WR99210
WR99210结构式
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常用名 | WR99210 | 英文名 | WR99210 |
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| CAS号 | 47326-86-3 | 分子量 | 394.68400 | |
| 密度 | N/A | 沸点 | N/A | |
| 分子式 | C14H18Cl3N5O2 | 熔点 | N/A | |
| MSDS | 中文版 美版 | 闪点 | N/A |
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Development of a genetic tool for functional screening of anti-malarial bioactive extracts in metagenomic libraries.
Malaria Journal 14 , 233, (2015) The chemical treatment of Plasmodium falciparum for human infections is losing efficacy each year due to the rise of resistance. One possible strategy to find novel anti-malarial drugs is to access the largest reservoir of genomic biodiversity source on earth... |
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Functional analysis of Plasmodium vivax dihydrofolate reductase-thymidylate synthase genes through stable transformation of Plasmodium falciparum.
PLoS ONE 7(7) , e40416, (2012) Mechanisms of drug resistance in Plasmodium vivax have been difficult to study partially because of the difficulties in culturing the parasite in vitro. This hampers monitoring drug resistance and research to develop or evaluate new drugs. There is an urgent ... |
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Novel Saccharomyces cerevisiae screen identifies WR99210 analogues that inhibit Mycobacterium tuberculosis dihydrofolate reductase.
Antimicrob. Agents Chemother. 46(11) , 3362-9, (2002) The ongoing selection of multidrug-resistant strains of Mycobacterium tuberculosis has markedly reduced the effectiveness of the standard treatment regimens. Thus, there is an urgent need for new drugs that are potent inhibitors of M. tuberculosis, that exhib... |
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Identification and analysis of dihydrofolate reductase alleles from Plasmodium falciparum present at low frequency in polyclonal patient samples.
Am. J. Trop. Med. Hyg. 61(1) , 131-40, (1999) As resistance to chloroquine spreads in sub-Saharan Africa, pyrimethamine plus sulfadoxine (PSD) is increasingly used as a first-line treatment for falciparum malaria. Populations of Plasmodium falciparum (Pf) resistant to PSD have been selected quickly in ot... |
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Novel alleles of the Plasmodium falciparum dhfr highly resistant to pyrimethamine and chlorcycloguanil, but not WR99210.
Mol. Biochem. Parasitol. 117(1) , 91-102, (2001) We have expressed dhfr alleles of Plasmodium falciparum in the budding yeast, Saccharomyces cerevisiae, and used this yeast model to identify single amino acid substitutions that confer high level pyrimethamine resistance on the background of the triple mutan... |
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Molecular modeling of wild-type and antifolate resistant mutant Plasmodium falciparum DHFR.
Biophys. Chem. 98(3) , 287-300, (2002) The development of drug resistance is reducing the efficiency of antifolates as antimalarials. This phenomenon has been linked to the occurrence of mutations in the parasite's dihydrofolate reductase (DHFR). In this way, the resistance to pyrimethamine and cy... |
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In silico structure-based design of a novel class of potent and selective small peptide inhibitor of Mycobacterium tuberculosis Dihydrofolate reductase, a potential target for anti-TB drug discovery.
Mol. Divers. 14(3) , 595-604, (2010) The worldwide TB structural genomics initiative has identified several new drug targets for Mycobacterium tuberculosis (M. tb). Dihydrofolate reductase (DHFR) catalyzes the NADPH-dependent reduction of dihydrofolate to tetrahydrofolate that is essential for D... |
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Translational up-regulation of antifolate drug targets in the human malaria parasite Plasmodium falciparum upon challenge with inhibitors.
Mol. Biochem. Parasitol. 136(1) , 63-70, (2004) The thymidylate cycle in Plasmodium falciparum is essential for cell growth and replication, and dihydrofolate reductase (DHFR), a key enzyme in this cycle, is the target of important antimalarial drugs such as pyrimethamine and cycloguanil. Following previou... |
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Pyrimethamine and WR99210 exert opposing selection on dihydrofolate reductase from Plasmodium vivax.
Proc. Natl. Acad. Sci. U. S. A. 99(20) , 13137-41, (2002) Plasmodium vivax is a major public health problem in Asia and South and Central America where it is most prevalent. Until very recently, the parasite has been effectively treated with chloroquine, but resistance to this drug has now been reported in several a... |
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The role of tryptophan-48 in catalysis and binding of inhibitors of Plasmodium falciparum dihydrofolate reductase.
Int. J. Parasitol. 37(7) , 787-93, (2007) Dihydrofolate reductases (DHFRs) from Plasmodium falciparum (Pf) and various species of both prokaryotic and eukaryotic organisms have a conserved tryptophan (Trp) at position 48 in the active site. The role in catalysis and binding of inhibitors of the conse... |