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

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

  • J Med Chem. 2009 Jan 8;52(1):105-16. doi: 10.1021/jm801144h.
William J Moore 1,  Jeffrey C Kern,  Ramesh Bhat,  Thomas J Commons,  Shoichi Fukayama,  Igor Goljer,  Girija Krishnamurthy,  Ronald L Magolda,  Lisa Nogle,  Keith Pitts,  Barb Stauffer,  Eugene J Trybulski,  Gregory S Welmaker,  Matthew Wilson,  Peter V N Bodine
Affiliations

Affiliation

  • 1 Chemical and Screening Sciences, Wyeth Research, Collegeville, Pennsylvania 19426, USA. moorew2@wyeth.com
PMID: 19072540 DOI: 10.1021/jm801144h
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.

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