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Items: 1 to 50 of 76

1.

The relative rate of kill of the MMV Malaria Box compounds provides links to the mode of antimalarial action and highlights scaffolds of medicinal chemistry interest.

Ullah I, Sharma R, Mete A, Biagini GA, Wetzel DM, Horrocks PD.

J Antimicrob Chemother. 2019 Oct 29. pii: dkz443. doi: 10.1093/jac/dkz443. [Epub ahead of print]

PMID:
31665424
2.

Intracellular pharmacodynamic modelling (PDi) is predictive of the clinical activity of fluoroquinolones against Tuberculosis.

Donnellan S, Aljayyoussi G, Moyo E, Ardrey A, Martinez-Rodriguez C, Ward SA, Biagini GA.

Antimicrob Agents Chemother. 2019 Oct 14. pii: AAC.00989-19. doi: 10.1128/AAC.00989-19. [Epub ahead of print]

3.

Antimalarial activity of primaquine operates via a two-step biochemical relay.

Camarda G, Jirawatcharadech P, Priestley RS, Saif A, March S, Wong MHL, Leung S, Miller AB, Baker DA, Alano P, Paine MJI, Bhatia SN, O'Neill PM, Ward SA, Biagini GA.

Nat Commun. 2019 Jul 19;10(1):3226. doi: 10.1038/s41467-019-11239-0.

4.

Intracellular PD Modelling (PDi) for the Prediction of Clinical Activity of Increased Rifampicin Dosing.

Aljayyoussi G, Donnellan S, Ward SA, Biagini GA.

Pharmaceutics. 2019 Jun 13;11(6). pii: E278. doi: 10.3390/pharmaceutics11060278.

5.

Potent Antimalarial 2-Pyrazolyl Quinolone bc 1 (Qi) Inhibitors with Improved Drug-like Properties.

David Hong W, Leung SC, Amporndanai K, Davies J, Priestley RS, Nixon GL, Berry NG, Samar Hasnain S, Antonyuk S, Ward SA, Biagini GA, O'Neill PM.

ACS Med Chem Lett. 2018 Oct 19;9(12):1205-1210. doi: 10.1021/acsmedchemlett.8b00371. eCollection 2018 Dec 13.

PMID:
30613327
6.

Synthesis and profiling of benzylmorpholine 1,2,4,5-tetraoxane analogue N205: Towards tetraoxane scaffolds with potential for single dose cure of malaria.

O' Neill PM, Stocks PA, Sabbani S, Roberts NL, Amewu RK, Shore ER, Aljayyoussi G, Angulo-Barturén I, Belén M, Jiménez-Díaz, Bazaga SF, Martínez MS, Campo B, Sharma R, Charman SA, Ryan E, Chen G, Shackleford DM, Davies J, Nixon GL, Biagini GA, Ward SA.

Bioorg Med Chem. 2018 Jul 15;26(11):2996-3005. doi: 10.1016/j.bmc.2018.05.006. Epub 2018 May 17.

PMID:
29779669
7.

A tetraoxane-based antimalarial drug candidate that overcomes PfK13-C580Y dependent artemisinin resistance.

O'Neill PM, Amewu RK, Charman SA, Sabbani S, Gnädig NF, Straimer J, Fidock DA, Shore ER, Roberts NL, Wong MH, Hong WD, Pidathala C, Riley C, Murphy B, Aljayyoussi G, Gamo FJ, Sanz L, Rodrigues J, Cortes CG, Herreros E, Angulo-Barturén I, Jiménez-Díaz MB, Bazaga SF, Martínez-Martínez MS, Campo B, Sharma R, Ryan E, Shackleford DM, Campbell S, Smith DA, Wirjanata G, Noviyanti R, Price RN, Marfurt J, Palmer MJ, Copple IM, Mercer AE, Ruecker A, Delves MJ, Sinden RE, Siegl P, Davies J, Rochford R, Kocken CHM, Zeeman AM, Nixon GL, Biagini GA, Ward SA.

Nat Commun. 2017 May 24;8:15159. doi: 10.1038/ncomms15159.

