J
Jiqing Jiang
Researcher at Genomics Institute of the Novartis Research Foundation
Publications - 12
Citations - 1154
Jiqing Jiang is an academic researcher from Genomics Institute of the Novartis Research Foundation. The author has contributed to research in topics: Smoothened & ALK inhibitor. The author has an hindex of 7, co-authored 12 publications receiving 1053 citations.
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Journal ArticleDOI
Identification of NVP-TAE684, a potent, selective, and efficacious inhibitor of NPM-ALK
Anna Galkin,Jonathan S. Melnick,Sungjoon Kim,Tami Hood,Nanxin Li,Lintong Li,Gang Xia,Ruo Steensma,Chopiuk Greg,Jiqing Jiang,Yongqin Wan,Peter Ding,Yi Liu,Fangxian Sun,Peter G. Schultz,Nathanael S. Gray,Markus Warmuth +16 more
TL;DR: A highly potent and selective small-molecule ALK inhibitor, NVP-TAE684, which blocked the growth of ALCL-derived and ALK-dependent cell lines with IC50 values between 2 and 10 nM and induced down-regulation of CD30 expression, suggesting that CD30 may be used as a biomarker of therapeutic NPM-ALK kinase activity inhibition.
Journal ArticleDOI
Synthesis, Structure–Activity Relationships, and in Vivo Efficacy of the Novel Potent and Selective Anaplastic Lymphoma Kinase (ALK) Inhibitor 5-Chloro-N2-(2-isopropoxy-5-methyl-4-(piperidin-4-yl)phenyl)-N4-(2-(isopropylsulfonyl)phenyl)pyrimidine-2,4-diamine (LDK378) Currently in Phase 1 and Phase 2 Clinical Trials
Thomas H. Marsilje,Wei Pei,Bei Chen,Wenshuo Lu,Tetsuo Uno,Jin Yunho,Tao Jiang,Sungjoon Kim,Nanxin Li,Markus Warmuth,Yelena Sarkisova,Frank Sun,Auzon Steffy,AnneMarie Culazzo Pferdekamper,Allen G. Li,Sean B. Joseph,Young Kim,Bo Liu,Tove Tuntland,Xiaoming Cui,Nathanael S. Gray,Ruo Steensma,Yongqin Wan,Jiqing Jiang,Chopiuk Greg,Jie Li,W. Perry Gordon,Wendy Richmond,Kevin Johnson,Jonathan Chang,Todd Groessl,You-Qun He,Andrew Phimister,Alex Aycinena,Christian C. Lee,Badry Bursulaya,Donald S. Karanewsky,H. Martin Seidel,Jennifer L. Harris,Pierre-Yves Michellys +39 more
TL;DR: In this initial report, preliminary structure-activity relationships (SARs) are described as well as the rational design strategy employed to overcome the development deficiencies of the first generation ALK inhibitor 4 (TAE684).
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
Discovery of Trifluoromethyl(pyrimidin-2-yl)azetidine-2-carboxamides as Potent, Orally Bioavailable TGR5 (GPBAR1) Agonists: Structure–Activity Relationships, Lead Optimization, and Chronic In Vivo Efficacy
Dean P. Phillips,Wenqi Gao,Yang Yang,Guobao Zhang,Lerario Isabelle K,Thomas Lau,Jiqing Jiang,Xia Wang,Deborah G. Nguyen,B. Ganesh Bhat,Carol Trotter,Heather Sullivan,Gustav Welzel,Jannine Landry,Yali Chen,Sean B. Joseph,Chun Li,W. Perry Gordon,Wendy Richmond,Kevin Johnson,Angela Bretz,Badry Bursulaya,Shifeng Pan,Peter McNamara,H. Martin Seidel +24 more
TL;DR: In genetically obese mice (ob/ob), 45h was as effective as a dipeptidyl peptidase-4 (DPP-4) inhibitor at reducing peak glucose levels in an acute oral glucose tolerance test (OGTT), but this effect was lost upon chronic dosing.
Patent
Compositions and methods for modulating lpa receptors
John Edward Tellew,Xia Wang,Yongqin Wan,Yun Feng Xie,Shifeng Pan,Jiqing Jiang,Yongping Xie,Thomas Anthony Hunt,Lee Edwards,David Beattie,Mark Patrick Healy,Ryan West,Andrew Lister +12 more
TL;DR: In this article, the present invention relates to compounds of Formula (1), or pharmaceutically acceptable salts thereof and their pharmaceutical compositions, wherein variables are as defined herein, which are useful as modulators of the activity of lysophosphatidic acid (LPA).