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Rational Design of 5-(4-(Isopropylsulfonyl)phenyl)-3-(3-(4-((methylamino)methyl)phenyl)isoxazol-5-yl)pyrazin-2-amine (VX-970, M6620): Optimization of Intra- and Intermolecular Polar Interactions of a New Ataxia Telangiectasia Mutated and Rad3-Related (ATR) Kinase Inhibitor.
Knegtel R, Charrier JD, Durrant S, Davis C, O'Donnell M, Storck P, MacCormick S, Kay D, Pinder J, Virani A, Twin H, Griffiths M, Reaper P, Littlewood P, Young S, Golec J, Pollard J. Knegtel R, et al. Among authors: pollard j. J Med Chem. 2019 Jun 13;62(11):5547-5561. doi: 10.1021/acs.jmedchem.9b00426. Epub 2019 May 16. J Med Chem. 2019. PMID: 31074988
The discovery of the potent aurora inhibitor MK-0457 (VX-680).
Bebbington D, Binch H, Charrier JD, Everitt S, Fraysse D, Golec J, Kay D, Knegtel R, Mak C, Mazzei F, Miller A, Mortimore M, O'Donnell M, Patel S, Pierard F, Pinder J, Pollard J, Ramaya S, Robinson D, Rutherford A, Studley J, Westcott J. Bebbington D, et al. Among authors: pollard j. Bioorg Med Chem Lett. 2009 Jul 1;19(13):3586-92. doi: 10.1016/j.bmcl.2009.04.136. Epub 2009 May 3. Bioorg Med Chem Lett. 2009. PMID: 19447622
Discovery of potent and selective inhibitors of ataxia telangiectasia mutated and Rad3 related (ATR) protein kinase as potential anticancer agents.
Charrier JD, Durrant SJ, Golec JM, Kay DP, Knegtel RM, MacCormick S, Mortimore M, O'Donnell ME, Pinder JL, Reaper PM, Rutherford AP, Wang PS, Young SC, Pollard JR. Charrier JD, et al. Among authors: pollard jr. J Med Chem. 2011 Apr 14;54(7):2320-30. doi: 10.1021/jm101488z. Epub 2011 Mar 17. J Med Chem. 2011. PMID: 21413798
Potentiation of tumor responses to DNA damaging therapy by the selective ATR inhibitor VX-970.
Hall AB, Newsome D, Wang Y, Boucher DM, Eustace B, Gu Y, Hare B, Johnson MA, Milton S, Murphy CE, Takemoto D, Tolman C, Wood M, Charlton P, Charrier JD, Furey B, Golec J, Reaper PM, Pollard JR. Hall AB, et al. Among authors: pollard jr. Oncotarget. 2014 Jul 30;5(14):5674-85. doi: 10.18632/oncotarget.2158. Oncotarget. 2014. PMID: 25010037 Free PMC article.
Development of pharmacodynamic biomarkers for ATR inhibitors.
Chen T, Middleton FK, Falcon S, Reaper PM, Pollard JR, Curtin NJ. Chen T, et al. Among authors: pollard jr. Mol Oncol. 2015 Feb;9(2):463-72. doi: 10.1016/j.molonc.2014.09.012. Epub 2014 Oct 13. Mol Oncol. 2015. PMID: 25459351 Free PMC article.
Cancer-Specific Synthetic Lethality between ATR and CHK1 Kinase Activities.
Sanjiv K, Hagenkort A, Calderón-Montaño JM, Koolmeister T, Reaper PM, Mortusewicz O, Jacques SA, Kuiper RV, Schultz N, Scobie M, Charlton PA, Pollard JR, Berglund UW, Altun M, Helleday T. Sanjiv K, et al. Cell Rep. 2016 Jan 12;14(2):298-309. doi: 10.1016/j.celrep.2015.12.032. Epub 2015 Dec 31. Cell Rep. 2016. PMID: 26748709 Free PMC article.
Kinetic and mechanistic characterisation of Choline Kinase-α.
Hudson CS, Knegtel RM, Brown K, Charlton PA, Pollard JR. Hudson CS, et al. Biochim Biophys Acta. 2013 Jun;1834(6):1107-16. doi: 10.1016/j.bbapap.2013.02.008. Epub 2013 Feb 13. Biochim Biophys Acta. 2013. PMID: 23416529
ATR inhibitors VE-821 and VX-970 sensitize cancer cells to topoisomerase i inhibitors by disabling DNA replication initiation and fork elongation responses.
Jossé R, Martin SE, Guha R, Ormanoglu P, Pfister TD, Reaper PM, Barnes CS, Jones J, Charlton P, Pollard JR, Morris J, Doroshow JH, Pommier Y. Jossé R, et al. Among authors: pollard jr. Cancer Res. 2014 Dec 1;74(23):6968-79. doi: 10.1158/0008-5472.CAN-13-3369. Epub 2014 Sep 30. Cancer Res. 2014. PMID: 25269479 Free PMC article.
ATR inhibitors as a synthetic lethal therapy for tumours deficient in ARID1A.
Williamson CT, Miller R, Pemberton HN, Jones SE, Campbell J, Konde A, Badham N, Rafiq R, Brough R, Gulati A, Ryan CJ, Francis J, Vermulen PB, Reynolds AR, Reaper PM, Pollard JR, Ashworth A, Lord CJ. Williamson CT, et al. Among authors: pollard jr. Nat Commun. 2016 Dec 13;7:13837. doi: 10.1038/ncomms13837. Nat Commun. 2016. PMID: 27958275 Free PMC article.
1,139 results