8.

Pharmacokinetic-Pharmacodynamic modelling of intracellular Mycobacterium tuberculosis growth and kill rates is predictive of clinical treatment duration.

Aljayyoussi G, Jenkins VA, Sharma R, Ardrey A, Donnellan S, Ward SA, Biagini GA.

Sci Rep. 2017 Mar 29;7(1):502. doi: 10.1038/s41598-017-00529-6.

9.

Rational Design, Synthesis, and Biological Evaluation of Heterocyclic Quinolones Targeting the Respiratory Chain of Mycobacterium tuberculosis.

Hong WD, Gibbons PD, Leung SC, Amewu R, Stocks PA, Stachulski A, Horta P, Cristiano MLS, Shone AE, Moss D, Ardrey A, Sharma R, Warman AJ, Bedingfield PTP, Fisher NE, Aljayyoussi G, Mead S, Caws M, Berry NG, Ward SA, Biagini GA, O'Neill PM, Nixon GL.

J Med Chem. 2017 May 11;60(9):3703-3726. doi: 10.1021/acs.jmedchem.6b01718. Epub 2017 Apr 25.

10.

A validated bioluminescence-based assay for the rapid determination of the initial rate of kill for discovery antimalarials.

Ullah I, Sharma R, Biagini GA, Horrocks P.

J Antimicrob Chemother. 2017 Mar 1;72(3):717-726. doi: 10.1093/jac/dkw449.

PMID:
27999014
11.

Corrigendum: A Click Chemistry-Based Proteomic Approach Reveals that 1,2,4-Trioxolane and Artemisinin Antimalarials Share a Common Protein Alkylation Profile.

Ismail HM, Barton VE, Panchana M, Charoensutthivarakul S, Biagini GA, Ward SA, O'Neill PM.

Angew Chem Int Ed Engl. 2016 Aug 26;55(36):10548. doi: 10.1002/anie.201607032. No abstract available.

PMID:
27552550
12.

A Click Chemistry-Based Proteomic Approach Reveals that 1,2,4-Trioxolane and Artemisinin Antimalarials Share a Common Protein Alkylation Profile.

Ismail HM, Barton VE, Panchana M, Charoensutthivarakul S, Biagini GA, Ward SA, O'Neill PM.

Angew Chem Weinheim Bergstr Ger. 2016 May 23;128(22):6511-6515. Epub 2016 Apr 18.

13.

OptiMal-PK: an internet-based, user-friendly interface for the mathematical-based design of optimized anti-malarial treatment regimens.

Aljayyoussi G, Kay K, Ward SA, Biagini GA.

Malar J. 2016 Jul 7;15(1):344. doi: 10.1186/s12936-016-1401-8.

14.

A Click Chemistry-Based Proteomic Approach Reveals that 1,2,4-Trioxolane and Artemisinin Antimalarials Share a Common Protein Alkylation Profile.

Ismail HM, Barton VE, Panchana M, Charoensutthivarakul S, Biagini GA, Ward SA, O'Neill PM.

Angew Chem Int Ed Engl. 2016 May 23;55(22):6401-5. doi: 10.1002/anie.201512062. Epub 2016 Apr 18. Erratum in: Angew Chem Int Ed Engl. 2016 Aug 26;55(36):10548.

15.

Artemisinin activity-based probes identify multiple molecular targets within the asexual stage of the malaria parasites Plasmodium falciparum 3D7.

Ismail HM, Barton V, Phanchana M, Charoensutthivarakul S, Wong MH, Hemingway J, Biagini GA, O'Neill PM, Ward SA.

Proc Natl Acad Sci U S A. 2016 Feb 23;113(8):2080-5. doi: 10.1073/pnas.1600459113. Epub 2016 Feb 8.

16.

Carbamoyl Triazoles, Known Serine Protease Inhibitors, Are a Potent New Class of Antimalarials.

