A new Set of chemical starting points with Plasmodium falciparum transmission-blocking potential for antimalarial drug discovery

PLoS ONE

Volumn 10, Issue 8, 2015, Pages

  Almela, Maria Jesus ^a,b   Lozano, Sonia ^a   Lelièvre, Joël ^a   Colmenarejo, Gonzalo ^a   Coterón, José Miguel ^a   Rodrigues, Janneth ^a   Gonzalez, Carolina ^a   Herreros, Esperanza ^a  

^a GLAXOSMITHKLINE   (Spain)

^b UNIVERSIDAD NACIONAL DE EDUCACIÓN A DISTANCIA   (Spain)

Author keywords

[No Author keywords available]

Indexed keywords

ANTIMALARIAL AGENT; MOLECULAR LIBRARY;

ANTIMALARIAL ACTIVITY; ARTICLE; ASEXUAL REPRODUCTION; CLUSTER ANALYSIS; CYTOTOXICITY ASSAY; DRUG IDENTIFICATION; DRUG RESEARCH; DRUG SCREENING; DRUG STRUCTURE; EX VIVO STUDY; GAMETOCYTE; GENET (CLONE); HEPG2 CELL LINE; HUMAN; HUMAN CELL; MALARIA CONTROL; NONHUMAN; PHYSICAL CHEMISTRY; PLASMODIUM FALCIPARUM; STRUCTURE ANALYSIS; DRUG DEVELOPMENT; DRUG EFFECTS; DRUG SENSITIVITY; HIGH THROUGHPUT SCREENING; IC50; LUMINESCENCE; MALARIA, FALCIPARUM; MOLECULAR LIBRARY; PRECLINICAL STUDY; PROCEDURES; REPRODUCIBILITY; TRANSMISSION;

ANTIMALARIALS; DRUG DISCOVERY; DRUG EVALUATION, PRECLINICAL; HIGH-THROUGHPUT SCREENING ASSAYS; HUMANS; INHIBITORY CONCENTRATION 50; LUMINESCENT MEASUREMENTS; MALARIA, FALCIPARUM; PARASITIC SENSITIVITY TESTS; PLASMODIUM FALCIPARUM; REPRODUCIBILITY OF RESULTS; SMALL MOLECULE LIBRARIES;

EID: 84943338940     PISSN: None     EISSN: 19326203     Source Type: Journal    
DOI: 10.1371/journal.pone.0135139     Document Type: Article

References (33)

