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Page 1
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. 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
Discovery and structure-activity relationship of 3-aminopyrid-2-ones as potent and selective interleukin-2 inducible T-cell kinase (Itk) inhibitors.
Charrier JD, Miller A, Kay DP, Brenchley G, Twin HC, Collier PN, Ramaya S, Keily SB, Durrant SJ, Knegtel RM, Tanner AJ, Brown K, Curnock AP, Jimenez JM. Charrier JD, et al. Among authors: knegtel rm. J Med Chem. 2011 Apr 14;54(7):2341-50. doi: 10.1021/jm101499u. Epub 2011 Mar 10. J Med Chem. 2011. PMID: 21391610
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: knegtel rm. J Med Chem. 2011 Apr 14;54(7):2320-30. doi: 10.1021/jm101488z. Epub 2011 Mar 17. J Med Chem. 2011. PMID: 21413798
Advances in the design of ITK inhibitors.
Charrier JD, Knegtel RM. Charrier JD, et al. Among authors: knegtel rm. Expert Opin Drug Discov. 2013 Apr;8(4):369-81. doi: 10.1517/17460441.2013.769520. Epub 2013 Feb 7. Expert Opin Drug Discov. 2013. PMID: 23387379 Review.
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: knegtel r. 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 Selective, Orally Bioavailable Pyrazolopyridine Inhibitors of Protein Kinase Cθ (PKCθ) That Ameliorate Symptoms of Experimental Autoimmune Encephalomyelitis.
Collier PN, Twin HC, Knegtel RMA, Boyall D, Brenchley G, Davis CJ, Keily S, Mak C, Miller A, Pierard F, Settimo L, Bolton CM, Chiu P, Curnock A, Doyle E, Tanner AJ, Jimenez JM. Collier PN, et al. Among authors: knegtel rma. ACS Med Chem Lett. 2019 Jun 27;10(8):1134-1139. doi: 10.1021/acsmedchemlett.9b00134. eCollection 2019 Aug 8. ACS Med Chem Lett. 2019. PMID: 31417666 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. Among authors: knegtel rm. 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
Structure-based optimization of aminopyridines as PKCθ inhibitors.
Jimenez JM, Davis C, Boyall D, Fraysse D, Knegtel R, Settimo L, Young S, Bolton C, Chiu P, Curnock A, Rasmussen R, Tanner A, Ager I. Jimenez JM, et al. Among authors: knegtel r. Bioorg Med Chem Lett. 2012 Jul 15;22(14):4645-9. doi: 10.1016/j.bmcl.2012.05.114. Epub 2012 Jun 6. Bioorg Med Chem Lett. 2012. PMID: 22738630
Crystal structure of aurora-2, an oncogenic serine/threonine kinase.
Cheetham GM, Knegtel RM, Coll JT, Renwick SB, Swenson L, Weber P, Lippke JA, Austen DA. Cheetham GM, et al. J Biol Chem. 2002 Nov 8;277(45):42419-22. doi: 10.1074/jbc.C200426200. Epub 2002 Sep 16. J Biol Chem. 2002. PMID: 12237287 Free article.
42 results