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Items: 1 to 50 of 73

1.

Inhibition of CorA-Dependent Magnesium Homeostasis Is Cidal in Mycobacterium tuberculosis.

Park Y, Ahn YM, Jonnala S, Oh S, Fisher JM, Goodwin MB, Ioerger TR, Via LE, Bayliss T, Green SR, Ray PC, Wyatt PG, Barry CE 3rd, Boshoff HI.

Antimicrob Agents Chemother. 2019 Sep 23;63(10). pii: e01006-19. doi: 10.1128/AAC.01006-19. Print 2019 Oct.

PMID:
31383669
2.

Preclinical candidate for the treatment of visceral leishmaniasis that acts through proteasome inhibition.

Wyllie S, Brand S, Thomas M, De Rycker M, Chung CW, Pena I, Bingham RP, Bueren-Calabuig JA, Cantizani J, Cebrian D, Craggs PD, Ferguson L, Goswami P, Hobrath J, Howe J, Jeacock L, Ko EJ, Korczynska J, MacLean L, Manthri S, Martinez MS, Mata-Cantero L, Moniz S, Nühs A, Osuna-Cabello M, Pinto E, Riley J, Robinson S, Rowland P, Simeons FRC, Shishikura Y, Spinks D, Stojanovski L, Thomas J, Thompson S, Viayna Gaza E, Wall RJ, Zuccotto F, Horn D, Ferguson MAJ, Fairlamb AH, Fiandor JM, Martin J, Gray DW, Miles TJ, Gilbert IH, Read KD, Marco M, Wyatt PG.

Proc Natl Acad Sci U S A. 2019 May 7;116(19):9318-9323. doi: 10.1073/pnas.1820175116. Epub 2019 Apr 8.

3.

Lysyl-tRNA synthetase as a drug target in malaria and cryptosporidiosis.

Baragaña B, Forte B, Choi R, Nakazawa Hewitt S, Bueren-Calabuig JA, Pisco JP, Peet C, Dranow DM, Robinson DA, Jansen C, Norcross NR, Vinayak S, Anderson M, Brooks CF, Cooper CA, Damerow S, Delves M, Dowers K, Duffy J, Edwards TE, Hallyburton I, Horst BG, Hulverson MA, Ferguson L, Jiménez-Díaz MB, Jumani RS, Lorimer DD, Love MS, Maher S, Matthews H, McNamara CW, Miller P, O'Neill S, Ojo KK, Osuna-Cabello M, Pinto E, Post J, Riley J, Rottmann M, Sanz LM, Scullion P, Sharma A, Shepherd SM, Shishikura Y, Simeons FRC, Stebbins EE, Stojanovski L, Straschil U, Tamaki FK, Tamjar J, Torrie LS, Vantaux A, Witkowski B, Wittlin S, Yogavel M, Zuccotto F, Angulo-Barturen I, Sinden R, Baum J, Gamo FJ, Mäser P, Kyle DE, Winzeler EA, Myler PJ, Wyatt PG, Floyd D, Matthews D, Sharma A, Striepen B, Huston CD, Gray DW, Fairlamb AH, Pisliakov AV, Walpole C, Read KD, Van Voorhis WC, Gilbert IH.

Proc Natl Acad Sci U S A. 2019 Apr 2;116(14):7015-7020. doi: 10.1073/pnas.1814685116. Epub 2019 Mar 20.

4.

Identification of GSK3186899/DDD853651 as a Preclinical Development Candidate for the Treatment of Visceral Leishmaniasis.

Thomas MG, De Rycker M, Ajakane M, Albrecht S, Álvarez-Pedraglio AI, Boesche M, Brand S, Campbell L, Cantizani-Perez J, Cleghorn LAT, Copley RCB, Crouch SD, Daugan A, Drewes G, Ferrer S, Ghidelli-Disse S, Gonzalez S, Gresham SL, Hill AP, Hindley SJ, Lowe RM, MacKenzie CJ, MacLean L, Manthri S, Martin F, Miguel-Siles J, Nguyen VL, Norval S, Osuna-Cabello M, Woodland A, Patterson S, Pena I, Quesada-Campos MT, Reid IH, Revill C, Riley J, Ruiz-Gomez JR, Shishikura Y, Simeons FRC, Smith A, Smith VC, Spinks D, Stojanovski L, Thomas J, Thompson S, Underwood T, Gray DW, Fiandor JM, Gilbert IH, Wyatt PG, Read KD, Miles TJ.

