Chromones as a privileged scaffold in drug discovery: A review

RS Keri, S Budagumpi, RK Pai… - European Journal of …, 2014 - Elsevier
The chromone and its derivatives are the most important heterocyclic compounds, which is a
common and integral feature of a variety of natural products and medicinal agents. These …

Cystic fibrosis: emergence of highly effective targeted therapeutics and potential clinical implications

MA Mall, N Mayer-Hamblett… - American journal of …, 2020 - atsjournals.org
Cystic fibrosis (CF) remains the most common life-shortening hereditary disease in white
populations, with high morbidity and mortality related to chronic airway mucus obstruction …

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 …

The combinatorial synthesis of bicyclic privileged structures or privileged substructures

DA Horton, GT Bourne, ML Smythe - Chemical reviews, 2003 - ACS Publications
The exploration of privileged structures in drug discovery is a rapidly emerging theme in
medicinal chemistry. These structures represent a class of molecules capable of binding to …

TMEM16A, a membrane protein associated with calcium-dependent chloride channel activity

A Caputo, E Caci, L Ferrera, N Pedemonte, C Barsanti… - Science, 2008 - science.org
Calcium-dependent chloride channels are required for normal electrolyte and fluid
secretion, olfactory perception, and neuronal and smooth muscle excitability. The molecular …

Ion channel modulators in cystic fibrosis

M Gentzsch, MA Mall - Chest, 2018 - Elsevier
Cystic fibrosis (CF) is caused by mutations in the cystic fibrosis transmembrane conductance
regulator (CFTR) gene and remains one of the most common life-shortening genetic …

CFTR modulators: shedding light on precision medicine for cystic fibrosis

M Lopes-Pacheco - Frontiers in pharmacology, 2016 - frontiersin.org
Cystic fibrosis (CF) is the most common life-threatening monogenic disease afflicting
Caucasian people. It affects the respiratory, gastrointestinal, glandular and reproductive …

Electrolyte transport in the mammalian colon: mechanisms and implications for disease

K Kunzelmann, M Mall - Physiological reviews, 2002 - journals.physiology.org
The colonic epithelium has both absorptive and secretory functions. The transport is
characterized by a net absorption of NaCl, short-chain fatty acids (SCFA), and water …

Thiazolidinone CFTR inhibitor identified by high-throughput screening blocks cholera toxin–induced intestinal fluid secretion

T Ma, JR Thiagarajah, H Yang… - The Journal of …, 2002 - Am Soc Clin Investig
Secretory diarrhea is the leading cause of infant death in developing countries and a major
cause of morbidity in adults. The cystic fibrosis transmembrane conductance regulator …

Chloride channels as drug targets

AS Verkman, LJV Galietta - Nature reviews Drug discovery, 2009 - nature.com
Chloride channels represent a relatively under-explored target class for drug discovery as
elucidation of their identity and physiological roles has lagged behind that of many other …