Screening for natural products that affect Wnt signaling activity.
TLDR
In this paper, a screening program targeting Wnt signaling activity using a cell-based luciferase screening system assessing TCF/β-catenin transcriptional activity was proposed.Abstract:
Wnt signaling has been implicated in numerous aspects of development, cell biology, and physiology. When aberrantly activated, Wnt signaling can also lead to the formation of tumors. Thus, Wnt signaling is an attractive target for cancer therapy. Based on our screening program targeting Wnt signaling activity using a cell-based luciferase screening system assessing TCF/β-catenin transcriptional activity, we isolated a series of terpenoids and heterocyclic aromatic compounds that affect the Wnt signaling pathway at different points. Here, we describe our recent results in screening for natural products that inhibit or activate Wnt signaling.read more
Citations
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New Insights about the Wnt/β-Catenin Signaling Pathway in Primary Bone Tumors and Their Microenvironment: A Promising Target to Develop Therapeutic Strategies?
Geoffroy Danieau,Sarah Morice,Françoise Rédini,Franck Verrecchia,Bénédicte Brounais-Le Royer +4 more
TL;DR: The role played by the Wnt/β-catenin signaling pathway in the development of primary bone tumors and the modulation of their specific microenvironment is focused on.
Journal ArticleDOI
Advances in targeting the WNT/β-catenin signaling pathway in cancer.
Manash K. Paul,Avradip Chatterjee,Sayan Paul,Bharti Bisht,Shelley Bhattacharya,Sudhakar Sivasubramaniam,Manash K. Paul +6 more
TL;DR: In this article, the authors discuss the pathway, potential targets for the development of WNT/β-catenin inhibitors, available inhibitors, and their specific molecular interactions with the target proteins.
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Small Molecule Wnt Pathway Modulators from Natural Sources: History, State of the Art and Perspectives.
Artem Blagodatski,Antonina Klimenko,Lee Jia,Vladimir L. Katanaev,Vladimir L. Katanaev,Vladimir L. Katanaev +5 more
TL;DR: An up-to-date overview of existing small molecule modulators of the Wnt pathway derived from natural products and inhibitors of the pathway, which are desired agents for targeted therapies against different cancers are provided.
Journal ArticleDOI
Advances in targeting the WNT/β-catenin signaling pathway in cancer
TL;DR: In this article , the authors discuss the pathway, potential targets for the development of WNT/β-catenin inhibitors, available inhibitors, and their specific molecular interactions with the target proteins.
Journal ArticleDOI
Linderapyrone: A Wnt signal inhibitor isolated from Lindera umbellata.
Takahiro Matsumoto,Takahiro Kitagawa,Daisuke Imahori,Atsushi Matsuzaki,Youhei Saito,Tomoe Ohta,Tatsusada Yoshida,Yuji Nakayama,Eishi Ashihara,Tetsushi Watanabe +9 more
TL;DR: Linderapyrone, a Wnt signal inhibitor was isolated from the methanolic extract of the stems and twigs of Lindera umbellata together with epi-(-)-linderol A as discussed by the authors.
References
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Journal ArticleDOI
Wnt/β-Catenin Signaling, Disease, and Emerging Therapeutic Modalities.
Roel Nusse,Hans Clevers +1 more
TL;DR: The core Wnt/β-catenin signaling pathway is described, how it controls stem cells, and contributes to disease, and strategies for Wnt-based therapies are discussed.
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WNT signalling pathways as therapeutic targets in cancer
Jamie N. Anastas,Randall T. Moon +1 more
TL;DR: This work has shown that WNTs and their downstream effectors regulate various processes that are important for cancer progression, including tumour initiation, tumour growth, cell senescence, cell death, differentiation and metastasis, and improved drug-discovery platforms and new technologies have facilitated the discovery of agents that can alter WNT signalling in preclinical models.
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Small-molecule inhibition of Wnt signaling through activation of casein kinase 1α
Curtis A. Thorne,Alison J. Hanson,Judsen Schneider,Emilios Tahinci,Darren Orton,Christopher S. Cselenyi,Kristin K. Jernigan,Kelly C. Meyers,Brian I. Hang,Alex G. Waterson,Kwangho Kim,Bruce J. Melancon,Victor P. Ghidu,Victor P. Ghidu,Gary A. Sulikowski,Bonnie LaFleur,Bonnie LaFleur,Adrian Salic,Laura A. Lee,Laura A. Lee,David M. Miller,Ethan Lee,Ethan Lee +22 more
TL;DR: The findings reveal allosteric activation of CK1α as an effective mechanism to inhibit Wnt signaling and highlight a new strategy for targeted therapeutics directed against the Wnt pathway.
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Studies on search for bioactive natural products targeting TRAIL signaling leading to tumor cell apoptosis.
Masami Ishibashi,Takashi Ohtsuki +1 more
TL;DR: Several new isoflavone natural products, named brandisianins, were isolated from Leguminosaeous plant, Millettia brandisiana, by the screening study targeting TRAIL‐receptor expression enhancement activity, and were found to exhibit reversal effect of TRAIL resistance activity.
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Catalytic Asymmetric Synthesis of Mixed 3,3′‐Bisindoles and Their Evaluation as Wnt Signaling Inhibitors
TL;DR: The first efficient catalytic asymmetric coupling reaction of indoles with isatin-derived nitroalkenes was accomplished by using a complex consisting of a chiral imidazoline aminophenol ligand and Cu(OTf)(2) to form chiral 3,3'-bisindoles.