1. World Health Organization. World Malaria Report 2014: WHO Press; 2014 [cited 2015 March]. Available: http://www.who.int/malaria/publications/world-malaria-report-2014/en/.
2. Noedl H, Se Y, Schaecher K, Smith BL, Socheat D, Fukuda MM, et al. Evidence of artemisinin-resistant malaria in western Cambodia. N Engl J Med. 2008;359(24):2619-20. doi: 10.1056/NEJMc0805011 PMID: 19064625.
3. Ashley EA, Dhorda M, Fairhurst RM, Amaratunga C, Lim P, Suon S, et al. Spread of artemisinin resistance in Plasmodium falciparum malaria. N Engl J Med. 2014;371(5):411-23. doi: 10.1056/NEJMoa1314981 PMID: 25075834; PubMed Central PMCID: PMC4143591.
4. Guiguemde WA, Shelat AA, Bouck D, Duffy S, Crowther GJ, Davis PH, et al. Chemical genetics of Plasmodium falciparum. Nature. 2010;465(7296):311-5. doi: 10.1038/nature09099 PMID: 20485428; PubMed Central PMCID: PMC2874979.
5. Plouffe D, Brinker A, McNamara C, Henson K, Kato N, Kuhen K, et al. In silico activity profiling reveals the mechanism of action of antimalarials discovered in a high-throughput screen. Proceedings of the National Academy of Sciences of the United States of America. 2008;105(26):9059-64. doi: 10.1073/pnas.0802982105 PMID: 18579783; PubMed Central PMCID: PMC2440361.
6. Gamo FJ, Sanz LM, Vidal J, de Cozar C, Alvarez E, Lavandera JL, et al. Thousands of chemical starting points for antimalarial lead identification. Nature. 2010;465(7296):305-10. doi: 10.1038/nature09107 PMID: 20485427.
7. Calderon F, Barros D, Bueno JM, Coteron JM, Fernandez E, Gamo FJ, et al. An invitation to open innovation in malaria drug discovery: 47 quality starting points from the TCAMS. ACS Med Chem Lett. 2011;2(10):741-6. doi: 10.1021/ml200135p PMID: 24900261; PubMed Central PMCID: PMC4018116.
8. Wells TN, Alonso PL, Gutteridge WE. New medicines to improve control and contribute to the eradication of malaria. Nat Rev Drug Discov. 2009;8(11):879-91. doi: 10.1038/nrd2972 PMID: 19834482.
9. Smith TG, Lourenco P, Carter R, Walliker D, Ranford-Cartwright LC. Commitment to sexual differentiation in the human malaria parasite, Plasmodium falciparum. Parasitology. 2000;121(Pt 2):127-33. PMID: 11085232.
10. Lelievre J, Almela MJ, Lozano S, Miguel C, Franco V, Leroy D, et al. Activity of clinically relevant antimalarial drugs on Plasmodium falciparum mature gametocytes in an ATP bioluminescence "transmission blocking" assay. PLoS One. 2012;7(4):e35019. doi: 10.1371/journal.pone.0035019 PMID: 22514702; PubMed Central PMCID: PMC3325938.
11. Lucantoni L, Duffy S, Adjalley SH, Fidock DA, Avery VM. Identification of MMV malaria box inhibitors of Plasmodium falciparum early-stage gametocytes using a luciferase-based high-throughput assay. Antimicrob Agents Chemother. 2013;57(12):6050-62. doi: 10.1128/AAC.00870-13 PMID: 24060871; PubMed Central PMCID: PMC3837862.
12. Duffy S, Avery VM. Identification of inhibitors of Plasmodium falciparum gametocyte development. Malar J. 2013;12:408. doi: 10.1186/1475-2875-12-408 PMID: 24206914; PubMed Central PMCID: PMC3842684.
13. D'Alessandro S, Silvestrini F, Dechering K, Corbett Y, Parapini S, Timmerman M, et al. A Plasmodium falciparum screening assay for anti-gametocyte drugs based on parasite lactate dehydrogenase detection. J Antimicrob Chemother. 2013;68(9):2048-58. doi: 10.1093/jac/dkt165 PMID: 23645588.
14. Bowman JD, Merino EF, Brooks CF, Striepen B, Carlier PR, Cassera MB. Antiapicoplast and gametocytocidal screening to identify the mechanisms of action of compounds within the malaria box. Antimicrob Agents Chemother. 2014;58(2):811-9. doi: 10.1128/AAC.01500-13 PMID: 24247137; PubMed Central PMCID: PMC3910863.
15. Sanders NG, Sullivan DJ, Mlambo G, Dimopoulos G, Tripathi AK. Gametocytocidal screen identifies novel chemical classes with Plasmodium falciparum transmission blocking activity. PLoS One. 2014;9(8):e105817. doi: 10.1371/journal.pone.0105817 PMID: 25157792; PubMed Central PMCID: PMC4144897.
