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Genomes and Genes | Yongyuth YuthavongSummaryCountry: Thailand Publications
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Publications
Development of 2,4-diaminopyrimidines as antimalarials based on inhibition of the S108N and C59R+S108N mutants of dihydrofolate reductase from pyrimethamine-resistant Plasmodium falciparumBongkoch Tarnchompoo
National Center for Genetic Engineering and Biotechnology, National Science and Technology Development Agency, Rama 6 Road, Bangkok 10400, Thailand
J Med Chem 45:1244-52. 2002..Some of these compounds show good antimalarial activities against pyrimethamine-resistant P. falciparum containing the mutant DHFRs with low cytotoxicity to three mammalian cell lines...- Malarial (Plasmodium falciparum) dihydrofolate reductase-thymidylate synthase: structural basis for antifolate resistance and development of effective inhibitorsY Yuthavong
National Centre for Genetic Engineering and Biotechnology, National Science and Technology Development Agency, Science Park, Pathumthani 12120, Thailand
Parasitology 130:249-59. 2005..falciparum bearing the mutant enzymes... - Basis for antifolate action and resistance in malariaYongyuth Yuthavong
National Center for Genetic Engineering and Biotechnology, National Science and Technology Development Agency, Rama 6 Road, 10400, Bangkok, Thailand
Microbes Infect 4:175-82. 2002..New synergistic combinations of drugs targeting DHFR and dihydropteroate synthase may be employed, with new provisions against development of resistance... - Crystal structure of dihydrofolate reductase from Plasmodium vivax: pyrimethamine displacement linked with mutation-induced resistancePalangpon Kongsaeree
Department of Chemistry and Center for Protein Structure and Function, Faculty of Science, Mahidol University, Rama 6 Road, Bangkok 10400, Thailand
Proc Natl Acad Sci U S A 102:13046-51. 2005..These structural insights suggest a general approach for developing new generations of antimalarial DHFR inhibitors that, by only occupying substrate space of the active site, would retain binding affinity with the mutant enzymes... - The role of tryptophan-48 in catalysis and binding of inhibitors of Plasmodium falciparum dihydrofolate reductaseSumalee Kamchonwongpaisan
National Center for Genetic Engineering and Biotechnology, National Science and Technology Development Agency, Pathumthani, Thailand
Int J Parasitol 37:787-93. 2007..Due to its conserved nature, Trp48 of PfDHFR is a potential site for interaction with antimalarial inhibitors which would not be compromised by its mutations... - Formation of catalytically active cross-species heterodimers of thymidylate synthase from Plasmodium falciparum and Plasmodium vivaxManee Chanama
Department of Microbiology, Faculty of Public Health, Mahidol University, Bangkok, 10400, Thailand
Mol Biol Rep 38:1029-37. 2011..falciparum and P. vivax. This is the first report to demonstrate that the TS subunit interface between Plasmodium species is sufficiently conserved to allow formation of fully active cross-species heterodimer... - 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 assaysSasinee Bunyarataphan
National Center for Genetic Engineering and Biotechnology, 113 Paholyothin Rd, Klong 1, Klong Luang, Pathumthani 12120, Thailand
Antimicrob Agents Chemother 50:3631-7. 2006..This rapid and convenient drug screening system should be useful for development of new antifolates against P. vivax, for which a continuous culture system is not yet available... - Stoichiometric selection of tight-binding inhibitors by wild-type and mutant forms of malarial (Plasmodium falciparum) dihydrofolate reductaseSumalee Kamchonwongpaisan
National Centre for Genetic Engineering and Biotechnology, National Science and Technology Development Agency, Thailand Science Park, Pathumthani 12120, Thailand
Anal Chem 77:1222-7. 2005.... - Insights into antifolate resistance from malarial DHFR-TS structuresJirundon Yuvaniyama
