D
Dai Cheng
Researcher at Genomics Institute of the Novartis Research Foundation
Publications - 12
Citations - 1117
Dai Cheng is an academic researcher from Genomics Institute of the Novartis Research Foundation. The author has contributed to research in topics: Wnt signaling pathway & Smoothened. The author has an hindex of 6, co-authored 12 publications receiving 956 citations.
Papers
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Journal ArticleDOI
Targeting Wnt-driven cancer through the inhibition of Porcupine by LGK974
Jun Liu,Shifeng Pan,Mindy H. Hsieh,Nicholas Ng,Fangxian Sun,Tao Wang,Shailaja Kasibhatla,Alwin Schuller,Allen G. Li,Dai Cheng,Jie Li,Celin Tompkins,Anne Marie Pferdekamper,Auzon Steffy,Jane Cheng,Colleen Kowal,Van Phung,Gui-Rong Guo,Yan Wang,Martin P. Graham,Shannon Flynn,J. Chad Brenner,Chun Li,M. Cristina Villarroel,Peter G. Schultz,Xu Wu,Peter McNamara,William R. Sellers,Lilli Petruzzelli,Anthony Boral,H. Martin Seidel,Margaret E. McLaughlin,Jianwei Che,Thomas E. Carey,Gary J. Vanasse,Jennifer L. Harris +35 more
TL;DR: LGK974 is potent and efficacious in multiple tumor models at well-tolerated doses in vivo, including murine and rat mechanistic breast cancer models driven by MMTV–Wnt1 and a human head and neck squamous cell carcinoma model (HN30).
Journal ArticleDOI
Discovery of NVP-LDE225, a Potent and Selective Smoothened Antagonist
Shifeng Pan,Xu Wu,Jiqing Jiang,Wenqi Gao,Yongqin Wan,Dai Cheng,Dong Han,Jun Liu,Nathan P. Englund,Yan Wang,Stefan Peukert,Karen Miller-Moslin,Jing Yuan,Ribo Guo,Melissa Matsumoto,Anthony Vattay,Yun Jiang,Jeffrey Tsao,Fangxian Sun,AnneMarie Culazzo Pferdekamper,Stephanie Kay Dodd,Tove Tuntland,Wieslawa Maniara,Joseph Kelleher,Yung-mae Yao,Markus Warmuth,Juliet Williams,Marion Dorsch +27 more
TL;DR: Structural-activity relationship studies led to the discovery of a potent and specific Smoothened antagonist N-(6-((2S,6R)-2,6-dimethylmorpholino)pyridin-3-yl)-2-methyl-4'-(trifluoromethoxy)biphenyl- 3-carboxamide (5m, NVP-LDE225), which is currently in clinical development.
Patent
N- (hetero)aryl, 2- (hetero)aryl-substituted acetamides for use as wnt signaling modulators
TL;DR: In this paper, a method for modulating the Wnt signaling pathway using compounds of formulae 1 and 2 was presented, wherein A1, A2, B, Y and Z all represent rings.
Journal ArticleDOI
Discovery of Pyridinyl Acetamide Derivatives as Potent, Selective, and Orally Bioavailable Porcupine Inhibitors.
Dai Cheng,Jun Liu,Dong Han,Guobao Zhang,Wenqi Gao,Mindy H. Hsieh,Nicholas Ng,Shailaja Kasibhatla,Celin Tompkins,Jie Li,Auzon Steffy,Fangxian Sun,Chun Li,H. Martin Seidel,Jennifer L. Harris,Shifeng Pan +15 more
TL;DR: A cellular high-throughput screen for inhibitors of Wnt secretion and pathway activation led to the discovery of a novel series of potent and selective Porcupine inhibitors.
Patent
Compositions and methods for modulating the wnt signaling pathway
TL;DR: In this article, compositions and methods for modulating the Wnt signaling pathway, using compounds having Formula (1) and (3): wherein A, B, Y and Z all represent rings, and R1, R2, R3 are as defined herein.