J Med Chem. 2019 Feb 14;62(3):1180-1202. doi: 10.1021/acs.jmedchem.8b01218. Epub 2018 Dec 20.

5.

Diversity-oriented synthesis of bicyclic fragments containing privileged azines.

Luise N, Wyatt PG.

Bioorg Med Chem Lett. 2019 Jan 15;29(2):248-251. doi: 10.1016/j.bmcl.2018.11.046. Epub 2018 Nov 24.

6.

Pharmacological Validation of N-Myristoyltransferase as a Drug Target in Leishmania donovani.

Corpas-Lopez V, Moniz S, Thomas M, Wall RJ, Torrie LS, Zander-Dinse D, Tinti M, Brand S, Stojanovski L, Manthri S, Hallyburton I, Zuccotto F, Wyatt PG, De Rycker M, Horn D, Ferguson MAJ, Clos J, Read KD, Fairlamb AH, Gilbert IH, Wyllie S.

ACS Infect Dis. 2019 Jan 11;5(1):111-122. doi: 10.1021/acsinfecdis.8b00226. Epub 2018 Nov 12.

7.

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.

J Med Chem. 2018 Sep 27;61(18):8374-8389. doi: 10.1021/acs.jmedchem.8b00884. Epub 2018 Sep 12.

8.

Author Correction: Anti-trypanosomatid drug discovery: an ongoing challenge and a continuing need.

Field MC, Horn D, Fairlamb AH, Ferguson MAJ, Gray DW, Read KD, De Rycker M, Torrie LS, Wyatt PG, Wyllie S, Gilbert IH.

Nat Rev Microbiol. 2018 Nov;16(11):714. doi: 10.1038/s41579-018-0085-1.

PMID:
30206344
9.

2,4-Diamino-6-methylpyrimidines for the potential treatment of Chagas' disease.

Thomas MG, De Rycker M, Cotillo Torrejon I, Thomas J, Riley J, Spinks D, Read KD, Miles TJ, Gilbert IH, Wyatt PG.

Bioorg Med Chem Lett. 2018 Oct 1;28(18):3025-3030. doi: 10.1016/j.bmcl.2018.08.005. Epub 2018 Aug 3.

PMID:
30104093
10.

Cyclin-dependent kinase 12 is a drug target for visceral leishmaniasis.

Wyllie S, Thomas M, Patterson S, Crouch S, De Rycker M, Lowe R, Gresham S, Urbaniak MD, Otto TD, Stojanovski L, Simeons FRC, Manthri S, MacLean LM, Zuccotto F, Homeyer N, Pflaumer H, Boesche M, Sastry L, Connolly P, Albrecht S, Berriman M, Drewes G, Gray DW, Ghidelli-Disse S, Dixon S, Fiandor JM, Wyatt PG, Ferguson MAJ, Fairlamb AH, Miles TJ, Read KD, Gilbert IH.

Nature. 2018 Aug;560(7717):192-197. doi: 10.1038/s41586-018-0356-z. Epub 2018 Jul 25.

11.

Identification of Morpholino Thiophenes as Novel Mycobacterium tuberculosis Inhibitors, Targeting QcrB.

Cleghorn LAT, Ray PC, Odingo J, Kumar A, Wescott H, Korkegian A, Masquelin T, Lopez Moure A, Wilson C, Davis S, Huggett M, Turner P, Smith A, Epemolu O, Zuccotto F, Riley J, Scullion P, Shishikura Y, Ferguson L, Rullas J, Guijarro L, Read KD, Green SR, Hipskind P, Parish T, Wyatt PG.

