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Targeting Mycobacterium tuberculosis CoaBC through Chemical Inhibition of 4'-Phosphopantothenoyl-l-cysteine Synthetase (CoaB) Activity.
Evans JC, Murugesan D, Post JM, Mendes V, Wang Z, Nahiyaan N, Lynch SL, Thompson S, Green SR, Ray PC, Hess J, Spry C, Coyne AG, Abell C, Boshoff HIM, Wyatt PG, Rhee KY, Blundell TL, Barry CE 3rd, Mizrahi V. Evans JC, et al. Among authors: thompson s. ACS Infect Dis. 2021 Jun 11;7(6):1666-1679. doi: 10.1021/acsinfecdis.0c00904. Epub 2021 May 3. ACS Infect Dis. 2021. PMID: 33939919 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: thompson s. 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.
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. Among authors: thompson s. ChemMedChem. 2015 Nov;10(11):1821-36. doi: 10.1002/cmdc.201500301. Epub 2015 Sep 23. ChemMedChem. 2015. PMID: 26395087 Free PMC article.
A Molecular Hybridization Approach for the Design of Potent, Highly Selective, and Brain-Penetrant N-Myristoyltransferase Inhibitors.
Harrison JR, Brand S, Smith V, Robinson DA, Thompson S, Smith A, Davies K, Mok N, Torrie LS, Collie I, Hallyburton I, Norval S, Simeons FRC, Stojanovski L, Frearson JA, Brenk R, Wyatt PG, Gilbert IH, Read KD. Harrison JR, et al. Among authors: thompson s. J Med Chem. 2018 Sep 27;61(18):8374-8389. doi: 10.1021/acs.jmedchem.8b00884. Epub 2018 Sep 12. J Med Chem. 2018. PMID: 30207721 Free PMC article.
The Qi Site of Cytochrome b is a Promiscuous Drug Target in Trypanosoma cruzi and Leishmania donovani.
Wall RJ, Carvalho S, Milne R, Bueren-Calabuig JA, Moniz S, Cantizani-Perez J, MacLean L, Kessler A, Cotillo I, Sastry L, Manthri S, Patterson S, Zuccotto F, Thompson S, Martin J, Marco M, Miles TJ, De Rycker M, Thomas MG, Fairlamb AH, Gilbert IH, Wyllie S. Wall RJ, et al. Among authors: thompson s. ACS Infect Dis. 2020 Mar 13;6(3):515-528. doi: 10.1021/acsinfecdis.9b00426. Epub 2020 Jan 30. ACS Infect Dis. 2020. PMID: 31967783 Free PMC article.
Identification and Optimization of a Series of 8-Hydroxy Naphthyridines with Potent In Vitro Antileishmanial Activity: Initial SAR and Assessment of In Vivo Activity.
Thomas MG, De Rycker M, Wall RJ, Spinks D, Epemolu O, Manthri S, Norval S, Osuna-Cabello M, Patterson S, Riley J, Simeons FRC, Stojanovski L, Thomas J, Thompson S, Naylor C, Fiandor JM, Wyatt PG, Marco M, Wyllie S, Read KD, Miles TJ, Gilbert IH. Thomas MG, et al. Among authors: thompson s. J Med Chem. 2020 Sep 10;63(17):9523-9539. doi: 10.1021/acs.jmedchem.0c00705. Epub 2020 Aug 13. J Med Chem. 2020. PMID: 32663005 Free PMC article.
Resistance of Mycobacterium tuberculosis to indole 4-carboxamides occurs through alterations in drug metabolism and tryptophan biosynthesis.
Libardo MDJ, Duncombe CJ, Green SR, Wyatt PG, Thompson S, Ray PC, Ioerger TR, Oh S, Goodwin MB, Boshoff HIM, Barry CE 3rd. Libardo MDJ, et al. Among authors: thompson s. Cell Chem Biol. 2021 Aug 19;28(8):1180-1191.e20. doi: 10.1016/j.chembiol.2021.02.023. Epub 2021 Mar 24. Cell Chem Biol. 2021. PMID: 33765439 Free PMC article.
Scaffold-Hopping Strategy on a Series of Proteasome Inhibitors Led to a Preclinical Candidate for the Treatment of Visceral Leishmaniasis.
Thomas M, Brand S, De Rycker M, Zuccotto F, Lukac I, Dodd PG, Ko EJ, Manthri S, McGonagle K, Osuna-Cabello M, Riley J, Pont C, Simeons F, Stojanovski L, Thomas J, Thompson S, Viayna E, Fiandor JM, Martin J, Wyatt PG, Miles TJ, Read KD, Marco M, Gilbert IH. Thomas M, et al. Among authors: thompson s. J Med Chem. 2021 May 13;64(9):5905-5930. doi: 10.1021/acs.jmedchem.1c00047. Epub 2021 Apr 27. J Med Chem. 2021. PMID: 33904304 Free PMC article.
4,664 results