Know your enemy: Understanding the role of PfCRT in drug resistance could lead to new antimalarial tactics

Cellular and Molecular Life Sciences

Volumn 69, Issue 12, 2012, Pages 1967-1995

  Summers, Robert L ^a   Nash, Megan N ^a   Martin, Rowena E ^a,b  

^a AUSTRALIAN NATIONAL UNIVERSITY   (Australia)

^b UNIVERSITY OF MELBOURNE   (Australia)

Author keywords

Chloroquine; Drug resistance; Malaria; PfCRT; Plasmodium falciparum; Quinoline

Indexed keywords

ABC TRANSPORTER; AMODIAQUINE; AMODIAQUINE PLUS ARTESUNATE; ANTIMALARIAL AGENT; ARTEMETHER; ARTEMETHER PLUS BENFLUMETOL; ARTESUNATE; ARTESUNATE PLUS PYRIMETHAMINE PLUS SULFADOXINE; BENFLUMETOL; CARRIER PROTEINS AND BINDING PROTEINS; CHLOROQUINE; CHLOROQUINE RESISTANCE TRANSPORTER; DIHYDROARTEMISININ PLUS PIPERAQUINE; FERROQUINE; HALOFANTRINE; MEFLOQUINE; MEPACRINE; MULTIDRUG RESISTANCE PROTEIN 1; PIPERAQUINE; PRIMAQUINE; PYRONARIDINE; QUININE; QUINOLINE DERIVED ANTIINFECTIVE AGENT; UNCLASSIFIED DRUG;

ABDOMINAL PAIN; ANTIMALARIAL ACTIVITY; ANTIMALARIAL DRUG RESISTANCE; BINDING SITE; COMBINATION CHEMOTHERAPY; DELIRIUM; DIARRHEA; DOSE RESPONSE; DRUG ACTIVITY; DRUG EFFICACY; DRUG MEGADOSE; DRUG POTENTIATION; DRUG PROTEIN BINDING; DRUG TARGETING; DRUG TOLERABILITY; GENE; HUMAN; IC 50; MALARIA; MONOTHERAPY; MULTIPLE CYCLE TREATMENT; NAUSEA; NONHUMAN; NUCLEOTIDE SEQUENCE; OUTCOME ASSESSMENT; PFCRT GENE; PHARMACODYNAMICS; PLASMODIUM FALCIPARUM; PROTEIN BINDING; PROTEIN FUNCTION; PRURITUS; REVIEW; STRUCTURE ACTIVITY RELATION; VOMITING;

ANIMALS; ANTIMALARIALS; CHLOROQUINE; DRUG RESISTANCE; HUMANS; MALARIA, FALCIPARUM; MEMBRANE TRANSPORT PROTEINS; MICE; MUTATION; PLASMODIUM FALCIPARUM; PROTOZOAN PROTEINS; QUINOLINES;

PLASMODIUM FALCIPARUM;

EID: 84862889731     PISSN: 1420682X     EISSN: 14209071     Source Type: Journal    
DOI: 10.1007/s00018-011-0906-0     Document Type: Review

References (232)