J Med Chem. 2018 Aug 9;61(15):6592-6608. doi: 10.1021/acs.jmedchem.8b00172. Epub 2018 Jul 26.

12.

Generation of Polar Semi-Saturated Bicyclic Pyrazoles for Fragment-Based Drug-Discovery Campaigns.

Luise N, Wyatt PG.

Chemistry. 2018 Jul 20;24(41):10443-10451. doi: 10.1002/chem.201801313. Epub 2018 Jun 19.

PMID:
29732638
13.

2-Mercapto-Quinazolinones as Inhibitors of Type II NADH Dehydrogenase and Mycobacterium tuberculosis: Structure-Activity Relationships, Mechanism of Action and Absorption, Distribution, Metabolism, and Excretion Characterization.

Murugesan D, Ray PC, Bayliss T, Prosser GA, Harrison JR, Green K, Soares de Melo C, Feng TS, Street LJ, Chibale K, Warner DF, Mizrahi V, Epemolu O, Scullion P, Ellis L, Riley J, Shishikura Y, Ferguson L, Osuna-Cabello M, Read KD, Green SR, Lamprecht DA, Finin PM, Steyn AJC, Ioerger TR, Sacchettini J, Rhee KY, Arora K, Barry CE 3rd, Wyatt PG, Boshoff HIM.

ACS Infect Dis. 2018 Jun 8;4(6):954-969. doi: 10.1021/acsinfecdis.7b00275. Epub 2018 Mar 26.

14.

Screening of a Novel Fragment Library with Functional Complexity against Mycobacterium tuberculosis InhA.

Prati F, Zuccotto F, Fletcher D, Convery MA, Fernandez-Menendez R, Bates R, Encinas L, Zeng J, Chung CW, De Dios Anton P, Mendoza-Losana A, Mackenzie C, Green SR, Huggett M, Barros D, Wyatt PG, Ray PC.

ChemMedChem. 2018 Apr 6;13(7):672-677. doi: 10.1002/cmdc.201700774. Epub 2018 Feb 19.

15.

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.

J Med Chem. 2017 Dec 14;60(23):9790-9806. doi: 10.1021/acs.jmedchem.7b01255. Epub 2017 Nov 22.

16.

Screening a protein kinase inhibitor library against Plasmodium falciparum.

Hallyburton I, Grimaldi R, Woodland A, Baragaña B, Luksch T, Spinks D, James D, Leroy D, Waterson D, Fairlamb AH, Wyatt PG, Gilbert IH, Frearson JA.

Malar J. 2017 Nov 7;16(1):446. doi: 10.1186/s12936-017-2085-4.

17.

Discovery and Optimization of 5-Amino-1,2,3-triazole-4-carboxamide Series against Trypanosoma cruzi.

Brand S, Ko EJ, Viayna E, Thompson S, Spinks D, Thomas M, Sandberg L, Francisco AF, Jayawardhana S, Smith VC, Jansen C, De Rycker M, Thomas J, MacLean L, Osuna-Cabello M, Riley J, Scullion P, Stojanovski L, Simeons FRC, Epemolu O, Shishikura Y, Crouch SD, Bakshi TS, Nixon CJ, Reid IH, Hill AP, Underwood TZ, Hindley SJ, Robinson SA, Kelly JM, Fiandor JM, Wyatt PG, Marco M, Miles TJ, Read KD, Gilbert IH.

J Med Chem. 2017 Sep 14;60(17):7284-7299. doi: 10.1021/acs.jmedchem.7b00463. Epub 2017 Aug 27.

18.

Correction for Arora et al., "Respiratory Flexibility in Response to Inhibition of Cytochrome c Oxidase in Mycobacterium tuberculosis".

Arora K, Ochoa-Montaño B, Tsang PS, Blundell TL, Dawes SS, Mizrahi V, Bayliss T, Mackenzie CJ, Cleghorn LAT, Ray PC, Wyatt PG, Uh E, Lee J, Barry CE 3rd, Boshoff HI.

