Publication receptor-interaction, model

Figure 6.5 Topographical interaction model of features are red for positively ionizable, green for ccia adrenergic receptor generated on the basis of hydrogen bond acceptors, light blue for public site-directed mutagenesis. Both hydrophobicandorangeforringaromatic.Shape...

Figure 13.5 Topographical interaction model of ana adrenergic receptor generated based on public site-directed mutagenesis. Both pharmacophore models have been mapped into the topographical model of the receptor. The model reveals putative receptor interaction sites for most of the pharmacophoric features observed within each antagonist class, (a) Class I pharmacophore with prazosin as reference compound (b) class II pharmacophore with compound 10 as reference. Pharmacophoric features are red for posi-...

A most recent publication of modification in this region describes a C6-C8 bridged analog that was designed to constrain the EC conformation [61]. Unfortunately, the molecule s lack of activity in cells presents the inverse ambiguity we described for C10-C12 phenylene analog constrained to NMR data above [59], Unlike the receptor interaction of the phenylene, the EC model provides ample room to accommodate the new methylene, however, we don t know if the molecule can attain the desired conformation. Likewise, lack of cellular activity may be caused by reduced transport or factors other than polymerization activity. 

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