1. WHO (2010) World malaria report 2010
2. J Sachs P Malaney 2002 The economic and social burden of malaria Nature 415 6872 680 685 11832956 1:CAS:528:DC%2BD38XhsVCjtrY%3D 10.1038/415680a (Pubitemid 34136401)
3. JL Gallup JD Sachs 2001 The economic burden of malaria Am J Trop Med Hyg 64 1-2 Suppl 85 96 11425181 1:STN:280:DC%2BD3MzmsVOjug%3D%3D (Pubitemid 32552575)
4. PA Holding RW Snow 2001 Impact of Plasmodium falciparum malaria on performance and learning: review of the evidence Am J Trop Med Hyg 64 1-2 Suppl 68 75 11425179 1:STN:280:DC%2BD3MzmsVOjtA%3D%3D (Pubitemid 32552573)
5. SC Murphy JG Breman 2001 Gaps in the childhood malaria burden in Africa: cerebral malaria, neurological sequelae, anemia, respiratory distress, hypoglycemia, and complications of pregnancy Am J Trop Med Hyg 64 1-2 Suppl 57 67 11425178 1:STN:280:DC%2BD3MzmsVOjtw%3D%3D (Pubitemid 32552572)
6. PJ Guerin P Olliaro F Nosten P Druilhe R Laxminarayan F Binka WL Kilama N Ford NJ White 2002 Malaria: current status of control, diagnosis, treatment, and a proposed agenda for research and development Lancet Infect Dis 2 9 564 573 12206972 10.1016/S1473-3099(02)00372-9 (Pubitemid 34966359)
7. K Kirk 2001 Membrane transport in the malaria-infected erythrocyte Physiol Rev 81 2 495 537 11274338 1:CAS:528:DC%2BD3MXislCrsLs%3D (Pubitemid 32267072)
8. D Greenwood 1992 The quinine connection J Antimicrob Chemother 30 4 417 427 1490916 1:CAS:528:DyaK38XmsFSlt7s%3D 10.1093/jac/30.4.417
9. Meshnick SR, Dobson MJ (2001) The history of antimalarial drugs. In: Rosenthal PJ (ed) Antimalarial chemotherapy: mechanisms of action resistance and new directions in drug discovery. Humana Press, Totowa, pp 15-25
10. CH Sibley JE Hyde PF Sims CV Plowe JG Kublin EK Mberu AF Cowman PA Winstanley WM Watkins AM Nzila 2001 Pyrimethamine-sulfadoxine resistance in Plasmodium falciparum: what next? Trends Parasitol 17 12 582 588 11756042 1:CAS:528:DC%2BD38XksF2rsA%3D%3D 10.1016/S1471-4922(01)02085-2 (Pubitemid 34088118)
11. VI Carrara J Zwang EA Ashley RN Price K Stepniewska M Barends A Brockman T Anderson R McGready L Phaiphun S Proux M van Vugt R Hutagalung KM Lwin AP Phyo P Preechapornkul M Imwong S Pukrittayakamee P Singhasivanon NJ White F Nosten 2009 Changes in the treatment responses to artesunate-mefloquine on the northwestern border of Thailand during 13 years of continuous deployment PLoS ONE 4 2 e4551 19234601 10.1371/journal.pone.0004551 1:CAS:528: DC%2BD1MXis1Knu7c%3D
12. AM Dondorp S Yeung L White C Nguon NP Day D Socheat L von Seidlein 2010 Artemisinin resistance: current status and scenarios for containment Nat Rev Microbiol 8 4 272 280 20208550 1:CAS:528:DC%2BC3cXivVKjsr0%3D
13. K Na-Bangchang R Ruengweerayut P Mahamad K Ruengweerayut W Chaijaroenkul 2010 Declining in efficacy of a three-day combination regimen of mefloquine-artesunate in a multi-drug resistance area along the Thai-Myanmar border Malar J 9 273 20929590 10.1186/1475-2875-9-273 1:CAS:528: DC%2BC3cXhtlSisb%2FM
14. WO Rogers R Sem T Tero P Chim P Lim S Muth D Socheat F Ariey C Wongsrichanalai 2009 Failure of artesunate-mefloquine combination therapy for uncomplicated Plasmodium falciparum malaria in southern Cambodia Malar J 8 10 19138388 10.1186/1475-2875-8-10 1:CAS:528:DC%2BD1MXlt1ahsrY%3D
15. WHO (2011) Update on artemisinin resistance-September 2011
16. R Hayward KJ Saliba K Kirk 2006 The pH of the digestive vacuole of Plasmodium falciparum is not associated with chloroquine resistance J Cell Sci 119 Pt 6 1016 1025 16492710 1:CAS:528:DC%2BD28Xjs1yrsbY%3D 10.1242/jcs.02795
17. N Klonis O Tan K Jackson D Goldberg M Klemba L Tilley 2007 Evaluation of pH during cytostomal endocytosis and vacuolar catabolism of haemoglobin in Plasmodium falciparum Biochem J 407 3 343 354 17696875 1:CAS:528: DC%2BD2sXhtFGgs7vO 10.1042/BJ20070934 (Pubitemid 350058468)
18. Y Kuhn P Rohrbach M Lanzer 2007 Quantitative pH measurements in Plasmodium falciparum-infected erythrocytes using pHluorin Cell Microbiol 9 4 1004 1013 17381432 1:CAS:528:DC%2BD2sXktFCmsbw%3D 10.1111/j.1462-5822.2006. 00847.x (Pubitemid 46394910)
19. A Yayon 1985 The antimalarial mode of action of chloroquine Rev Clin Basic Pharm 5 1-2 99 139 3916306 1:CAS:528:DyaL28Xht1agsbs%3D (Pubitemid 16024490)
20. PG Bray M Mungthin IM Hastings GA Biagini DK Saidu V Lakshmanan DJ Johnson RH Hughes PA Stocks PM O'Neill DA Fidock DC Warhurst SA Ward 2006 PfCRT and the trans-vacuolar proton electrochemical gradient: regulating the access of chloroquine to ferriprotoporphyrin IX Mol Microbiol 62 1 238 251 16956382 1:CAS:528:DC%2BD28XhtFWgsLnP 10.1111/j.1365-2958.2006.05368.x (Pubitemid 44386563)
21. TJ Egan 2006 Chloroquine and primaquine: combining old drugs as a new weapon against falciparum malaria? Trends Parasitol 22 6 235 237 16580880 1:CAS:528:DC%2BD28XlvF2lt7Y%3D 10.1016/j.pt.2006.03.006 (Pubitemid 43884905)
22. S Auparakkitanon S Chapoomram K Kuaha T Chirachariyavej P Wilairat 2006 Targeting of hematin by the antimalarial pyronaridine Antimicrob Agents Chemother 50 6 2197 2200 16723583 1:CAS:528:DC%2BD28XlsVOiu70%3D 10.1128/AAC.00119-06 (Pubitemid 43807543)
23. TME Davis TY Hung IK Sim HA Karunajeewa KF Ilett 2005 Piperaquine-a resurgent antimalarial drug Drugs 65 1 75 87 15610051 1:CAS:528: DC%2BD2MXhs1WmtL8%3D 10.2165/00003495-200565010-00004
24. CD Fitch 2004 Ferriprotoporphyrin IX, phospholipids, and the antimalarial actions of quinoline drugs Life Sci 74 16 1957 1972 14967191 1:CAS:528:DC%2BD2cXht1yqt78%3D 10.1016/j.lfs.2003.10.003 (Pubitemid 38210349)
25. M Foley L Tilley 1998 Quinoline antimalarials: mechanisms of action and resistance and prospects for new agents Pharmacol Ther 79 1 55 87 9719345 1:CAS:528:DyaK1cXjvFKjs7k%3D 10.1016/S0163-7258(98)00012-6 (Pubitemid 28318262)
26. SR Hawley PG Bray M Mungthin JD Atkinson PM O'Neill SA Ward 1998 Relationship between antimalarial drug activity, accumulation, and inhibition of heme polymerization in Plasmodium falciparum in vitro Antimicrob Agents Chemother 42 3 682 686 9517951 1:CAS:528:DyaK1cXhvV2ktbg%3D (Pubitemid 28114827)
27. M Mungthin PG Bray RG Ridley SA Ward 1998 Central role of hemoglobin degradation in mechanisms of action of 4-aminoquinolines, quinoline methanols, and phenanthrene methanols Antimicrob Agents Chemother 42 11 2973 2977 9797235 1:CAS:528:DyaK1cXnt1Sju7Y%3D (Pubitemid 28501235)
28. AC Chou R Chevli CD Fitch 1980 Ferriprotoporphyrin IX fulfills the criteria for identification as the chloroquine receptor of malaria parasites Biochemistry 19 8 1543 1549 6990976 1:STN:280:DyaL3c7pvVaktw%3D%3D 10.1021/bi00549a600 (Pubitemid 10088203)
29. KA de Villiers HM Marques TJ Egan 2008 The crystal structure of halofantrine-ferriprotoporphyrin IX and the mechanism of action of arylmethanol antimalarials J Inorg Biochem 102 8 1660 1667 18508124 10.1016/j.jinorgbio.2008. 04.001 1:CAS:528:DC%2BD1cXosVylsrw%3D
30. CD Fitch 1969 Chloroquine resistance in malaria: a deficiency of chloroquine binding Proc Natl Acad Sci USA 64 4 1181 1187 5271747 1:CAS:528:DyaE3cXns1SmsQ%3D%3D 10.1073/pnas.64.4.1181
31. DJ Krogstad IY Gluzman DE Kyle AM Oduola SK Martin WK Milhous PH Schlesinger 1987 Efflux of chloroquine from Plasmodium falciparum: mechanism of chloroquine resistance Science 238 4831 1283 1285 3317830 1:CAS:528: DyaL1cXlt1KmtQ%3D%3D 10.1126/science.3317830
32. SK Martin AM Oduola WK Milhous 1987 Reversal of chloroquine resistance in Plasmodium falciparum by verapamil Science 235 4791 899 901 3544220 1:CAS:528:DyaL2sXhtlWgs74%3D 10.1126/science.3544220 (Pubitemid 17019130)
33. G Watt GW Long M Grogl SK Martin 1990 Reversal of drug-resistant falciparum malaria by calcium antagonists: potential for host cell toxicity Trans R Soc Trop Med Hyg 84 2 187 190 1975136 1:STN:280:DyaK3czlslensQ%3D%3D 10.1016/0035-9203(90)90248-D (Pubitemid 20171998)
34. TE Wellems A Walker-Jonah LJ Panton 1991 Genetic mapping of the chloroquine-resistance locus on Plasmodium falciparum chromosome 7 Proc Natl Acad Sci USA 88 8 3382 3386 1673031 1:CAS:528:DyaK3MXisVWrsb4%3D 10.1073/pnas.88.8.3382 (Pubitemid 21916625)
35. Su X, Kirkman LA, Fujioka H, Wellems TE (1997) Complex polymorphisms in an approximately 330 kDa protein are linked to chloroquine-resistant P. falciparum in Southeast Asia and Africa. Cell 91(5):593-603 (Pubitemid 27513651)
36. Fidock DA, Nomura T, Talley AK, Cooper RA, Dzekunov SM, Ferdig MT, Ursos LM, Sidhu AB, Naude B, Deitsch KW, Su XZ, Wootton JC, Roepe PD, Wellems TE (2000) Mutations in the P. falciparum digestive vacuole transmembrane protein PfCRT and evidence for their role in chloroquine resistance. Mol Cell 6(4):861-871
37. AB Sidhu D Verdier-Pinard DA Fidock 2002 Chloroquine resistance in Plasmodium falciparum malaria parasites conferred by pfcrt mutations Science 298 5591 210 213 12364805 1:CAS:528:DC%2BD38XnsFSgs70%3D 10.1126/science.1074045
38. RE Martin K Kirk 2004 The malaria parasite's chloroquine resistance transporter is a member of the drug/metabolite transporter superfamily Mol Biol Evol 21 10 1938 1949 15240840 1:CAS:528:DC%2BD2cXnvFeju7k%3D 10.1093/molbev/msh205 (Pubitemid 39331640)
