M
Melissa Matsumoto
Researcher at Novartis
Publications - 2
Citations - 407
Melissa Matsumoto is an academic researcher from Novartis. The author has contributed to research in topics: Smoothened & Smoothened Receptor. The author has an hindex of 2, co-authored 2 publications receiving 369 citations.
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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.
Journal ArticleDOI
1-amino-4-benzylphthalazines as orally bioavailable smoothened antagonists with antitumor activity.
Karen Miller-Moslin,Stefan Peukert,Rishi K. Jain,Michael A Mcewan,Rajesh Karki,Luis Llamas,Naeem Yusuff,Feng He,Yanhong Li,Yingchuan Sun,Miao Dai,Lawrence Blas Perez,Walter Michael,Tao Sheng,Lei Huangshu,Rui Zhang,Juliet Williams,Aaron Bourret,Arun Ramamurthy,Jing Yuan,Ribo Guo,Melissa Matsumoto,Anthony Vattay,Wieslawa Maniara,Adam Amaral,Marion Dorsch,Joseph Kelleher +26 more
TL;DR: A cell-based screen performed in the laboratories identified a new class of Hh pathway inhibitors, 1-amino-4-benzylphthalazines, that act via antagonism of the Smoothened receptor that displayed a good pharmacokinetic profile and also afforded tumor regression in a genetic mouse model of medulloblastoma.