Zobrazeno 1 - 10
of 36
pro vyhledávání: '"Alena Randáková"'
Publikováno v:
Scientific Reports, Vol 13, Iss 1, Pp 1-15 (2023)
Abstract Agonist efficacy denoting the “strength” of agonist action is a cornerstone in the proper assessment of agonist selectivity and signalling bias. The simulation models are very accurate but complex and hard to fit experimental data. The p
Externí odkaz:
https://doaj.org/article/93e657224a974635a025309073addb3d
Autor:
Ewa Szczurowska, Eszter Szánti-Pintér, Nikolai Chetverikov, Alena Randáková, Eva Kudová, Jan Jakubík
Publikováno v:
International Journal of Molecular Sciences, Vol 24, Iss 1, p 507 (2022)
Muscarinic acetylcholine receptors expressed in the central nervous system mediate various functions, including cognition, memory, or reward. Therefore, muscarinic receptors represent potential pharmacological targets for various diseases and conditi
Externí odkaz:
https://doaj.org/article/1ba22ba0a7a84192b0a6a42c5d1c8e16
Allosteric Modulation of Muscarinic Receptors by Cholesterol, Neurosteroids and Neuroactive Steroids
Publikováno v:
International Journal of Molecular Sciences, Vol 23, Iss 21, p 13075 (2022)
Muscarinic acetylcholine receptors are membrane receptors involved in many physiological processes. Malfunction of muscarinic signaling is a cause of various internal diseases, as well as psychiatric and neurologic conditions. Cholesterol, neurostero
Externí odkaz:
https://doaj.org/article/55e89d5dab5446babb00af227aef3ed0
Autor:
Alena Randáková, Dominik Nelic, Martina Hochmalová, Pavel Zimčík, Mutale Jane Mulenga, John Boulos, Jan Jakubík
Publikováno v:
International Journal of Molecular Sciences, Vol 22, Iss 18, p 10089 (2021)
A complex evaluation of agonist bias at G-protein coupled receptors at the level of G-protein classes and isoforms including non-preferential ones is essential for advanced agonist screening and drug development. Molecular crosstalk in downstream sig
Externí odkaz:
https://doaj.org/article/02b106b875504802b6a348b058fbf887
Publikováno v:
PLoS ONE, Vol 14, Iss 3, p e0214255 (2019)
Allosteric ligands bind to receptors at sites that are distinct from those endogenous agonists and orthosteric pharmacological agents interact with. Both an allosteric and orthosteric ligand bind simultaneously to the receptor to form a ternary compl
Externí odkaz:
https://doaj.org/article/e8ad7ac52da14a309279b4a8c25752c4
Publikováno v:
PLoS ONE, Vol 6, Iss 11, p e27732 (2011)
Based on the kinetics of interaction between a receptor and G-protein, a myriad of possibilities may result. Two extreme cases are represented by: 1/Collision coupling, where an agonist binds to the free receptor and then the agonist-receptor complex
Externí odkaz:
https://doaj.org/article/58d46b86f0364896b73fb79d7669db8b
Autor:
Jan Jakubík, Alena Randáková
Publikováno v:
Expert opinion on drug discovery. 17(11)
Accurate ranking of efficacies and potencies of agonists is essential in the discovery of new selective agonists. For the purpose of system-independent ranking of agonists, the operational model of agonism (OMA) has become a standard. Many receptors
Autor:
Jan Jakubík, Dominik Nelic, Alena Randáková, Esam E. El-Fakahany, John Boulos, Vladimír Doležal
Publikováno v:
Journal of Chemical Information and Modeling. 60:2325-2338
Binding of muscarinic ligands, both antagonists and agonists, and their effects on the conformation of the M2 acetylcholine receptor were modeled in silico and compared to experimental data. After docking of antagonists to the M2 receptor in an inact
Although being a relative term, agonist efficacy is a cornerstone in the proper assessment of agonist selectivity and signalling bias. The operational model of agonism (OMA) has become successful in the determination of agonist efficacies and ranking
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::2c202369d4aec036d1095b538ddd7b12
https://doi.org/10.21203/rs.3.rs-900678/v1
https://doi.org/10.21203/rs.3.rs-900678/v1
Autor:
Alena Randáková, JakubíkJan Jakubík
Publikováno v:
Pharmacological research. 169
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 Sjogr