Analysis of agonism by dopamine at the dopaminergic D 2 G-protein coupled receptor based on comparative modelling of rhodopsin |
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| Authors: | Benjamin G. Tehan Edward J. Lloyd Margaret G. Wong David K. Chalmers |
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| Affiliation: | 1. Department of Medicinal Chemistry, Victorian College of Pharmacy , Monash University , 381 Royal Parade, Parkville, 3052, Australia;2. Department of Applied Chemistry , Swinburne University of Technology , John Street, Hawthorn, 3122, Australia |
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| Abstract: | A number of theoretical dopaminergic D 2 models were constructed using comparative modelling techniques. The models constructed were based on the recently published crystal structure of rhodopsin. D 2 models were constructed without any ligands bound in the active site and also with the endogenous agonist, dopamine, bound in the active site. Comparison of the bound and unbound models revealed the importance of the chi angle of serine 197 and the effect this has on the bending of helix 5 when an agonist is present in the binding site. |
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| Keywords: | Dopamine, D 2 G-protein Coupled Receptor Rhodopsin Agonists Activation |
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