Structure, gating, and regulation of the CFTR anion channel

L Csanády, P Vergani, DC Gadsby - Physiological reviews, 2019 - journals.physiology.org
The cystic fibrosis transmembrane conductance regulator (CFTR) belongs to the ATP
binding cassette (ABC) transporter superfamily but functions as an anion channel crucial for …

Functionalized quinoxalinones as privileged structures with broad-ranging pharmacological activities

X Jiang, K Wu, R Bai, P Zhang, Y Zhang - European Journal of Medicinal …, 2022 - Elsevier
Quinoxalinones are a class of heterocyclic compounds which attract extensive attention
owing to their potential in the field of organic synthesis and medicinal chemistry. During the …

Calcium-sensing receptor activator cinacalcet for treatment of cyclic nucleotide-mediated secretory diarrheas

T Chu, P Yottasan, L de Souza Goncalves, AA Oak… - Translational …, 2024 - Elsevier
Cyclic nucleotide elevation in intestinal epithelial cells is the key pathology causing
intestinal fluid loss in secretory diarrheas such as cholera. Current secretory diarrhea …

Chloride transport modulators as drug candidates

AS Verkman, LJV Galietta - American Journal of Physiology …, 2021 - journals.physiology.org
Chloride transport across cell membranes is broadly involved in epithelial fluid transport, cell
volume and pH regulation, muscle contraction, membrane excitability, and organellar …

[HTML][HTML] Small-molecule inhibitor of intestinal anion exchanger SLC26A3 for treatment of hyperoxaluria and nephrolithiasis

O Cil, T Chu, S Lee, PM Haggie, AS Verkman - JCI insight, 2022 - ncbi.nlm.nih.gov
Nephrolithiasis is a common and recurrent disease affecting 9% of the US population.
Hyperoxaluria is major risk factor for calcium oxalate kidney stones, which constitute two …

Small molecule inhibitors of intestinal epithelial anion exchanger SLC26A3 (DRA) with a luminal, extracellular site of action

O Cil, MO Anderson, L de Souza Goncalves… - European journal of …, 2023 - Elsevier
The anion exchanger protein SLC26A3 (down-regulated in adenoma, DRA) is expressed in
the luminal membrane of intestinal epithelial cells in colon, where it facilitates the absorption …

[HTML][HTML] SLC26A3 inhibitor identified in small molecule screen blocks colonic fluid absorption and reduces constipation

PM Haggie, O Cil, S Lee, JA Tan, AA Rivera… - JCI insight, 2018 - ncbi.nlm.nih.gov
SLC26A3 (downregulated in adenoma; DRA) is a Cl–/anion exchanger expressed in the
luminal membrane of intestinal epithelial cells, where it facilitates electroneutral NaCl …

Sulfur-Promoted Access to 3-Arylquinoxalin-2-ones by Oxidative Coupling of o-Phenylenediamines with Arylacetates

LA Nguyen, TY Tran, QA Ngo, DH Mac… - Organic …, 2024 - ACS Publications
We disclose the synthesis of 3-arylquinoxalin-2-ones from o-phenylenediamines and readily
available arylacetates. The method harnesses the selective oxidative property of elemental …

High-potency phenylquinoxalinone cystic fibrosis transmembrane conductance regulator (CFTR) activators

JH Son, JS Zhu, PW Phuan, O Cil… - Journal of medicinal …, 2017 - ACS Publications
We previously identified phenylquinoxalinone CFTRact-J027 (4) as a cystic fibrosis
transmembrane conductance regulator (CFTR) activator with an EC50 of∼ 200 nM and …

[HTML][HTML] SLC26A6-selective inhibitor identified in a small-molecule screen blocks fluid absorption in small intestine

O Cil, PM Haggie, JAT Tan, AA Rivera, AS Verkman - JCI insight, 2021 - ncbi.nlm.nih.gov
SLC26A6 (also known as putative anion transporter 1 [PAT1]) is a Cl–/HCO 3–exchanger
expressed at the luminal membrane of enterocytes where it facilitates intestinal Cl–and fluid …