Addressing the malaria drug resistance challenge using flow cytometry to discover new antimalarials

被引:22
作者
Grimberg, Brian T. [1 ]
Jaworska, Maria M. [2 ]
Hough, Lindsay B. [3 ]
Zimmerman, Peter A. [1 ]
Phillips, James G. [2 ]
机构
[1] Case Western Reserve Univ, Ctr Global Hlth & Dis, Cleveland, OH 44106 USA
[2] Curragh Chem Inc, Sherwin Williams Cradle, Valley View, OH 44125 USA
[3] Albany Med Coll, Ctr Neuropharmacol & Neurosci, Albany, NY 12208 USA
关键词
Cytometry; Malarial; Drug discovery; PARASITE PLASMODIUM-FALCIPARUM; IN-VITRO; CHLOROQUINE RESISTANCE; HEMOGLOBIN DEGRADATION; PROTEIN-KINASES; INHIBITORS; AMPLIFICATION; HALOFANTRINE; SENSITIVITY; MEFLOQUINE;
D O I
10.1016/j.bmcl.2009.07.095
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
A new flow cytometry method that uses an optimized DNA and RNA staining strategy to monitor the growth and development of the Plasmodium falciparum strain W2mef has been used in a pilot study and has identified Bay 43-9006 1, SU 11274 2, and TMC 125 5 as compounds that exhibit potent (<1 mu M) overall and ring stage in vitro antimalarial activity. (C) 2009 Elsevier Ltd. All rights reserved.
引用
收藏
页码:5452 / 5457
页数:6
相关论文
共 46 条
[1]   Evaluation of selected Sudanese medicinal plants for their in vitro activity against hemoflagellates, selected bacteria, HIV-1-RT and tyrosine kinase inhibitory, and for cytotoxicity [J].
Ali, H ;
König, GM ;
Khalid, SA ;
Wright, AD ;
Kaminsky, R .
JOURNAL OF ETHNOPHARMACOLOGY, 2002, 83 (03) :219-228
[2]  
ANDREWS CW, 2004, Patent No. 2004014899
[3]   Potencies of human immunodeficiency virus protease inhibitors in vitro against Plasmodium falciparum and in vivo against murine malaria [J].
Andrews, KT ;
Fairlie, DP ;
Madala, PK ;
Ray, J ;
Wyatt, DM ;
Hilton, PM ;
Melville, LA ;
Beattie, L ;
Gardiner, DL ;
Reid, RC ;
Stoermer, MJ ;
Skinner-Adams, T ;
Berry, C ;
McCarthy, JS .
ANTIMICROBIAL AGENTS AND CHEMOTHERAPY, 2006, 50 (02) :639-648
[4]   Synthesis routes towards the farnesyl protein transferase inhibitor ZARNESTRA™ [J].
Angibaud, PR ;
Venet, MG ;
Filliers, W ;
Broeckx, R ;
Ligny, YA ;
Muller, P ;
Poncelet, VS ;
End, DW .
EUROPEAN JOURNAL OF ORGANIC CHEMISTRY, 2004, 2004 (03) :479-486
[5]  
Aregawi M., 2008, WORLD MALARIA REPORT
[6]   High-throughput Plasmodium falciparum growth assay for malaria drug discovery [J].
Baniecki, Mary Lynn ;
Wirth, Dyann F. ;
Clardy, Jon .
ANTIMICROBIAL AGENTS AND CHEMOTHERAPY, 2007, 51 (02) :716-723
[7]   The Met kinase inhibitor SU11274 exhibits a selective inhibition pattern toward different receptor mutated variants [J].
Berthou, S ;
Aebersold, DM ;
Schmidt, LS ;
Stroka, D ;
Heigl, C ;
Streit, B ;
Stalder, D ;
Gruber, G ;
Liang, CX ;
Howlett, AR ;
Candinas, D ;
Greiner, RH ;
Lipson, KE ;
Zimmer, Y .
ONCOGENE, 2004, 23 (31) :5387-5393
[8]   Synthesis and SAR of 4-(3-hydroxyphenylamino)pyrrolo-[2,1-f][1,2,4]triazine based VEGFR-2 kinase inhibitors [J].
Borzilleri, RM ;
Cai, ZW ;
Ellis, C ;
Fargnoli, J ;
Fura, A ;
Gerhardt, T ;
Goyal, B ;
Hunt, JT ;
Mortillo, S ;
Qian, LG ;
Tokarski, J ;
Vyas, V ;
Wautlet, B ;
Zheng, XP ;
Bhide, RS .
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2005, 15 (05) :1429-1433
[9]   Evaluation of the activities of pyrimethamine analogs against Plasmodium vivax and Plasmodium falciparum dihydrofolate reductase-thymidylate synthase using in vitro enzyme inhibition and bacterial complementation assays [J].
Bunyarataphan, Sasinee ;
Leartsakulpanich, Ubolsree ;
Taweechai, Supannee ;
Tarnchompoo, Bongkoch ;
Kamchonwongpaisan, Sumalee ;
Yuthavong, Yongyuth .
ANTIMICROBIAL AGENTS AND CHEMOTHERAPY, 2006, 50 (11) :3631-3637
[10]   Identification and activity of a series of azole-based compounds with lactate dehydrogenase-directed anti-malarial activity [J].
Cameron, A ;
Read, J ;
Tranter, R ;
Winter, VJ ;
Sessions, RB ;
Brady, RL ;
Vivas, L ;
Easton, A ;
Kendrick, H ;
Croft, SL ;
Barros, D ;
Lavandera, JL ;
Martin, JJ ;
Risco, F ;
García-Ochoa, S ;
Gamo, FJ ;
Sanz, L ;
Leon, L ;
Ruiz, JR ;
Gabarro, R ;
Mallo, A ;
de las Heras, FG .
JOURNAL OF BIOLOGICAL CHEMISTRY, 2004, 279 (30) :31429-31439