Insights into the operational model of agonism of receptor dimers

Result code in IS VaVaI
<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F67985823%3A_____%2F22%3A00566162" target="_blank" >RIV/67985823:_____/22:00566162 - isvavai.cz</a>
Result on the web
<a href="https://doi.org/10.1080/17460441.2023.2147502" target="_blank" >https://doi.org/10.1080/17460441.2023.2147502</a>
DOI - Digital Object Identifier
<a href="http://dx.doi.org/10.1080/17460441.2023.2147502" target="_blank" >10.1080/17460441.2023.2147502</a>

Result language
angličtina
Original language name
Insights into the operational model of agonism of receptor dimers
Original language description
Introduction: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 function as oligomers which makes functional responses more complex, requiring an extension of the original OMA.Areas covered:Explicit equations of the operational model of agonism of receptor dimers (OMARD) were derived. The OMARD can be applied to any receptor possessing two orthosteric sites. The behavior of OMARD was analyzed to demonstrate its complexity and relation to experimental data. Properties of OMARD and OMA equations were compared to demonstrate their pros and cons.Expert opinion:Extension of OMA by slope factors gives simple equations of functional response that are easy to fit experimental data but results may be inaccurate because of exponentiation of operational efficacy. Also, such equations cannot accommodate bell-shaped curves. Explicit equations of OMARD give accurate results but are complex and tedious to fit experimental data. All operational models use inter-dependent parameters that are a hurdle in the fitting. A good understanding of OMARD behavior helps to overcome such obstacles.
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
2022
Confidentiality
S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů

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