Read e-book online Antiparasitic and antibacterial drug discovery: from PDF

By Paul M. Selzer

ISBN-10: 1282118463

ISBN-13: 9781282118461

ISBN-10: 3527323279

ISBN-13: 9783527323272

ISBN-10: 3527626816

ISBN-13: 9783527626816

Addressing parasitic ailments and people brought on by micro organism, this a lot wanted reference and instruction manual offers a special perception into the procedure followed by way of advertisement technology in the direction of infectious ailments, 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 illnesses from educational teams and non revenue businesses

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Read e-book online Antiparasitic and antibacterial drug discovery: from PDF

Addressing parasitic illnesses and people attributable to micro organism, this a lot wanted reference and guide presents a distinct perception into the procedure followed through advertisement technology in the direction of infectious illnesses, together with the paintings of medicinal chemists. a few of the authors are scientists with hands-on event of drug discovery devices in the pharmaceutical undefined.

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

Sample text

The ability of the compound to select a protein target is optimal only if binding is stable and occurs rapidly with high affinity [14]. Some proteins may be inactivated by proteolysis during cell lysis, detergents may change protein conformation, membrane proteins may not be extracted at all [14, 81]. One option here is to use cross-linkers that bind the drug to the target before lysis [152]. Covalent attachment of drug to target has the additional virtue of allowing more stringent, and even denaturating, wash conditions [14, 15, 149].

CAMP response protein 1 (CARP1) is unique to kinetoplastid parasites, and CARP3 is unique to T. brucei; they are all believed to be part of a novel cAMP signaling pathway [128]. Proteins and Proteomes In the field of drug target deconvolution, high-sensitivity mass spectrometry is finding increased use in two areas: identification of proteins that bind to affinity columns and comparison of drug sensitive and resistant lines [18]. Proteomes CNVs can suggest that a protein might be overexpressed in a line with additional copies, but changes in expression due to changes in regulatory sequences cannot be predicted.

Benznidazole caused small differences, mostly in trypanothione metabolism, supporting the oxidative stress MoA; as a bonus, some benznidazole metabolites were detected [107]. An NMR metabolomic study of T. cruzi treated with plant extracts focused on the culture medium: a mitochondrial reductase was proposed as a target [179]. In contrast, an untargeted study of L. infantum promastigotes treated with miltefosine yielded so many differences in the metabolome that no obvious primary targets could be postulated; there were alterations in internal lipid metabolism and increases in alkanes, sugars, and nucleotides.

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


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