Antimicrob Agents Chemother. 2017 Aug 24;61(9). pii: e01429-17. doi: 10.1128/AAC.01429-17. Print 2017 Sep. No abstract available.

19.

Anti-trypanosomatid drug discovery: an ongoing challenge and a continuing need.

Field MC, Horn D, Fairlamb AH, Ferguson MAJ, Gray DW, Read KD, De Rycker M, Torrie LS, Wyatt PG, Wyllie S, Gilbert IH.

Nat Rev Microbiol. 2017 Jul;15(7):447. doi: 10.1038/nrmicro.2017.69. Epub 2017 Jun 5. No abstract available.

PMID:
28579611
20.

Drug discovery for male subfertility using high-throughput screening: a new approach to an unsolved problem.

Martins da Silva SJ, Brown SG, Sutton K, King LV, Ruso H, Gray DW, Wyatt PG, Kelly MC, Barratt CLR, Hope AG.

Hum Reprod. 2017 May 1;32(5):974-984. doi: 10.1093/humrep/dex055.

21.

Anti-trypanosomatid drug discovery: an ongoing challenge and a continuing need.

Field MC, Horn D, Fairlamb AH, Ferguson MA, Gray DW, Read KD, De Rycker M, Torrie LS, Wyatt PG, Wyllie S, Gilbert IH.

Nat Rev Microbiol. 2017 Feb 27;15(4):217-231. doi: 10.1038/nrmicro.2016.193. [Epub ahead of print] Review. Erratum in: Nat Rev Microbiol. 2017 Jul;15(7):447. Nat Rev Microbiol. 2018 Nov;16(11):714.

22.

Fragment library design, synthesis and expansion: nurturing a synthesis and training platform.

Ray PC, Kiczun M, Huggett M, Lim A, Prati F, Gilbert IH, Wyatt PG.

Drug Discov Today. 2017 Jan;22(1):43-56. doi: 10.1016/j.drudis.2016.10.005. Epub 2016 Oct 26. Review.

PMID:
27793744
23.

Discovery of a Quinoline-4-carboxamide Derivative with a Novel Mechanism of Action, Multistage Antimalarial Activity, and Potent in Vivo Efficacy.

Baragaña B, Norcross NR, Wilson C, Porzelle A, Hallyburton I, Grimaldi R, Osuna-Cabello M, Norval S, Riley J, Stojanovski L, Simeons FR, Wyatt PG, Delves MJ, Meister S, Duffy S, Avery VM, Winzeler EA, Sinden RE, Wittlin S, Frearson JA, Gray DW, Fairlamb AH, Waterson D, Campbell SF, Willis P, Read KD, Gilbert IH.

J Med Chem. 2016 Nov 10;59(21):9672-9685. Epub 2016 Sep 10.

24.

Corrigendum: 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, Martínez MS, Bolscher JM, Woodland A, Luksch T, 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.

Nature. 2016 Sep 1;537(7618):122. doi: 10.1038/nature18280. Epub 2016 May 25. No abstract available.

25.

Discovery of Indoline-2-carboxamide Derivatives as a New Class of Brain-Penetrant Inhibitors of Trypanosoma brucei.

Cleghorn LA, Albrecht S, Stojanovski L, Simeons FR, Norval S, Kime R, Collie IT, De Rycker M, Campbell L, Hallyburton I, Frearson JA, Wyatt PG, Read KD, Gilbert IH.

J Med Chem. 2015 Oct 8;58(19):7695-706. doi: 10.1021/acs.jmedchem.5b00596. Epub 2015 Sep 29.

26.

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.

ChemMedChem. 2015 Nov;10(11):1821-36. doi: 10.1002/cmdc.201500301. Epub 2015 Sep 23.

27.

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.

ChemMedChem. 2015 Nov;10(11):1809-20. doi: 10.1002/cmdc.201500300. Epub 2015 Sep 18.

28.

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.

