Biased Signaling and Its Role in the Genesis of Short- and Long-Acting β₂-Adrenoceptor Agonists.

ABSTRACT: Drug discovery is a costly and time-intensive process that is often limited by efficacy issues and unforeseen side effects. GPCR-targeting ligands, which account for one-third of marketed drugs, have been shown to exhibit biased signaling and preferential activation of one signaling pathway over another. While designing biased ligands is a recent advancement, their therapeutic benefits remain uncertain. However, the success of existing drugs raises the following question: do they inherently exhibit signaling bias that enhances efficacy or safety? This study examines the signaling profiles of short- and long-acting β₂AR agonists (SABAs and LABAs), key treatments for asthma and COPD, using biosensors to measure G protein and β-arrestin coupling. Older SABAs, such as isoprenaline a

SUBMITTER: Phan NTN 

PROVIDER: S-EPMC12369021 | biostudies-literature | 2025 Aug

REPOSITORIES: biostudies-literature