Abstract
Receptors are signaling proteins that are responsible for converting extracellular stimuli to intracellular responses. These responses can occur on millisecond time scales or take minutes or even hours. In addition to temporal dynamics of signaling, receptors mediate signal amplification and signal processing. Signal amplification occurs by receptor activity-mediated increase in the concentration of many intracellular molecules. Signal processing occurs when a variety of intracellular events produced upon activation of the receptor lead to an appropriate response. According to the classic model of receptor activation, a specific receptor responds to one specific chemical neurotransmitter. This model is continuing to be revised since in many cases, a specific ligand is able to activate a number of distinct targets and alternatively, different ligands are able to bind and activate the same receptor. The types of endogenous ligands that stimulate receptors vary widely in their physiochemical properties ranging from amino acids (glutamate), peptides (enkephalin, neuropeptide Y), large proteins (follicle-stimulating hormone), nucleosides (adenosine), lipids (2-arachidonoylglycerol), divalent ions (calcium), or steroids (estrogen). These ligands activate four major classes of receptors: ligand-gated ion channels, G-protein-coupled receptors, enzyme-linked receptors, and nuclear hormone receptors. The structure and mechanism of action of receptors are diverse because of the diversity of ligands activating the receptor and the time scales that the signal needs to be transmitted. Approximately half of all drug targets are receptors. Therefore, an understanding of receptors is important both for basic neuroscience as well as neuropharmacology and applied biomedical sciences.
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Further Reading
Barbacid M (1996) Neurotrophic factors and their receptors. Curr Biol 7:148–155
Barnard EA (1992) Receptor classes and the transmitter-gated ion channels. Trends Biochem Sci 17:368–374
Evans RM (1988) The steroid and thyroid hormone receptor superfamily. Science 240:889–895
Gudermann T, Kalkbrenner F, Schultz G (1996) Diversity and selectivity of receptor-G protein signaling. Ann Rev Pharmacol Toxicol 36:429–459
Kenakin T (1995) Agonist-receptor efficacy II: agonist trafficking of receptor signals. Trends Pharmacol Sci 16:232–238
Moghal N, Sternberg PW (1999) Multiple positive and negative regulators of signaling by the EGF receptor. Curr Opinions Cell Biol 11:190–196
Neer EJ (1995) Heterotrimeric G proteins: organizers of transmembrane signals. Cell 80:249–257
Olsen RW (1982) Drug interactions at the GABA receptor-ionophore complex. Annu Rev Pharmacol Toxicol 22:245–277
Rozenfeld R, Devi LA (2010) Exploring a role for heteromerization in GPCR signaling specificity. Biochem J 433:11–18
Shukla AK, Xiao K, Lefkowitz RJ (2011) Emerging paradigms of Beta-arrestin-dependent seven transmembrane receptor signaling. Trends Biochem Sci (Epub ahead of print) 36:457–461
Snyder SH (1984) Drug and neurotransmitter receptors in the brain. Science 224:22–31
Unwin N (1995) Acetylcholine receptor channel imaged in the open state. Nature 373:37–43
Wallas SI, Greengard P (1991) Protein phosphorylation and neuronal function. Pharmacol Rev 43:299–349
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Devi, L.A., Fricker, L.D. (2013). Transmitter and Peptide Receptors: Basic Principles. In: Pfaff, D.W. (eds) Neuroscience in the 21st Century. Springer, New York, NY. https://doi.org/10.1007/978-1-4614-1997-6_52
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DOI: https://doi.org/10.1007/978-1-4614-1997-6_52
Publisher Name: Springer, New York, NY
Print ISBN: 978-1-4614-1996-9
Online ISBN: 978-1-4614-1997-6
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