39. Y Kuhn CP Sanchez D Ayoub T Saridaki A van Dorsselaer M Lanzer 2010 Trafficking of the phosphoprotein PfCRT to the digestive vacuolar membrane in Plasmodium falciparum Traffic 11 2 236 249 20015114 1:CAS:528: DC%2BC3cXhtVahu78%3D 10.1111/j.1600-0854.2009.01018.x
40. V Lakshmanan PG Bray D Verdier-Pinard DJ Johnson P Horrocks RA Muhle GE Alakpa RH Hughes SA Ward DJ Krogstad AB Sidhu DA Fidock 2005 A critical role for PfCRT K76T in Plasmodium falciparum verapamil-reversible chloroquine resistance EMBO J 24 13 2294 2305 15944738 1:CAS:528:DC%2BD2MXlvVWqsLc%3D 10.1038/sj.emboj.7600681 (Pubitemid 41032582)
41. W Chaijaroenkul SA Ward M Mungthin D Johnson A Owen PG Bray K Na-Bangchang 2011 Sequence and gene expression of chloroquine resistance transporter (pfcrt) in the association of in vitro drugs resistance of Plasmodium falciparum Malar J 10 1 42 21320353 1:CAS:528:DC%2BC3MXislChur8%3D 10.1186/1475-2875-10-42
42. CP Sanchez A Dave WD Stein M Lanzer 2010 Transporters as mediators of drug resistance in Plasmodium falciparum Int J Parasitol 40 10 1109 1118 20399785 1:CAS:528:DC%2BC3cXotVWqu7o%3D 10.1016/j.ijpara.2010.04.001
43. RL Summers RE Martin 2010 Functional characteristics of the malaria parasite's "chloroquine resistance transporter": implications for chemotherapy Virulence 1 4 304 308 21178460 10.4161/viru.1.4.12012
44. CP Sanchez JE McLean P Rohrbach DA Fidock WD Stein M Lanzer 2005 Evidence for a pfcrt-associated chloroquine efflux system in the human malarial parasite Plasmodium falciparum Biochemistry 44 29 9862 9870 16026158 1:CAS:528:DC%2BD2MXlsF2mtL4%3D 10.1021/bi050061f (Pubitemid 41033452)
45. CP Sanchez P Rohrbach JE McLean DA Fidock WD Stein M Lanzer 2007 Differences in trans-stimulated chloroquine efflux kinetics are linked to PfCRT in Plasmodium falciparum Mol Microbiol 64 2 407 420 17493125 1:CAS:528:DC%2BD2sXltlamurc%3D 10.1111/j.1365-2958.2007.05664.x (Pubitemid 46632624)
46. + leak from the digestive vacuole in chloroquine-resistant malaria parasites J Cell Sci 121 1624 1632 18445688 1:CAS:528:DC%2BD1cXotVyiurw%3D 10.1242/jcs.016758 (Pubitemid 351911819)
47. AM Lehane K Kirk 2008 Chloroquine resistance-conferring mutations in pfcrt give rise to a chloroquine-associated H + leak from the malaria parasite's digestive vacuole Antimicrob Agents Chemother 52 12 4374 4380 18852275 1:CAS:528:DC%2BD1cXhsV2mu77O 10.1128/AAC.00666-08
48. B Naude JA Brzostowski AR Kimmel TE Wellems 2005 Dictyostelium discoideum expresses a malaria chloroquine resistance mechanism upon transfection with mutant, but not wild-type, Plasmodium falciparum transporter PfCRT J Biol Chem 280 27 25596 25603 15883156 1:CAS:528:DC%2BD2MXlslylu7s%3D 10.1074/jbc. M503227200 (Pubitemid 40962267)
49. RE Martin RV Marchetti AI Cowan SM Howitt S Bröer K Kirk 2009 Chloroquine transport via the malaria parasite's chloroquine resistance transporter Science 325 5948 1680 1682 19779197 1:CAS:528:DC%2BD1MXhtFGqt7%2FO 10.1126/science.1175667
50. DJ Johnson DA Fidock M Mungthin V Lakshmanan AB Sidhu PG Bray SA Ward 2004 Evidence for a central role for PfCRT in conferring Plasmodium falciparum resistance to diverse antimalarial agents Mol Cell 15 6 867 877 15383277 1:CAS:528:DC%2BD2cXosl2jsbw%3D 10.1016/j.molcel.2004.09.012 (Pubitemid 39277984)
51. KL Waller RA Muhle LM Ursos P Horrocks D Verdier-Pinard AB Sidhu H Fujioka PD Roepe DA Fidock 2003 Chloroquine resistance modulated in vitro by expression levels of the Plasmodium falciparum chloroquine resistance transporter J Biol Chem 278 35 33593 33601 12813054 1:CAS:528: DC%2BD3sXms1altb8%3D 10.1074/jbc.M302215200 (Pubitemid 37055813)
52. Carlton JM, Fidock DA, Djimde A, Plowe CV, Wellems TE (2001) Conservation of a novel vacuolar transporter in Plasmodium species and its central role in chloroquine resistance of P. falciparum. Curr Opin Microbiol 4(4):415-420 (Pubitemid 32720521)
53. DA van Schalkwyk TJ Egan 2006 Quinoline-resistance reversing agents for the malaria parasite Plasmodium falciparum Drug Resist Updat 9 4-5 211 226 17064951 10.1016/j.drup.2006.09.002 1:CAS:528:DC%2BD28Xht1ersL%2FE (Pubitemid 44781212)
54. TJ Egan CH Kaschula 2007 Strategies to reverse drug resistance in malaria Curr Opin Infect Dis 20 6 598 604 17975410 1:CAS:528:DC%2BD2sXht1CnsLvO 10.1097/QCO.0b013e3282f1673a (Pubitemid 350059519)
55. E Guantai K Chibale 2010 Chloroquine resistance: proposed mechanisms and countermeasures Curr Drug Deliv 7 4 312 323 20695842 1:CAS:528: DC%2BC3cXht1WgtLrM 10.2174/156720110793360577
56. MR Pereira PP Henrich AB Sidhu D Johnson J Hardink J Van Deusen J Lin K Gore C O'Brien M Wele A Djimde R Chandra DA Fidock 2011 In vivo and in vitro antimalarial properties of azithromycin-chloroquine combinations that include the resistance reversal agent amlodipine Antimicrob Agents Chemother 55 7 3115 3124 21464242 1:CAS:528:DC%2BC3MXos1OrsL0%3D 10.1128/AAC.01566-10
57. A Sowunmi AM Oduola OA Ogundahunsi CO Falade GO Gbotosho LA Salako 1997 Enhanced efficacy of chloroquine-chlorpheniramine combination in acute uncomplicated falciparum malaria in children Trans R Soc Trop Med Hyg 91 1 63 67 9093632 1:CAS:528:DyaK2sXitFSnsb8%3D 10.1016/S0035-9203(97)90399-0 (Pubitemid 27095504)
58. TO Ogungbamigbe O Ojurongbe PS Ogunro BM Okanlawon SO Kolawole 2008 Chloroquine resistant Plasmodium falciparum malaria in Osogbo Nigeria: efficacy of amodiaquine + sulfadoxine-pyrimethamine and chloroquine + chlorpheniramine for treatment Mem Inst Oswaldo Cruz 103 1 79 84 18368238 1:CAS:528: DC%2BD1cXmvV2gtLs%3D 10.1590/S0074-02762008000100012 (Pubitemid 351439726)
59. S Alibert C Santelli-Rouvier B Pradines C Houdoin D Parzy J Karolak-Wojciechowska J Barbe 2002 Synthesis and effects on chloroquine susceptibility in Plasmodium falciparum of a series of new dihydroanthracene derivatives J Med Chem 45 15 3195 3209 12109904 1:CAS:528:DC%2BD38Xks1aru70%3D 10.1021/jm011046l (Pubitemid 34774271)
60. AK Bhattacharjee DE Kyle JL Vennerstrom 2001 Structural analysis of chloroquine resistance reversal by imipramine analogs Antimicrob Agents Chemother 45 9 2655 2657 11502547 1:CAS:528:DC%2BD3MXmt1emtLg%3D 10.1128/AAC.45.9.2655-2657.2001 (Pubitemid 32801928)
61. J Guan DE Kyle L Gerena Q Zhang WK Milhous AJ Lin 2002 Design, synthesis, and evaluation of new chemosensitizers in multi-drug-resistant Plasmodium falciparum J Med Chem 45 13 2741 2748 12061877 1:CAS:528:DC%2BD38Xjslans78%3D 10.1021/jm010549o (Pubitemid 34627646)
62. JX Kelly MJ Smilkstein RA Cooper KD Lane RA Johnson A Janowsky RA Dodean DJ Hinrichs R Winter M Riscoe 2007 Design, synthesis, and evaluation of 10-N-substituted acridones as novel chemosensitizers in Plasmodium falciparum Antimicrob Agents Chemother 51 11 4133 4140 17846138 1:CAS:528: DC%2BD2sXht1ygtLrI 10.1128/AAC.00669-07 (Pubitemid 350057815)
63. AK Bhattacharjee DE Kyle JL Vennerstrom WK Milhous 2002 A 3D QSAR pharmacophore model and quantum chemical structure-activity analysis of chloroquine (CQ)-resistance reversal J Chem Inf Comput Sci 42 5 1212 1220 12377011 1:CAS:528:DC%2BD38XlslaisbY%3D 10.1021/ci0200265 (Pubitemid 35360307)
64. RK Mehlotra H Fujioka PD Roepe O Janneh LM Ursos V Jacobs-Lorena DT McNamara MJ Bockarie JW Kazura DE Kyle DA Fidock PA Zimmerman 2001 Evolution of a unique Plasmodium falciparum chloroquine-resistance phenotype in association with pfcrt polymorphism in Papua New Guinea and South America Proc Natl Acad Sci USA 98 22 12689 12694 11675500 1:CAS:528:DC%2BD3MXotFahsr8%3D 10.1073/pnas.221440898 (Pubitemid 33020007)
65. JJ Patel D Thacker JC Tan P Pleeter L Checkley JM Gonzales B Deng PD Roepe RA Cooper MT Ferdig 2010 Chloroquine susceptibility and reversibility in a Plasmodium falciparum genetic cross Mol Microbiol 78 3 770 787 20807203 1:CAS:528:DC%2BC3cXhsFSgtbnF 10.1111/j.1365-2958.2010.07366.x
66. JM Sá O Twu K Hayton S Reyes MP Fay P Ringwald TE Wellems 2009 Geographic patterns of Plasmodium falciparum drug resistance distinguished by differential responses to amodiaquine and chloroquine Proc Natl Acad Sci USA 106 45 18883 18889 19884511 10.1073/pnas.0911317106
67. VK Zishiri R Hunter PJ Smith D Taylor R Summers K Kirk RE Martin TJ Egan 2011 A series of structurally simple chloroquine chemosensitizing dibemethin derivatives that inhibit chloroquine transport by PfCRT Eur J Med Chem 46 5 1729 1742 21396749 1:CAS:528:DC%2BC3MXjvFSitr4%3D 10.1016/j.ejmech.2011.02.026
68. AM Lehane K Kirk 2010 Efflux of a range of antimalarial drugs and 'chloroquine resistance reversers' from the digestive vacuole in malaria parasites with mutant PfCRT Mol Microbiol 77 4 1039 1051 1:CAS:528: DC%2BC3cXhtFaisrvO
69. W Peters R Ekong BL Robinson DC Warhurst XQ Pan 1989 Antihistaminic drugs that reverse chloroquine resistance in Plasmodium falciparum Lancet 2 8658 334 335 2569137 1:CAS:528:DyaL1MXmtVykt78%3D 10.1016/S0140-6736(89)90522-9 (Pubitemid 19187062)
70. J Yuan KC Cheng RL Johnson R Huang S Pattaradilokrat A Liu R Guha DA Fidock J Inglese TE Wellems CP Austin XZ Su 2011 Chemical genomic profiling for antimalarial therapies, response signatures, and molecular targets Science 333 6043 724 729 21817045 1:CAS:528:DC%2BC3MXps1SgtbY%3D 10.1126/science.1205216
