporter-1 (NKCC1) is an electroneutral Na(+)-dependent transporter responsible for simultaneously translocating Na(+), K(+), and Cl(-) ions into cells. In human tissue, NKCC1 plays a critical role in regulating cytoplasmic volume, fluid intake, chloride homeostasis, and cell polarity. Here, we report four structures of human NKCC1 (hNKCC1), both in the absence and presence of loop diuretic (bumetanide or furosemide), using single-particle cryo-electron microscopy. These structures allow us to directly observe various novel conformations of the hNKCC1 dimer. They also reveal two drug-binding sites located at the transmembrane and cytosolic carboxyl-terminal domains, respectively. Together, our findings enable us to delineate an inhibition mechanism that involves a coupled movement between the cytosolic and transmembrane domains of hNKCC1. Inhibition mechanism of NKCC1 involves the carboxyl terminus and long-range conformational coupling.,Moseng MA, Su CC, Rios K, Cui M, Lyu M, Glaza P, Klenotic PA, Delpire E, Yu EW Sci Adv. 2022 Oct 28;8(43):eabq0952. doi: 10.1126/sciadv.abq0952. Epub 2022 Oct , 28. PMID:36306358 From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.

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