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96 results

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Combination drug scheduling defines a "window of opportunity" for chemopotentiation of gemcitabine by an orally bioavailable, selective ChK1 inhibitor, GNE-900.
Blackwood E, Epler J, Yen I, Flagella M, O'Brien T, Evangelista M, Schmidt S, Xiao Y, Choi J, Kowanetz K, Ramiscal J, Wong K, Jakubiak D, Yee S, Cain G, Gazzard L, Williams K, Halladay J, Jackson PK, Malek S. Blackwood E, et al. Mol Cancer Ther. 2013 Oct;12(10):1968-80. doi: 10.1158/1535-7163.MCT-12-1218. Epub 2013 Jul 19. Mol Cancer Ther. 2013. PMID: 23873850
Potent, selective, and orally bioavailable inhibitors of the mammalian target of rapamycin kinase domain exhibiting single agent antiproliferative activity.
Koehler MF, Bergeron P, Blackwood E, Bowman KK, Chen YH, Deshmukh G, Ding X, Epler J, Lau K, Lee L, Liu L, Ly C, Malek S, Nonomiya J, Oeh J, Ortwine DF, Sampath D, Sideris S, Trinh L, Truong T, Wu J, Pei Z, Lyssikatos JP. Koehler MF, et al. Among authors: blackwood e. J Med Chem. 2012 Dec 27;55(24):10958-71. doi: 10.1021/jm301389h. Epub 2012 Dec 12. J Med Chem. 2012. PMID: 23199076
Mitigation of Acetylcholine Esterase Activity in the 1,7-Diazacarbazole Series of Inhibitors of Checkpoint Kinase 1.
Gazzard L, Williams K, Chen H, Axford L, Blackwood E, Burton B, Chapman K, Crackett P, Drobnick J, Ellwood C, Epler J, Flagella M, Gancia E, Gill M, Goodacre S, Halladay J, Hewitt J, Hunt H, Kintz S, Lyssikatos J, Macleod C, Major S, Médard G, Narukulla R, Ramiscal J, Schmidt S, Seward E, Wiesmann C, Wu P, Yee S, Yen I, Malek S. Gazzard L, et al. Among authors: blackwood e. J Med Chem. 2015 Jun 25;58(12):5053-74. doi: 10.1021/acs.jmedchem.5b00464. Epub 2015 Jun 4. J Med Chem. 2015. PMID: 25988399
Phase I Study of GDC-0425, a Checkpoint Kinase 1 Inhibitor, in Combination with Gemcitabine in Patients with Refractory Solid Tumors.
Infante JR, Hollebecque A, Postel-Vinay S, Bauer TM, Blackwood EM, Evangelista M, Mahrus S, Peale FV, Lu X, Sahasranaman S, Zhu R, Chen Y, Ding X, Murray ER, Schutzman JL, Lauchle JO, Soria JC, LoRusso PM. Infante JR, et al. Clin Cancer Res. 2017 May 15;23(10):2423-2432. doi: 10.1158/1078-0432.CCR-16-1782. Epub 2016 Nov 4. Clin Cancer Res. 2017. PMID: 27815358 Clinical Trial.
Potent, selective, and orally bioavailable inhibitors of mammalian target of rapamycin (mTOR) kinase based on a quaternary substituted dihydrofuropyrimidine.
Cohen F, Bergeron P, Blackwood E, Bowman KK, Chen H, Dipasquale AG, Epler JA, Koehler MF, Lau K, Lewis C, Liu L, Ly CQ, Malek S, Nonomiya J, Ortwine DF, Pei Z, Robarge KD, Sideris S, Trinh L, Truong T, Wu J, Zhao X, Lyssikatos JP. Cohen F, et al. Among authors: blackwood e. J Med Chem. 2011 May 12;54(9):3426-35. doi: 10.1021/jm200215y. Epub 2011 Apr 15. J Med Chem. 2011. PMID: 21495671
P21-activated kinase 1 (PAK1) as a therapeutic target in BRAF wild-type melanoma.
Ong CC, Jubb AM, Jakubiak D, Zhou W, Rudolph J, Haverty PM, Kowanetz M, Yan Y, Tremayne J, Lisle R, Harris AL, Friedman LS, Belvin M, Middleton MR, Blackwood EM, Koeppen H, Hoeflich KP. Ong CC, et al. J Natl Cancer Inst. 2013 May 1;105(9):606-7. doi: 10.1093/jnci/djt054. Epub 2013 Mar 27. J Natl Cancer Inst. 2013. PMID: 23535073
Discovery and Biological Profiling of Potent and Selective mTOR Inhibitor GDC-0349.
Pei Z, Blackwood E, Liu L, Malek S, Belvin M, Koehler MF, Ortwine DF, Chen H, Cohen F, Kenny JR, Bergeron P, Lau K, Ly C, Zhao X, Estrada AA, Truong T, Epler JA, Nonomiya J, Trinh L, Sideris S, Lesnick J, Bao L, Vijapurkar U, Mukadam S, Tay S, Deshmukh G, Chen YH, Ding X, Friedman LS, Lyssikatos JP. Pei Z, et al. Among authors: blackwood e. ACS Med Chem Lett. 2012 Nov 29;4(1):103-7. doi: 10.1021/ml3003132. eCollection 2013 Jan 10. ACS Med Chem Lett. 2012. PMID: 24900569 Free PMC article.
Pyrimidoaminotropanes as potent, selective, and efficacious small molecule kinase inhibitors of the mammalian target of rapamycin (mTOR).
Estrada AA, Shore DG, Blackwood E, Chen YH, Deshmukh G, Ding X, Dipasquale AG, Epler JA, Friedman LS, Koehler MF, Liu L, Malek S, Nonomiya J, Ortwine DF, Pei Z, Sideris S, St-Jean F, Trinh L, Truong T, Lyssikatos JP. Estrada AA, et al. Among authors: blackwood e. J Med Chem. 2013 Apr 11;56(7):3090-101. doi: 10.1021/jm400194n. Epub 2013 Mar 29. J Med Chem. 2013. PMID: 23473235
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