Počet záznamů: 1  

Functionally selective and biased agonists of muscarinic receptors

  1. 1.
    0542922 - FGÚ 2022 RIV GB eng J - Článek v odborném periodiku
    Randáková, Alena - Jakubík, Jan
    Functionally selective and biased agonists of muscarinic receptors.
    Pharmacological Research. Roč. 169, July (2021), č. článku 105641. ISSN 1043-6618. E-ISSN 1096-1186
    Grant CEP: GA ČR(CZ) GJ19-06106Y
    Institucionální podpora: RVO:67985823
    Klíčová slova: muscarinic receptors * signalling bias * functional selectivity * G-proteins * beta-arrestins
    Obor OECD: Pharmacology and pharmacy
    Impakt faktor: 10.334, rok: 2021
    Způsob publikování: Open access
    https://doi.org/10.1016/j.phrs.2021.105641

    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.
    Trvalý link: http://hdl.handle.net/11104/0320252

     
     
Počet záznamů: 1  

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