Department of Biochemistry, Faculty of Science, Mahidol University, Rama 6 Road, Bangkok 10400, Thailand
Nat Struct Biol 10:357-65. 2003..These features provide possible approaches for the design of new drugs to overcome antifolate resistance... - Inhibitors of multiple mutants of Plasmodium falciparum dihydrofolate reductase and their antimalarial activitiesSumalee Kamchonwongpaisan
National Center for Genetic Engineering and Biotechnology, National Science and Technology Development Agency, Pathumthani 12120, Thailand
J Med Chem 47:673-80. 2004..These compounds in the Pyr and Cyc series exhibit low and moderate cytotoxicity to nontumor (Vero) and tumor (KB, BC) cell lines. Some of these inhibitors are therefore potential candidates for further development as antimalarials... - Serine hydroxymethyltransferase from Plasmodium vivax is different in substrate specificity from its homologuesKittipat Sopitthummakhun
Department of Biochemistry and Center for Excellence in Protein Structure and Function, Faculty of Science, Mahidol University, Bangkok, Thailand
FEBS J 276:4023-36. 2009..The substrate specificity difference between PvSHMT and the mammalian enzyme indicates the dissimilarity between their active sites, which could be exploited for the development of specific inhibitors against PvSHMT... - Transgenic Plasmodium parasites stably expressing Plasmodium vivax dihydrofolate reductase-thymidylate synthase as in vitro and in vivo models for antifolate screeningVoravuth Somsak
Protein Ligand Engineering and Molecular Biology Laboratory, National Center for Genetic Engineering and Biotechnology BIOTEC, National Science and Technology Development Agency, Thailand Science Park, Pathumthani 12120, Thailand
Malar J 10:291. 2011..vivax parasites... - Target guided synthesis of 5-benzyl-2,4-diamonopyrimidines: their antimalarial activities and binding affinities to wild type and mutant dihydrofolate reductases from Plasmodium falciparumChawanee Sirichaiwat
National Center for Genetic Engineering and Biotechnology, National Science and Technology Development Agency, 113 Thailand Science Park, Pahonyothin Road, Klong 1, Klongluang, Pathumtani 12120, Thailand
J Med Chem 47:345-54. 2004..In addition, some compounds with 6-alkyl substituents showed relatively less decrease in binding constants with the mutant enzymes and relatively good antimalarial activities against the parasites bearing the mutant enzymes... - Selection of drug resistant mutants from random library of Plasmodium falciparum dihydrofolate reductase in Plasmodium berghei modelWachiraporn Tipsuwan
National Center for Genetic Engineering and Biotechnology BIOTEC, National Science and Technology Development Agency, 113 Thailand Science Park, Pathumthani 12120, Thailand
Malar J 10:119. 2011..Therefore, identification of possible new Plasmodium falciparum dihydrofolate reductase (PfDHFR) mutants that confer resistance to antifolate drugs is essential in the process of antifolate anti-malarial drug development... - Crystallization and preliminary crystallographic studies of dihydrofolate reductase-thymidylate synthase from Trypanosoma cruzi, the Chagas disease pathogenPenchit Chitnumsub
National Center for Genetic Engineering and Biotechnology, Pathumthani, Thailand
Acta Crystallogr Sect F Struct Biol Cryst Commun 65:1175-8. 2009..1, 2.6 and 2.8 angstrom resolution, respectively. Crystals belonging to the two different space groups were suitable for structure determination... - Conflicting requirements of Plasmodium falciparum dihydrofolate reductase mutations conferring resistance to pyrimethamine-WR99210 combinationDeanpen Japrung
BIOTEC, National Science and Technology Development Agency, 113 Paholyothin Road, Klong 1, Klong Luang, Pathumthani 12120, Thailand