71. SJ Foote DE Kyle RK Martin AMJ Oduola K Forsyth DJ Kemp AF Cowman 1990 Several alleles of the multidrug-resistance gene are closely linked to chloroquine resistance in Plasmodium falciparum Nature 345 6272 255 258 2185424 1:CAS:528:DyaK3cXkvFansLc%3D 10.1038/345255a0 (Pubitemid 20163056)
72. CM Wilson AE Serrano A Wasley MP Bogenschutz AH Shankar DF Wirth 1989 Amplification of a gene related to mammalian mdr genes in drug-resistant Plasmodium falciparum Science 244 4909 1184 1186 2658061 1:CAS:528: DyaL1MXksFWmtLY%3D 10.1126/science.2658061 (Pubitemid 19170490)
73. AF Cowman S Karcz D Galatis JG Culvenor 1991 A P-glycoprotein homologue of Plasmodium falciparum is localized on the digestive vacuole J Cell Biol 113 5 1033 1042 1674943 1:CAS:528:DyaK3MXit1Ggs7Y%3D 10.1083/jcb.113.5.1033 (Pubitemid 21909736)
74. SR Karcz D Galatis AF Cowman 1993 Nucleotide binding-properties of a P-glycoprotein homolog from Plasmodium falciparum Mol Biochem Parasitol 58 2 269 276 8097560 1:CAS:528:DyaK3sXit12rtr0%3D 10.1016/0166-6851(93)90048-3
75. P Rohrbach CP Sanchez K Hayton O Friedrich J Patel ABS Sidhu MT Ferdig DA Fidock M Lanzer 2006 Genetic linkage of pfmdr1 with food vacuolar solute import in Plasmodium falciparum EMBO J 25 13 3000 3011 16794577 1:CAS:528: DC%2BD28XmvFaju78%3D 10.1038/sj.emboj.7601203 (Pubitemid 44106753)
76. CP Sanchez A Rotmann WD Stein M Lanzer 2008 Polymorphisms within PfMDR1 alter the substrate specificity for anti-malarial drugs in Plasmodium falciparum Mol Microbiol 70 4 786 798 18713316 1:CAS:528:DC%2BD1cXhsVarur3O
77. HHG van Es S Karcz F Chu AF Cowman S Vidal P Gros E Schurr 1994 Expression of the plasmodial pfmdr1 gene in mammalian cells is associated with increased susceptibility to chloroquine Mol Cell Biol 14 4 2419 2428 7511206 10.1128/MCB.14.4.2419 (Pubitemid 24108224)
78. SK Volkman AF Cowman DF Wirth 1995 Functional complementation of the ste6 gene of Saccharomyces cerevisiae with the pfmdr1 gene of Plasmodium falciparum Proc Natl Acad Sci USA 92 8921 8925 7568044 1:CAS:528:DyaK2MXotVGqtrs%3D 10.1073/pnas.92.19.8921
79. MB Reed KJ Saliba SR Caruana K Kirk AF Cowman 2000 Pgh1 modulates sensitivity and resistance to multiple antimalarials in Plasmodium falciparum Nature 403 906 909 10706290 1:CAS:528:DC%2BD3cXhs1Ors7o%3D 10.1038/35002615 (Pubitemid 30130994)
80. ABS Sidhu SG Valderramos DA Fidock 2005 pfmdr1 mutations contribute to quinine resistance and enhance mefloquine and artemisinin sensitivity in Plasmodium falciparum Mol Microbiol 57 4 913 926 16091034 1:CAS:528: DC%2BD2MXpsFCltb4%3D 10.1111/j.1365-2958.2005.04729.x (Pubitemid 41139856)
81. N Khim C Bouchier MT Ekala S Incardona P Lim E Legrand R Jambou S Doung OM Puijalon T Fandeur 2005 Countrywide survey shows very high prevalence of Plasmodium falciparum multilocus resistance genotypes in Cambodia Antimicrob Agents Chemother 49 8 3147 3152 16048916 1:CAS:528:DC%2BD2MXntFCht7w%3D 10.1128/AAC.49.8.3147-3152.2005 (Pubitemid 41060552)
82. MI Veiga PE Ferreira L Jornhagen M Malmberg A Kone BA Schmidt M Petzold A Bjorkman F Nosten JP Gil 2011 Novel polymorphisms in Plasmodium falciparum ABC transporter genes are associated with major ACT antimalarial drug resistance PLoS One 6 5 e20212 21633513 1:CAS:528:DC%2BC3MXmvFCrsbo%3D 10.1371/journal. pone.0020212
83. JB Mu MT Ferdig XR Feng DA Joy JH Duan T Furuya G Subramanian L Aravind RA Cooper JC Wootton M Xiong XZ Su 2003 Multiple transporters associated with malaria parasite responses to chloroquine and quinine Mol Microbiol 49 4 977 989 12890022 1:CAS:528:DC%2BD3sXmslKltLg%3D 10.1046/j.1365-2958.2003.03627.x (Pubitemid 36981343)
84. TJC Anderson S Nair H Qin S Singlam A Brockman L Paiphun F Nosten 2005 Are transporter genes other than the chloroquine resistance locus (pfcrt) and multidrug resistance gene (pfmdr) associated with antimalarial drug resistance? Antimicrob Agents Chemother 49 6 2180 2188 15917511 1:CAS:528: DC%2BD2MXkvFChurc%3D 10.1128/AAC.49.6.2180-2188.2005 (Pubitemid 40734444)
85. S Briolant M Henry C Oeuvray R Amalvict E Baret E Didillon C Rogier B Pradines 2010 Absence of association between piperaquine in vitro responses and polymorphisms in the pfcrt, pfmdr1, pfmrp, and pfnhe genes in Plasmodium falciparum Antimicrob Agents Chemother 54 9 3537 3544 20547801 10.1128/AAC.00183-10
86. DK Raj JB Mu HY Jiang J Kabat S Singh M Sullivan MP Fay TF McCutchan XZ Su 2009 Disruption of a Plasmodium falciparum Multidrug Resistance-associated Protein (PfMRP) alters its fitness and transport of antimalarial drugs and glutathione J Biol Chem 284 12 7687 7696 19117944 1:CAS:528:DC%2BD1MXjtVSmsbo%3D 10.1074/jbc.M806944200
87. Barnes DA, Foote SJ, Galatis D, Kemp DJ, Cowman AF (1992) Selection for high-level chloroquine resistance results in deamplification of the pfmdr1 gene and increased sensitivity to mefloquine in Plasmodium falciparum. EMBO J 11(8):3067-3075
88. W Chaijaroenkul R Wisedpanichkij K Na-Bangchang 2010 Monitoring of in vitro susceptibilities and molecular markers of resistance of Plasmodium falciparum isolates from Thai-Myanmar border to chloroquine, quinine, mefloquine and artesunate Acta Trop 113 2 190 194 19879850 1:CAS:528: DC%2BC3cXntlSisw%3D%3D 10.1016/j.actatropica.2009.10.016
89. Cowman AF, Galatis D, Thompson JK (1994) Selection for mefloquine resistance in Plasmodium falciparum is linked to amplification of the pfmdr1 gene and cross-resistance to halofantrine and quinine. Proc Natl Acad Sci USA 91(3):1143-1147 (Pubitemid 24048525)
90. SA Peel P Bright B Yount J Handy RS Baric 1994 A strong association between mefloquine and halofantrine resistance and amplification, overexpression, and mutation in the P-glycoprotein gene homologue (pfmdr1) of Plasmodium falciparum in vitro Am J Trop Med Hyg 51 5 648 658 7985758 1:CAS:528:DyaK2MXivVGrtL4%3D (Pubitemid 24378562)
91. AL Pickard C Wongsrichanalai A Purfield D Kamwendo K Emery C Zalewski F Kawamoto RS Miller SR Meshnick 2003 Resistance to antimalarials in Southeast Asia and genetic polymorphisms in pfmdr1 Antimicrob Agents Chemother 47 8 2418 2423 12878499 1:CAS:528:DC%2BD3sXlvFCmurs%3D 10.1128/AAC.47.8.2418-2423.2003 (Pubitemid 36919439)
92. RN Price C Cassar A Brockman M Duraisingh M van Vugt NJ White F Nosten S Krishna 1999 The pfmdr1 gene is associated with a multidrug-resistant phenotype in Plasmodium falciparum from the western border of Thailand Antimicrob Agents Chemother 43 12 2943 2949 10582887 1:CAS:528:DyaK1MXnvVCqtrw%3D
93. RN Price AC Uhlemann A Brockman R McGready E Ashley L Phaipun R Patel K Laing S Looareesuwan NJ White F Nosten S Krishna 2004 Mefloquine resistance in Plasmodium falciparum and increased pfmdr1 gene copy number Lancet 364 9432 438 447 15288742 1:CAS:528:DC%2BD2cXmt1Wjurs%3D 10.1016/S0140-6736(04)16767-6 (Pubitemid 39036891)
94. ABS Sidhu AC Uhlemann SG Valderramos JC Valderramos S Krishna DA Fidock 2006 Decreasing pfmdr1 copy number in Plasmodium falciparum malaria heightens susceptibility to mefloquine, lumefantrine, halofantrine, quinine, and artemisinin J Infect Dis 194 4 528 535 16845638 10.1086/507115 (Pubitemid 44162666)
95. RA Cooper MT Ferdig XZ Su LM Ursos J Mu T Nomura H Fujioka DA Fidock PD Roepe TE Wellems 2002 Alternative mutations at position 76 of the vacuolar transmembrane protein PfCRT are associated with chloroquine resistance and unique stereospecific quinine and quinidine responses in Plasmodium falciparum Mol Pharmacol 61 1 35 42 11752204 1:CAS:528:DC%2BD38XltlSn 10.1124/mol.61.1.35 (Pubitemid 34049510)
96. PG Bray RE Martin L Tilley SA Ward K Kirk DA Fidock 2005 Defining the role of PfCRT in Plasmodium falciparum chloroquine resistance Mol Microbiol 56 2 323 333 15813727 1:CAS:528:DC%2BD2MXjsFWmt7w%3D 10.1111/j.1365-2958.2005.04556. x (Pubitemid 40516774)
97. I Petersen R Eastman M Lanzer 2011 Drug-resistant malaria: molecular mechanisms and implications for public health FEBS Lett 585 11 1551 1562 21530510 1:CAS:528:DC%2BC3MXmvFaisbs%3D 10.1016/j.febslet.2011.04.042
98. AC Uhlemann M Ramharter B Lell PG Kremsner S Krishna 2005 Amplification of Plasmodium falciparum multidrug resistance gene 1 in isolates from Gabon J Infect Dis 192 10 1830 1835 16235185 1:CAS:528:DC%2BD2MXht1Cns7vN 10.1086/497337 (Pubitemid 41587837)
99. C Dokomajilar ZM Lankoande G Dorsey I Zongo JB Ouedraogo PJ Rosenthal 2006 Roles of specific Plasmodium falciparum mutations in resistance to amodiaquine and sulfadoxine-pyrimethamine in Burkina Faso Am J Trop Med Hyg 75 1 162 165 16837725 1:CAS:528:DC%2BD28XnslKhtb4%3D (Pubitemid 351627587)
100. MC Huaman N Roncal S Nakazawa TTA Long L Gerena C Garcia L Solari AJ Magill H Kanbara 2004 Polymorphism of the Plasmodium falciparum multidrug resistance and chloroquine resistance transporter genes and in vitro susceptibility to aminoquinolines in isolates from the Peruvian Amazon Am J Trop Med Hyg 70 5 461 466 15155976 1:CAS:528:DC%2BD2cXlt1elt7s%3D (Pubitemid 38658138)
101. SL Nsobya M Kiggundu S Nanyunja M Joloba B Greenhouse PJ Rosenthal 2010 In vitro sensitivities of Plasmodium falciparum to different antimalarial drugs in Uganda Antimicrob Agents Chemother 54 3 1200 1206 20065051 1:CAS:528:DC%2BC3cXjtFWqsb8%3D 10.1128/AAC.01412-09
