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Preclinical assessment of galunisertib (LY2157299 monohydrate), a first-in-class transforming growth factor-β receptor type I inhibitor.
Yingling JM, McMillen WT, Yan L, Huang H, Sawyer JS, Graff J, Clawson DK, Britt KS, Anderson BD, Beight DW, Desaiah D, Lahn MM, Benhadji KA, Lallena MJ, Holmgaard RB, Xu X, Zhang F, Manro JR, Iversen PW, Iyer CV, Brekken RA, Kalos MD, Driscoll KE. Yingling JM, et al. Among authors: brekken ra. Oncotarget. 2017 Dec 31;9(6):6659-6677. doi: 10.18632/oncotarget.23795. eCollection 2018 Jan 23. Oncotarget. 2017. PMID: 29467918 Free PMC article.
Design, Synthesis, and Biological Evaluation of 3-(Imidazo[1,2- a]pyrazin-3-ylethynyl)-4-isopropyl- N-(3-((4-methylpiperazin-1-yl)methyl)-5-(trifluoromethyl)phenyl)benzamide as a Dual Inhibitor of Discoidin Domain Receptors 1 and 2.
Wang Z, Zhang Y, Pinkas DM, Fox AE, Luo J, Huang H, Cui S, Xiang Q, Xu T, Xun Q, Zhu D, Tu Z, Ren X, Brekken RA, Bullock AN, Liang G, Ding K, Lu X. Wang Z, et al. Among authors: brekken ra. J Med Chem. 2018 Sep 13;61(17):7977-7990. doi: 10.1021/acs.jmedchem.8b01045. Epub 2018 Aug 20. J Med Chem. 2018. PMID: 30075624 Free PMC article.
Cyclooxygenase-2 Inhibition Potentiates the Efficacy of Vascular Endothelial Growth Factor Blockade and Promotes an Immune Stimulatory Microenvironment in Preclinical Models of Pancreatic Cancer.
Zhang Y, Kirane A, Huang H, Sorrelle NB, Burrows FJ, Dellinger MT, Brekken RA. Zhang Y, et al. Among authors: brekken ra. Mol Cancer Res. 2019 Feb;17(2):348-355. doi: 10.1158/1541-7786.MCR-18-0427. Epub 2018 Oct 17. Mol Cancer Res. 2019. PMID: 30333153 Free PMC article.
229 results