Abstract
Piperidinyl diphenylsulfonyl sulfonamides are a novel class of molecules that have inhibitory binding affinity for sFRP-1. As a secreted protein sFRP-1 inhibits the function of the secreted Wnt glycoprotein. Therefore, as inhibitors of sFRP-1 these small molecules facilitate the Wnt/beta-catenin canonical signaling pathway. Details of the structure-activity relationships and biological activity of this structural class of compounds will be discussed.
Copyright (c) 2009 Elsevier Ltd. All rights reserved.
MeSH terms
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Animals
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Cell Line, Tumor
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Glycoproteins / antagonists & inhibitors*
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Glycoproteins / metabolism
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Humans
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Intracellular Signaling Peptides and Proteins
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Mice
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Microsomes, Liver / metabolism
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Organ Culture Techniques
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Osteogenesis / drug effects
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Rats
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Signal Transduction / drug effects*
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Skull / cytology
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Skull / drug effects
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Structure-Activity Relationship
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Sulfonamides / chemistry*
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Sulfonamides / pharmacology*
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Wnt Proteins / metabolism*
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beta Catenin / metabolism
Substances
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Glycoproteins
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Intracellular Signaling Peptides and Proteins
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Sulfonamides
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WD repeat containing planar cell polarity effector
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Wnt Proteins
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beta Catenin