McConville M, Fernández J, Angulo-Barturen Í, Bahamontes-Rosa N, Ballell-Pages L, Castañeda P, de Cózar C, Crespo B, Guijarro L, Jiménez-Díaz MB, Martínez-Martínez MS, de Mercado J, Santos-Villarejo Á, Sanz LM, Frigerio M, Washbourn G, Ward SA, Nixon GL, Biagini GA, Berry NG, Blackman MJ, Calderón F, O'Neill PM.

J Med Chem. 2015 Aug 27;58(16):6448-55. doi: 10.1021/acs.jmedchem.5b00434. Epub 2015 Aug 17.

PMID:
26222445
17.

Antimalarial 4(1H)-pyridones bind to the Qi site of cytochrome bc1.

Capper MJ, O'Neill PM, Fisher N, Strange RW, Moss D, Ward SA, Berry NG, Lawrenson AS, Hasnain SS, Biagini GA, Antonyuk SV.

Proc Natl Acad Sci U S A. 2015 Jan 20;112(3):755-60. doi: 10.1073/pnas.1416611112. Epub 2015 Jan 6.

18.

The proliferating cell hypothesis: a metabolic framework for Plasmodium growth and development.

Salcedo-Sora JE, Caamano-Gutierrez E, Ward SA, Biagini GA.

Trends Parasitol. 2014 Apr;30(4):170-5. doi: 10.1016/j.pt.2014.02.001. Epub 2014 Mar 11. Review.

19.

Novel inhibitors of the Plasmodium falciparum electron transport chain.

Stocks PA, Barton V, Antoine T, Biagini GA, Ward SA, O'Neill PM.

Parasitology. 2014 Jan;141(1):50-65. doi: 10.1017/S0031182013001571. Review.

PMID:
24401337
20.

Rapid kill of malaria parasites by artemisinin and semi-synthetic endoperoxides involves ROS-dependent depolarization of the membrane potential.

Antoine T, Fisher N, Amewu R, O'Neill PM, Ward SA, Biagini GA.

J Antimicrob Chemother. 2014 Apr;69(4):1005-16. doi: 10.1093/jac/dkt486. Epub 2013 Dec 12.

21.

Targeting the mitochondrial electron transport chain of Plasmodium falciparum: new strategies towards the development of improved antimalarials for the elimination era.

Nixon GL, Pidathala C, Shone AE, Antoine T, Fisher N, O'Neill PM, Ward SA, Biagini GA.

Future Med Chem. 2013 Sep;5(13):1573-91. doi: 10.4155/fmc.13.121. Erratum in: Future Med Chem. 2013 Oct;5(16):2010.

22.

Structural optimization of quinolon-4(1H)-imines as dual-stage antimalarials: toward increased potency and metabolic stability.

Ressurreição AS, Gonçalves D, Sitoe AR, Albuquerque IS, Gut J, Góis A, Gonçalves LM, Bronze MR, Hanscheid T, Biagini GA, Rosenthal PJ, Prudêncio M, O'Neill P, Mota MM, Lopes F, Moreira R.

J Med Chem. 2013 Oct 10;56(19):7679-90. doi: 10.1021/jm4011466. Epub 2013 Sep 30.

PMID:
24020770
23.

Loss of pH control in Plasmodium falciparum parasites subjected to oxidative stress.

van Schalkwyk DA, Saliba KJ, Biagini GA, Bray PG, Kirk K.

PLoS One. 2013;8(3):e58933. doi: 10.1371/journal.pone.0058933. Epub 2013 Mar 11.

24.

Antimalarial pharmacology and therapeutics of atovaquone.

Nixon GL, Moss DM, Shone AE, Lalloo DG, Fisher N, O'Neill PM, Ward SA, Biagini GA.

J Antimicrob Chemother. 2013 May;68(5):977-85. doi: 10.1093/jac/dks504. Epub 2013 Jan 4. Review.

25.

Antitubercular pharmacodynamics of phenothiazines.

Warman AJ, Rito TS, Fisher NE, Moss DM, Berry NG, O'Neill PM, Ward SA, Biagini GA.

J Antimicrob Chemother. 2013 Apr;68(4):869-80. doi: 10.1093/jac/dks483. Epub 2012 Dec 9.

26.

