Identification of Loop D Domain Amino Acids in the Human Aquaporin-1 Channel Involved in Activation of the Ionic Conductance and Inhibition by AqB011

Frontiers in Chemistry
Mohamad KourghiAndrea J Yool

Abstract

Aquaporins are integral proteins that facilitate the transmembrane transport of water and small solutes. In addition to enabling water flux, mammalian Aquaporin-1 (AQP1) channels activated by cyclic GMP can carry non-selective monovalent cation currents, selectively blocked by arylsulfonamide compounds AqB007 (IC50 170 μM) and AqB011 (IC50 14 μM). In silico models suggested that ligand docking might involve the cytoplasmic loop D (between AQP1 transmembrane domains 4 and 5), but the predicted site of interaction remained to be tested. Work here shows that mutagenesis of two conserved arginine residues in loop D slowed the activation of the AQP1 ion conductance and impaired the sensitivity of the channel to block by AqB011. Substitution of residues in loop D with proline showed effects on ion conductance amplitude that varied with position, suggesting that the structural conformation of loop D is important for AQP1 channel gating. Human AQP1 wild type, AQP1 mutant channels with alanines substituted for two arginines (R159A+R160A), and mutants with proline substituted for single residues threonine (T157P), aspartate (D158P), arginine (R159P, R160P), or glycine (G165P) were expressed in Xenopus laevis oocytes. Conductance response...Continue Reading

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Citations

Nov 15, 2018·Cells·Marcelo OzuGabriela Amodeo
Sep 11, 2019·DNA Research : an International Journal for Rapid Publication of Reports on Genes and Genomes·Andrew D CalcinoAndreas Wanninger
Jun 21, 2018·Frontiers in Chemistry·Michael L De Ieso, Andrea J Yool
Apr 16, 2020·Frontiers in Pharmacology·Andrea J Yool, Sunita Ramesh
Feb 13, 2021·Annual Review of Plant Biology·Stephen D TyermanCaitlin S Byrt

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Methods Mentioned

BETA
environmental stress
confocal microscopy

Software Mentioned

GraphPad
Image J
Clampex
pClamp
Prism
BlastP

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