By Thomas Lengauer, Raimund Mannhold, Hugo Kubinyi, Hendrik Timmerman
Offers a large, application-oriented review of this know-how. The state of the art in bioinformatics is evaluated both from an international view via introducing actual program eventualities.
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Extra info for Biology - Molecular Biology In Medicinal Chemistry
Extracellular signals, after interacting with appropriate receptor molecules at the cell surface, initiate a cascade of intracellular events which often leads to alterations in the expression of a set of genes. One or several of these genes can be used as an indicator for the modulation of targets within speciﬁc signaling pathways. The activation of a certain gene can be easily identiﬁed by ‘‘tagging’’ the particular gene with a so-called reporter gene. For this, plasmids need to be constructed which contain the promoter or regulatory region of the gene of interest linked to the reporter gene.
E. uniporters and coupled transporters, of which the former transport a single solute from one side of the membrane to the other and, for the latter, the transfer of one solute depends on the simultaneous or sequential transport of a second solute. 2 Membrane Proteins and Fast Cellular Responses Coupled transporters are further divided into symporters moving compounds in the same direction and antiporters moving the compounds in opposite directions. Some speciﬁc transporters act in a passive manner moving molecules down a concentration gradient, as is the case with many nutrients such as glucose, which are found at high concentrations in the extracellular space of tissues.
Exposure of the cells to MDR pump inhibitors will reduce eﬄux of the substrate and therefore leads to an increased ﬂuorescence readout. However, these assays are not homogeneous and involve washing steps after loading of the cells with the corresponding dye. A novel MDR pump substrate was recently developed to run fully homogeneous assays on a FLIPR system. The FLIPR Multidrug Resistance Assay (Molecular Devices) is a fully homogeneous application needing only 15 min of incubation at room temperature with a proprietary dye, which is transported by the MDR1 gene product and changes its ﬂuorescent properties only after modiﬁcation by intracellular enzymes.
Biology - Molecular Biology In Medicinal Chemistry by Thomas Lengauer, Raimund Mannhold, Hugo Kubinyi, Hendrik Timmerman