Abstract
The molecular mechanisms by which drugs bind to and regulate G-proteincoupled receptors (GPCR) remains a major unsolved problem for modern molecular biologists, biochemists and structural biologists. Ideally, we would like to ultimately define drug binding at the atomic level. An ideal molecular model would also be able to demonstrate why it is that agonists activate receptors while antagonists, which may or may not bind in overlap** domains, do not activate receptors. A perfect molecular explanation of drug action would elucidate the molecular determinants responsible for cellular regulation processes (e.g. desensitization, internalization and downregulation). At the present time, there are no verifiable models which elucidate these properties for any G-protein-coupled receptor.
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Roth, B.L., Hyde, E.G. (2000). Pharmacology of 5-HT2 Receptors. In: Baumgarten, H.G., Göthert, M. (eds) Serotoninergic Neurons and 5-HT Receptors in the CNS. Handbook of Experimental Pharmacology, vol 129. Springer, Berlin, Heidelberg. https://doi.org/10.1007/978-3-642-60921-3_14
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DOI: https://doi.org/10.1007/978-3-642-60921-3_14
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