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Page 1
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: flemington v. Nat Commun. 2019 Nov 14;10(1):5167. doi: 10.1038/s41467-019-12409-w. Nat Commun. 2019. PMID: 31727888 Free PMC article.
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. 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
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. Among authors: flemington v. 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
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: flemington v. 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
Challenges and Opportunities in Cancer Drug Resistance.
Ward RA, Fawell S, Floc'h N, Flemington V, McKerrecher D, Smith PD. Ward RA, et al. Among authors: flemington v. Chem Rev. 2021 Mar 24;121(6):3297-3351. doi: 10.1021/acs.chemrev.0c00383. Epub 2020 Jul 21. Chem Rev. 2021. PMID: 32692162 Review.
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: flemington v. 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.
Potent, selective small molecule inhibitors of type III phosphatidylinositol-4-kinase α- but not β-inhibit the phosphatidylinositol signaling cascade and cancer cell proliferation.
Waring MJ, Andrews DM, Faulder PF, Flemington V, McKelvie JC, Maman S, Preston M, Raubo P, Robb GR, Roberts K, Rowlinson R, Smith JM, Swarbrick ME, Treinies I, Winter JJ, Wood RJ. Waring MJ, et al. Among authors: flemington v. Chem Commun (Camb). 2014 May 25;50(40):5388-90. doi: 10.1039/c3cc48391f. Epub 2013 Dec 24. Chem Commun (Camb). 2014. PMID: 24366037
Identification and optimization of a novel series of selective PIP5K inhibitors.
Andrews DM, Cartic S, Cosulich S, Divecha N, Faulder P, Flemington V, Kern O, Kettle JG, MacDonald E, McKelvie J, Pike KG, Roberts B, Rowlinson R, Smith JM, Stockley M, Swarbrick ME, Treinies I, Waring MJ. Andrews DM, et al. Among authors: flemington v. Bioorg Med Chem. 2022 Jan 15;54:116557. doi: 10.1016/j.bmc.2021.116557. Epub 2021 Dec 12. Bioorg Med Chem. 2022. PMID: 34922306
Structure-Guided Design of Highly Selective and Potent Covalent Inhibitors of ERK1/2.
Ward RA, Colclough N, Challinor M, Debreczeni JE, Eckersley K, Fairley G, Feron L, Flemington V, Graham MA, Greenwood R, Hopcroft P, Howard TD, James M, Jones CD, Jones CR, Renshaw J, Roberts K, Snow L, Tonge M, Yeung K. Ward RA, et al. Among authors: flemington v. J Med Chem. 2015 Jun 11;58(11):4790-801. doi: 10.1021/acs.jmedchem.5b00466. Epub 2015 May 28. J Med Chem. 2015. PMID: 25977981
11 results