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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: purkiss ag. 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.
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: purkiss ag. 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.
Architecture and regulation of a GDNF-GFRα1 synaptic adhesion assembly.
Houghton FM, Adams SE, Ríos AS, Masino L, Purkiss AG, Briggs DC, Ledda F, McDonald NQ. Houghton FM, et al. Among authors: purkiss ag. Nat Commun. 2023 Nov 20;14(1):7551. doi: 10.1038/s41467-023-43148-8. Nat Commun. 2023. PMID: 37985758 Free PMC article.
46 results