Secreted and transmembrane wnt inhibitors and activators.

By Cristina Cruciat, Christof Niehrs. Cold Spring Harbor Perspectives in Biology, 2013

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The R-spondin/Lgr5/Rnf43 module: regulator of Wnt signal strength (2014, neutral): “The Wnt signaling pathway is regulated extensively at the receptor–ligand level (Cruciat and Niehrs 2013).”
Wnt/ b -Catenin Signaling, Disease, and Emerging Therapeutic Modalities (2017, background): “These molecules antagonize Wnt signaling by binding LRP5/6, possibly disrupting Wnt-induced FZD-LRP6 dimerization (Cruciat and Niehrs, 2013).”
Carboxylesterase Notum Is a Druggable Target to Modulate Wnt Signaling (2021, methodology): “82 A ligand-based drug design approach was then used to optimize hit WAY-316606 (not shown) cumulating in the potent lead compound WAY-362692 ( 22 ) with activity in both a ﬂ uorescent polarization binding assay (IC 50 20 nM) and a Wnt-activation reporter assay (EC 50 30 nM).”
Alternative Wnt Signaling Activates YAP/TAZ (2015, background): “These include WNT5A, DKK1, BMP4, and IGFBP4 (Figure 5E) (Cruciat and Niehrs, 2013; Haramis et al., 2004; He et al., 2004; Kikuchi et al., 2012; van Amerongen, 2012; Zhu et al., 2008).”
Notum is required for neural and head induction via Wnt deacylation, oxidation and inactivation (2015, neutral): “The Organizer promotes head development via secreting Wnt antagonists such as secreted frizzled-related proteins (sFRPs) and Dickkopf-1 (Dkk1), which bind to and inhibit Wnt/Fz and LRP6, respectively (Cruciat and Niehrs, 2013; De Robertis and Kuroda, 2004).”