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AZD0364 Is a Potent and Selective ERK1/2 Inhibitor That Enhances Antitumor Activity in KRAS-Mutant Tumor Models when Combined with the MEK Inhibitor, Selumetinib.
Flemington V, Davies EJ, Robinson D, Sandin LC, Delpuech O, Zhang P, Hanson L, Farrington P, Bell S, Falenta K, Gibbons FD, Lindsay N, Smith A, Wilson J, Roberts K, Tonge M, Hopcroft P, Willis SE, Roudier MP, Rooney C, Coker EA, Jaaks P, Garnett MJ, Fawell SE, Jones CD, Ward RA, Simpson I, Cosulich SC, Pease JE, Smith PD. Flemington V, et al. Among authors: davies ej. Mol Cancer Ther. 2021 Feb;20(2):238-249. doi: 10.1158/1535-7163.MCT-20-0002. Epub 2020 Dec 3. Mol Cancer Ther. 2021. PMID: 33273059
Discovery of a Potent and Selective Oral Inhibitor of ERK1/2 (AZD0364) That Is Efficacious in Both Monotherapy and Combination Therapy in Models of Nonsmall Cell Lung Cancer (NSCLC).
Ward RA, Anderton MJ, Bethel P, Breed J, Cook C, Davies EJ, Dobson A, Dong Z, Fairley G, Farrington P, Feron L, Flemington V, Gibbons FD, Graham MA, Greenwood R, Hanson L, Hopcroft P, Howells R, Hudson J, James M, Jones CD, Jones CR, Li Y, Lamont S, Lewis R, Lindsay N, McCabe J, McGuire T, Rawlins P, Roberts K, Sandin L, Simpson I, Swallow S, Tang J, Tomkinson G, Tonge M, Wang Z, Zhai B. Ward RA, et al. Among authors: davies ej. J Med Chem. 2019 Dec 26;62(24):11004-11018. doi: 10.1021/acs.jmedchem.9b01295. Epub 2019 Nov 25. J Med Chem. 2019. PMID: 31710489
Structure-Guided Discovery of Potent and Selective Inhibitors of ERK1/2 from a Modestly Active and Promiscuous Chemical Start Point.
Ward RA, Bethel P, Cook C, Davies E, Debreczeni JE, Fairley G, Feron L, Flemington V, Graham MA, Greenwood R, Griffin N, Hanson L, Hopcroft P, Howard TD, Hudson J, James M, Jones CD, Jones CR, Lamont S, Lewis R, Lindsay N, Roberts K, Simpson I, St-Gallay S, Swallow S, Tang J, Tonge M, Wang Z, Zhai B. Ward RA, et al. J Med Chem. 2017 Apr 27;60(8):3438-3450. doi: 10.1021/acs.jmedchem.7b00267. Epub 2017 Apr 14. J Med Chem. 2017. PMID: 28376306
Selumetinib-based therapy in uveal melanoma patient-derived xenografts.
Decaudin D, El Botty R, Diallo B, Massonnet G, Fleury J, Naguez A, Raymondie C, Davies E, Smith A, Wilson J, Howes C, Smith PD, Cassoux N, Piperno-Neumann S, Roman-Roman S, Némati F. Decaudin D, et al. Oncotarget. 2018 Apr 24;9(31):21674-21686. doi: 10.18632/oncotarget.24670. eCollection 2018 Apr 24. Oncotarget. 2018. PMID: 29774094 Free PMC article.
A microfluidic system that replicates pharmacokinetic (PK) profiles in vitro improves prediction of in vivo efficacy in preclinical models.
Singh D, Deosarkar SP, Cadogan E, Flemington V, Bray A, Zhang J, Reiserer RS, Schaffer DK, Gerken GB, Britt CM, Werner EM, Gibbons FD, Kostrzewski T, Chambers CE, Davies EJ, Montoya AR, Fok JHL, Hughes D, Fabre K, Wagoner MP, Wikswo JP, Scott CW. Singh D, et al. Among authors: davies ej. PLoS Biol. 2022 May 26;20(5):e3001624. doi: 10.1371/journal.pbio.3001624. eCollection 2022 May. PLoS Biol. 2022. PMID: 35617197 Free PMC article.
Targeting melanoma's MCL1 bias unleashes the apoptotic potential of BRAF and ERK1/2 pathway inhibitors.
Sale MJ, Minihane E, Monks NR, Gilley R, Richards FM, Schifferli KP, Andersen CL, Davies EJ, Vicente MA, Ozono E, Markovets A, Dry JR, Drew L, Flemington V, Proia T, Jodrell DI, Smith PD, Cook SJ. Sale MJ, et al. Among authors: davies ej. Nat Commun. 2019 Nov 14;10(1):5167. doi: 10.1038/s41467-019-12409-w. Nat Commun. 2019. PMID: 31727888 Free PMC article.
Development of an ObLiGaRe Doxycycline Inducible Cas9 system for pre-clinical cancer drug discovery.
Lundin A, Porritt MJ, Jaiswal H, Seeliger F, Johansson C, Bidar AW, Badertscher L, Wimberger S, Davies EJ, Hardaker E, Martins CP, James E, Admyre T, Taheri-Ghahfarokhi A, Bradley J, Schantz A, Alaeimahabadi B, Clausen M, Xu X, Mayr LM, Nitsch R, Bohlooly-Y M, Barry ST, Maresca M. Lundin A, et al. Among authors: davies ej. Nat Commun. 2020 Sep 29;11(1):4903. doi: 10.1038/s41467-020-18548-9. Nat Commun. 2020. PMID: 32994412 Free PMC article.
89 results