Modulation of Wnt signaling through inhibition of secreted frizzled-related protein I (sFRP-1) with N-substituted piperidinyl diphenylsulfonyl sulfonamides

Autor:	Jeffrey Curtis Kern, Peter V.N. Bodine, Shoichi Fukayama, Gregory S. Welmaker, Girija Krishnamurthy, Thomas Joseph Commons, Lisa Nogle, William Jay Moore, Ramesh A. Bhat, Keith Pitts, Eugene John Trybulski, Barb Stauffer, Wilson Matthew Allan, Igor Goljer, Ronald L. Magolda
Rok vydání:	2008
Předmět:	Frizzled Plasma protein binding Inhibitory Concentration 50 Mice Structure-Activity Relationship Isomerism Piperidines Genes Reporter Cell Line Tumor Drug Discovery Sulfanilamides Animals Humans chemistry.chemical_classification Molecular Structure Chemistry Skull Wnt signaling pathway Intracellular Signaling Peptides and Proteins LRP6 Proteins Biological activity LRP5 Small molecule Wnt Proteins Biochemistry Molecular Medicine Glycoprotein Protein Binding Signal Transduction
Zdroj:	Journal of medicinal chemistry. 52(1)
ISSN:	1520-4804
Popis:	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.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::0856734d48b2f78ae9483671c5b4443c https://pubmed.ncbi.nlm.nih.gov/19072540 Zobrazit plný text záznamu