Abstract
The diphenylsulfonyl sulfonamide scaffold represented by 1 (WAY-316606) are small molecule inhibitors of the secreted protein sFRP-1, an endogenous antagonist of the secreted glycoprotein Wnt. Modulators of the Wnt pathway have been proposed as anabolic agents for the treatment of osteoporosis or other bone-related disorders. Details of the structure-activity relationships and biological activity from the first structural class of this scaffold will be discussed.
MeSH terms
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Animals
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Cell Line, Tumor
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Genes, Reporter / genetics
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Humans
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Inhibitory Concentration 50
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Intracellular Signaling Peptides and Proteins
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Isomerism
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Mice
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Molecular Structure
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Piperidines / chemistry*
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Protein Binding
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Proteins / antagonists & inhibitors*
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Proteins / metabolism*
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Signal Transduction / drug effects*
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Skull / drug effects
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Structure-Activity Relationship
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Sulfanilamides / chemical synthesis*
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Sulfanilamides / chemistry
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Sulfanilamides / pharmacology*
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Wnt Proteins / genetics
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Wnt Proteins / metabolism*
Substances
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Intracellular Signaling Peptides and Proteins
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Piperidines
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Proteins
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Sulfanilamides
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WD repeat containing planar cell polarity effector
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Wnt Proteins
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piperidine