Agonists binding and activation

Hwa, J. and Perez, D.M. (1996) The unique nature of the serine interactions for alpha 1-adrenergic receptor agonist binding and activation. The Journal of Biological Chemistry, 271, 6322-6327. 

Using the information obtained through these biophysical studies on the /TAR (Ghanouni et al., 2001a Swaminath et al., 2004, 2005), we proposed a model whereby agonist binding and activation occur through a series of conformational intermediates (Fig. 10). Within this model, catechol and... 

Direct agonist, indirect agonist A direct agonist binds and activates the receptor an indirect one brings about receptor activation by binding to some other molecule, eg, a reuptake carrier, and causing an increase in the synaptic concentration of the normal transmitter... 

The first physically plausible mechanism for receptor activation was proposed by del Castillo and Katz (1957). They made the important distinction that agonist binding and channel opening of the AChR must occur as two separate steps ... 

Recent work has identified a critical role for a conserved arginine Arg-34 in the N-terminus for agonist binding and receptor activation, loss of which leads to a dysfunctional receptor [134]. 

The Distinction between Agonist Binding and Receptor Activation... 

E. The P 2AR as a Model System for Ligand Binding and Activation Biophysical Analysis of Agonist-Induced Conformational Changes... 

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