Nature. 2015 Jun 18;522(7556):315-20. doi: 10.1038/nature14451. Erratum in: Nature. 2016 Sep 1;537(7618):122.

29.

Identification and structure solution of fragment hits against kinetoplastid N-myristoyltransferase.

Robinson DA, Wyatt PG.

Acta Crystallogr F Struct Biol Commun. 2015 May;71(Pt 5):586-93. doi: 10.1107/S2053230X15003040. Epub 2015 Apr 21.

30.

N-myristoyltransferase is a cell wall target in Aspergillus fumigatus.

Fang W, Robinson DA, Raimi OG, Blair DE, Harrison JR, Lockhart DE, Torrie LS, Ruda GF, Wyatt PG, Gilbert IH, van Aalten DM.

ACS Chem Biol. 2015 Jun 19;10(6):1425-34. doi: 10.1021/cb5008647. Epub 2015 Feb 27.

31.

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.

J Med Chem. 2014 Dec 11;57(23):9855-69. doi: 10.1021/jm500809c. Epub 2014 Nov 20.

32.

The design and synthesis of potent and selective inhibitors of Trypanosoma brucei glycogen synthase kinase 3 for the treatment of human african trypanosomiasis.

Urich R, Grimaldi R, Luksch T, Frearson JA, Brenk R, Wyatt PG.

J Med Chem. 2014 Sep 25;57(18):7536-49. doi: 10.1021/jm500239b. Epub 2014 Sep 8.

33.

A target repurposing approach identifies N-myristoyltransferase as a new candidate drug target in filarial nematodes.

Galvin BD, Li Z, Villemaine E, Poole CB, Chapman MS, Pollastri MP, Wyatt PG, Carlow CK.

PLoS Negl Trop Dis. 2014 Sep 4;8(9):e3145. doi: 10.1371/journal.pntd.0003145. eCollection 2014 Sep.

34.

Respiratory flexibility in response to inhibition of cytochrome C oxidase in Mycobacterium tuberculosis.

Arora K, Ochoa-Montaño B, Tsang PS, Blundell TL, Dawes SS, Mizrahi V, Bayliss T, Mackenzie CJ, Cleghorn LA, Ray PC, Wyatt PG, Uh E, Lee J, Barry CE 3rd, Boshoff HI.

Antimicrob Agents Chemother. 2014 Nov;58(11):6962-5. doi: 10.1128/AAC.03486-14. Epub 2014 Aug 25. Erratum in: Antimicrob Agents Chemother. 2017 Aug 24;61(9):.

35.

Clinically relevant enhancement of human sperm motility using compounds with reported phosphodiesterase inhibitor activity.

Tardif S, Madamidola OA, Brown SG, Frame L, Lefièvre L, Wyatt PG, Barratt CL, Martins Da Silva SJ.

Hum Reprod. 2014 Oct 10;29(10):2123-35. doi: 10.1093/humrep/deu196. Epub 2014 Aug 14.

36.

Exploring the Trypanosoma brucei Hsp83 potential as a target for structure guided drug design.

Pizarro JC, Hills T, Senisterra G, Wernimont AK, Mackenzie C, Norcross NR, Ferguson MA, Wyatt PG, Gilbert IH, Hui R.

PLoS Negl Trop Dis. 2013 Oct 17;7(10):e2492. doi: 10.1371/journal.pntd.0002492. eCollection 2013.

37.

Structure-activity relationship studies of pyrrolone antimalarial agents.

Murugesan D, Kaiser M, White KL, Norval S, Riley J, Wyatt PG, Charman SA, Read KD, Yeates C, Gilbert IH.

ChemMedChem. 2013 Sep;8(9):1537-44. doi: 10.1002/cmdc.201300177. Epub 2013 Aug 5.

38.

Fragment-based hit identification: thinking in 3D.

Morley AD, Pugliese A, Birchall K, Bower J, Brennan P, Brown N, Chapman T, Drysdale M, Gilbert IH, Hoelder S, Jordan A, Ley SV, Merritt A, Miller D, Swarbrick ME, Wyatt PG.

