Abstract
There are several interesting chemical features that are associated with the primary structures of the endothelins73 and sarafotoxins (e.g., SRT-b).33 Certain physical and spectroscopic properties of endothelin-1 are provided in order to consider these features and the conformational studies that have been conducted specifically on this molecule. A working model is developed that portrays the structural significance and functional implications of the chemical features derived during this initial analysis. The biological activity of the endothelins as it pertains to their differences in chemical structure, i.e., endothelin structure—activity relationships (SARs) is then reviewed. The latter will be accomplished by considering separately the results obtained from receptorbinding studies, in vitro studies with isolated tissues, and, finally, in vivo studies in intact animals. The data for binding and in vitro studies are standardized and tabulated to allow for their quick perusal. It should be noted at the outset that generation of endothelin SARs will be complicated by the likelihood that different tissues contain different ratios of endothelin receptor subtypes, with each subtype presumably having its own set of SARs. For the purpose of provoking further thought and experiment, a fair amount of speculation is offered at various points in this chapter. In the summary, general SAR statements are derived and assessed relative to the working model.
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Erhardt, P.W. (1992). Endothelin Structure and Structure—Activity Relationships. In: Rubanyi, G.M. (eds) Endothelin. Clinical Physiology Series. Springer, New York, NY. https://doi.org/10.1007/978-1-4614-7514-9_4
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