Discovery of Environment-Sensitive Fluorescent Ligands of β-Adrenergic Receptors for Cell Imaging and NanoBRET Assay.
Sign Up to like & getrecommendations! Published in 2022 at "Analytical chemistry"
DOI: 10.1021/acs.analchem.1c05646
Abstract: By fusing several environment-sensitive fluorophores to the pharmacophore mirabegron, a series of new fluorescent ligands for β-adrenergic receptors (β-ARs) were produced with a turn-on mechanism and high binding affinity to β-ARs efficiently. Compound L5 with… read more here.
Keywords: ligands adrenergic; fluorescent ligands; environment; environment sensitive ... See more keywords
Fluorescent Ligands Targeting the Intracellular Allosteric Binding Site of the Chemokine Receptor CCR2.
Sign Up to like & getrecommendations! Published in 2022 at "ACS chemical biology"
DOI: 10.1021/acschembio.2c00263
Abstract: Fluorescently labeled ligands are versatile molecular tools to study G protein-coupled receptors (GPCRs) and can be used for a range of different applications, including bioluminescence resonance energy transfer (BRET) assays. Here, we report the structure-based… read more here.
Keywords: fluorescent ligands; ccr2; allosteric binding; targeting intracellular ... See more keywords
Design and development of selective competitive fluorescent ligands for the detection and visualization of Kv7.2/7.3 in vitro.
Sign Up to like & getrecommendations! Published in 2022 at "Chemical communications"
DOI: 10.1039/d2cc00372d
Abstract: A series of specific and potent fluorescent ligands were developed for labelling and visualizing Kv7.2/7.3 based molecular rotation restriction. Probes 21b and 24a were found to be safe and convenient tools to detect and visualize… read more here.
Keywords: design development; fluorescent ligands; development selective; ligands detection ... See more keywords
Expanding the apelin receptor pharmacological toolbox using novel fluorescent ligands
Sign Up to like & getrecommendations! Published in 2023 at "Frontiers in Endocrinology"
DOI: 10.3389/fendo.2023.1139121
Abstract: Introduction The apelin receptor binds two distinct endogenous peptides, apelin and ELA, which act in an autocrine/paracrine manner to regulate the human cardiovascular system. As a class A GPCR, targeting the apelin receptor is an… read more here.
Keywords: fluorescent ligands; apelin receptor; pharmacological toolbox; receptor ... See more keywords