A yeast expression system for functional and pharmacological studies of the malaria parasite Ca²⁺/H⁺ antiporter.

Salcedo-Sora JE, Ward SA, Biagini GA.

Malar J. 2012 Aug 1;11:254. doi: 10.1186/1475-2875-11-254.

27.

Generation of quinolone antimalarials targeting the Plasmodium falciparum mitochondrial respiratory chain for the treatment and prophylaxis of malaria.

Biagini GA, Fisher N, Shone AE, Mubaraki MA, Srivastava A, Hill A, Antoine T, Warman AJ, Davies J, Pidathala C, Amewu RK, Leung SC, Sharma R, Gibbons P, Hong DW, Pacorel B, Lawrenson AS, Charoensutthivarakul S, Taylor L, Berger O, Mbekeani A, Stocks PA, Nixon GL, Chadwick J, Hemingway J, Delves MJ, Sinden RE, Zeeman AM, Kocken CH, Berry NG, O'Neill PM, Ward SA.

Proc Natl Acad Sci U S A. 2012 May 22;109(21):8298-303. doi: 10.1073/pnas.1205651109. Epub 2012 May 7.

28.

HDQ, a potent inhibitor of Plasmodium falciparum proliferation, binds to the quinone reduction site of the cytochrome bc1 complex.

Vallières C, Fisher N, Antoine T, Al-Helal M, Stocks P, Berry NG, Lawrenson AS, Ward SA, O'Neill PM, Biagini GA, Meunier B.

Antimicrob Agents Chemother. 2012 Jul;56(7):3739-47. doi: 10.1128/AAC.00486-12. Epub 2012 Apr 30.

29.

Identification of novel antimalarial chemotypes via chemoinformatic compound selection methods for a high-throughput screening program against the novel malarial target, PfNDH2: increasing hit rate via virtual screening methods.

Sharma R, Lawrenson AS, Fisher NE, Warman AJ, Shone AE, Hill A, Mbekeani A, Pidathala C, Amewu RK, Leung S, Gibbons P, Hong DW, Stocks P, Nixon GL, Chadwick J, Shearer J, Gowers I, Cronk D, Parel SP, O'Neill PM, Ward SA, Biagini GA, Berry NG.

J Med Chem. 2012 Apr 12;55(7):3144-54. doi: 10.1021/jm3001482. Epub 2012 Mar 22.

30.

Identification, design and biological evaluation of heterocyclic quinolones targeting Plasmodium falciparum type II NADH:quinone oxidoreductase (PfNDH2).

Leung SC, Gibbons P, Amewu R, Nixon GL, Pidathala C, Hong WD, Pacorel B, Berry NG, Sharma R, Stocks PA, Srivastava A, Shone AE, Charoensutthivarakul S, Taylor L, Berger O, Mbekeani A, Hill A, Fisher NE, Warman AJ, Biagini GA, Ward SA, O'Neill PM.

J Med Chem. 2012 Mar 8;55(5):1844-57. doi: 10.1021/jm201184h. Epub 2012 Feb 24.

31.

Identification, design and biological evaluation of bisaryl quinolones targeting Plasmodium falciparum type II NADH:quinone oxidoreductase (PfNDH2).

Pidathala C, Amewu R, Pacorel B, Nixon GL, Gibbons P, Hong WD, Leung SC, Berry NG, Sharma R, Stocks PA, Srivastava A, Shone AE, Charoensutthivarakul S, Taylor L, Berger O, Mbekeani A, Hill A, Fisher NE, Warman AJ, Biagini GA, Ward SA, O'Neill PM.

J Med Chem. 2012 Mar 8;55(5):1831-43. doi: 10.1021/jm201179h. Epub 2012 Feb 24.

32.

Cytochrome b mutation Y268S conferring atovaquone resistance phenotype in malaria parasite results in reduced parasite bc1 catalytic turnover and protein expression.

Fisher N, Abd Majid R, Antoine T, Al-Helal M, Warman AJ, Johnson DJ, Lawrenson AS, Ranson H, O'Neill PM, Ward SA, Biagini GA.

