APA
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Morales, P., Scharf, M. M., Bermudez, M., Egyed, A., Franco, R., Hansen, O. K., … Wingler, L. (2024). Progress on the development of Class A GPCR-biased ligands. British Journal of Pharmacology.
Chicago/Turabian
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Morales, Paula, Magdalena M Scharf, Marcel Bermudez, Attila Egyed, Rafael Franco, Olivia K Hansen, Nadine Jagerovic, et al. “Progress on the Development of Class A GPCR-Biased Ligands.” British Journal of Pharmacology (2024).
MLA
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Morales, Paula, et al. “Progress on the Development of Class A GPCR-Biased Ligands.” British Journal of Pharmacology, 2024.
BibTeX Click to copy
@article{paula2024a,
title = {Progress on the development of Class A GPCR-biased ligands.},
year = {2024},
journal = {British Journal of Pharmacology},
author = {Morales, Paula and Scharf, Magdalena M and Bermudez, Marcel and Egyed, Attila and Franco, Rafael and Hansen, Olivia K and Jagerovic, Nadine and Jakubík, Jan and Keserű, György M and Kiss, Dóra Judit and Kozielewicz, P. and Larsen, Olav and Majellaro, Maria and Mallo-Abreu, Ana and Navarro, Gemma and Prieto-Díaz, Rubén and Rosenkilde, M. and Sotelo, Eddy and Stark, Holger and Werner, Tobias and Wingler, L.}
}
Class A G protein-coupled receptors (GPCRs) continue to garner interest for their essential roles in cell signalling and their importance as drug targets. Although numerous drugs in the clinic target these receptors, over 60% GPCRs remain unexploited. Moreover, the adverse effects triggered by the available unbiased GPCR modulators, limit their use and therapeutic value. In this context, the elucidation of biased signalling has opened up new pharmacological avenues holding promise for safer therapeutics. Functionally selective ligands favour receptor conformations facilitating the recruitment of specific effectors and the modulation of the associated pathways. This review surveys the current drug discovery landscape of GPCR-biased modulators with a focus on recent advances. Understanding the biological effects of this preferential coupling is at different stages depending on the Class A GPCR family. Therefore, with a focus on individual GPCR families, we present a compilation of the functionally selective modulators reported over the past few years. In doing so, we dissect their therapeutic relevance, molecular determinants and potential clinical applications.
