title: Modulating the wnt signaling pathway with small molecules.
abstract: Wnt signaling is a critical component during embryonic development and also plays an important role in regulating adult tissue homeostasis. Abnormal activation of Wnt signaling has been implicated in many cancers, while reduced activity of Wnt signaling leads to poor wound healing and structural formations. Thus, extensive efforts have been focused on developing small molecules that have potential to either inhibit or activate the pathway, hoping these molecules can offer leads for novel approaches in treating different human diseases. Many small-molecule inhibitors specifically target various elements, such as Frizzled, Disheveled, Porcupine, or Tankyrase, within the Wnt signaling pathways. These small molecules not only have the potential to be further developed as therapeutic reagents, but they may also be used as chemical probes to dissect the underlying mechanism of the Wnt signaling pathways. Therefore, their respective mechanisms and effective dosages are highly pertinent. Aiming to provide an overview of those molecules in a concise, easy-to-use manner, we summarize and organize the current research on them so that it may be helpful for utilization in different studies.
authors.affiliation: Department of Ophthalmology, Stein Eye Institute, David Geffen School of Medicine at UCLA, Los Angeles, California, 90095.
authors.forename: Freddi Huan
authors.initials: FH
authors.lastname: Tran
authors.affiliation: Department of Ophthalmology, Stein Eye Institute, David Geffen School of Medicine at UCLA, Los Angeles, California, 90095.|Molecular Biology Institute, University of California, Los Angeles, Los Angeles, California, 90095.
authors.forename: Jie J
authors.identifier: 0000-0001-6524-6800
authors.initials: JJ
authors.lastname: Zheng
mesh_terms: D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000737:chemistry* / Q000494:pharmacology*; D006801:Humans; D051153:Wnt Proteins / Q000037:antagonists & inhibitors* / Q000737:chemistry* / Q000378:metabolism; D060449:Wnt Signaling Pathway / Q000187:drug effects*
chemical_list: D000894:Anti-Inflammatory Agents, Non-Steroidal; D051153:Wnt Proteins
keywords: Axin; Disheveled; Frizzled; GSK-3β; Porcupine; T-cell factor/lymphoid enhancer-binding factor; Wnt signaling pathway; and Tankyrase; cancer; small-molecule inhibitors; stem cells; β-catenin