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Discovery of a Small Molecule Drug Candidate for Selective NKCC1 Inhibition in Brain Disorders

CheM, 2020
Summary Aberrant expression ratio of Cl− transporters, NKCC1 and KCC2, is implicated in several brain conditions. NKCC1 inhibition by the FDA-approved diuretic drug, bumetanide, rescues core symptoms in rodent models and/or clinical trials with patients.
Annalisa Savardi, Marco Borgogno, Giuseppina La Sala   +2 more
exaly   +2 more sources

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Kinase docking to NKCC1 is essential for function

The FASEB Journal, 2007
The secretory Na‐K‐2Cl cotransporter, NKCC1, is highly expressed on the basolateral membrane of Cl − ‐secreting epithelia such as salivary, sweat and lacrimal glands as well as lung, stomach, colon, where it participates to salt/fluid secretion.
Kenneth B. Gagnon, Roger England, Eric Delpire   +2 more
openaire   +1 more source

Novel scaffolds of key regulators of NKCC1

The FASEB Journal, 2007
Recent work from our laboratory has identified an association between the widely expressed NKCC1 and two Ste20p‐like serine/threonine kinases, SPAK and OSR1. Activation of the widely expressed NKCC1 is mediated by SPAK/OSR1 phosphorylation.
Kenneth B. Gagnon, Roger England, Lisa Diehl, Eric Delpire   +3 more
openaire   +1 more source

The search for brain-permeant NKCC1 inhibitors for the treatment of seizures: Pharmacokinetic-pharmacodynamic modelling of NKCC1 inhibition by azosemide, torasemide, and bumetanide in mouse brain

Epilepsy & Behavior, 2021
Because of its potent inhibitory effect on the Na+-K+-2Cl- symporter isotype 1 (NKCC1) in brain neurons, bumetanide has been tested with varying results for treatment of seizures that potentially evolve as a consequence of abnormal NKCC1 activity. However, because of its physicochemical properties, bumetanide only poorly penetrates into the brain.
Philip Hampel, Kerstin Römermann, Martina Gramer, Wolfgang Löscher   +3 more
openaire   +2 more sources

Hypotension inNKCC1null mice: role of the kidneys

American Journal of Physiology-Renal Physiology, 2006
NKCC1 null mice are hypotensive, in part, from the absence of NKCC1-mediated vasoconstriction. Whether these mice have renal defects in NaCl and water handling which contribute to the hypotension is unexplored. Therefore, we asked 1) whether NKCC1 ( −/−) mice have a defect in the regulation of NaCl and water balance, which might contribute to the ...
Susan M, Wall, Mark A, Knepper, Kathryn A, Hassell, Michael P, Fischer, Adetola, Shodeinde, Wonkyong, Shin, Truyen Derek, Pham, Jamie W, Meyer, John N, Lorenz, William H, Beierwaltes, John R, Dietz, Gary E, Shull, Young-Hee, Kim   +12 more
openaire   +2 more sources

Alternative renin regulatory pathways and the NKCC1 isoform

American Journal of Physiology-Renal Physiology, 2005
the macula densa is one of the classic regulatory pathways that control the release of renin from the juxtaglomerular cells ([11][1]). It senses the distal luminal NaCl concentration in the thick ascending limb and sends a signal to increase renin secretion in response to sustained decreases ...
openaire   +2 more sources

NKCC1 a Regulator of Glioblastoma Progression

Abstract Glioblastoma (GBM) is the most common and aggressive primary brain tumor in adults, with poor prognosis despite multimodal therapy. Chloride cotransporters NKCC1 and KCC2 are key regulators of intracellular chloride levels and thereby determine whether GABA acts inhibitory or excitatory.
Anja Thomsen, Diana Freitag, Madlen Haase, Christian Senft, Falko Schwarz, Silke Keiner   +5 more
openaire   +1 more source

Essential role of NKCC1 in NGF-induced neurite outgrowth

Biochemical and Biophysical Research Communications, 2007
The Na(+)/K(+)/2Cl(-) cotransporter (NKCC) mediates electroneutral transport of 2Cl(-) coupled with Na(+) and K(+) across the plasma membrane, and plays crucial roles in Cl(-) uptake into the cells, homeostasis of cellular Cl(-), and cell volume regulation.
Ken-ichi, Nakajima, Hiroaki, Miyazaki, Naomi, Niisato, Yoshinori, Marunaka   +3 more
openaire   +2 more sources

A Novel Small Molecule Targets NKCC1 To Restore Synaptic Inhibition

Trends in Pharmacological Sciences, 2020
Finely tuned excitation-inhibition balance is essential for proper brain function, and loss of balance resulting from reduced synaptic inhibition is associated with neurological disorders. Savardi and colleagues have discovered a novel inhibitor of a cation-chloride transporter that is required for synaptic inhibition, and which restores behaviors ...
Vineeth A, Raveendran, Jessica C, Pressey, Melanie A, Woodin   +2 more
openaire   +2 more sources

Alterations in airway ion transport in NKCC1-deficient mice

American Journal of Physiology-Cell Physiology, 2001
Airways of Na+-K+-2Cl−(NKCC1)-deficient mice (−/−) were studied in Ussing chambers to determine the role of the basolateral NKCC1 in transepithelial anion secretion. The basal short-circuit current ( I sc) of tracheae and bronchi from adult mice did not differ between NKCC1−/− and normal mice, whereas NKCC1−/− tracheae from neonatal mice exhibited a ...
B R, Grubb, A J, Pace, E, Lee, B H, Koller, R C, Boucher   +4 more
openaire   +2 more sources