102. MT Ferdig RA Cooper J Mu B Deng DA Joy X Su TE Wellems 2004 Dissecting the loci of low-level quinine resistance in malaria parasites Mol Microbiol 52 4 985 997 15130119 1:CAS:528:DC%2BD2cXktlKktro%3D 10.1111/j.1365-2958.2004.04035. x (Pubitemid 38916169)
103. CP Sanchez WD Stein M Lanzer 2008 Dissecting the components of quinine accumulation in Plasmodium falciparum Mol Microbiol 67 5 1081 1093 18194156 1:CAS:528:DC%2BD1cXis12ntr4%3D 10.1111/j.1365-2958.2008.06108.x (Pubitemid 351207335)
104. A Yayon ZI Cabantchik H Ginsburg 1984 Identification of the acidic compartment of Plasmodium falciparum-human erythrocytes as the target of the antimalarial drug chloroquine EMBO J 3 11 2695 2700 6391917 1:CAS:528: DyaL2MXhslWrug%3D%3D
105. Valderramos SG, Valderramos JC, Musset L, Purcell LA, Mercereau-Puijalon O, Legrand E, Fidock DA (2010) Identification of a mutant PfCRT-mediated chloroquine tolerance phenotype in Plasmodium falciparum. PloS Pathog 6(5):e1000887
106. + exchanger 1 transporter is involved in reduced susceptibility to quinine Antimicrob Agents Chemother 53 5 1926 1930 19273668 1:CAS:528:DC%2BD1MXlvVGgtb0%3D 10.1128/AAC.01243-08
107. H Meng RP Zhang HL Yang Q Fan XZ Su J Miao LW Cui ZQ Yang 2010 In vitro sensitivity of Plasmodium falciparum clinical isolates from the China-Myanmar border area to quinine and association with polymorphism in the Na(+)/H(+) exchanger Antimicrob Agents Chemother 54 10 4306 4313 20643902 1:CAS:528:DC%2BC3cXhtlegtrzO 10.1128/AAC.00321-10
108. + exchanger is indicative of a low in vitro quinine susceptibility in isolates from Viet Nam. Malar J 10:164
109. + exchanger (Pfnhe-1) gene with reduced in vitro susceptibility to quinine: lack of confirmation in clinical isolates from Africa Am J Trop Med Hyg 82 5 782 787 20439955 1:CAS:528:DC%2BC3cXnsVeis78%3D 10.4269/ajtmh.2010.09-0327
110. FN Baliraine SL Nsobya J Achan JK Tibenderana AO Talisuna B Greenhouse PJ Rosenthal 2011 Limited ability of Plasmodium falciparum pfcrt, pfmdr1, and pfnhe1 polymorphisms to predict quinine in vitro sensitivity or clinical effectiveness in Uganda Antimicrob Agents Chemother 55 2 615 622 21078941 1:CAS:528:DC%2BC3MXisVyjsb8%3D 10.1128/AAC.00954-10
111. + exchanger (Pfnhe-1) gene: the absence of association in clinical isolates from the Republic of Congo. Malar J 10(1):37
112. J Okombo SM Kiara J Rono L Mwai L Pole E Ohuma S Borrmann LI Ochola A Nzila 2010 In vitro activities of quinine and other antimalarials and pfnhe polymorphisms in Plasmodium Isolates from Kenya Antimicrob Agents Chemother 54 8 3302 3307 20516285 1:CAS:528:DC%2BC3cXhtVOms7fL 10.1128/AAC.00325-10
113. TN Bennett J Patel MT Ferdig PD Roepe 2007 Plasmodium falciparum Na +/H + exchanger activity and quinine resistance Mol Biochem Parasitol 153 1 48 58 17353059 1:CAS:528:DC%2BD2sXjvFaltb8%3D 10.1016/j.molbiopara.2007.01.018 (Pubitemid 46517676)
114. + exchanger Mol Biochem Parasitol 162 1 96 99 18675853 1:CAS:528: DC%2BD1cXhtFCkur%2FF 10.1016/j.molbiopara.2008.07.001
115. LJ Nkrumah PM Riegelhaupt P Moura DJ Johnson J Patel K Hayton MT Ferdig TE Wellems MH Akabas DA Fidock 2009 Probing the multifactorial basis of Plasmodium falciparum quinine resistance: Evidence for a strain-specific contribution of the sodium-proton exchanger PfNHE Mol Biochem Parasitol 165 2 122 131 19428659 1:CAS:528:DC%2BD1MXjsFWlurk%3D 10.1016/j.molbiopara.2009.01.011
116. NB Molta S Oguche SD Paw ICJ Omalu BM Afolabi JB Odujok CN Amajoh B Adeniji VP Wuyep OJ Ekanem 2003 Amodiaquine treatment of uncomplicated malaria in children, in an area of chloroquine-resistant Plasmodium falciparum in north-central Nigeria Ann Trop Med Parasitol 97 7 663 669 14613625 1:CAS:528:DC%2BD3sXhtVSqtrvN 10.1179/000349803225002417 (Pubitemid 37468131)
117. H Sendagire M Kaddumukasa D Ndagire C Aguttu M Nassejje M Pettersson G Swedberg F Kironde 2005 Rapid increase in resistance of Plasmodium falciparum to chloroquine-Fansidar in Uganda and the potential of amodiaquine-Fansidar as a better alternative Acta Trop 95 3 172 182 16018959 1:CAS:528: DC%2BD2MXpt1emtLg%3D 10.1016/j.actatropica.2005.06.003 (Pubitemid 41207280)
118. A Sowunmi AI Ayede AG Falade VN Ndikum CO Sowunmi AA Adedeji CO Falade TC Happi AMJ Oduola 2001 Randomized comparison of chloroquine and amodiaquine in the treatment of acute, uncomplicated, Plasmodium falciparum malaria in children
119. M Alifrangis MB Dalgaard JP Lusingu LS Vestergaard T Staalsoe ATR Jensen A Enevold AM Ronn IF Khalil DC Warhurst MM Lemnge TG Theander IC Bygbjerg 2006 Occurrence of the southeast Asian/south American SVMNT haplotype of the chloroquine-resistance transporter gene in Plasmodium falciparum in Tanzania J Infect Dis 193 12 1738 1741 16703518 1:CAS:528:DC%2BD28XmtlGrtbg%3D 10.1086/504269 (Pubitemid 43839479)
120. DC Warhurst 2003 Polymorphism in the Plasmodium falciparum chloroquine-resistance transporter protein links verapamil enhancement of chloroquine sensitivity with the clinical efficacy of amodiaquine Malar J 2 1 31 14599295 10.1186/1475-2875-2-31
121. RK Mehlotra G Mattera MJ Bockarie JD Maguire JK Baird YD Sharma M Alifrangis G Dorsey PJ Rosenthal DJ Fryauff JW Kazura M Stoneking A Zimmerman 2008 Discordant patterns of genetic variation at two chloroquine resistance loci in worldwide populations of the malaria parasite Plasmodium falciparum Antimicrob Agents Chemother 52 6 2212 2222 18411325 1:CAS:528: DC%2BD1cXmvVait7o%3D 10.1128/AAC.00089-08 (Pubitemid 351758561)
122. Gama BE, Pereira-Carvalho GAL, Kosi F, de Oliveira NKA, Fortes F, Rosenthal PJ, Daniel-Ribeiro CT, Ferreira-Da-Cruz MD (2010) Plasmodium falciparum isolates from Angola show the S(tct)VMNT haplotype in the pfcrt gene. Malar J 9:174
123. Sá JM, Twu O (2010) Protecting the malaria drug arsenal: halting the rise and spread of amodiaquine resistance by monitoring the PfCRT SVMNT type. Malar J 9:374
124. I Danquah B Coulibaly P Meissner I Petruschke O Muller FP Mockenhaupt 2010 Selection of pfmdr1 and pfcrt alleles in amodiaquine treatment failure in north-western Burkina Faso Acta Trop 114 1 63 66 20060374 1:CAS:528: DC%2BC3cXisF2ltLw%3D 10.1016/j.actatropica.2009.12.008
125. SL Nsobya C Dokomajilar M Joloba G Dorsey PJ Rosenthal 2007 Resistance-mediating Plasmodium falciparum pfcrt and pfmdr1 alleles after treatment with artesunate-amodiaquine in Uganda Antimicrob Agents Chemother 51 8 3023 3025 17562798 1:CAS:528:DC%2BD2sXoslOis7g%3D 10.1128/AAC.00012-07 (Pubitemid 47206253)
126. S Muangnoicharoen DJ Johnson S Looareesuwan S Krudsood SA Ward 2009 Role of known molecular markers of resistance in the antimalarial potency of piperaquine and dihydroartemisinin in vitro Antimicrob Agents Chemother 53 4 1362 1366 19188388 1:CAS:528:DC%2BD1MXksFWksrc%3D 10.1128/AAC.01656-08
127. LK Basco P Ringwald 2003 In vitro activities of piperaquine and other 4-aminoquinolines against clinical isolates of Plasmodium falciparum in Cameroon Antimicrob Agents Chemother 47 4 1391 1394 12654675 1:CAS:528: DC%2BD3sXivVSms78%3D 10.1128/AAC.47.4.1391-1394.2003 (Pubitemid 36368602)
128. RT Eastman NV Dharia EA Winzeler DA Fidock 2011 Piperaquine resistance is associated with a copy number variation on chromosome 5 in drug-pressured Plasmodium falciparum parasites Antimicrob Agents Chemother 55 8 3908 3916 21576453 1:CAS:528:DC%2BC3MXpslGgtLo%3D 10.1128/AAC.01793-10
129. JN Burrows K Chibale TN Wells 2011 The state of the art in anti-malarial drug discovery and development Curr Top Med Chem 11 10 1226 1254 21401508 1:CAS:528:DC%2BC3MXnt1CnsLY%3D 10.2174/156802611795429194
130. GE Childs EF Boudreau WK Milhous T Wimonwattratee N Pooyindee L Pang JDE Davidson 1989 A comparison of the in vitro activities of amodiaquine and desethylamodiaquine against isolates of Plasmodium falciparum Am J Trop Med Hyg 40 1 7 11 2644858 1:CAS:528:DyaL1MXhvV2ht78%3D (Pubitemid 19063924)
131. EI Elueze SL Croft DC Warhurst 1996 Activity of pyronaridine and mepacrine against twelve strains of Plasmodium falciparum in vitro J Antimicrob Chemother 37 3 511 518 9182108 1:CAS:528:DyaK28XitVamu7k%3D 10.1093/jac/37.3.511 (Pubitemid 26116966)
132. B Pradines M Mabika Mamfoumbi D Parzy M Owono Medang C Lebeau JR Mourou Mbina JC Doury M Kombila 1999 In vitro susceptibility of African isolates of Plasmodium falciparum from Gabon to pyronaridine Am J Trop Med Hyg 60 1 105 108 9988332 1:CAS:528:DyaK1MXht1GnsrY%3D (Pubitemid 29066013)
133. RN Price J Marfurt F Chalfein E Kenangalem KA Piera E Tjitra NM Anstey B Russell 2010 In vitro activity of pyronaridine against multidrug-resistant Plasmodium falciparum and Plasmodium vivax Antimicrob Agents Chemother 54 12 5146 5150 20876370 1:CAS:528:DC%2BC3cXhsF2nu7bK 10.1128/AAC.00801-10
134. HL Yang DQ Liu YM Yang KG Huang Y Dong PF Yang MZ Liao CY Zhang 1997 In vitro sensitivity of Plasmodium falciparum to eight antimalarials in China-Myanmar and China-Lao PDR border areas Southeast Asian J Trop Med Public Health 28 3 460 464 9561592 1:STN:280:DyaK1c3it1ektQ%3D%3D (Pubitemid 127523372)
