排序方式: 共有5条查询结果,搜索用时 15 毫秒
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Wanwipa Ittarat Wichai Pornthanakasem Mathirut Mungthin Nantana Suwandittakul Saovanee Leelayoova Bongkoch Tarnchompoo Yongyuth Yuthavong Darin Kongkasuriyachai Ubolsree Leartsakulpanich 《Parasitology international》2018,67(6):787-792
Malaria caused by an infection of Plasmodium knowlesi can result in high parasitemia and deaths. Therefore, effective and prompt treatment is necessary to reduce morbidity and mortality. The study aims to characterize P. knowlesi dihydrofolate reductase-thymidylate synthase enzyme (PkDHFR-TS) and its sensitivity to antifolates. The putative Pkdhfr gene was PCR amplified from field isolates collected from the Southern Thailand. Molecular analysis showed 11 polymorphisms in the dhfr domain of the bifunctional dhfr-ts gene. Of these, 1 polymorphism was a non-synonymous substitution (R34L) that had previously been reported but not associated with antifolate resistance. The recombinant PkDHFR-TS enzyme was found to be sensitive to standard antifolates—pyrimethamine and cycloguanil—as well as P218, a registered candidate drug currently first in human clinical trial. Results suggest that antifolates class of compounds should be effective against P. knowlesi infection. 相似文献
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Maitarad P Saparpakorn P Hannongbua S Kamchonwongpaisan S Tarnchompoo B Yuthavong Y 《Journal of enzyme inhibition and medicinal chemistry》2009,24(2):471-479
Comparative molecular field analysis (CoMFA) was performed on twenty-three pyrimethamine (pyr) derivatives active against quadruple mutant type (Asn51Ile, Cys59Arg, Ser108Asn, Ile164Leu) dihydrofolate reductase of Plasmodium falcipaarum (PfDHFR). The represented CoMFA models were evaluated based on the various three different probe atoms, C(sp3) (+1), O(sp3) (-1) and H (+1), resulting in the best model with combined three types of probe atoms. The statistical results were r(2)(cv) = 0.702, S(press) = 0.608, r(2)(nv) = 0.980, s = 0.156, and r(2)(test-set) = 0.698 which can explain steric contribution of about 50%. In addition, an understanding of particular interaction energy between inhibitor and surrounding residues in the binding pocket was performed by using MP2/6-31G(d,p) quantum chemical calculations. The obtained results clearly demonstrate that Asn108 is the cause of pyr resistance with the highest repulsive interaction energy. 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. 相似文献
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Phornphimon Maitarad Patchreenart Saparpakorn Sumalee Kamchonwongpaisan Bongkoch Tarnchompoo Yongyuth Yuthavong 《Journal of enzyme inhibition and medicinal chemistry》2013,28(2):471-479
Comparative molecular field analysis (CoMFA) was performed on twenty-three pyrimethamine (pyr) derivatives active against quadruple mutant type (Asn51Ile, Cys59Arg, Ser108Asn, Ile164Leu) dihydrofolate reductase of Plasmodium falcipaarum (PfDHFR). The represented CoMFA models were evaluated based on the various three different probe atoms, Csp3 (+1), Osp3 ( ? 1) and H (+1), resulting in the best model with combined three types of probe atoms. The statistical results were = 0.702, Spress = 0.608, = 0.980, s = 0.156, and = 0.698 which can explain steric contribution of about 50%. In addition, an understanding of particular interaction energy between inhibitor and surrounding residues in the binding pocket was performed by using MP2/6-31G(d,p) quantum chemical calculations. The obtained results clearly demonstrate that Asn108 is the cause of pyr resistance with the highest repulsive interaction energy. 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. 相似文献
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Jeffrey S. A. Stringer Michelle S. McConnell James Kiarie Omotayo Bolu Thanomsak Anekthananon Tavatchai Jariyasethpong Dara Potter Winnie Mutsotso Craig B. Borkowf Dorothy Mbori-Ngacha Peter Muiruri John Odero Ong'ech Isaac Zulu Lungowe Njobvu Bongkoch Jetsawang Sonal Pathak Marc Bulterys Nathan Shaffer Paul J. Weidle 《PLoS medicine》2010,7(2)
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Bongkoch Turathum Kulnasan Saikhun Parisatcha Sangsuwan Yindee Kitiyanant 《Reproductive biology and endocrinology : RB&E》2010,8(1):70
Background
Cryopreservation of oocytes, which is an interesting procedure to conserve female gametes, is an essential part of reproductive biotechnology. The objective of the present study was to investigate the effects of vitrification on nuclear maturation, ultrastructural changes and gene expression of canine oocytes. 相似文献
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