Download e-book for kindle: Antiparasitic and antibacterial drug discovery: from by Paul M. Selzer


By Paul M. Selzer

ISBN-10: 1282118463

ISBN-13: 9781282118461

ISBN-10: 3527323279

ISBN-13: 9783527323272

ISBN-10: 3527626816

ISBN-13: 9783527626816

Addressing parasitic illnesses and people brought on by micro organism, this a lot wanted reference and instruction manual offers a distinct perception into the procedure followed by means of advertisement technological know-how in the direction of infectious illnesses, together with the paintings of medicinal chemists. a few of the authors are scientists with hands-on adventure of drug discovery devices in the pharmaceutical undefined. moreover, the textual content covers efforts in the direction of drug improvement in infectious ailments from educational teams and non revenue companies

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Extra info for Antiparasitic and antibacterial drug discovery: from molecular targets to drug candidates

Sample text

Nifurtimox, on the other hand, caused an increase in nucleotides and nucleobases: it was speculated that this was a consequence of DNA and RNA degradation [112]. The drug combination did not result in any additional changes [112]. Both benznidazole and nifurtimox are used to treat T. cruzi and are thought to have similar modes of action: activation by type 1 NTR and subsequent oxidative stress [107, 178]. Metabolomic analysis of T. cruzi resulted in identification of about 1000 metabolites [107].

Contain a secondary plastid-derived organelle called the apicoplast. This contains various pathways 7 8 1 Discovery the Mechanism of Action and has a genome that encodes the essential proteins [31]; in the blood form, the only apicoplast-specific metabolic pathway that is required for multiplication and survival is isoprenoid biosynthesis [32]. Compounds that inhibit apicoplast replication and protein expression affect the parasites only gradually: defects in apicoplast division and segregation are seen and the cells undergo “delayed death,” after several cell divisions [33–35].

Brucei MRPA), γ-glutamylcysteine synthetase, and glutathione synthetase was detected [98]. Glutathione synthetase and γ-glutamylcysteine synthetase are enzymes on the trypanothione synthesis pathway, and MRPA/PGPA exports antimonials and arsenicals as conjugates with trypanothione. Using the same gene array with RNA from methotrexate-resistant cells, increased expressions of the target (dihydrofolate reductase) and pteridine reductase and S-adenosylmethionine synthase were found [98]. Using a different mini-array containing all Leishmania genes encoding ABC proteins, three were found to be overexpressed in antimony-resistant cells [99].

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Antiparasitic and antibacterial drug discovery: from molecular targets to drug candidates by Paul M. Selzer

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