التفاصيل البيبلوغرافية
| العنوان: |
Signalling in response to sub-picomolar concentrations of active compounds: Pushing the boundaries of GPCR sensitivity. |
| المؤلفون: |
Civciristov, Srgjan1 (AUTHOR), Halls, Michelle L.1 (AUTHOR) michelle.halls@monash.edu |
| المصدر: |
British Journal of Pharmacology. Jul2019, Vol. 176 Issue 14, p2382-2401. 20p. 5 Charts, 2 Graphs. |
| مصطلحات موضوعية: |
*MUSCARINIC receptors, *CHEMOTAXIS, *PROTEIN receptors, *MUSCLE contraction, *ADRENERGIC receptors, *GEOGRAPHIC boundaries |
| مستخلص: |
There is evidence for ultra-sensitive responses to active compounds at concentrations below picomolar levels by proteins and receptors found in species ranging from bacteria to mammals. We have recently shown that such ultra-sensitivity is also demonstrated by a wide range of prototypical GPCRs, and we have determined the molecular mechanisms behind these responses for three family A GPCRs: the relaxin receptor, RXFP1; the β2 -adrenoceptor; and the M3 muscarinic ACh receptor. Interestingly, there are reports of similar ultra-sensitivity by more than 15 human GPCR families, in addition to other human receptors and channels. These occur through a diverse range of signalling pathways and produce modulation of important physiological processes, including neuronal transmission, chemotaxis, gene transcription, protein/ion uptake and secretion, muscle contraction and relaxation, and phagocytosis. Here, we summarise the accumulating evidence of ultra-sensitive receptor signalling to show that this is a common, though currently underappreciated, property of GPCRs. LINKED ARTICLES: This article is part of a themed section on Adrenoceptors-New Roles for Old Players. To view the other articles in this section visit http://onlinelibrary.wiley.com/doi/10.1111/bph.v176.14/issuetocTest. [ABSTRACT FROM AUTHOR] |
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