J Biol Chem. 2012 Mar 23;287(13):9731-41. doi: 10.1074/jbc.M111.324319. Epub 2012 Jan 26.

33.

The molecular basis of folate salvage in Plasmodium falciparum: characterization of two folate transporters.

Salcedo-Sora JE, Ochong E, Beveridge S, Johnson D, Nzila A, Biagini GA, Stocks PA, O'Neill PM, Krishna S, Bray PG, Ward SA.

J Biol Chem. 2011 Dec 30;286(52):44659-68. doi: 10.1074/jbc.M111.286054. Epub 2011 Oct 13.

34.

Identification of new antimalarial leads by use of virtual screening against cytochrome bc₁.

Rodrigues T, Moreira R, Gut J, Rosenthal PJ, O Neill PM, Biagini GA, Lopes F, dos Santos DJ, Guedes RC.

Bioorg Med Chem. 2011 Nov 1;19(21):6302-8. doi: 10.1016/j.bmc.2011.09.004. Epub 2011 Sep 10.

PMID:
21958736
35.

Synthesis and antimalarial activities of a diverse set of triazole-containing furamidine analogues.

Berger O, Kaniti A, van Ba CT, Vial H, Ward SA, Biagini GA, Bray PG, O'Neill PM.

ChemMedChem. 2011 Nov 4;6(11):2094-108. doi: 10.1002/cmdc.201100265. Epub 2011 Sep 8.

PMID:
21905228
36.

Endoperoxide carbonyl falcipain 2/3 inhibitor hybrids: toward combination chemotherapy of malaria through a single chemical entity.

Gibbons P, Verissimo E, Araujo NC, Barton V, Nixon GL, Amewu RK, Chadwick J, Stocks PA, Biagini GA, Srivastava A, Rosenthal PJ, Gut J, Guedes RC, Moreira R, Sharma R, Berry N, Cristiano ML, Shone AE, Ward SA, O'Neill PM.

J Med Chem. 2010 Nov 25;53(22):8202-6. doi: 10.1021/jm1009567. Epub 2010 Oct 27.

PMID:
20979352
37.

Inhibiting Plasmodium cytochrome bc1: a complex issue.

Barton V, Fisher N, Biagini GA, Ward SA, O'Neill PM.

Curr Opin Chem Biol. 2010 Aug;14(4):440-6. doi: 10.1016/j.cbpa.2010.05.005. Review.

PMID:
20570550
38.

Discovery of potent small-molecule inhibitors of multidrug-resistant Plasmodium falciparum using a novel miniaturized high-throughput luciferase-based assay.

Lucumi E, Darling C, Jo H, Napper AD, Chandramohanadas R, Fisher N, Shone AE, Jing H, Ward SA, Biagini GA, DeGrado WF, Diamond SL, Greenbaum DC.

Antimicrob Agents Chemother. 2010 Sep;54(9):3597-604. doi: 10.1128/AAC.00431-10. Epub 2010 Jun 14.

39.

An acid-loading chloride transport pathway in the intraerythrocytic malaria parasite, Plasmodium falciparum.

Henry RI, Cobbold SA, Allen RJ, Khan A, Hayward R, Lehane AM, Bray PG, Howitt SM, Biagini GA, Saliba KJ, Kirk K.

J Biol Chem. 2010 Jun 11;285(24):18615-26. doi: 10.1074/jbc.M110.120980. Epub 2010 Mar 23.

40.

Transforming rhinacanthin analogues from potent anticancer agents into potent antimalarial agents.

Kongkathip N, Pradidphol N, Hasitapan K, Grigg R, Kao WC, Hunte C, Fisher N, Warman AJ, Biagini GA, Kongsaeree P, Chuawong P, Kongkathip B.

J Med Chem. 2010 Feb 11;53(3):1211-21. doi: 10.1021/jm901545z.

PMID:
20067272
41.

Continued cytoadherence of Plasmodium falciparum infected red blood cells after antimalarial treatment.

Hughes KR, Biagini GA, Craig AG.

