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Page 1
Molecular basis of USP7 inhibition by selective small-molecule inhibitors.
Turnbull AP, Ioannidis S, Krajewski WW, Pinto-Fernandez A, Heride C, Martin ACL, Tonkin LM, Townsend EC, Buker SM, Lancia DR, Caravella JA, Toms AV, Charlton TM, Lahdenranta J, Wilker E, Follows BC, Evans NJ, Stead L, Alli C, Zarayskiy VV, Talbot AC, Buckmelter AJ, Wang M, McKinnon CL, Saab F, McGouran JF, Century H, Gersch M, Pittman MS, Marshall CG, Raynham TM, Simcox M, Stewart LMD, McLoughlin SB, Escobedo JA, Bair KW, Dinsmore CJ, Hammonds TR, Kim S, Urbé S, Clague MJ, Kessler BM, Komander D. Turnbull AP, et al. Nature. 2017 Oct 26;550(7677):481-486. doi: 10.1038/nature24451. Epub 2017 Oct 18. Nature. 2017. PMID: 29045389 Free PMC article.
USP28 deletion and small-molecule inhibition destabilizes c-MYC and elicits regression of squamous cell lung carcinoma.
Ruiz EJ, Pinto-Fernandez A, Turnbull AP, Lan L, Charlton TM, Scott HC, Damianou A, Vere G, Riising EM, Da Costa C, Krajewski WW, Guerin D, Kearns JD, Ioannidis S, Katz M, McKinnon C, O'Connell J, Moncaut N, Rosewell I, Nye E, Jones N, Heride C, Gersch M, Wu M, Dinsmore CJ, Hammonds TR, Kim S, Komander D, Urbe S, Clague MJ, Kessler BM, Behrens A. Ruiz EJ, et al. Among authors: turnbull ap. Elife. 2021 Oct 12;10:e71596. doi: 10.7554/eLife.71596. Elife. 2021. PMID: 34636321 Free PMC article.
Structure-Based Design of Potent and Selective Inhibitors of the Metabolic Kinase PFKFB3.
Boyd S, Brookfield JL, Critchlow SE, Cumming IA, Curtis NJ, Debreczeni J, Degorce SL, Donald C, Evans NJ, Groombridge S, Hopcroft P, Jones NP, Kettle JG, Lamont S, Lewis HJ, MacFaull P, McLoughlin SB, Rigoreau LJ, Smith JM, St-Gallay S, Stock JK, Turnbull AP, Wheatley ER, Winter J, Wingfield J. Boyd S, et al. Among authors: turnbull ap. J Med Chem. 2015 Apr 23;58(8):3611-25. doi: 10.1021/acs.jmedchem.5b00352. Epub 2015 Apr 13. J Med Chem. 2015. PMID: 25849762
A High-Throughput Screening Triage Workflow to Authenticate a Novel Series of PFKFB3 Inhibitors.
St-Gallay SA, Bennett N, Critchlow SE, Curtis N, Davies G, Debreczeni J, Evans N, Hardern I, Holdgate G, Jones NP, Leach L, Maman S, McLoughlin S, Preston M, Rigoreau L, Thomas A, Turnbull AP, Walker G, Walsh J, Ward RA, Wheatley E, Winter-Holt J. St-Gallay SA, et al. Among authors: turnbull ap. SLAS Discov. 2018 Jan;23(1):11-22. doi: 10.1177/2472555217732289. Epub 2017 Sep 25. SLAS Discov. 2018. PMID: 28945981 Free article.
Discovery of potent inhibitors of the lysophospholipase autotaxin.
Shah P, Cheasty A, Foxton C, Raynham T, Farooq M, Gutierrez IF, Lejeune A, Pritchard M, Turnbull A, Pang L, Owen P, Boyd S, Stowell A, Jordan A, Hamilton NM, Hitchin JR, Stockley M, MacDonald E, Quesada MJ, Trivier E, Skeete J, Ovaa H, Moolenaar WH, Ryder H. Shah P, et al. Bioorg Med Chem Lett. 2016 Nov 15;26(22):5403-5410. doi: 10.1016/j.bmcl.2016.10.036. Epub 2016 Oct 14. Bioorg Med Chem Lett. 2016. PMID: 27780639
Discovery, Characterization, and Structure-Based Optimization of Small-Molecule In Vitro and In Vivo Probes for Human DNA Polymerase Theta.
Stockley ML, Ferdinand A, Benedetti G, Blencowe P, Boyd SM, Calder M, Charles MD, Edwardes LV, Ekwuru T, Finch H, Galbiati A, Geo L, Grande D, Grinkevich V, Holliday ND, Krajewski WW, MacDonald E, Majithiya JB, McCarron H, McWhirter CL, Patel V, Pedder C, Rajendra E, Ranzani M, Rigoreau LJM, Robinson HMR, Schaedler T, Sirina J, Smith GCM, Swarbrick ME, Turnbull AP, Willis S, Heald RA. Stockley ML, et al. Among authors: turnbull ap. J Med Chem. 2022 Oct 27;65(20):13879-13891. doi: 10.1021/acs.jmedchem.2c01142. Epub 2022 Oct 6. J Med Chem. 2022. PMID: 36200480
Synthesis and structure-activity relationships for 1-(4-(piperidin-1-ylsulfonyl)phenyl)pyrrolidin-2-ones as novel non-carboxylate inhibitors of the aldo-keto reductase enzyme AKR1C3.
Heinrich DM, Flanagan JU, Jamieson SM, Silva S, Rigoreau LJ, Trivier E, Raynham T, Turnbull AP, Denny WA. Heinrich DM, et al. Among authors: turnbull ap. Eur J Med Chem. 2013 Apr;62:738-44. doi: 10.1016/j.ejmech.2013.01.047. Epub 2013 Feb 9. Eur J Med Chem. 2013. PMID: 23454516
3-(3,4-Dihydroisoquinolin-2(1H)-ylsulfonyl)benzoic Acids: highly potent and selective inhibitors of the type 5 17-β-hydroxysteroid dehydrogenase AKR1C3.
Jamieson SM, Brooke DG, Heinrich D, Atwell GJ, Silva S, Hamilton EJ, Turnbull AP, Rigoreau LJ, Trivier E, Soudy C, Samlal SS, Owen PJ, Schroeder E, Raynham T, Flanagan JU, Denny WA. Jamieson SM, et al. Among authors: turnbull ap. J Med Chem. 2012 Sep 13;55(17):7746-58. doi: 10.1021/jm3007867. Epub 2012 Aug 21. J Med Chem. 2012. PMID: 22877157
71 results