Thiazolidinone CFTR inhibitors with improved water solubility identified by structure–activity analysis
نویسندگان
چکیده
منابع مشابه
Thiazolidinone CFTR inhibitor identified by high-throughput screening blocks cholera toxin-induced intestinal fluid secretion.
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 (CFTR) protein is required for fluid secretion in the intestine and airways and, when defective, causes the lethal genetic disease cystic fibrosis. We screened 50,000 chemically diverse compounds for inhibition of cAMP/...
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in the pathogenesis of secretory diarrhea. It is a passive process driven by the active secretion of ion, predominantly chloride. The cellular transport mechanism of intestinal chloride secretion is well defined. Chloride is taken up across the basolateral membrane via a Na /K /2Cl cotransporter (NKCC1) and exits across the apical membrane via cAMP-sensitive (CFTR) and calcium-sensitive (CaCC) ...
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ژورنال
عنوان ژورنال: Bioorganic & Medicinal Chemistry
سال: 2008
ISSN: 0968-0896
DOI: 10.1016/j.bmc.2008.07.044