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Page 1
Spirocycle MmpL3 Inhibitors with Improved hERG and Cytotoxicity Profiles as Inhibitors of Mycobacterium tuberculosis Growth.
Ray PC, Huggett M, Turner PA, Taylor M, Cleghorn LAT, Early J, Kumar A, Bonnett SA, Flint L, Joerss D, Johnson J, Korkegian A, Mullen S, Moure AL, Davis SH, Murugesan D, Mathieson M, Caldwell N, Engelhart CA, Schnappinger D, Epemolu O, Zuccotto F, Riley J, Scullion P, Stojanovski L, Massoudi L, Robertson GT, Lenaerts AJ, Freiberg G, Kempf DJ, Masquelin T, Hipskind PA, Odingo J, Read KD, Green SR, Wyatt PG, Parish T. Ray PC, et al. Among authors: cleghorn lat. ACS Omega. 2021 Jan 13;6(3):2284-2311. doi: 10.1021/acsomega.0c05589. eCollection 2021 Jan 26. ACS Omega. 2021. PMID: 33521468 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. Nature. 2010 Apr 1;464(7289):728-32. doi: 10.1038/nature08893. Nature. 2010. PMID: 20360736 Free PMC article.
Optimisation of the anti-Trypanosoma brucei activity of the opioid agonist U50488.
Smith VC, Cleghorn LA, Woodland A, Spinks D, Hallyburton I, Collie IT, Mok NY, Norval S, Brenk R, Fairlamb AH, Frearson JA, Read KD, Gilbert IH, Wyatt PG. Smith VC, et al. ChemMedChem. 2011 Oct 4;6(10):1832-40. doi: 10.1002/cmdc.201100278. Epub 2011 Aug 10. ChemMedChem. 2011. PMID: 21834094 Free PMC article.
Identification of inhibitors of the Leishmania cdc2-related protein kinase CRK3.
Cleghorn LA, Woodland A, Collie IT, Torrie LS, Norcross N, Luksch T, Mpamhanga C, Walker RG, Mottram JC, Brenk R, Frearson JA, Gilbert IH, Wyatt PG. Cleghorn LA, et al. ChemMedChem. 2011 Dec 9;6(12):2214-24. doi: 10.1002/cmdc.201100344. Epub 2011 Sep 13. ChemMedChem. 2011. PMID: 21913331 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. 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.
From on-target to off-target activity: identification and optimisation of Trypanosoma brucei GSK3 inhibitors and their characterisation as anti-Trypanosoma brucei drug discovery lead molecules.
Woodland A, Grimaldi R, Luksch T, Cleghorn LA, Ojo KK, Van Voorhis WC, Brenk R, Frearson JA, Gilbert IH, Wyatt PG. Woodland A, et al. ChemMedChem. 2013 Jul;8(7):1127-37. doi: 10.1002/cmdc.201300072. Epub 2013 Jun 14. ChemMedChem. 2013. PMID: 23776181 Free PMC article.
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