16. Ruecker A, Mathias DK, Straschil U, Churcher TS, Dinglasan RR, Leroy D, et al. A male and female gametocyte functional viability assay to identify biologically relevant malaria transmission-blocking drugs. Antimicrob Agents Chemother. 2014;58(12):7292-302. doi: 10.1128/AAC.03666-14 PMID: 25267664.
17. Cree IA, Andreotti PE. Measurement of cytotoxicity by ATP-based luminescence assay in primary cell cultures and cell lines. Toxicology in Vitro. 1997;11(5):553-6. doi: 10.1016/S0887-2333 (97) 00060-X PMID: 20654351
18. Kangas L, Gronroos M, Nieminen AL. Bioluminescence of cellular ATP: a new method for evaluating cytotoxic agents in vitro. Med Biol. 1984;62(6):338-43. Epub 1984/01/01. PMID: 6543460.
19. Drug Discovery Through High-Throughput Screening Technique. General Chemicals; [cited 2015 March]. General Chemicals. Available: http://www.worldofchemicals.com/15/chemistry-articles/rapidleadcompounds-discovery-through-high-throughput-screening.html.
20. Crowther GJ, Napuli AJ, Gilligan JH, Gagaring K, Borboa R, Francek C, et al. Identification of inhibitors for putative malaria drug targets among novel antimalarial compounds. Mol Biochem Parasitol. 2011;175(1):21-9. doi: 10.1016/j.molbiopara.2010.08.005 PMID: 20813141; PubMed Central PMCID: PMC3108854.
21. Flannery EL, Chatterjee AK, Winzeler EA. Antimalarial drug discovery-approaches and progress towards new medicines. Nat Rev Microbiol. 2013;11(12):849-62. doi: 10.1038/nrmicro3138 PMID: 24217412; PubMed Central PMCID: PMC3941073.
22. Avery VM, Bashyam S, Burrows JN, Duffy S, Papadatos G, Puthukkuti S, et al. Screening and hit evaluation of a chemical library against blood-stage Plasmodium falciparum. Malar J. 2014;13:190. doi: 10. 1186/1475-2875-13-190 PMID: 24886460; PubMed Central PMCID: PMC4094919.
23. Vaidya AB, Morrisey JM, Zhang Z, Das S, Daly TM, Otto TD, et al. Pyrazoleamide compounds are potent antimalarials that target Na+ homeostasis in intraerythrocytic Plasmodium falciparum. Nature communications. 2014;5:5521. doi: 10.1038/ncomms6521 PMID: 25422853; PubMed Central PMCID: PMC4263321.
24. Jimenez-Diaz MB, Ebert D, Salinas Y, Pradhan A, Lehane AM, Myrand-Lapierre ME, et al. (+)-SJ733, a clinical candidate for malaria that acts through ATP4 to induce rapid host-mediated clearance of Plasmodium. Proceedings of the National Academy of Sciences of the United States of America. 2014;111(50):E5455-62. doi: 10.1073/pnas.1414221111 PMID: 25453091; PubMed Central PMCID: PMC4273362.
25. Prole DL, Marrion NV. Identification of putative potassium channel homologues in pathogenic protozoa. PLoS One. 2012;7(2):e32264. doi: 10.1371/journal.pone.0032264 PMID: 22363819; PubMed Central PMCID: PMC3283738.
26. Fredriksson R, Schioth HB. The repertoire of G-protein-coupled receptors in fully sequenced genomes. Mol Pharmacol. 2005;67(5):1414-25. PMID: 15687224.
27. Open access Malaria Box. Medicines for Malaria Venture; 2015 [cited 2015 June]. Available: http://www.mmv.org/malariabox.
28. Trager W, Jensen JB. Human malaria parasites in continuous culture. Science. 1976;193(4254):673-5. PMID: 781840.
29. Van Huyssen W, Rieckmann KH. Disposable environmental chamber for assessing the drug susceptibility of malaria parasites. Trop Med Parasitol. 1993;44(4):329-30. PMID: 8134776.
30. Miret S, De Groene EM, Klaffke W. Comparison of in vitro assays of cellular toxicity in the human hepatic cell line HepG2. J Biomol Screen. 2006;11(2):184-93. doi: 10.1177/1087057105283787 PMID: 16314402.
31. Wetzel S, Klein K, Renner S, Rauh D, Oprea TI, Mutzel P, et al. Interactive exploration of chemical space with Scaffold Hunter. Nat Chem Biol. 2009;5(8):581-3. doi: 10.1038/nchembio.187 PMID: 19561620.
32. RDKit: Cheminformatics and Machine Learning Software. Sourceforge; 2014 [cited 2014 July]. Available: http://www.rdkit.org.
33. Delves MJ, Ruecker A, Straschil U, Lelievre J, Marques S, Lopez-Barragan MJ, et al. Male and female Plasmodium falciparum mature gametocytes show different responses to antimalarial drugs. Antimicrob Agents Chemother. 2013;57(7):3268-74. doi: 10.1128/AAC.00325-13 PMID: 23629698; PubMed Central PMCID: PMC3697345.