Toward the Bioactive Conformation of Tachykinins?
The knowledge of binding-site topography is an essential step in the understanding of a receptor-substrate recognition process. However, the direct study of such complex is presently limited in application. Nevertheless, a binding site can be considered as being the imprint of the three-dimensional structure of its substrate. Taking into account the associative properties of the substance P to phospholipids and the aggregation behaviour of the tachykinins, we propose a two-step binding mechanism of these peptides to their receptors. First, the substrate binds to the phospholipids component of the membrane. This is followed by a two-dimensional diffusion of the tachykinins and of its receptor on the surface of the membrane, resulting in the formation of the substrate-receptor complex.
KeywordsExchange Rate Helical Conformation Slow Exchange Associative Property Bioactive Conformation
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