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Review

Clinical development of galunisertib (LY2157299 monohydrate), a small molecule inhibitor of transforming growth factor-beta signaling pathway

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Pages 4479-4499 | Published online: 10 Aug 2015

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Crossref
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Crossref
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Crossref
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Crossref
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Crossref
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Crossref
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Crossref
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Crossref
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Yuanke Li, Zhen Zhao, Hao Liu, John Peter Fetse, Akshay Jain, Chien-Yu Lin & Kun Cheng. (2019) Development of a Tumor-Responsive Nanopolyplex Targeting Pancreatic Cancer Cells and Stroma. ACS Applied Materials & Interfaces 11:49, pages 45390-45403.
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Linh Huynh, Christopher Hipolito & Peter ten Dijke. (2019) A Perspective on the Development of TGF-β Inhibitors for Cancer Treatment. Biomolecules 9:11, pages 743.
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Crossref
Xuan Zhu, Lijie Chen, Ling Liu & Xing Niu. (2019) EMT-Mediated Acquired EGFR-TKI Resistance in NSCLC: Mechanisms and Strategies. Frontiers in Oncology 9.
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Rajni M. Bhardwaj, Jennifer A. McMahon, Jonas Nyman, Louise S. Price, Sumit Konar, Iain D. H. Oswald, Colin R. Pulham, Sarah L. Price & Susan M. Reutzel-Edens. (2019) A Prolific Solvate Former, Galunisertib, under the Pressure of Crystal Structure Prediction, Produces Ten Diverse Polymorphs. Journal of the American Chemical Society 141:35, pages 13887-13897.
Crossref
Brown & Marshall. (2019) Integrin-Mediated TGFβ Activation Modulates the Tumour Microenvironment. Cancers 11:9, pages 1221.
Crossref
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Crossref
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Shweta Joshi & Donald L. Durden. (2019) Combinatorial Approach to Improve Cancer Immunotherapy: Rational Drug Design Strategy to Simultaneously Hit Multiple Targets to Kill Tumor Cells and to Activate the Immune System. Journal of Oncology 2019, pages 1-18.
Crossref
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Crossref
Katherine E. Liu. (2018) Rethinking Causation in Cancer with Evolutionary Developmental Biology. Biological Theory 13:4, pages 228-242.
Crossref
Arjan van Caam, Madelon Vonk, Frank van den Hoogen, Peter van Lent & Peter van der Kraan. (2018) Unraveling SSc Pathophysiology; The Myofibroblast. Frontiers in Immunology 9.
Crossref
Yong Zhang, Yufen Zhao, Andrew J. Tebben, Steven Sheriff, Max Ruzanov, Mark P. Fereshteh, Yi Fan, Jonathan Lippy, Jesse Swanson, Ching-Ping Ho, Barri S. Wautlet, Anne Rose, Karen Parrish, Zheng Yang, Andrew F. Donnell, Liping Zhang, Brian E. Fink, Gregory D. Vite, Karen Augustine-Rauch, Joseph Fargnoli & Robert M. Borzilleri. (2018) Discovery of 4-Azaindole Inhibitors of TGFβRI as Immuno-oncology Agents. ACS Medicinal Chemistry Letters 9:11, pages 1117-1122.
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Bin Han, Fang-yuan Mao, Yong-liang Zhao, Yi-pin Lv, Yong-sheng Teng, Mubing Duan, Weisan Chen, Ping Cheng, Ting-ting Wang, Zhong-yuan Liang, Jin-yu Zhang, Yu-gang Liu, Gang Guo, Quan-ming Zou, Yuan Zhuang & Liu-sheng Peng. (2018) Altered NKp30, NKp46, NKG2D, and DNAM-1 Expression on Circulating NK Cells Is Associated with Tumor Progression in Human Gastric Cancer. Journal of Immunology Research 2018, pages 1-9.
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Qing Zhang, Xiaonan Hou, Bradley Evans, Jamison VanBlaricom, Saravut Weroha & William Cliby. (2018) LY2157299 Monohydrate, a TGF-βR1 Inhibitor, Suppresses Tumor Growth and Ascites Development in Ovarian Cancer. Cancers 10:8, pages 260.
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Yangyang Liu, Yadi Cai, Li Liu, Yudong Wu & Xiangyang Xiong. (2018) Crucial biological functions of CCL7 in cancer. PeerJ 6, pages e4928.
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Amira Ouanouki, Sylvie Lamy & Borhane Annabi. (2018) Periostin, a signal transduction intermediate in TGF-β-induced EMT in U-87MG human glioblastoma cells, and its inhibition by anthocyanidins. Oncotarget 9:31, pages 22023-22037.
