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Discovery of a Potent, Cell Penetrant, and Selective p300/CBP-Associated Factor (PCAF)/General Control Nonderepressible 5 (GCN5) Bromodomain Chemical Probe.
Humphreys PG, Bamborough P, Chung CW, Craggs PD, Gordon L, Grandi P, Hayhow TG, Hussain J, Jones KL, Lindon M, Michon AM, Renaux JF, Suckling CJ, Tough DF, Prinjha RK. Humphreys PG, et al. Among authors: Lindon M. J Med Chem. 2017 Jan 26;60(2):695-709. doi: 10.1021/acs.jmedchem.6b01566. Epub 2017 Jan 9. J Med Chem. 2017. PMID: 28002667
A novel series of potent gamma-secretase inhibitors based on a benzobicyclo[4.2.1]nonane core.
Lewis SJ, Smith AL, Neduvelil JG, Stevenson GI, Lindon MJ, Jones AB, Shearman MS, Beher D, Clarke E, Best JD, Peachey JE, Harrison T, Castro JL. Lewis SJ, et al. Among authors: Lindon MJ. Bioorg Med Chem Lett. 2005 Jan 17;15(2):373-8. doi: 10.1016/j.bmcl.2004.10.062. Bioorg Med Chem Lett. 2005. PMID: 15603957
Oxazolidinones as novel human CCR8 antagonists.
Jin J, Wang Y, Wang F, Kerns JK, Vinader VM, Hancock AP, Lindon MJ, Stevenson GI, Morrow DM, Rao P, Nguyen C, Barrett VJ, Browning C, Hartmann G, Andrew DP, Sarau HM, Foley JJ, Jurewicz AJ, Fornwald JA, Harker AJ, Moore ML, Rivero RA, Belmonte KE, Connor HE. Jin J, et al. Among authors: Lindon MJ. Bioorg Med Chem Lett. 2007 Mar 15;17(6):1722-5. doi: 10.1016/j.bmcl.2006.12.076. Epub 2006 Dec 24. Bioorg Med Chem Lett. 2007. PMID: 17267215
Discovery of thiadiazole amides as potent, S1P₃-sparing agonists of sphingosine-1-phosphate 1 (S1P₁) receptor.
Xu H, Zhang H, Luan L, Xu Y, Li C, Wang Y, Han F, Yang T, Ren F, Xiang JN, Elliott JD, Zhao Y, Guo TB, Lu H, Zhang W, Hirst D, Lindon M, Lin X. Xu H, et al. Among authors: Lindon M. Bioorg Med Chem Lett. 2012 Apr 1;22(7):2456-9. doi: 10.1016/j.bmcl.2012.02.016. Epub 2012 Feb 15. Bioorg Med Chem Lett. 2012. PMID: 22386243
The commonly used PI3-kinase probe LY294002 is an inhibitor of BET bromodomains.
Dittmann A, Werner T, Chung CW, Savitski MM, Fälth Savitski M, Grandi P, Hopf C, Lindon M, Neubauer G, Prinjha RK, Bantscheff M, Drewes G. Dittmann A, et al. Among authors: Lindon M. ACS Chem Biol. 2014 Feb 21;9(2):495-502. doi: 10.1021/cb400789e. Epub 2013 Dec 10. ACS Chem Biol. 2014. PMID: 24533473
Discovery and Characterization of GSK2801, a Selective Chemical Probe for the Bromodomains BAZ2A and BAZ2B.
Chen P, Chaikuad A, Bamborough P, Bantscheff M, Bountra C, Chung CW, Fedorov O, Grandi P, Jung D, Lesniak R, Lindon M, Müller S, Philpott M, Prinjha R, Rogers C, Selenski C, Tallant C, Werner T, Willson TM, Knapp S, Drewry DH. Chen P, et al. Among authors: Lindon M. J Med Chem. 2016 Feb 25;59(4):1410-24. doi: 10.1021/acs.jmedchem.5b00209. Epub 2015 Apr 6. J Med Chem. 2016. PMID: 25799074 Free PMC article.
Discovery of I-BRD9, a Selective Cell Active Chemical Probe for Bromodomain Containing Protein 9 Inhibition.
Theodoulou NH, Bamborough P, Bannister AJ, Becher I, Bit RA, Che KH, Chung CW, Dittmann A, Drewes G, Drewry DH, Gordon L, Grandi P, Leveridge M, Lindon M, Michon AM, Molnar J, Robson SC, Tomkinson NC, Kouzarides T, Prinjha RK, Humphreys PG. Theodoulou NH, et al. Among authors: Lindon M. J Med Chem. 2016 Feb 25;59(4):1425-39. doi: 10.1021/acs.jmedchem.5b00256. Epub 2015 Apr 30. J Med Chem. 2016. PMID: 25856009 Free article.
Discovery of Tetrahydroquinoxalines as Bromodomain and Extra-Terminal Domain (BET) Inhibitors with Selectivity for the Second Bromodomain.
Law RP, Atkinson SJ, Bamborough P, Chung CW, Demont EH, Gordon LJ, Lindon M, Prinjha RK, Watson AJB, Hirst DJ. Law RP, et al. Among authors: Lindon M. J Med Chem. 2018 May 24;61(10):4317-4334. doi: 10.1021/acs.jmedchem.7b01666. Epub 2018 May 3. J Med Chem. 2018. PMID: 29656650
Discovery of a Bromodomain and Extraterminal Inhibitor with a Low Predicted Human Dose through Synergistic Use of Encoded Library Technology and Fragment Screening.
Wellaway CR, Amans D, Bamborough P, Barnett H, Bit RA, Brown JA, Carlson NR, Chung CW, Cooper AWJ, Craggs PD, Davis RP, Dean TW, Evans JP, Gordon L, Harada IL, Hirst DJ, Humphreys PG, Jones KL, Lewis AJ, Lindon MJ, Lugo D, Mahmood M, McCleary S, Medeiros P, Mitchell DJ, O'Sullivan M, Le Gall A, Patel VK, Patten C, Poole DL, Shah RR, Smith JE, Stafford KAJ, Thomas PJ, Vimal M, Wall ID, Watson RJ, Wellaway N, Yao G, Prinjha RK. Wellaway CR, et al. Among authors: Lindon MJ. J Med Chem. 2020 Jan 23;63(2):714-746. doi: 10.1021/acs.jmedchem.9b01670. Epub 2020 Jan 6. J Med Chem. 2020. PMID: 31904959
Selective targeting of BD1 and BD2 of the BET proteins in cancer and immuno-inflammation.
Gilan O, Rioja I, Knezevic K, Bell MJ, Yeung MM, Harker NR, Lam EYN, Chung CW, Bamborough P, Petretich M, Urh M, Atkinson SJ, Bassil AK, Roberts EJ, Vassiliadis D, Burr ML, Preston AGS, Wellaway C, Werner T, Gray JR, Michon AM, Gobbetti T, Kumar V, Soden PE, Haynes A, Vappiani J, Tough DF, Taylor S, Dawson SJ, Bantscheff M, Lindon M, Drewes G, Demont EH, Daniels DL, Grandi P, Prinjha RK, Dawson MA. Gilan O, et al. Among authors: Lindon M. Science. 2020 Mar 19:eaaz8455. doi: 10.1126/science.aaz8455. Online ahead of print. Science. 2020. PMID: 32193360
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