MultiBacMam Technology for Studying the Downstream cAMP Signaling Pathway of M2 Muscarinic Acetylcholine Receptor

Allikalt, Anni; Veiksina, Santa; Tahk, Maris-Johanna; Vavers, Edijs; Laaneväli, Elen; Rinken, Ago; Kopanchuk, Sergei

doi:10.1007/978-1-0716-4015-9_7

Neuromethods

2024

DOI: 10.1007/978-1-0716-4015-9_7

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MultiBacMam Technology for Studying the Downstream cAMP Signaling Pathway of M2 Muscarinic Acetylcholine Receptor

Anni Allikalt,

Santa Veiksina,

Maris-Johanna Tahk

et al.

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Dually Labeled Neurotensin NTS₁R Ligands for Probing Radiochemical and Fluorescence-Based Binding Assays

Ertl,

Kopanchuk,

Dijon

et al. 2024

J. Med. Chem.

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The determination of ligand–receptor binding affinities plays a key role in the development process of pharmaceuticals. While the classical radiochemical binding assay uses radioligands, fluorescence-based binding assays require fluorescent probes. Usually, radio- and fluorescence-labeled ligands are dissimilar in terms of structure and bioactivity, and can be used in either radiochemical or fluorescence-based assays. Aiming for a close comparison of both assay types, we synthesized tritiated fluorescent neurotensin receptor ligands ([3H]13, [3H]18) and their nontritiated analogues (13, 18). The labeled probes were studied in radiochemical and fluorescence-based (high-content imaging, flow cytometry, fluorescence anisotropy) binding assays. Equilibrium saturation binding yielded well-comparable ligand–receptor affinities, indicating that all these setups can be used for the screening of new drugs. In contrast, discrepancies were found in the kinetic behavior of the probes, which can be attributed to technical differences of the methods and require further studies with respect to the elucidation of the underlying mechanisms.

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Dually Labeled Neurotensin NTS₁R Ligands for Probing Radiochemical and Fluorescence-Based Binding Assays

Ertl,

Kopanchuk,

Dijon

et al. 2024

J. Med. Chem.

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show abstract

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MultiBacMam Technology for Studying the Downstream cAMP Signaling Pathway of M2 Muscarinic Acetylcholine Receptor

Cited by 1 publication

References 28 publications

Dually Labeled Neurotensin NTS₁R Ligands for Probing Radiochemical and Fluorescence-Based Binding Assays

Dually Labeled Neurotensin NTS₁R Ligands for Probing Radiochemical and Fluorescence-Based Binding Assays

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MultiBacMam Technology for Studying the Downstream cAMP Signaling Pathway of M2 Muscarinic Acetylcholine Receptor

Cited by 1 publication

References 28 publications

Dually Labeled Neurotensin NTS1R Ligands for Probing Radiochemical and Fluorescence-Based Binding Assays

Dually Labeled Neurotensin NTS1R Ligands for Probing Radiochemical and Fluorescence-Based Binding Assays

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Dually Labeled Neurotensin NTS₁R Ligands for Probing Radiochemical and Fluorescence-Based Binding Assays

Dually Labeled Neurotensin NTS₁R Ligands for Probing Radiochemical and Fluorescence-Based Binding Assays