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Page 1
Structure and chemical inhibition of the RET tyrosine kinase domain.
Knowles PP, Murray-Rust J, Kjaer S, Scott RP, Hanrahan S, Santoro M, Ibáñez CF, McDonald NQ. Knowles PP, et al. Among authors: mcdonald nq. J Biol Chem. 2006 Nov 3;281(44):33577-87. doi: 10.1074/jbc.M605604200. Epub 2006 Aug 23. J Biol Chem. 2006. PMID: 16928683 Free article.
The discovery of 2-substituted phenol quinazolines as potent RET kinase inhibitors with improved KDR selectivity.
Newton R, Bowler KA, Burns EM, Chapman PJ, Fairweather EE, Fritzl SJR, Goldberg KM, Hamilton NM, Holt SV, Hopkins GV, Jones SD, Jordan AM, Lyons AJ, Nikki March H, McDonald NQ, Maguire LA, Mould DP, Purkiss AG, Small HF, Stowell AIJ, Thomson GJ, Waddell ID, Waszkowycz B, Watson AJ, Ogilvie DJ. Newton R, et al. Among authors: mcdonald nq. Eur J Med Chem. 2016 Apr 13;112:20-32. doi: 10.1016/j.ejmech.2016.01.039. Epub 2016 Jan 29. Eur J Med Chem. 2016. PMID: 26874741 Free PMC article.
Drugging the catalytically inactive state of RET kinase in RET-rearranged tumors.
Plenker D, Riedel M, Brägelmann J, Dammert MA, Chauhan R, Knowles PP, Lorenz C, Keul M, Bührmann M, Pagel O, Tischler V, Scheel AH, Schütte D, Song Y, Stark J, Mrugalla F, Alber Y, Richters A, Engel J, Leenders F, Heuckmann JM, Wolf J, Diebold J, Pall G, Peifer M, Aerts M, Gevaert K, Zahedi RP, Buettner R, Shokat KM, McDonald NQ, Kast SM, Gautschi O, Thomas RK, Sos ML. Plenker D, et al. Among authors: mcdonald nq. Sci Transl Med. 2017 Jun 14;9(394):eaah6144. doi: 10.1126/scitranslmed.aah6144. Sci Transl Med. 2017. PMID: 28615362 Free PMC article.
A secondary RET mutation in the activation loop conferring resistance to vandetanib.
Nakaoku T, Kohno T, Araki M, Niho S, Chauhan R, Knowles PP, Tsuchihara K, Matsumoto S, Shimada Y, Mimaki S, Ishii G, Ichikawa H, Nagatoishi S, Tsumoto K, Okuno Y, Yoh K, McDonald NQ, Goto K. Nakaoku T, et al. Among authors: mcdonald nq. Nat Commun. 2018 Feb 12;9(1):625. doi: 10.1038/s41467-018-02994-7. Nat Commun. 2018. PMID: 29434222 Free PMC article.
A two-site flexible clamp mechanism for RET-GDNF-GFRα1 assembly reveals both conformational adaptation and strict geometric spacing.
Adams SE, Purkiss AG, Knowles PP, Nans A, Briggs DC, Borg A, Earl CP, Goodman KM, Nawrotek A, Borg AJ, McIntosh PB, Houghton FM, Kjær S, McDonald NQ. Adams SE, et al. Among authors: mcdonald nq. Structure. 2021 Jul 1;29(7):694-708.e7. doi: 10.1016/j.str.2020.12.012. Epub 2021 Jan 22. Structure. 2021. PMID: 33484636 Free PMC article.
Discovery of N-Trisubstituted Pyrimidine Derivatives as Type I RET and RET Gatekeeper Mutant Inhibitors with a Novel Kinase Binding Pose.
Zhang L, Moccia M, Briggs DC, Bharate JB, Lakkaniga NR, Knowles P, Yan W, Tran P, Kharbanda A, Wang X, Leung YK, Frett B, Santoro M, McDonald NQ, Carlomagno F, Li HY. Zhang L, et al. Among authors: mcdonald nq. J Med Chem. 2022 Jan 27;65(2):1536-1551. doi: 10.1021/acs.jmedchem.1c01280. J Med Chem. 2022. PMID: 35081714 Free PMC article.
108 results