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Ajay P. Nayak, Deepak A. Deshpande & Raymond B. Penn. (2018) New targets for resolution of airway remodeling in obstructive lung diseases. F1000Research 7, pages 680.
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Anna Mies, Amit Verma & Uwe Platzbecker. 2018. Myelodysplastic Syndromes. Myelodysplastic Syndromes 97 104 .
Jan L. Christian & Carl-Henrik Heldin. (2017) The TGFβ superfamily in Lisbon: navigating through development and disease. Development 144:24, pages 4476-4480.
Crossref
Qi Wu, Ying Tian, Jingqiu Zhang, Hongpeng Zhang, Fengming Gu, Yongdie Lu, Shengnan Zou, Yuji Chen, Pengxiang Sun, Mengyue Xu, Xiaoming Sun, Chao Xia, Hao Chi, A Ying Zhu, Dong Tang & Daorong Wang. (2017) Functions of pancreatic stellate cell-derived soluble factors in the microenvironment of pancreatic ductal carcinoma. Oncotarget 8:60, pages 102721-102738.
Crossref
Sugandha Bhatia, James Monkman, Alan Kie Leong Toh, Shivashankar H. Nagaraj & Erik W. Thompson. (2017) Targeting epithelial–mesenchymal plasticity in cancer: clinical and preclinical advances in therapy and monitoring. Biochemical Journal 474:19, pages 3269-3306.
Crossref
Maria Villalba, Stephanie R. Evans, Fernando Vidal-Vanaclocha & Alfonso Calvo. (2017) Role of TGF-β in metastatic colon cancer: it is finally time for targeted therapy. Cell and Tissue Research 370:1, pages 29-39.
Crossref
Masafumi Ikeda, Hideaki Takahashi, Shunsuke Kondo, Michael Mauritius Fabio Lahn, Ken Ogasawara, Karim A. Benhadji, Hisaki Fujii & Hideki Ueno. (2017) Phase 1b study of galunisertib in combination with gemcitabine in Japanese patients with metastatic or locally advanced pancreatic cancer. Cancer Chemotherapy and Pharmacology 79:6, pages 1169-1177.
Crossref
Yiran Zheng, Li Tang, Llian Mabardi, Sudha Kumari & Darrell J. Irvine. (2017) Enhancing Adoptive Cell Therapy of Cancer through Targeted Delivery of Small-Molecule Immunomodulators to Internalizing or Noninternalizing Receptors. ACS Nano 11:3, pages 3089-3100.
Crossref
Devon M Fitzgerald & Susan M Rosenberg. (2017) Driving cancer evolution. eLife 6.
Crossref
Janusz Franco-Barraza, Ralph Francescone, Tiffany Luong, Neelima Shah, Raj Madhani, Gil Cukierman, Essel Dulaimi, Karthik Devarajan, Brian L Egleston, Emmanuelle Nicolas, R Katherine Alpaugh, Ruchi Malik, Robert G Uzzo, John P Hoffman, Erica A Golemis & Edna Cukierman. (2017) Matrix-regulated integrin αvβ5 maintains α5β1-dependent desmoplastic traits prognostic of neoplastic recurrence. eLife 6.
Crossref
Lindsay C. Spender & Gareth J. Inman. (2017) Targeting BRAF-mutant tumours with TGFBR1 inhibitors. Aging 9:1, pages 5-6.
Crossref
Boyuan Huang, Hongbo Zhang, Lijuan Gu, Bainxin Ye, Zhihong Jian, Creed Stary & Xiaoxing Xiong. (2017) Advances in Immunotherapy for Glioblastoma Multiforme. Journal of Immunology Research 2017, pages 1-11.
Crossref
Amanda Tivnan, Tatjana Heilinger, Ed C. Lavelle & Jochen H. M. Prehn. (2016) Advances in immunotherapy for the treatment of glioblastoma. Journal of Neuro-Oncology 131:1, pages 1-9.
Crossref
Sioned Owen, Catherine Zabkiewicz, Lin Ye, Andrew J. Sanders, Chang Gong & Wen G. Jiang. 2017. Translational Research in Breast Cancer. Translational Research in Breast Cancer 197 216 .
Juan Du, Yu Yu, Jun Zhan & Hongquan Zhang. 2017. Translational Research in Breast Cancer. Translational Research in Breast Cancer 125 146 .
Lindsay C. Spender, G. John Ferguson, Sijia Liu, Chao Cui, Maria Romina Girotti, Gary Sibbet, Ellen B. Higgs, Morven K. Shuttleworth, Tom Hamilton, Paul Lorigan, Michael Weller, David F. Vincent, Owen J. Sansom, Margaret Frame, Peter ten Dijke, Richard Marais & Gareth J. Inman. (2016) Mutational activation of BRAF confers sensitivity to transforming growth factor beta inhibitors in human cancer cells. Oncotarget 7:50, pages 81995-82012.
Crossref
Lukáš Tenora, Juraj Galeta, Eva Řezníčková, Vladimír Kryštof & Milan Potáček. (2016) Application of Pd-Catalyzed Cross-Coupling Reactions in the Synthesis of 5,5-Dimethyl-5,6-dihydro-4 H -pyrrolo[1,2- b ]pyrazoles that Inhibit ALK5 Kinase . The Journal of Organic Chemistry 81:23, pages 11841-11856.
Crossref
Timothy P. Heffron. (2016) Small Molecule Kinase Inhibitors for the Treatment of Brain Cancer. Journal of Medicinal Chemistry 59:22, pages 10030-10066.
Crossref
Ying Qu, Bo Zhou, Wei Yang, Bingchen Han, Yi Yu-Rice, Bowen Gao, Jeffery Johnson, Clive N. Svendsen, Michael R. Freeman, Armando E. Giuliano, Dhruv Sareen & Xiaojiang Cui. (2016) Transcriptome and proteome characterization of surface ectoderm cells differentiated from human iPSCs. Scientific Reports 6:1.
Crossref