135. Pradines B, Briolant S, Henry M, Oeuvray C, Baret E, Amalvict R, Didillon E, Rogier C (2010) Absence of association between pyronaridine in vitro responses and polymorphisms in genes involved in quinoline resistance in Plasmodium falciparum. Malar J 9:339
136. G Kokwaro L Mwai A Nzila 2007 Artemether/lumefantrine in the treatment of uncomplicated falciparum malaria Expert Opin Pharmacother 8 1 75 94 17163809 1:CAS:528:DC%2BD28XhtlSrsL%2FF 10.1517/14656566.8.1.75 (Pubitemid 46070831)
137. NJ White M van Vugt F Ezzet 1999 Clinical Pharmacokinetics and Pharmacodynamics of Artemether-Lumefantrine Clin Pharmacokinet 37 2 105 125 10496300 1:CAS:528:DyaK1MXmsVGjtb8%3D 10.2165/00003088-199937020-00002 (Pubitemid 29431479)
138. WHO (2010) Guidelines for the treatment of malaira, 2nd edn
139. RJ Maude CJ Woodrow LJ White 2010 Artemisinin antimalarials: preserving the "Magic Bullet" Drug Dev Res 71 1 12 19 21399699 1:CAS:528:DC%2BC3cXhslWrs7o%3D
140. C Morris M Onyamboko E Capparelli M Koch J Atibu V Lokomba M Douoguih J Hemingway-Foday D Wesche R Ryder C Bose L Wright A Tshefu S Meshnick L Fleckenstein 2011 Population pharmacokinetics of artesunate and dihydroartemisinin in pregnant and non-pregnant women with malaria Malar J 10 1 114 21548983 1:CAS:528:DC%2BC3MXmtlKltbs%3D 10.1186/1475-2875-10-114
141. F Ezzet M van Vugt F Nosten S Looareesuwan NJ White 2000 Pharmacokinetics and pharmacodynamics of lumefantrine (benflumetol) in acute falciparum malaria Antimicrob Agents Chemother 44 3 697 704 10681341 1:CAS:528:DC%2BD3cXhsVGgsr8%3D 10.1128/AAC.44.3.697-704.2000 (Pubitemid 30117964)
142. KJ Palmer SM Holliday RN Brogden 1993 Mefloquine: a review of its antimalarial activity, pharmacokinetic properties and therapeutic efficacy Drugs 45 3 430 475 7682911 1:CAS:528:DyaK3sXisVKkt74%3D 10.2165/00003495-199345030- 00009 (Pubitemid 23104127)
143. WHO (2010) Global report on antimalarial drug efficacy and drug resistance: 2000-2010
144. EA Ashley R McGready R Hutagalung L Phaiphun T Slight S Proux KL Thwai M Barends S Looareesuwan NJ White F Nosten 2005 A randomized, controlled study of a simple, once-daily regimen of dihydroartemisinin-piperaquine for the treatment of uncomplicated, multidrug-resistant falciparum malaria Clin Infect Dis 41 4 425 432 16028147 1:CAS:528:DC%2BD2MXps1yisr0%3D 10.1086/432011 (Pubitemid 41099632)
145. F Nosten C Luxemburger FO ter Kuile C Woodrow JP Eh T Chongsuphajaisiddhi NJ White 1994 Treatment of multidrug-resistant Plasmodium falciparum malaria with 3-day artesunate-mefloquine combination J Infect Dis 170 4 971 977 7930743 1:STN:280:DyaK2M%2Fhs1Smsw%3D%3D 10.1093/infdis/170.4.971 (Pubitemid 24296580)
146. M Chavchich L Gerena J Peters NH Chen Q Cheng DE Kyle 2010 Role of pfmdr1 amplification and expression in induction of resistance to artemisinin derivatives in Plasmodium falciparum Antimicrob Agents Chemother 54 6 2455 2464 20350946 1:CAS:528:DC%2BC3cXos1Ohu7w%3D 10.1128/AAC.00947-09
147. T Ngo M Duraisingh MB Reed D Hipgrave B Biggs AF Cowman 2003 Analysis of pfcrt, pfmdr1 dhfr, and dhps mutations and drug sensitivities in Plasmodium falciparum isolates from patients in Vietnam before and after treatment with artemisinin Am J Trop Med Hyg 68 3 350 356 12685644 1:CAS:528: DC%2BD3sXivFenur4%3D (Pubitemid 38240527)
148. A Martinelli R Moreira PV Ravo 2008 Malaria combination therapies: advantages and shortcomings Mini Rev Med Chem 8 3 201 212 18336340 1:CAS:528:DC%2BD1cXivFalsrs%3D 10.2174/138955708783744092 (Pubitemid 351611823)
149. AM Dondorp F Nosten P Yi D Das AP Phyo J Tarning KM Lwin F Ariey W Hanpithakpong SJ Lee P Ringwald K Silamut M Imwong K Chotivanich P Lim T Herdman SS An S Yeung P Singhasivanon NP Day N Lindegardh D Socheat NJ White 2009 Artemisinin resistance in Plasmodium falciparum malaria N Engl J Med 361 5 455 467 19641202 1:CAS:528:DC%2BD1MXpt1CrsLk%3D 10.1056/NEJMoa0808859
150. H Noedl Y Se S Sriwichai K Schaecher P Teja-Isavadharm B Smith W Rutvisuttinunt D Bethell S Surasri MM Fukuda D Socheat L Chan Thap 2010 Artemisinin resistance in Cambodia: a clinical trial designed to address an emerging problem in Southeast Asia Clin Infect Dis 51 11 e82 e89 21028985 10.1086/657120
151. Tucker MS, Mutka T, Sparks K, Patel J, Kyle DE (2011) Phenotypic and genotypic analysis of in vitro selected artemisinin-resistant progeny of Plasmodium falciparum. Antimicrob Agents Chemother 56(1):302-314
152. D Beez CP Sanchez WD Stein M Lanzer 2011 Genetic predisposition favors the acquisition of stable artemisinin resistance in malaria parasites Antimicrob Agents Chemother 55 1 50 55 21041511 1:CAS:528:DC%2BC3MXisVehtb0%3D 10.1128/AAC.00916-10
153. WHO (2011) Consideration of mass drug administration for the containment of artemisinin resistant malaria in the Greater Mekong subregion: report of a consensus meeting, 27-28 September 2010, Geneva, Switzerland
154. M Enserink 2010 Malaria's drug miracle in danger Science 328 5980 844 846 20466917 1:CAS:528:DC%2BC3cXmsFSitrY%3D 10.1126/science.328.5980.844
155. MD Loeb WM Clark LTC Coatney GR FR Dieuaide MD Dochez EG Hakansson EK Marshall Jr CS Marvel OR McCoy JJ Sapero WH Sebrell JA Shannon GA Carden Jr 1946 Activity of a new antimalarial agent, chloroquine (SN 7618) J Am Med Assoc 130 1069 10.1001/jama.1946.02870160015006
156. H Most IM London, et al. 1946 Chloroquine for treatment of acute attacks of vivax malaria J Am Med Assoc 131 963 967 20989979 1:STN:280: DyaH28%2FgvVSrtg%3D%3D 10.1001/jama.1946.02870290013005
157. Most H (1963) Clinical trials of antimalarial drugs. In: Coates JB (ed) Internal medicine in world war II. Office of the Surgeon General, Medical Department, United States Army, Washington DC, pp 562-576
158. RM Chico D Chandramohan 2011 Azithromycin plus chloroquine: combination therapy for protection against malaria and sexually transmitted infections in pregnancy Expert Opin Drug Metab Toxicol 7 9 1153 1167 21736423 1:CAS:528:DC%2BC3MXhtVWmsLrI 10.1517/17425255.2011.598506
159. WHO (2001) The use of antimalarial drugs: report of an informal consultation
160. M Berger J Beytout P Ringwald M Cambon M Rey 1990 A case of Plasmodium falciparum malaria contracted in Guinea-Bissau during chemoprophylaxis with chloroquine Presse Med 19 36 1682 2147276 1:STN:280:DyaK3M%2Fmt1eguw%3D%3D (Pubitemid 20379480)
161. U Hellgren I Johansson F Dias O Ericsson J Stenbeck L Rombo 1991 Chloroquine resistant Plasmodium falciparum malaria in Guinea-Bissau Trans R Soc Trop Med Hyg 85 1 36 2068753 1:STN:280:DyaK3M3pslOitw%3D%3D 10.1016/0035-9203(91)90144-N
162. J Ursing PE Kofoed A Rodrigues Y Bergqvist L Rombo 2009 Chloroquine is grossly overdosed and overused but well tolerated in Guinea-bissau Antimicrob Agents Chemother 53 1 180 185 18955514 1:CAS:528:DC%2BD1MXhs1KksL4%3D 10.1128/AAC.01111-08
163. J Ursing BA Schmidt M Lebbad PE Kofoed F Dias JP Gil L Rombo 2007 Chloroquine resistant P. falciparum prevalence is low, unchanged between 1990 and 2005 in Guinea-Bissau: an effect of high chloroquine dosage? Infect Genet Evol 7 5 555 561 17467343 1:CAS:528:DC%2BD2sXhtVWhsr%2FF 10.1016/j.meegid.2007. 03.006 (Pubitemid 47342374)
164. J Ursing PE Kofoed A Rodrigues D Blessborn R Thoft-Nielsen A Bjorkman L Rombo 2011 Similar efficacy and tolerability of double-dose chloroquine and artemether-lumefantrine for treatment of Plasmodium falciparum infection in Guinea-Bissau: a randomized trial J Infect Dis 203 1 109 116 21148503 1:CAS:528:DC%2BC3MXhtlOmt7g%3D 10.1093/infdis/jiq001
165. CC Hand SR Meshnick 2011 Is chloroquine making a comeback? J Infect Dis 203 1 11 12 21148490 1:CAS:528:DC%2BC3MXhtlOmtrk%3D 10.1093/infdis/jiq002
166. E Pussard JP Lepers F Clavier L Raharimalala J Le Bras M Frisk-Holmberg Y Bergqvist F Verdier 1991 Efficacy of a loading dose of oral chloroquine in a 36-h treatment schedule for uncomplicated Plasmodium falciparum malaria Antimicrob Agents Chemother 35 3 406 409 2039190 1:STN:280:DyaK3M3kslOlsQ%3D%3D
167. NJ White 1992 Antimalarial pharmacokinetics and treatment regimens Br J Clin Pharmacol 34 1 1 10 1633062 1:CAS:528:DyaK38Xlt1eru78%3D
168. SL Hoffman S Masbar PR Hussein A Soewarta S Harun HA Marwoto JR Campbell L Smrkovski Wiady I Purnomo 1984 Absence of malaria mortality in villagers with chloroquine-resistant Plasmodium falciparum treated with chloroquine Trans R Soc Trop Med Hyg 78 2 175 178 6380012 1:STN:280:DyaL2c3nsFCkuw%3D%3D 10.1016/0035-9203(84)90271-2 (Pubitemid 14143733)
169. H Ginsburg 2005 Should chloroquine be laid to rest? Acta Trop 96 1 16 23 16054105 1:CAS:528:DC%2BD2MXpt1emtbc%3D 10.1016/j.actatropica.2005.06.021 (Pubitemid 41207719)
170. J Ursing PE Kofoed A Rodrigues L Rombo JP Gil 2007 Plasmodium falciparum genotypes associated with chloroquine and amodiaquine resistance in Guinea-Bissau Am J Trop Med Hyg 76 5 844 848 17488902 1:CAS:528: DC%2BD2sXmsVyisbs%3D (Pubitemid 351627666)
171. HO AlKadi 2007 Antimalarial drug toxicity: a review Chemotherapy 53 6 385 391 17934257 1:CAS:528:DC%2BD2sXht1OksbjO 10.1159/000109767 (Pubitemid 350085250)
172. P Murambiwa B Masola T Govender S Mukaratirwa CT Musabayane 2011 Anti-malarial drug formulations and novel delivery systems: a review Acta Trop 118 2 71 79 21439929 1:CAS:528:DC%2BC3MXlsFGltbY%3D 10.1016/j.actatropica.2011. 03.005
