Functionally selective and biased agonists of muscarinic receptors

Result code in IS VaVaI
<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F67985823%3A_____%2F21%3A00542922" target="_blank" >RIV/67985823:_____/21:00542922 - isvavai.cz</a>
Result on the web
<a href="https://doi.org/10.1016/j.phrs.2021.105641" target="_blank" >https://doi.org/10.1016/j.phrs.2021.105641</a>
DOI - Digital Object Identifier
<a href="http://dx.doi.org/10.1016/j.phrs.2021.105641" target="_blank" >10.1016/j.phrs.2021.105641</a>

Result language
angličtina
Original language name
Functionally selective and biased agonists of muscarinic receptors
Original language description
Disruption of cholinergic signalling via muscarinic receptors is associated with various pathologies, like Alzheimer’s disease or schizophrenia. Selective muscarinic agonists possess therapeutic potential in the treatment of diabetes, pain or Sjögren's syndrome. The orthosteric binding site of all subtypes of the muscarinic receptor is structurally identical, making the development of affinity-based selective agonists virtually impossible. Some agonists, however, are functionally selective, they activate only a subset of receptors or signalling pathways. Others may stabilise specific conformations of the receptor leading to non-uniform modulation of individual signalling pathways (biased agonists). Functionally selective and biased agonists represent a promising approach for selective activation of individual subtypes of muscarinic receptors. In this work we review chemical structures, receptor binding and agonist-specific conformations of currently known functionally selective and biased muscarinic agonists in the context of their intricate intracellular signalling. Further, we take a perspective on the possible use of biased agonists for tissue and organ-specific activation of muscarinic receptors.
Czech name
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Czech description
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Type
J<sub>imp</sub> - Article in a specialist periodical, which is included in the Web of Science database
CEP classification
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OECD FORD branch
30104 - Pharmacology and pharmacy

Project
<a href="/en/project/GJ19-06106Y" target="_blank" >GJ19-06106Y: Analysis of signalling bias of novel synthetic muscarinic agonists</a><br>
Continuities
P - Projekt vyzkumu a vyvoje financovany z verejnych zdroju (s odkazem do CEP)

Publication year
2021
Confidentiality
S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů

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