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Page 1
Development of Chemical Entities Endowed with Potent Fast-Killing Properties against Plasmodium falciparum Malaria Parasites.
Matralis AN, Malik A, Penzo M, Moreno I, Almela MJ, Camino I, Crespo B, Saadeddin A, Ghidelli-Disse S, Rueda L, Calderon F, Osborne SA, Drewes G, Böesche M, Fernández-Álvaro E, Martin Hernando JI, Baker DA. Matralis AN, et al. Among authors: drewes g. J Med Chem. 2019 Oct 24;62(20):9217-9235. doi: 10.1021/acs.jmedchem.9b01099. Epub 2019 Oct 14. J Med Chem. 2019. PMID: 31566384 Free PMC article.
Quantitative chemical proteomics reveals mechanisms of action of clinical ABL kinase inhibitors.
Bantscheff M, Eberhard D, Abraham Y, Bastuck S, Boesche M, Hobson S, Mathieson T, Perrin J, Raida M, Rau C, Reader V, Sweetman G, Bauer A, Bouwmeester T, Hopf C, Kruse U, Neubauer G, Ramsden N, Rick J, Kuster B, Drewes G. Bantscheff M, et al. Among authors: drewes g. Nat Biotechnol. 2007 Sep;25(9):1035-44. doi: 10.1038/nbt1328. Epub 2007 Aug 26. Nat Biotechnol. 2007. PMID: 17721511
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: drewes g. 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 PMC article.
Cell Penetrant Inhibitors of the KDM4 and KDM5 Families of Histone Lysine Demethylases. 1. 3-Amino-4-pyridine Carboxylate Derivatives.
Westaway SM, Preston AG, Barker MD, Brown F, Brown JA, Campbell M, Chung CW, Diallo H, Douault C, Drewes G, Eagle R, Gordon L, Haslam C, Hayhow TG, Humphreys PG, Joberty G, Katso R, Kruidenier L, Leveridge M, Liddle J, Mosley J, Muelbaier M, Randle R, Rioja I, Rueger A, Seal GA, Sheppard RJ, Singh O, Taylor J, Thomas P, Thomson D, Wilson DM, Lee K, Prinjha RK. Westaway SM, et al. Among authors: drewes g. J Med Chem. 2016 Feb 25;59(4):1357-69. doi: 10.1021/acs.jmedchem.5b01537. Epub 2016 Jan 15. J Med Chem. 2016. PMID: 26771107
Cell Penetrant Inhibitors of the KDM4 and KDM5 Families of Histone Lysine Demethylases. 2. Pyrido[3,4-d]pyrimidin-4(3H)-one Derivatives.
Westaway SM, Preston AG, Barker MD, Brown F, Brown JA, Campbell M, Chung CW, Drewes G, Eagle R, Garton N, Gordon L, Haslam C, Hayhow TG, Humphreys PG, Joberty G, Katso R, Kruidenier L, Leveridge M, Pemberton M, Rioja I, Seal GA, Shipley T, Singh O, Suckling CJ, Taylor J, Thomas P, Wilson DM, Lee K, Prinjha RK. Westaway SM, et al. Among authors: drewes g. J Med Chem. 2016 Feb 25;59(4):1370-87. doi: 10.1021/acs.jmedchem.5b01538. Epub 2016 Jan 15. J Med Chem. 2016. PMID: 26771203
Biochemical Screening of Five Protein Kinases from Plasmodium falciparum against 14,000 Cell-Active Compounds.
Crowther GJ, Hillesland HK, Keyloun KR, Reid MC, Lafuente-Monasterio MJ, Ghidelli-Disse S, Leonard SE, He P, Jones JC, Krahn MM, Mo JS, Dasari KS, Fox AM, Boesche M, El Bakkouri M, Rivas KL, Leroy D, Hui R, Drewes G, Maly DJ, Van Voorhis WC, Ojo KK. Crowther GJ, et al. Among authors: drewes g. PLoS One. 2016 Mar 2;11(3):e0149996. doi: 10.1371/journal.pone.0149996. eCollection 2016. PLoS One. 2016. PMID: 26934697 Free PMC article.
Interrogating the Druggability of the 2-Oxoglutarate-Dependent Dioxygenase Target Class by Chemical Proteomics.
Joberty G, Boesche M, Brown JA, Eberhard D, Garton NS, Humphreys PG, Mathieson T, Muelbaier M, Ramsden NG, Reader V, Rueger A, Sheppard RJ, Westaway SM, Bantscheff M, Lee K, Wilson DM, Prinjha RK, Drewes G. Joberty G, et al. Among authors: drewes g. ACS Chem Biol. 2016 Jul 15;11(7):2002-10. doi: 10.1021/acschembio.6b00080. Epub 2016 May 19. ACS Chem Biol. 2016. PMID: 27197014
THPP target assignment reveals EchA6 as an essential fatty acid shuttle in mycobacteria.
Cox JA, Abrahams KA, Alemparte C, Ghidelli-Disse S, Rullas J, Angulo-Barturen I, Singh A, Gurcha SS, Nataraj V, Bethell S, Remuiñán MJ, Encinas L, Jervis PJ, Cammack NC, Bhatt A, Kruse U, Bantscheff M, Fütterer K, Barros D, Ballell L, Drewes G, Besra GS. Cox JA, et al. Among authors: drewes g. Nat Microbiol. 2016 Jan 18;1:15006. doi: 10.1038/nmicrobiol.2015.6. Nat Microbiol. 2016. PMID: 27571973
Identification of KasA as the cellular target of an anti-tubercular scaffold.
Abrahams KA, Chung CW, Ghidelli-Disse S, Rullas J, Rebollo-López MJ, Gurcha SS, Cox JA, Mendoza A, Jiménez-Navarro E, Martínez-Martínez MS, Neu M, Shillings A, Homes P, Argyrou A, Casanueva R, Loman NJ, Moynihan PJ, Lelièvre J, Selenski C, Axtman M, Kremer L, Bantscheff M, Angulo-Barturen I, Izquierdo MC, Cammack NC, Drewes G, Ballell L, Barros D, Besra GS, Bates RH. Abrahams KA, et al. Among authors: drewes g. Nat Commun. 2016 Sep 1;7:12581. doi: 10.1038/ncomms12581. Nat Commun. 2016. PMID: 27581223 Free PMC article.
115 results