Antimicrob Agents Chemother 51:4356-60. 2007..Thus, a combination of inhibitors from these two drug classes should be effective in impeding the emergence of P. falciparum resistance to antifolates... - Particular interaction between pyrimethamine derivatives and quadruple mutant type dihydrofolate reductase of Plasmodium falciparum: CoMFA and quantum chemical calculations studiesPhornphimon Maitarad
Department of Chemistry, Faculty of Science, Kasetsart University, Bangkok, Thailand
J Enzyme Inhib Med Chem 24:471-9. 2009..Therefore, CoMFA and particular interaction energy analyses can be useful for identifying the structural features of potent pyr derivatives active against quadruple mutant type PfDHFR... - Immobilization of malarial (Plasmodium falciparum) dihydrofolate reductase for the selection of tight-binding inhibitors from combinatorial libraryChawanee Thongpanchang
National Center for Genetic Engineering and Biotechnology, National Science and Technology Development Agency, Klong 1, Klongluang, Pathumtani 12120, Thailand
Anal Chem 79:5006-12. 2007..Results could be confirmed by quantitative analysis of the bound ligands released from the enzyme by guanidine hydrochloride treatment... - Characterization, crystallization and preliminary X-ray analysis of bifunctional dihydrofolate reductase-thymidylate synthase from Plasmodium falciparumPenchit Chitnumsub
BIOTEC, National Science and Technology Development Agency, Thailand Science Park, Pathumthani 12120, Thailand
Acta Crystallogr D Biol Crystallogr 60:780-3. 2004..6 A3 Da-1). The use of a particular type of baby oil in the microbatch setup appeared to be beneficial to PfDHFR-TS crystallization and a preliminary comparison with another commonly used oil is described... - Characterization of Plasmodium falciparum serine hydroxymethyltransferase-A potential antimalarial targetSomchart Maenpuen
Department of Biochemistry and Center for Excellence in Protein Structure and Function, Faculty of Science, Mahidol University, Rama 6 Road, Bangkok, Thailand
Mol Biochem Parasitol 168:63-73. 2009..Kinetic data in combination with expression result support the proposal of SHMT reaction being a regulatory step for dTMP cycle. This finding suggests that PfSHMT can be a potential target for antimalarial chemotherapy... - Mutational analysis of Plasmodium falciparum dihydrofolate reductase: the role of aspartate 54 and phenylalanine 223 on catalytic activity and antifolate bindingWorachart Sirawaraporn
Department of Biochemistry, Faculty of Science, Mahidol University, Rama 6 Rd, 10400, Bangkok 10400, Thailand
Mol Biochem Parasitol 121:185-93. 2002..Our data not only indicate the importance of Asp-54 of pfDHFR in catalysis and inhibitor binding, but also provide evidence that infer the potentially crucial function of the C-terminal portion of pfDHFR domain... - Folate metabolism as a source of molecular targets for antimalarialsYongyuth Yuthavong
National Centre for Genetic Engineering and Biotechnology, Thailand
Future Microbiol 1:113-25. 2006.... - Cloning and characterization of Plasmodium vivax serine hydroxymethyltransferaseUbolsree Leartsakulpanich
National Center for Genetic Engineering and Biotechnology, 113 Paholyothin Road, Klong 1, Klong Luang, Pathumthani 12120, Thailand
Parasitol Int 57:223-8. 2008..Sequencing of 12 P. vivax isolates revealed limited polymorphisms in 3 noncoding regions. Its biological function is also reported... - Characterization of human malaria parasite Plasmodium falciparum eIF4E homologue and mRNA 5' cap statusPhilip J Shaw
National Center for Genetic Engineering and Biotechnology BIOTEC, National Science and Technology Development Agency, 113 Pahonyothin Road, Klong 1, Klong Luang, Pathumthani 12120, Thailand
Mol Biochem Parasitol 155:146-55. 2007..The putatively uncapped nuclear transcripts may represent a class of mRNAs targeted for storage and cap removal... - Trypanosomal dihydrofolate reductase reveals natural antifolate resistanceJarunee Vanichtanankul
National Center for Genetic Engineering and Biotechnology, National Science and Technology Development Agency, Klong Luang, Pathumthani, Thailand
