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Page 1
Discovery of a highly potent, selective, orally bioavailable inhibitor of KAT6A/B histone acetyltransferases with efficacy against KAT6A-high ER+ breast cancer.
Sharma S, Chung CY, Uryu S, Petrovic J, Cao J, Rickard A, Nady N, Greasley S, Johnson E, Brodsky O, Khan S, Wang H, Wang Z, Zhang Y, Tsaparikos K, Chen L, Mazurek A, Lapek J, Kung PP, Sutton S, Richardson PF, Greenwald EC, Yamazaki S, Jones R, Maegley KA, Bingham P, Lam H, Stupple AE, Kamal A, Chueh A, Cuzzupe A, Morrow BJ, Ren B, Carrasco-Pozo C, Tan CW, Bhuva DD, Allan E, Surgenor E, Vaillant F, Pehlivanoglu H, Falk H, Whittle JR, Newman J, Cursons J, Doherty JP, White KL, MacPherson L, Devlin M, Dennis ML, Hattarki MK, De Silva M, Camerino MA, Butler MS, Dolezal O, Pilling P, Foitzik R, Stupple PA, Lagiakos HR, Walker SR, Hediyeh-Zadeh S, Nuttall S, Spall SK, Charman SA, Connor T, Peat TS, Avery VM, Bozikis YE, Yang Y, Zhang M, Monahan BJ, Voss AK, Thomas T, Street IP, Dawson SJ, Dawson MA, Lindeman GJ, Davis MJ, Visvader JE, Paul TA. Sharma S, et al. Among authors: stupple pa. Cell Chem Biol. 2023 Oct 19;30(10):1191-1210.e20. doi: 10.1016/j.chembiol.2023.07.005. Epub 2023 Aug 8. Cell Chem Biol. 2023. PMID: 37557181 Free article.
Fragment screening for a protein-protein interaction inhibitor to WDR5.
Dennis ML, Morrow BJ, Dolezal O, Cuzzupe AN, Stupple AE, Newman J, Bentley J, Hattarki M, Nuttall SD, Foitzik RC, Street IP, Stupple PA, Monahan BJ, Peat TS. Dennis ML, et al. Among authors: stupple pa. Struct Dyn. 2019 Nov 14;6(6):064701. doi: 10.1063/1.5122849. eCollection 2019 Nov. Struct Dyn. 2019. PMID: 31768400 Free PMC article.
HBO1 is required for the maintenance of leukaemia stem cells.
MacPherson L, Anokye J, Yeung MM, Lam EYN, Chan YC, Weng CF, Yeh P, Knezevic K, Butler MS, Hoegl A, Chan KL, Burr ML, Gearing LJ, Willson T, Liu J, Choi J, Yang Y, Bilardi RA, Falk H, Nguyen N, Stupple PA, Peat TS, Zhang M, de Silva M, Carrasco-Pozo C, Avery VM, Khoo PS, Dolezal O, Dennis ML, Nuttall S, Surjadi R, Newman J, Ren B, Leaver DJ, Sun Y, Baell JB, Dovey O, Vassiliou GS, Grebien F, Dawson SJ, Street IP, Monahan BJ, Burns CJ, Choudhary C, Blewitt ME, Voss AK, Thomas T, Dawson MA. MacPherson L, et al. Among authors: stupple pa. Nature. 2020 Jan;577(7789):266-270. doi: 10.1038/s41586-019-1835-6. Epub 2019 Dec 11. Nature. 2020. PMID: 31827282
Temporal Analysis of Brd4 Displacement in the Control of B Cell Survival, Proliferation, and Differentiation.
Kong IY, Rimes JS, Light A, Todorovski I, Jones S, Morand E, Knight DA, Bergman YE, Hogg SJ, Falk H, Monahan BJ, Stupple PA, Street IP, Heinzel S, Bouillet P, Johnstone RW, Hodgkin PD, Vervoort SJ, Hawkins ED. Kong IY, et al. Among authors: stupple pa. Cell Rep. 2020 Oct 20;33(3):108290. doi: 10.1016/j.celrep.2020.108290. Cell Rep. 2020. PMID: 33086063 Free article.
Regulation of PRMT5-MDM4 axis is critical in the response to CDK4/6 inhibitors in melanoma.
AbuHammad S, Cullinane C, Martin C, Bacolas Z, Ward T, Chen H, Slater A, Ardley K, Kirby L, Chan KT, Brajanovski N, Smith LK, Rao AD, Lelliott EJ, Kleinschmidt M, Vergara IA, Papenfuss AT, Lau P, Ghosh P, Haupt S, Haupt Y, Sanij E, Poortinga G, Pearson RB, Falk H, Curtis DJ, Stupple P, Devlin M, Street I, Davies MA, McArthur GA, Sheppard KE. AbuHammad S, et al. Proc Natl Acad Sci U S A. 2019 Sep 3;116(36):17990-18000. doi: 10.1073/pnas.1901323116. Epub 2019 Aug 22. Proc Natl Acad Sci U S A. 2019. PMID: 31439820 Free PMC article.
An imidazopiperidine series of CCR5 antagonists for the treatment of HIV: the discovery of N-{(1S)-1-(3-fluorophenyl)-3-[(3-endo)-3-(5-isobutyryl-2-methyl-4,5,6,7-tetrahydro-1H-imidazo[4,5-c]pyridin-1-yl)-8-azabicyclo[3.2.1]oct-8-yl]propyl}acetamide (PF-232798).
Stupple PA, Batchelor DV, Corless M, Dorr PK, Ellis D, Fenwick DR, Galan SR, Jones RM, Mason HJ, Middleton DS, Perros M, Perruccio F, Platts MY, Pryde DC, Rodrigues D, Smith NN, Stephenson PT, Webster R, Westby M, Wood A. Stupple PA, et al. J Med Chem. 2011 Jan 13;54(1):67-77. doi: 10.1021/jm100978n. Epub 2010 Dec 3. J Med Chem. 2011. PMID: 21128663
The discovery of a potent Nav1.3 inhibitor with good oral pharmacokinetics.
Pryde DC, Swain NA, Stupple PA, West CW, Marron B, Markworth CJ, Printzenhoff D, Lin Z, Cox PJ, Suzuki R, McMurray S, Waldron GJ, Payne CE, Warmus JS, Chapman ML. Pryde DC, et al. Among authors: stupple pa. Medchemcomm. 2017 Apr 28;8(6):1255-1267. doi: 10.1039/c7md00131b. eCollection 2017 Jun 1. Medchemcomm. 2017. PMID: 30108836 Free PMC article.
Pyrazole NNRTIs 4: selection of UK-453,061 (lersivirine) as a development candidate.
Mowbray CE, Burt C, Corbau R, Gayton S, Hawes M, Perros M, Tran I, Price DA, Quinton FJ, Selby MD, Stupple PA, Webster R, Wood A. Mowbray CE, et al. Among authors: stupple pa. Bioorg Med Chem Lett. 2009 Oct 15;19(20):5857-60. doi: 10.1016/j.bmcl.2009.08.080. Epub 2009 Aug 27. Bioorg Med Chem Lett. 2009. PMID: 19748778
Pyrazole NNRTIs 1: design and initial optimisation of a novel template.
Mowbray CE, Burt C, Corbau R, Perros M, Tran I, Stupple PA, Webster R, Wood A. Mowbray CE, et al. Among authors: stupple pa. Bioorg Med Chem Lett. 2009 Oct 1;19(19):5599-602. doi: 10.1016/j.bmcl.2009.08.039. Epub 2009 Aug 13. Bioorg Med Chem Lett. 2009. PMID: 19709880
17 results