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Cryo-EM structure of human NKCC1 K289NA492EL671C bound with bumetanide


ABSTRACT:

SUBMITTER: Yongxiang Zhao 

PROVIDER: EMPIAR-11049 | biostudies-other |

REPOSITORIES: biostudies-other

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Structural basis for inhibition of the Cation-chloride cotransporter NKCC1 by the diuretic drug bumetanide.

Zhao Yongxiang Y   Roy Kasturi K   Vidossich Pietro P   Cancedda Laura L   De Vivo Marco M   Forbush Biff B   Cao Erhu E  

Nature communications 20220518 1


Cation-chloride cotransporters (CCCs) NKCC1 and NKCC2 catalyze electroneutral symport of 1 Na<sup>+</sup>, 1 K<sup>+</sup>, and 2 Cl<sup>-</sup> across cell membranes. NKCC1 mediates trans-epithelial Cl<sup>-</sup> secretion and regulates excitability of some neurons and NKCC2 is critical to renal salt reabsorption. Both transporters are inhibited by the so-called loop diuretics including bumetanide, and these drugs are a mainstay for treating edema and hypertension. Here, our single-particle el  ...[more]

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