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Insights into the operational model of agonism of receptor dimers
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SYSNO ASEP 0566162 Druh ASEP J - Článek v odborném periodiku Zařazení RIV J - Článek v odborném periodiku Poddruh J Článek ve WOS Název Insights into the operational model of agonism of receptor dimers Tvůrce(i) Jakubík, Jan (FGU-C) RID, ORCID
Randáková, Alena (FGU-C) RID, ORCIDZdroj.dok. Expert Opinion on Drug Discovery. - : Taylor & Francis - ISSN 1746-0441
Roč. 17, č. 11 (2022), s. 1181-1191Poč.str. 11 s. Jazyk dok. eng - angličtina Země vyd. GB - Velká Británie Klíč. slova operational model of agonism ; operational efficacy ; allosteric modulation ; receptor dimers ; GPCRs ; receptor channels Obor OECD Pharmacology and pharmacy CEP GJ19-06106Y GA ČR - Grantová agentura ČR Způsob publikování Omezený přístup Institucionální podpora FGU-C - RVO:67985823 UT WOS 000889990400001 EID SCOPUS 85142285798 DOI 10.1080/17460441.2023.2147502 Anotace 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. Pracoviště Fyziologický ústav Kontakt Lucie Trajhanová, lucie.trajhanova@fgu.cas.cz, Tel.: 241 062 400 Rok sběru 2023 Elektronická adresa https://doi.org/10.1080/17460441.2023.2147502
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