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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: sawyer js. Oncotarget. 2017 Dec 31;9(6):6659-6677. doi: 10.18632/oncotarget.23795. eCollection 2018 Jan 23. Oncotarget. 2017. PMID: 29467918 Free PMC article.
Clinical development of galunisertib (LY2157299 monohydrate), a small molecule inhibitor of transforming growth factor-beta signaling pathway.
Herbertz S, Sawyer JS, Stauber AJ, Gueorguieva I, Driscoll KE, Estrem ST, Cleverly AL, Desaiah D, Guba SC, Benhadji KA, Slapak CA, Lahn MM. Herbertz S, et al. Among authors: sawyer js. Drug Des Devel Ther. 2015 Aug 10;9:4479-99. doi: 10.2147/DDDT.S86621. eCollection 2015. Drug Des Devel Ther. 2015. PMID: 26309397 Free PMC article. Review.
Optimization of a dihydropyrrolopyrazole series of transforming growth factor-beta type I receptor kinase domain inhibitors: discovery of an orally bioavailable transforming growth factor-beta receptor type I inhibitor as antitumor agent.
Li HY, McMillen WT, Heap CR, McCann DJ, Yan L, Campbell RM, Mundla SR, King CH, Dierks EA, Anderson BD, Britt KS, Huss KL, Voss MD, Wang Y, Clawson DK, Yingling JM, Sawyer JS. Li HY, et al. Among authors: sawyer js. J Med Chem. 2008 Apr 10;51(7):2302-6. doi: 10.1021/jm701199p. Epub 2008 Mar 4. J Med Chem. 2008. PMID: 18314943
Synthesis and activity of new aryl- and heteroaryl-substituted 5,6-dihydro-4H-pyrrolo[1,2-b]pyrazole inhibitors of the transforming growth factor-beta type I receptor kinase domain.
Sawyer JS, Beight DW, Britt KS, Anderson BD, Campbell RM, Goodson T Jr, Herron DK, Li HY, McMillen WT, Mort N, Parsons S, Smith EC, Wagner JR, Yan L, Zhang F, Yingling JM. Sawyer JS, et al. Bioorg Med Chem Lett. 2004 Jul 5;14(13):3581-4. doi: 10.1016/j.bmcl.2004.04.007. Bioorg Med Chem Lett. 2004. PMID: 15177479
N(2)-Aroylanthranilamide inhibitors of human factor Xa.
Yee YK, Tebbe AL, Linebarger JH, Beight DW, Craft TJ, Gifford-Moore D, Goodson T Jr, Herron DK, Klimkowski VJ, Kyle JA, Sawyer JS, Smith GF, Tinsley JM, Towner RD, Weir L, Wiley MR. Yee YK, et al. Among authors: sawyer js. J Med Chem. 2000 Mar 9;43(5):873-82. doi: 10.1021/jm990327e. J Med Chem. 2000. PMID: 10715154
34 results