Shilong Zheng1,2, Jiawang Liu1,2, Yanyuan Wu3,4, Tien L Huang1,5, Guangdi Wang1,2. 1. RCMI Cancer Research Center, Xavier University of Louisiana, New Orleans, LA 70125, USA. 2. Department of Chemistry, Xavier University of Louisiana, New Orleans, LA 70125, USA. 3. Division of Cancer Research & Training, Charles R. Drew University of Medicine and Science, Los Angeles, CA 90059, USA. 4. Department of Medicine, Charles R. Drew University of Medicine and Science, Los Angeles, CA 90059, USA. 5. School of Pharmacy, Xavier University of Louisiana, New Orleans, LA 70125, USA.
Abstract
BACKGROUND: The Wnt signaling pathway involves secreted glycoproteins that bind to the Frizzled family receptors to activate intracellular signal transduction events that regulate cell proliferation, apoptosis, cell migration and many critical aspects of developmental biology. DISCUSSION: Aberrant Wnt signaling underlies a wide range of pathologies in humans including tumor initiation, tumor growth, cell senescence, cell death, differentiation and metastasis. The inhibition of Wnt signaling offers a novel approach for anticancer therapeutics. CONCLUSION: Focusing on recent developments, we reviewed the small-molecule inhibitors targeting various components of Wnt signaling pathways and the progress from the discovery of lead compounds to highly potent inhibitors with significant therapeutic potential.
BACKGROUND: The Wnt signaling pathway involves secreted glycoproteins that bind to the Frizzled family receptors to activate intracellular signal transduction events that regulate cell proliferation, apoptosis, cell migration and many critical aspects of developmental biology. DISCUSSION: Aberrant Wnt signaling underlies a wide range of pathologies in humans including tumor initiation, tumor growth, cell senescence, cell death, differentiation and metastasis. The inhibition of Wnt signaling offers a novel approach for anticancer therapeutics. CONCLUSION: Focusing on recent developments, we reviewed the small-molecule inhibitors targeting various components of Wnt signaling pathways and the progress from the discovery of lead compounds to highly potent inhibitors with significant therapeutic potential.
Authors: 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 Melancon; Victor P Ghidu; Gary A Sulikowski; Bonnie LaFleur; Adrian Salic; Laura A Lee; David M Miller; Ethan Lee Journal: Nat Chem Biol Date: 2010-10-03 Impact factor: 15.040
Authors: Jijun Hao; Ada Ao; Li Zhou; Clare K Murphy; Audrey Y Frist; Jessica J Keel; Curtis A Thorne; Kwangho Kim; Ethan Lee; Charles C Hong Journal: Cell Rep Date: 2013-09-05 Impact factor: 9.423
Authors: Marion Lanier; Dennis Schade; Erik Willems; Masanao Tsuda; Sean Spiering; Jaroslaw Kalisiak; Mark Mercola; John R Cashman Journal: J Med Chem Date: 2012-01-13 Impact factor: 7.446
Authors: Tobias Karlberg; Natalia Markova; Ida Johansson; Martin Hammarström; Patrick Schütz; Johan Weigelt; Herwig Schüler Journal: J Med Chem Date: 2010-07-22 Impact factor: 7.446
Authors: Katayoon H Emami; Cu Nguyen; Hong Ma; Dae Hoon Kim; Kwang Won Jeong; Masakatsu Eguchi; Randall T Moon; Jia-Ling Teo; Se Woong Oh; Hak Yeop Kim; Sung Hwan Moon; Jong Ryul Ha; Michael Kahn Journal: Proc Natl Acad Sci U S A Date: 2004-08-16 Impact factor: 11.205
Authors: Oscar Aguilera; Cristina Peña; José Miguel García; María Jesús Larriba; Paloma Ordóñez-Morán; Diego Navarro; Antonio Barbáchano; Isabel López de Silanes; Esteban Ballestar; Mario F Fraga; Manel Esteller; Carlos Gamallo; Félix Bonilla; José Manuel González-Sancho; Alberto Muñoz Journal: Carcinogenesis Date: 2007-04-21 Impact factor: 4.944
Authors: Maria Cristina Rangel; Daniel Bertolette; Nadia P Castro; Malgorzata Klauzinska; Frank Cuttitta; David S Salomon Journal: Breast Cancer Res Treat Date: 2016-03-11 Impact factor: 4.872
Authors: Elliott D Bayle; Fredrik Svensson; Benjamin N Atkinson; David Steadman; Nicky J Willis; Hannah L Woodward; Paul Whiting; Jean-Paul Vincent; Paul V Fish Journal: J Med Chem Date: 2021-03-30 Impact factor: 7.446