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Start Over Descriptor "Cell receptors -- Chemical properties" Publisher rockefeller university press
1 results on '"Cell receptors -- Chemical properties"'

1. Discovery of glycine hydrazide pore-occluding CFTR inhibitors: mechanism, structure-activity analysis, and in vivo efficacy

Author

Muanprasat, Chatchai, Sonawane, N.D., Salinas, Danieli, Taddei, Alessandro, Galietta, Luis J.V., and Verkman, A.S.

Subjects
Cystic fibrosis -- Analysis, Cell receptors -- Chemical properties, Cell receptors -- Analysis, Biological sciences, Health
Abstract

The cystic fibrosis transmembrane conductance regulator (CFTR) protein is a cAMP-regulated epithelial [Cl.sup.-] channel that, when defective, causes cystic fibrosis. Screening of a collection of 100,000 diverse small molecules revealed tour novel chemical classes of CFTR inhibitors with [K.sub.i] 10 [micro]M, one of which (glycine hydrazides) had many active structural analogues. Analysis of a series of synthesized glycine hydrazide analogues revealed maximal inhibitory potency for N-(2-naphthalenyl) and 3,5-dibromo-2,4-dihydroxyphenyl substituents. The compound N-(2-naphthalenyl)-[(3,5-dibromo-2,4-dihydroxyphenyl)methylene] glycine hydrazide (GlyH-101) reversibly inhibited CFTR [C1.sup.-] conductance in KEY WORDS: cystic fibrosis * diarrhea * high-throughput screening * patch-clamp * drug discovery

Published
2004

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