173. BR Moore M Page-Sharp JR Stoney KF Ilett JD Jago KT Batty 2011 Pharmacokinetics, pharmacodynamics, and allometric scaling of chloroquine in a murine malaria model Antimicrob Agents Chemother 55 8 3899 3907 21646487 1:CAS:528:DC%2BC3MXpslGgtL4%3D 10.1128/AAC.00067-11
174. I Angulo-Barturen MB Jimenez-Diaz T Mulet J Rullas E Herreros S Ferrer E Jimenez A Mendoza J Regadera PJ Rosenthal I Bathurst DL Pompliano F Gomez de las Heras D Gargallo-Viola 2008 A murine model of falciparum-malaria by in vivo selection of competent strains in non-myelodepleted mice engrafted with human erythrocytes PLoS One 3 5 e2252 18493601 10.1371/journal.pone.0002252 1:CAS:528:DC%2BD1cXnsVOgtrY%3D
175. D Bethell Y Se C Lon S Tyner D Saunders S Sriwichai S Darapiseth P Teja-Isavadharm P Khemawoot K Schaecher W Ruttvisutinunt J Lin W Kuntawungin P Gosi A Timmermans B Smith D Socheat MM Fukuda 2011 Artesunate dose escalation for the treatment of uncomplicated malaria in a region of reported artemisinin resistance: a randomized clinical trial PLoS One 6 5 e19283 21603629 1:CAS:528:DC%2BC3MXmsV2isrk%3D 10.1371/journal.pone.0019283
176. D Bethell Y Se C Lon D Socheat D Saunders P Teja-Isavadharm P Khemawoot S Darapiseth J Lin S Sriwichai W Kuntawungin S Surasri SJ Lee S Sarim S Tyner B Smith MM Fukuda 2010 Dose-dependent risk of neutropenia after 7-day courses of artesunate monotherapy in Cambodian patients with acute Plasmodium falciparum malaria Clin Infect Dis 51 12 e105 e114 21070142 1:CAS:528:DC%2BC3MXotlWr 10.1086/657402
177. J Achan AO Talisuna A Erhart A Yeka JK Tibenderana FN Baliraine PJ Rosenthal U D'Alessandro 2011 Quinine, an old anti-malarial drug in a modern world: role in the treatment of malaria Malar J 10 144 21609473 1:CAS:528:DC%2BC3MXntVajsLc%3D 10.1186/1475-2875-10-144
178. DA Fidock 2010 Drug discovery: Priming the antimalarial pipeline Nature 465 7296 297 298 20485420 1:CAS:528:DC%2BC3cXmt1Oju7w%3D 10.1038/465297a
179. TN Wells PL Alonso WE Gutteridge 2009 New medicines to improve control and contribute to the eradication of malaria Nat Rev Drug Discov 8 11 879 891 19834482 1:CAS:528:DC%2BD1MXht1KqsLfP 10.1038/nrd2972
180. FJ Gamo LM Sanz J Vidal C de Cozar E Alvarez JL Lavandera DE Vanderwall DV Green V Kumar S Hasan JR Brown CE Peishoff LR Cardon JF Garcia-Bustos 2010 Thousands of chemical starting points for antimalarial lead identification Nature 465 7296 305 310 20485427 1:CAS:528:DC%2BC3cXmt1Ois7k%3D 10.1038/nature09107
181. WA Guiguemde AA Shelat D Bouck S Duffy GJ Crowther PH Davis DC Smithson M Connelly J Clark F Zhu MB Jimenez-Diaz MS Martinez EB Wilson AK Tripathi J Gut ER Sharlow I Bathurst F El Mazouni JW Fowble I Forquer PL McGinley S Castro I Angulo-Barturen S Ferrer PJ Rosenthal JL Derisi DJ Sullivan JS Lazo DS Roos MK Riscoe MA Phillips PK Rathod WC Van Voorhis VM Avery RK Guy 2010 Chemical genetics of Plasmodium falciparum Nature 465 7296 311 315 20485428 1:CAS:528:DC%2BC3cXmt1OjtL4%3D 10.1038/nature09099
182. D Plouffe A Brinker C McNamara K Henson N Kato K Kuhen A Nagle F Adrian JT Matzen P Anderson TG Nam NS Gray A Chatterjee J Janes SF Yan R Trager JS Caldwell PG Schultz Y Zhou EA Winzeler 2008 In silico activity profiling reveals the mechanism of action of antimalarials discovered in a high-throughput screen Proc Natl Acad Sci USA 105 26 9059 9064 18579783 1:CAS:528:DC%2BD1cXosVCiurw%3D 10.1073/pnas.0802982105
183. M Rottmann C McNamara BK Yeung MC Lee B Zou B Russell P Seitz DM Plouffe NV Dharia J Tan SB Cohen KR Spencer GE Gonzalez-Paez SB Lakshminarayana A Goh R Suwanarusk T Jegla EK Schmitt HP Beck R Brun F Nosten L Renia V Dartois TH Keller DA Fidock EA Winzeler TT Diagana 2010 Spiroindolones, a potent compound class for the treatment of malaria Science 329 5996 1175 1180 20813948 1:CAS:528:DC%2BC3cXhtV2hsr%2FJ 10.1126/science.1193225
184. Wells TN (2010) Microbiology. Is the tide turning for new malaria medicines? Science 329(5996):1153-1154
185. BK Yeung B Zou M Rottmann SB Lakshminarayana SH Ang SY Leong J Tan J Wong S Keller-Maerki C Fischli A Goh EK Schmitt P Krastel E Francotte K Kuhen D Plouffe K Henson T Wagner EA Winzeler F Petersen R Brun V Dartois TT Diagana TH Keller 2010 Spirotetrahydro beta-carbolines (spiroindolones): a new class of potent and orally efficacious compounds for the treatment of malaria J Med Chem 53 14 5155 5164 20568778 1:CAS:528:DC%2BC3cXnvVKqu78%3D 10.1021/jm100410f
186. BT Grimberg RK Mehlotra 2011 Expanding the antimalarial drug arsenal-now, but how? Pharmaceuticals (Basel) 4 5 681 712
187. CJ Canfield RS Rozman 1974 Clinical testing of new antimalarial compounds Bull World Health Organ 50 3-4 203 212 4613503 1:STN:280:DyaE2M%2FnsVCrsg%3D%3D
188. RL Jacobs DW Alling WF Cantrell 1963 An Evaluation of Antimalarial Combinations against Plasmodium Berghei in the Mouse J Parasitol 49 920 925 14084196 1:CAS:528:DyaF2cXkvVaktw%3D%3D 10.2307/3275719
189. Singh T, Stein RG, Hoops JF, Biel JH, Hoya WK, Cruz DR (1971) Antimalarials. 7-chloro-4-(substituted amino)quinolines. J Med Chem 14(4):283-286
190. PE Thompson JW Reinertson A Bayles AM Moore 1953 The curative action of antimalarial drugs against Plasmodium lophurae in chicks J Infect Dis 92 1 40 51 13022989 1:STN:280:DyaG3s%2FkslKntQ%3D%3D 10.1093/infdis/92.1.40
191. PM O'Neill BK Park AE Shone JL Maggs P Roberts PA Stocks GA Biagini PG Bray P Gibbons N Berry PA Winstanley A Mukhtar R Bonar-Law S Hindley RB Bambal CB Davis M Bates TK Hart SL Gresham RM Lawrence RA Brigandi FM Gomez-delas-Heras DV Gargallo SA Ward 2009 Candidate selection and preclinical evaluation of N-tert-butyl isoquine (GSK369796), an affordable and effective 4-aminoquinoline antimalarial for the 21st century J Med Chem 52 5 1408 1415 19222165 10.1021/jm8012618 1:CAS:528:DC%2BD1MXhvFShsbo%3D
192. E Milner W McCalmont J Bhonsle D Caridha J Cobar S Gardner L Gerena D Goodine C Lanteri V Melendez N Roncal J Sousa P Wipf GS Dow 2010 Anti-malarial activity of a non-piperidine library of next-generation quinoline methanols Malar J 9 51 20149249 10.1186/1475-2875-9-51 1:CAS:528:DC%2BC3cXitFWmsro%3D
193. D De FM Krogstad FB Cogswell DJ Krogstad 1996 Aminoquinolines that circumvent resistance in Plasmodium falciparum in vitro Am J Trop Med Hyg 55 6 579 583 9025680 1:CAS:528:DyaK2sXhsVOgtbk%3D (Pubitemid 27110989)
194. SJ Hocart H Liu H Deng D De FM Krogstad DJ Krogstad 2011 4-aminoquinolines active against chloroquine-resistant Plasmodium falciparum: basis of antiparasite activity and quantitative structure-activity relationship analyses Antimicrob Agents Chemother 55 5 2233 2244 21383099 1:CAS:528:DC%2BC3MXhsFClsLzJ 10.1128/AAC.00675-10
195. RG Ridley W Hofheinz H Matile C Jaquet A Dorn R Masciadri S Jolidon WF Richter A Guenzi MA Girometta H Urwyler W Huber S Thaithong W Peters 1996 4-aminoquinoline analogs of chloroquine with shortened side chains retain activity against chloroquine-resistant Plasmodium falciparum Antimicrob Agents Chemother 40 8 1846 1854 8843292 1:CAS:528:DyaK28Xks12qsrk%3D (Pubitemid 26277804)
196. F Mzayek H Deng FJ Mather EC Wasilevich H Liu CM Hadi DH Chansolme HA Murphy BH Melek AN Tenaglia DM Mushatt AW Dreisbach JJ Lertora DJ Krogstad 2007 Randomized dose-ranging controlled trial of AQ-13, a candidate antimalarial, and chloroquine in healthy volunteers PLoS Clin Trials 2 1 e6 17213921 10.1371/journal.pctr.0020006 1:CAS:528:DC%2BD2sXhtFagsbo%3D
197. A Kumar K Srivastava SR Kumar SK Puri PM Chauhan 2010 Synthesis of new 4-aminoquinolines and quinoline-acridine hybrids as antimalarial agents Bioorg Med Chem Lett 20 23 7059 7063 20951034 1:CAS:528:DC%2BC3cXhtl2gtLbM 10.1016/j.bmcl.2010.09.107
198. S Ray PB Madrid P Catz SE LeValley MJ Furniss LL Rausch RK Guy JL DeRisi LV Iyer CE Green JC Mirsalis 2010 Development of a new generation of 4-aminoquinoline antimalarial compounds using predictive pharmacokinetic and toxicology models J Med Chem 53 9 3685 3695 20361799 1:CAS:528: DC%2BC3cXkt1Wksr8%3D 10.1021/jm100057h
199. Madrid PB, Liou AP, DeRisi JL, Guy RK (2006) Incorporation of an intramolecular hydrogen-bonding motif in the side chain of 4-aminoquinolines enhances activity against drug-resistant P. falciparum. J Med Chem 49(15):4535-4543 (Pubitemid 44162680)
200. C Biot G Glorian LA Maciejewski JS Brocard 1997 Synthesis and antimalarial activity in vitro and in vivo of a new ferrocene-chloroquine analogue J Med Chem 40 23 3715 3718 9371235 1:CAS:528:DyaK2sXmslWhs7g%3D 10.1021/jm970401y (Pubitemid 27481715)
201. F Dubar TJ Egan B Pradines D Kuter KK Ncokazi D Forge JF Paul C Pierrot H Kalamou J Khalife E Buisine C Rogier H Vezin I Forfar C Slomianny X Trivelli S Kapishnikov L Leiserowitz D Dive C Biot 2011 The antimalarial ferroquine: role of the metal and intramolecular hydrogen bond in activity and resistance ACS Chem Biol 6 3 275 287 21162558 1:CAS:528:DC%2BC3MXivFersg%3D%3D 10.1021/cb100322v
