Immobilization of Malarial (Plasmodium falciparum) Dihydrofolate Reductase for the Selection of Tight-Binding Inhibitors from Combinatorial Library

2007 ◽  
Vol 79 (13) ◽  
pp. 5006-5012 ◽  
Author(s):  
Chawanee Thongpanchang ◽  
Supannee Taweechai ◽  
Sumalee Kamchonwongpaisan ◽  
Yongyuth Yuthavong ◽  
Yodhathai Thebtaranonth
Keyword(s):  
Plasmodium Falciparum ◽  
Dihydrofolate Reductase ◽  
Combinatorial Library ◽  
Tight Binding ◽  
Selection Of ◽  
Binding Inhibitors

Stoichiometric Selection of Tight-Binding Inhibitors by Wild-Type and Mutant Forms of Malarial (Plasmodiumfalciparum) Dihydrofolate Reductase

2005 ◽  
Vol 77 (5) ◽  
pp. 1222-1227 ◽  
Author(s):  
Sumalee Kamchonwongpaisan ◽  
Jarunee Vanichtanankul ◽  
Bongkoch Tarnchompoo ◽  
Jirundon Yuvaniyama ◽  
Supannee Taweechai ◽  
...  
Keyword(s):  
Dihydrofolate Reductase ◽  
Tight Binding ◽  
Wild Type ◽  
Mutant Forms ◽  
Selection Of ◽  
Binding Inhibitors

scholarly journals In vitro activities of novel antifolate drug combinations against Plasmodium falciparum and human granulocyte CFUs.

1995 ◽  
Vol 39 (4) ◽  
pp. 948-952 ◽  
Author(s):  
P A Winstanley ◽  
E K Mberu ◽  
I S Szwandt ◽  
A M Breckenridge ◽  
W M Watkins
Keyword(s):  
Plasmodium Falciparum ◽  
Dihydrofolate Reductase ◽  
Bone Marrow Cells ◽  
Rank Order ◽  
Drug Combinations ◽  
Reductase Inhibitors ◽  
Potent Drug ◽  
Dihydrofolate Reductase Inhibitors ◽  
Selection Of

The potency of antimalarial dihydrofolate reductase inhibitors, alone and in synergistic combination with dihydropteroate synthetase inhibitors, against the Kenyan K39 strain of Plasmodium falciparum (pyrimethamine resistant) and against normal replicating human bone marrow cells in in vitro culture has been studied. Therapeutic indices and rank order of synergistic potency were derived. Trimethoprim, pyrimethamine, and the quinazolines WR159412 and WR158122 had the smallest therapeutic indices (1.39, 4.38, 2.56, and 90.0, respectively), while the three triazines clociguanil, WR99210, and chlorcycloguanil had the largest (3,562, 3,000, and 2,000, respectively). In rank order of decreasing activity against P. falciparum, the six most potent drug combinations were WR99210-dapsone, chlorcycloguanil-dapsone, WR158122-dapsone, WR159412-dapsone, WR159412-sulfamethoxazole, and chlorcycloguanil-sulfamethoxazole; pyrimethamine-sulfadoxine was the least potent combination. These experiments form a basis for the selection of rapidly eliminated antifolate combinations for further clinical testing.

Tight-binding inhibitors efficiently inactivate both reaction centers of monomeric Plasmodium falciparum glyoxalase 1

FEBS Journal ◽  
2012 ◽  
Vol 279 (14) ◽  
pp. 2568-2578 ◽  
Author(s):  
Miriam Urscher ◽  
Swati S. More ◽  
Romy Alisch ◽  
Robert Vince ◽  
Marcel Deponte
Keyword(s):  
Plasmodium Falciparum ◽  
Tight Binding ◽  
Reaction Centers ◽  
Glyoxalase 1 ◽  
Binding Inhibitors

scholarly journals Selection of drug resistant mutants from random library of Plasmodium falciparum dihydrofolate reductase in Plasmodium berghei model

2011 ◽  
Vol 10 (1) ◽  
pp. 119 ◽  
Author(s):  
Wachiraporn Tipsuwan ◽  
Somdet Srichairatanakool ◽  
Sumalee Kamchonwongpaisan ◽  
Yongyuth Yuthavong ◽  
Chairat Uthaipibull
Keyword(s):  
Plasmodium Falciparum ◽  
Dihydrofolate Reductase ◽  
Plasmodium Berghei ◽  
Drug Resistant ◽  
Random Library ◽  
Resistant Mutants ◽  
Selection Of

scholarly journals In Vitro Selection of Highly Modified Cyclic Peptides That Act as Tight Binding Inhibitors

2012 ◽  
Vol 134 (25) ◽  
pp. 10469-10477 ◽  
Author(s):  
Yollete V. Guillen Schlippe ◽  
Matthew C. T. Hartman ◽  
Kristopher Josephson ◽  
Jack W. Szostak
Keyword(s):  
Cyclic Peptides ◽  
In Vitro Selection ◽  
Tight Binding ◽  
Selection Of ◽  
Binding Inhibitors

Synthesis of Solution-Phase Combinatorial Library of 4,6-Diamino-1,2-dihydro-1,3,5-triazine and Identification of New Leads Against A16V+S108T Mutant Dihydrofolate Reductase of Plasmodium falciparum

2003 ◽  
Vol 11 (2) ◽  
pp. 217-224 ◽  
Author(s):  
Tirayut Vilaivan ◽  
Neungruthai Saesaengseerung ◽  
Deanpen Jarprung ◽  
Sumalee Kamchonwongpaisan ◽  
Worachart Sirawaraporn ◽  
...  
Keyword(s):  
Plasmodium Falciparum ◽  
Dihydrofolate Reductase ◽  
Combinatorial Library ◽  
Solution Phase
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