Mol Biochem Parasitol. 2010 Feb;169(2):71-8. doi: 10.1016/j.molbiopara.2009.09.007. Epub 2009 Oct 1.

42.

Chapter 17 Type II NADH: quinone oxidoreductases of Plasmodium falciparum and Mycobacterium tuberculosis kinetic and high-throughput assays.

Fisher N, Warman AJ, Ward SA, Biagini GA.

Methods Enzymol. 2009;456:303-20. doi: 10.1016/S0076-6879(08)04417-0.

PMID:
19348896
43.

Glycerol: an unexpected major metabolite of energy metabolism by the human malaria parasite.

Lian LY, Al-Helal M, Roslaini AM, Fisher N, Bray PG, Ward SA, Biagini GA.

Malar J. 2009 Mar 6;8:38. doi: 10.1186/1475-2875-8-38.

44.

Candidate selection and preclinical evaluation of N-tert-butyl isoquine (GSK369796), an affordable and effective 4-aminoquinoline antimalarial for the 21st century.

O'Neill PM, Park BK, Shone AE, Maggs JL, Roberts P, Stocks PA, Biagini GA, Bray PG, Gibbons P, Berry N, Winstanley PA, Mukhtar A, Bonar-Law R, Hindley S, Bambal RB, Davis CB, Bates M, Hart TK, Gresham SL, Lawrence RM, Brigandi RA, Gomez-delas-Heras FM, Gargallo DV, Ward SA.

J Med Chem. 2009 Mar 12;52(5):1408-15. doi: 10.1021/jm8012618.

PMID:
19222165
45.

Open-label comparative clinical study of chlorproguanil-dapsone fixed dose combination (Lapdap) alone or with three different doses of artesunate for uncomplicated Plasmodium falciparum malaria.

Wootton DG, Opara H, Biagini GA, Kanjala MK, Duparc S, Kirby PL, Woessner M, Neate C, Nyirenda M, Blencowe H, Dube-Mbeye Q, Kanyok T, Ward S, Molyneux M, Dunyo S, Winstanley PA.

PLoS One. 2008 Mar 5;3(3):e1779. doi: 10.1371/journal.pone.0001779.

46.

Acridinediones: selective and potent inhibitors of the malaria parasite mitochondrial bc1 complex.

Biagini GA, Fisher N, Berry N, Stocks PA, Meunier B, Williams DP, Bonar-Law R, Bray PG, Owen A, O'Neill PM, Ward SA.

Mol Pharmacol. 2008 May;73(5):1347-55. doi: 10.1124/mol.108.045120. Epub 2008 Mar 4.

PMID:
18319379
47.

A comprehensive model of purine uptake by the malaria parasite Plasmodium falciparum: identification of four purine transport activities in intraerythrocytic parasites.

Quashie NB, Dorin-Semblat D, Bray PG, Biagini GA, Doerig C, Ranford-Cartwright LC, De Koning HP.

Biochem J. 2008 Apr 15;411(2):287-95. doi: 10.1042/BJ20071460.

PMID:
18215139
48.

Malaria-parasite mitochondrial dehydrogenases as drug targets: too early to write the obituary.

Fisher N, Bray PG, Ward SA, Biagini GA.

Trends Parasitol. 2008 Jan;24(1):9-10. Epub 2007 Nov 19. No abstract available.

PMID:
18024199
49.

Evidence for a common non-heme chelatable-iron-dependent activation mechanism for semisynthetic and synthetic endoperoxide antimalarial drugs.

Stocks PA, Bray PG, Barton VE, Al-Helal M, Jones M, Araujo NC, Gibbons P, Ward SA, Hughes RH, Biagini GA, Davies J, Amewu R, Mercer AE, Ellis G, O'Neill PM.

Angew Chem Int Ed Engl. 2007;46(33):6278-83. No abstract available.

PMID:
17640025
50.

The malaria parasite type II NADH:quinone oxidoreductase: an alternative enzyme for an alternative lifestyle.

Fisher N, Bray PG, Ward SA, Biagini GA.

Trends Parasitol. 2007 Jul;23(7):305-10. Epub 2007 May 10.

PMID:
17499024

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