Synonyms: compound 1 [PMID: 19072540]
Compound class:
Synthetic organic
Comment: WAY-316606 was originally identified as a small molecule inhibitor of the endogenous Wnt antagonist sFRP-1 (a.k.a. SARP2), as a novel anabolic agent for the treatment of osteoporosis or other bone-related disorders [3]. Mechanistically it binds to sFRP-1 and out-competes Wnt binding to sFRP-1, thereby releasing Wnt for binding to the LRP-frizzled receptor complex, an effect that ultimately promotes canonical Wnt signaling and increases anabolic bone formation [1]. Subsequent study has found that WAY-316606 may have potential as a hair re-growth strategy with potential clinical relevance for treatment of human hair loss disorders [2]. WAY-316606 was found to enhance hair shaft production, hair shaft keratin expression, and reduce spontaneous hair follicle regression in ex vivo human scalp explants, via a canonical Wnt/β-catenin-dependent mechanism.
Ligand Activity Visualisation ChartsThese are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts. ✖ |
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References |
1. Bodine PV, Stauffer B, Ponce-de-Leon H, Bhat RA, Mangine A, Seestaller-Wehr LM, Moran RA, Billiard J, Fukayama S, Komm BS et al.. (2009)
A small molecule inhibitor of the Wnt antagonist secreted frizzled-related protein-1 stimulates bone formation. Bone, 44 (6): 1063-8. [PMID:19254787] |
2. Hawkshaw NJ, Hardman JA, Haslam IS, Shahmalak A, Gilhar A, Lim X, Paus R. (2018)
Identifying novel strategies for treating human hair loss disorders: Cyclosporine A suppresses the Wnt inhibitor, SFRP1, in the dermal papilla of human scalp hair follicles. PLoS Biol, 16 (5): e2003705. [PMID:29738529] |
3. Moore WJ, Kern JC, Bhat R, Commons TJ, Fukayama S, Goljer I, Krishnamurthy G, Magolda RL, Nogle L, Pitts K et al.. (2009)
Modulation of Wnt signaling through inhibition of secreted frizzled-related protein I (sFRP-1) with N-substituted piperidinyl diphenylsulfonyl sulfonamides. J Med Chem, 52 (1): 105-16. [PMID:19072540] |