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Design and Synthesis of Brain Penetrant Trypanocidal N-Myristoyltransferase Inhibitors.
Bayliss T, Robinson DA, Smith VC, Brand S, McElroy SP, Torrie LS, Mpamhanga C, Norval S, Stojanovski L, Brenk R, Frearson JA, Read KD, Gilbert IH, Wyatt PG. Bayliss T, et al. Among authors: stojanovski l. J Med Chem. 2017 Dec 14;60(23):9790-9806. doi: 10.1021/acs.jmedchem.7b01255. Epub 2017 Nov 22. J Med Chem. 2017. PMID: 29125744 Free PMC article.
N-myristoyltransferase inhibitors as new leads to treat sleeping sickness.
Frearson JA, Brand S, McElroy SP, Cleghorn LA, Smid O, Stojanovski L, Price HP, Guther ML, Torrie LS, Robinson DA, Hallyburton I, Mpamhanga CP, Brannigan JA, Wilkinson AJ, Hodgkinson M, Hui R, Qiu W, Raimi OG, van Aalten DM, Brenk R, Gilbert IH, Read KD, Fairlamb AH, Ferguson MA, Smith DF, Wyatt PG. Frearson JA, et al. Among authors: stojanovski l. Nature. 2010 Apr 1;464(7289):728-32. doi: 10.1038/nature08893. Nature. 2010. PMID: 20360736 Free PMC article.
Discovery of a novel class of orally active trypanocidal N-myristoyltransferase inhibitors.
Brand S, Cleghorn LA, McElroy SP, Robinson DA, Smith VC, Hallyburton I, Harrison JR, Norcross NR, Spinks D, Bayliss T, Norval S, Stojanovski L, Torrie LS, Frearson JA, Brenk R, Fairlamb AH, Ferguson MA, Read KD, Wyatt PG, Gilbert IH. Brand S, et al. Among authors: stojanovski l. J Med Chem. 2012 Jan 12;55(1):140-52. doi: 10.1021/jm201091t. Epub 2011 Dec 7. J Med Chem. 2012. PMID: 22148754 Free PMC article.
Automated design of ligands to polypharmacological profiles.
Besnard J, Ruda GF, Setola V, Abecassis K, Rodriguiz RM, Huang XP, Norval S, Sassano MF, Shin AI, Webster LA, Simeons FR, Stojanovski L, Prat A, Seidah NG, Constam DB, Bickerton GR, Read KD, Wetsel WC, Gilbert IH, Roth BL, Hopkins AL. Besnard J, et al. Among authors: stojanovski l. Nature. 2012 Dec 13;492(7428):215-20. doi: 10.1038/nature11691. Nature. 2012. PMID: 23235874 Free PMC article.
Lead optimization of a pyrazole sulfonamide series of Trypanosoma brucei N-myristoyltransferase inhibitors: identification and evaluation of CNS penetrant compounds as potential treatments for stage 2 human African trypanosomiasis.
Brand S, Norcross NR, Thompson S, Harrison JR, Smith VC, Robinson DA, Torrie LS, McElroy SP, Hallyburton I, Norval S, Scullion P, Stojanovski L, Simeons FR, van Aalten D, Frearson JA, Brenk R, Fairlamb AH, Ferguson MA, Wyatt PG, Gilbert IH, Read KD. Brand S, et al. Among authors: stojanovski l. J Med Chem. 2014 Dec 11;57(23):9855-69. doi: 10.1021/jm500809c. Epub 2014 Nov 20. J Med Chem. 2014. PMID: 25412409 Free PMC article.
A novel multiple-stage antimalarial agent that inhibits protein synthesis.
Baragaña B, Hallyburton I, Lee MC, Norcross NR, Grimaldi R, Otto TD, Proto WR, Blagborough AM, Meister S, Wirjanata G, Ruecker A, Upton LM, Abraham TS, Almeida MJ, Pradhan A, Porzelle A, Luksch T, Martínez MS, Luksch T, Bolscher JM, Woodland A, Norval S, Zuccotto F, Thomas J, Simeons F, Stojanovski L, Osuna-Cabello M, Brock PM, Churcher TS, Sala KA, Zakutansky SE, Jiménez-Díaz MB, Sanz LM, Riley J, Basak R, Campbell M, Avery VM, Sauerwein RW, Dechering KJ, Noviyanti R, Campo B, Frearson JA, Angulo-Barturen I, Ferrer-Bazaga S, Gamo FJ, Wyatt PG, Leroy D, Siegl P, Delves MJ, Kyle DE, Wittlin S, Marfurt J, Price RN, Sinden RE, Winzeler EA, Charman SA, Bebrevska L, Gray DW, Campbell S, Fairlamb AH, Willis PA, Rayner JC, Fidock DA, Read KD, Gilbert IH. Baragaña B, et al. Among authors: stojanovski l. Nature. 2015 Jun 18;522(7556):315-20. doi: 10.1038/nature14451. Nature. 2015. PMID: 26085270 Free PMC article.
Discovery of Inhibitors of Trypanosoma brucei by Phenotypic Screening of a Focused Protein Kinase Library.
Woodland A, Thompson S, Cleghorn LA, Norcross N, De Rycker M, Grimaldi R, Hallyburton I, Rao B, Norval S, Stojanovski L, Brun R, Kaiser M, Frearson JA, Gray DW, Wyatt PG, Read KD, Gilbert IH. Woodland A, et al. Among authors: stojanovski l. ChemMedChem. 2015 Nov;10(11):1809-20. doi: 10.1002/cmdc.201500300. Epub 2015 Sep 18. ChemMedChem. 2015. PMID: 26381210 Free PMC article.
43 results