Receptor activation, molecular processes

Almost all contributions to the two volumes highlight the fact that ligand-protein complexes cannot be treated as static ensembles. On both sides, the ligand and the receptor side, dynamic processes contribute to the molecular recognition. In this sense it is hoped that these two volumes of Bio active Confer-... 

A recent study found that cortical peripheral benzodiazepine receptors, as assessed with PET and [ C]PK11195, were increased by 30-40% in patients with AD when compared with healthy controls. This suggests active inflammatory processes in AD since PK11195 binds to activated microglia [72]. Several F-labeled tracers of the peripheral benzodiazepine receptor have been developed, and [i8p]PK14105 [73] and [i8p]FEDAA1106 [74] are the most well characterized. However, no reports have been published on the use of either of the two radiotracers in AD. The molecular structures of F-labeled tracers for the peripheral benzodiazepine receptor are shown in Fig. 5. 

Carrieri, A., Centeno, N.B., Rodrigo, J., Sanz, F., Carotti, A. Theoretical evidence of a salt bridge disruption as the initiating process for the a1(j-adrenergic receptor activation a molecular dynamics and docking study. Proteins 2001, 43, 382-394. 

Pardo, L. Campillo, M. Giraldo, J. (1997) The effect of the molecular mechanism of G protein-coupled receptor activation on the process of signal transduction. Eur. J. Pharmacol. 335, 73-87. 

Transport of solutes and water occurs both across and between the epithelial cells that line the renal tubules. Transport is both active (energy requiring) and passive, but many of the so-called passive transport processes are dependent upon or secondary to active transport processes, particularly those involving sodium transport. All known transport processes involve receptor or mediator molecules, many of which have now been identified and characterized using molecular biological teclmiques. The activity of many of these molecules is regulated by phosphorylation facilitated by protein kinase C or Their renal distribution has... 

In this chapter we summarize some aspects of the structure-functional relationship of the ala and alb-adrenergic receptor subtypes related to the receptor activation process as well as the effect of different alpha-blockers on the constitutive activity of the receptor. Molecular modeling of the ala and alb-adrenergic receptor subtypes and computational simulation of receptor dynamics were useful to interpret the experimental findings derived from site directed mutagenesis studies. 2000 Elsevier Science B.V. All rights reserved. 

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