202. G Mombo-Ngoma C Supan MP Dal-Bianco MA Missinou PB Matsiegui CL Ospina Salazar S Issifou D Ter-Minassian M Ramharter M Kombila PG Kremsner B Lell 2011 Phase I randomized dose-ascending placebo-controlled trials of ferroquine-a candidate anti-malarial drug-in adults with asymptomatic Plasmodium falciparum infection Malar J 10 53 21362162 1:CAS:528:DC%2BC3MXjslKltrk%3D 10.1186/1475-2875-10-53
203. PM O'Neill SA Ward NG Berry JP Jeyadevan GA Biagini E Asadollaly BK Park PG Bray 2006 A medicinal chemistry perspective on 4-aminoquinoline antimalarial drugs Curr Top Med Chem 6 5 479 507 16719804 10.2174/156802606776743147
204. SJ Burgess JX Kelly S Shomloo S Wittlin R Brun K Liebmann DH Peyton 2010 Synthesis, structure-activity relationship, and mode-of-action studies of antimalarial reversed chloroquine compounds J Med Chem 53 17 6477 6489 20684562 1:CAS:528:DC%2BC3cXpvVaqsb8%3D 10.1021/jm1006484
205. SJ Burgess A Selzer JX Kelly MJ Smilkstein MK Riscoe DH Peyton 2006 A chloroquine-like molecule designed to reverse resistance in Plasmodium falciparum J Med Chem 49 18 5623 5625 16942036 1:CAS:528:DC%2BD28XnvFOqs7k%3D 10.1021/jm060399n (Pubitemid 44373193)
206. JX Kelly MJ Smilkstein R Brun S Wittlin RA Cooper KD Lane A Janowsky RA Johnson RA Dodean R Winter DJ Hinrichs MK Riscoe 2009 Discovery of dual function acridones as a new antimalarial chemotype Nature 459 7244 270 273 19357645 1:CAS:528:DC%2BD1MXkt1Srtrc%3D 10.1038/nature07937
207. N October ND Watermeyer V Yardley TJ Egan K Ncokazi K Chibale 2008 Reversed chloroquines based on the 3, 4-dihydropyrimidin-2(1H)-one scaffold: synthesis and evaluation for antimalarial, beta-haematin inhibition, and cytotoxic activity ChemMedChem 3 11 1649 1653 18846586 1:CAS:528: DC%2BD1cXhsV2mtb7K 10.1002/cmdc.200800172
208. Zishiri VK, Joshi MC, Hunter R, Chibale K, Smith PJ, Summers RL, Martin RE, Egan TJ (2011) Quinoline Antimalarials Containing a Dibemethin Group are Active against Chloroquine Resistant P. falciparum and Inhibit Chloroquine Transport via the Plasmodium falciparum Chloroquine-Resistance Transporter (PfCRT). J Med Chem 54(19):6956-6968
209. F Cosledan L Fraisse A Pellet F Guillou B Mordmuller PG Kremsner A Moreno D Mazier JP Maffrand B Meunier 2008 Selection of a trioxaquine as an antimalarial drug candidate Proc Natl Acad Sci USA 105 45 17579 17584 18987321 1:CAS:528:DC%2BD1cXhsVWntbnP 10.1073/pnas.0804338105
210. FW Muregi A Ishih 2010 Next-generation antimalarial drugs: hybrid molecules as a new strategy in drug design Drug Dev Res 71 1 20 32 21399701 1:CAS:528:DC%2BC3cXhslWrs7s%3D
211. AL Nelson A Purfield P McDaniel N Uthaimongkol N Buathong S Sriwichai RS Miller C Wongsrichanalai SR Meshnick 2005 pfmdr1 genotyping and in vivo mefloquine resistance on the Thai-Myanmar border Am J Trop Med Hyg 72 5 586 592 15891133 1:CAS:528:DC%2BD2MXltV2qtLs%3D (Pubitemid 41278828)
212. Picot S, Olliaro P, de Monbrison F, Bienvenu AL, Price RN, Ringwald P (2009) A systematic review and meta-analysis of evidence for correlation between molecular markers of parasite resistance and treatment outcome in falciparum malaria. Malar J 8:89
213. AC Uhlemann R McGready EA Ashley A Brockman P Singhasivanon S Krishna NJ White F Nosten RN Price 2007 Intrahost selection of Plasmodium falciparum pfmdr1 alleles after antimalarial treatment on the northwestern border of Thailand J Infect Dis 195 1 134 141 17152017 1:CAS:528:DC%2BD2sXpslSmtw%3D%3D 10.1086/509809 (Pubitemid 44958235)
214. N Chen DE Kyle C Pasay EV Fowler J Baker JM Peters Q Cheng 2003 pfcrt Allelic types with two novel amino acid mutations in chloroquine-resistant Plasmodium falciparum isolates from the Philippines Antimicrob Agents Chemother 47 11 3500 3505 14576108 1:CAS:528:DC%2BD3sXovVait7g%3D 10.1128/AAC.47.11.3500- 3505.2003 (Pubitemid 37345710)
215. RA Cooper CL Hartwig MT Ferdig 2005 pfcrt is more than the Plasmodium falciparum chloroquine resistance gene: a functional and evolutionary perspective Acta Trop 94 3 170 180 15866507 1:CAS:528:DC%2BD2MXks1agt7c%3D 10.1016/j.actatropica.2005.04.004 (Pubitemid 40720324)
216. T Hatabu M Iwagami S Kawazu N Taguchi AD Escueta EA Villacorte PT Rivera S Kano 2009 Association of molecular markers in Plasmodium falciparum crt and mdr1 with in vitro chloroquine resistance: a Philippine study Parasitol Int 58 2 166 170 19567229 1:CAS:528:DC%2BD1MXltVCqt7c%3D 10.1016/j.parint.2009.01.010
217. MC Huaman K Yoshinaga A Suryanatha N Suarsana H Kanbara 2004 Short report: polymorphisms in the chloroquine resistance transporter gene in Plasmodium falciparum isolates from Lombok, Indonesia Am J Trop Med Hyg 71 1 40 42 15238686 1:CAS:528:DC%2BD2cXmsVagurg%3D (Pubitemid 38902641)
218. P Lim S Chy F Ariey S Incardona P Chim R Sem MB Denis S Hewitt S Hoyer D Socheat O Merecreau-Puijalon T Fandeur 2003 pfcrt polymorphism and chloroquine resistance in Plasmodium falciparum strains isolated in Cambodia Antimicrob Agents Chemother 47 1 87 94 12499174 1:CAS:528:DC%2BD3sXis12hsw%3D%3D 10.1128/AAC.47.1.87-94.2003 (Pubitemid 36070347)
219. Z Yang Z Zhang X Sun W Wan L Cui X Zhang D Zhong G Yan 2007 Molecular analysis of chloroquine resistance in Plasmodium falciparum in Yunnan Province, China Trop Med Int Health 12 9 1051 1060 17875016 1:CAS:528:DC%2BD2sXht1Gqs7fM 10.1111/j.1365-3156.2007.01882.x (Pubitemid 47414938)
220. V Durrand A Berry R Sem P Glaziou J Beaudou T Fandeur 2004 Variations in the sequence and expression of the Plasmodium falciparum chloroquine resistance transporter (Pfcrt) and their relationship to chloroquine resistance in vitro Mol Biochem Parasitol 136 2 273 285 15478806 1:CAS:528:DC%2BD2cXkvV2jtLo%3D 10.1016/j.molbiopara.2004.03.016 (Pubitemid 38757996)
221. RA Cooper KD Lane B Deng J Mu JJ Patel TE Wellems X Su MT Ferdig 2007 Mutations in transmembrane domains 1, 4 and 9 of the Plasmodium falciparum chloroquine resistance transporter alter susceptibility to chloroquine, quinine and quinidine Mol Microbiol 63 1 270 282 17163969 1:CAS:528:DC%2BD2sXhsVyisbw%3D 10.1111/j.1365-2958.2006.05511.x (Pubitemid 44968124)
222. HS Nagesha GJ Casey KH Rieckmann DJ Fryauff BS Laksana JC Reeder JD Maguire JK Baird 2003 New haplotypes of the Plasmodium falciparum chloroquine resistance transporter (pfcrt) gene among chloroquine-resistant parasite isolates Am J Trop Med Hyg 68 4 398 402 12875286 1:CAS:528:DC%2BD3sXjslymtrk%3D (Pubitemid 38230637)
223. MH Coosemans L Hendrix M Barutwanayo G Butoyi E Onori 1985 Drug resistance of Plasmodium falciparum in Burundi Bull World Health Organ 63 2 331 338 3893777 1:STN:280:DyaL2M3lsFakug%3D%3D (Pubitemid 15234175)
224. JD Sexton P Deloron L Bugilimfura A Ntilivamunda M Neill 1988 Parasitologic and clinical efficacy of 25 and 50 mg/kg of chloroquine for treatment of Plasmodium falciparum malaria in Rwandan children Am J Trop Med Hyg 38 2 237 243 3281488 1:STN:280:DyaL1c7otFentg%3D%3D (Pubitemid 18086101)
225. JG de Andrade AL de Andrade ES Araujo RM Oliveira SA Silva CM Martelli F Zicker 1992 A randomized clinical trial with high dose of chloroquine for treatment of Plasmodium falciparum malaria in Brazil Rev Inst Med Trop Sao Paulo 34 5 467 473 1342112 10.1590/S0036-46651992000500015
226. PG Kremsner S Winkler C Brandts S Neifer U Bienzle W Graninger 1994 Clindamycin in combination with chloroquine or quinine is an effective therapy for uncomplicated Plasmodium falciparum malaria in children from Gabon J Infect Dis 169 2 467 470 8106787 1:STN:280:DyaK2c7kvFentg%3D%3D 10.1093/infdis/169.2. 467 (Pubitemid 24045618)
227. E Wildling L Jenne W Graninger U Bienzle PG Kremsner 1994 High dose chloroquine versus micronized halofantrine in chloroquine-resistant Plasmodium falciparum malaria J Antimicrob Chemother 33 4 871 875 8056708 1:STN:280:DyaK2czjsVagsQ%3D%3D 10.1093/jac/33.4.871 (Pubitemid 24149825)
228. W Metzger B Mordmuller W Graninger U Bienzle PG Kremsner 1995 Sulfadoxine/pyrimethamine or chloroquine/clindamycin treatment of Gabonese school children infected with chloroquine resistant malaria J Antimicrob Chemother 36 4 723 728 8591949 1:CAS:528:DyaK2MXpsVGgtbY%3D 10.1093/jac/36.4.723
229. N Howard N Durrani S Sanda K Beshir R Hallett M Rowland 2011 Clinical trial of extended-dose chloroquine for treatment of resistant falciparum malaria among Afghan refugees in Pakistan Malar J 10 171 21699697 1:CAS:528: DC%2BC3MXosVyqurg%3D 10.1186/1475-2875-10-171
230. PE Kofoed F Lopez P Johansson A Sandstrom K Hedegaard P Aaby L Rombo 2002 Treatment of children with Plasmodium falciparum malaria with chloroquine in Guinea-Bissau Am J Trop Med Hyg 67 1 28 31 12363060 1:CAS:528: DC%2BD38XnvF2itr4%3D (Pubitemid 35034316)
231. PE Kofoed F Co P Johansson F Dias C Cabral K Hedegaard P Aaby L Rombo 2002 Treatment of uncomplicated malaria in children in Guinea-Bissau with chloroquine, quinine, and sulfadoxine-pyrimethamine Trans R Soc Trop Med Hyg 96 3 304 309 12174785 10.1016/S0035-9203(02)90107-0 (Pubitemid 34785071)
232. PE Kofoed J Ursing A Poulsen A Rodrigues Y Bergquist P Aaby L Rombo 2007 Different doses of amodiaquine and chloroquine for treatment of uncomplicated malaria in children in Guinea-Bissau: implications for future treatment recommendations Trans R Soc Trop Med Hyg 101 3 231 238 16904718 1:CAS:528:DC%2BD2sXjs1GmtL4%3D 10.1016/j.trstmh.2006.05.008 (Pubitemid 46043055)