ACS Chem Biol 6:905-11. 2011..Natural resistance to antifolates of TbDHFR can therefore be explained, and potential antifolate chemotherapy of trypanosomiasis should be possible taking this into account... - Effect of N-terminal truncation of Plasmodium falciparum dihydrofolate reductase on dihydrofolate reductase and thymidylate synthase activityJantanee Wattanarangsan
National Center for Genetic Engineering and Biotechnology, National Science and Technology Development Agency, Pathumthani 12120, Thailand
Mol Biochem Parasitol 126:97-102. 2003 - Novel antifolate resistant mutations of Plasmodium falciparum dihydrofolate reductase selected in Escherichia coliSudsanguan Chusacultanachai
National Center for Genetic Engineering and Biotechnology, National Science and Technology Development Agency, 10400, Bangkok, Thailand
Mol Biochem Parasitol 120:61-72. 2002..Kinetic analysis of these mutants suggested that apart from the active site residues that are crucial for DHFR activity, residues remote from the binding pocket also play essential roles in substrate and inhibitor binding... - Flow cytometric enumeration of Plasmodium berghei-infected red blood cells stained with SYBR Green IVoravuth Somsak
National Center for Genetic Engineering and Biotechnology, National Science and Technology Development Agency, 113 Thailand Science Park, Pathumthani 12120, Thailand
Acta Trop 122:113-8. 2012..The SYBR Green I flow cytometric protocol is thus a rapid and precise tool for high-throughput in vivo antimalarial drug screening... - Artemisinin effectiveness in erythrocytes is reduced by heme and heme-containing proteinsNapawan Ponmee
National Center for Genetic Engineering and Biotechnology, National Science and Technology Development Agency, 113 Thailand Science Park, Klong Luang, Pathumthani 12120, Thailand
Biochem Pharmacol 74:153-60. 2007.... - Cloning and heterologous expression of Plasmodium ovale dihydrofolate reductase-thymidylate synthase geneSrisuda Tirakarn
Department of Chemistry, Mahidol University, Rama 6 Road, Bangkok 10400, Thailand
Parasitol Int 61:324-32. 2012..Importantly, the PoDHFR from Thai isolate EU266602 remains sensitive to the antimalarials pyrimethamine and cycloguanil, in contrast to P. falciparum and P. vivax isolates where resistance to these drugs is widespread... - Random mutagenesis strategies for construction of large and diverse clone libraries of mutated DNA fragmentsSudsanguan Chusacultanachai
National Center for Genetic Engineering and Biotechnology, National Science and Technology Development Agency, Science Park, Pathumthani, Thailand
Methods Mol Biol 270:319-34. 2004..After plasmid DNA template encoding wild-type sequence is eliminated from the reaction by DpnI digestion, the pool of mutagenized plasmids can then be used directly in screening procedures... - Molecular characterization of dihydrofolate reductase in relation to antifolate resistance in Plasmodium vivaxUbolsree Leartsakulpanich
National Centre for Genetic Engineering and Biotechnology, National Science and Technology Development Agency, Rama 6 Road, 10400, Bangkok, Thailand
Mol Biochem Parasitol 119:63-73. 2002..Data on kinetic parameters and inhibitory constant suggest that the wild-type P. vivax is susceptible to antimalarial antifolates and that point mutations in the DHFR domain of P. vivax are responsible for antifolate resistance... - Subunit complementation of thymidylate synthase in Plasmodium falciparum bifunctional dihydrofolate reductase-thymidylate synthaseManee Chanama
Department of Microbiology, Faculty of Public Health, Mahidol University, Rajvithi Road, Bangkok 10400, Thailand
Mol Biochem Parasitol 139:83-90. 2005..falciparum DHFR-TS... - 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 falciparumTirayut Vilaivan
Organic Synthesis Research Unit, Department of Chemistry, Faculty of Science, Chulalongkorn University, Phayathai Road, Patumwan, Bangkok 10330, Thailand
Bioorg Med Chem 11:217-24. 2003....