FRP-2 inhibitors comprise a diverse class of chemicals that modulate the activity of Frizzled-related protein 2 (FRP-2) through various indirect mechanisms. These chemicals target specific signaling pathways and cellular processes, influencing FRP-2 expression and function without directly binding to the protein itself. One notable inhibitor, LDN-193189, indirectly modulates FRP-2 by inhibiting BMP signaling through ALK2, a kinase linked to FRP-2 regulation. Another compound, XAV-939, suppresses Wnt signaling by inhibiting tankyrase activity, leading to the stabilization of Axin, a crucial regulator in the Wnt pathway, indirectly affecting FRP-2. The inhibitor ICG-001 disrupts Wnt signaling by targeting CBP-β-catenin interaction, showcasing how chemicals can indirectly impact FRP-2 expression through interconnected pathways. LY2090314 inhibits GSK-3, a critical regulator of Wnt signaling, indirectly modulating FRP-2 by influencing downstream targets in the Wnt pathway. SIS3 selectively inhibits the TGF-β/Smad3 pathway, indirectly affecting FRP-2 expression due to the crosstalk between TGF-β and Wnt signaling.
R428 (BGB324) targets Axl, affecting multiple signaling pathways, including Wnt, thereby indirectly influencing FRP-2. JNK Inhibitor VIII disrupts the MAPK pathway, intersecting with Wnt pathways and indirectly impacting FRP-2 expression. SB431542 targets the TGF-β receptor, altering crosstalk between TGF-β and Wnt signaling, indirectly modulating FRP-2. Y-27632 inhibits ROCK, influencing various signaling pathways, including Wnt, and indirectly impacting FRP-2. SAG (Smoothened Agonist) activates Hedgehog signaling, which crosstalks with Wnt pathways, indirectly influencing FRP-2 expression. AZD8055 inhibits mTOR, a central regulator of multiple pathways, including Wnt, indirectly modulating FRP-2. Finally, C646 inhibits p300, a histone acetyltransferase, influencing gene expression and indirectly modulating FRP-2 through p300-mediated transcriptional regulation within relevant pathways. Collectively, these FRP-2 inhibitors exemplify a nuanced approach to modulating protein activity by targeting interconnected signaling pathways and cellular processes.