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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: mcelroy sp. 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.
Identification of small molecule inhibitors of pre-mRNA splicing.
Pawellek A, McElroy S, Samatov T, Mitchell L, Woodland A, Ryder U, Gray D, Lührmann R, Lamond AI. Pawellek A, et al. J Biol Chem. 2014 Dec 12;289(50):34683-98. doi: 10.1074/jbc.M114.590976. Epub 2014 Oct 3. J Biol Chem. 2014. PMID: 25281741 Free PMC article.
Development of Small-Molecule Trypanosoma brucei N-Myristoyltransferase Inhibitors: Discovery and Optimisation of a Novel Binding Mode.
Spinks D, Smith V, Thompson S, Robinson DA, Luksch T, Smith A, Torrie LS, McElroy S, Stojanovski L, Norval S, Collie IT, Hallyburton I, Rao B, Brand S, Brenk R, Frearson JA, Read KD, Wyatt PG, Gilbert IH. Spinks D, et al. ChemMedChem. 2015 Nov;10(11):1821-36. doi: 10.1002/cmdc.201500301. Epub 2015 Sep 23. ChemMedChem. 2015. PMID: 26395087 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: mcelroy sp. 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: mcelroy sp. 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.
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: mcelroy sp. 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.
Identification of small molecule inhibitors of pre-mRNA splicing.
Pawallek A, McElroy S, Samatov T, Mitchell L, Woodland A, Ryder U, Gray D, Lührmann R, Lamond AI. Pawallek A, et al. J Biol Chem. 2015 Mar 6;290(10):6005. doi: 10.1074/jbc.A114.590976. J Biol Chem. 2015. PMID: 25750262 Free PMC article. No abstract available.
34 results