Drug Discov Today. 2013 Dec;18(23-24):1221-7. doi: 10.1016/j.drudis.2013.07.011. Epub 2013 Jul 30. Review.

PMID:
23906694
39.

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.

ChemMedChem. 2013 Jul;8(7):1127-37. doi: 10.1002/cmdc.201300072. Epub 2013 Jun 14.

40.

Comparison of a high-throughput high-content intracellular Leishmania donovani assay with an axenic amastigote assay.

De Rycker M, Hallyburton I, Thomas J, Campbell L, Wyllie S, Joshi D, Cameron S, Gilbert IH, Wyatt PG, Frearson JA, Fairlamb AH, Gray DW.

Antimicrob Agents Chemother. 2013 Jul;57(7):2913-22. doi: 10.1128/AAC.02398-12. Epub 2013 Apr 9. Erratum in: Antimicrob Agents Chemother. 2014 Dec;58(12):7622.

41.

De novo design of protein kinase inhibitors by in silico identification of hinge region-binding fragments.

Urich R, Wishart G, Kiczun M, Richters A, Tidten-Luksch N, Rauh D, Sherborne B, Wyatt PG, Brenk R.

ACS Chem Biol. 2013 May 17;8(5):1044-52. doi: 10.1021/cb300729y. Epub 2013 Mar 27.

42.

Quinol derivatives as potential trypanocidal agents.

Capes A, Patterson S, Wyllie S, Hallyburton I, Collie IT, McCarroll AJ, Stevens MF, Frearson JA, Wyatt PG, Fairlamb AH, Gilbert IH.

Bioorg Med Chem. 2012 Feb 15;20(4):1607-15. doi: 10.1016/j.bmc.2011.12.018. Epub 2011 Dec 27.

43.

Design, synthesis and biological evaluation of Trypanosoma brucei trypanothione synthetase inhibitors.

Spinks D, Torrie LS, Thompson S, Harrison JR, Frearson JA, Read KD, Fairlamb AH, Wyatt PG, Gilbert IH.

ChemMedChem. 2012 Jan 2;7(1):95-106. doi: 10.1002/cmdc.201100420. Epub 2011 Dec 8.

44.

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.

J Med Chem. 2012 Jan 12;55(1):140-52. doi: 10.1021/jm201091t. Epub 2011 Dec 7.

45.

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.

ChemMedChem. 2011 Dec 9;6(12):2214-24. doi: 10.1002/cmdc.201100344. Epub 2011 Sep 13.

46.

Dihydroquinazolines as a novel class of Trypanosoma brucei trypanothione reductase inhibitors: discovery, synthesis, and characterization of their binding mode by protein crystallography.

Patterson S, Alphey MS, Jones DC, Shanks EJ, Street IP, Frearson JA, Wyatt PG, Gilbert IH, Fairlamb AH.

J Med Chem. 2011 Oct 13;54(19):6514-30. doi: 10.1021/jm200312v. Epub 2011 Sep 1.

47.

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.

ChemMedChem. 2011 Oct 4;6(10):1832-40. doi: 10.1002/cmdc.201100278. Epub 2011 Aug 10.

48.

Progress in neglected disease drug discovery.

Hopkins AL, Wyatt PG.

Curr Top Med Chem. 2011;11(10):1215. No abstract available.

PMID:
21401510
49.

Target validation: linking target and chemical properties to desired product profile.

Wyatt PG, Gilbert IH, Read KD, Fairlamb AH.

Curr Top Med Chem. 2011;11(10):1275-83. Review.

50.

Design, synthesis and biological evaluation of novel inhibitors of Trypanosoma brucei pteridine reductase 1.

Spinks D, Ong HB, Mpamhanga CP, Shanks EJ, Robinson DA, Collie IT, Read KD, Frearson JA, Wyatt PG, Brenk R, Fairlamb AH, Gilbert IH.

ChemMedChem. 2011 Feb 7;6(2):302-8. doi: 10.1002/cmdc.201000450. Epub 2010 Dec 29.

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