ArticleMethods in molecular biology (Clifton, N.J.)2022
NanoBRET and NanoBiT/BRET-Based Ligand Binding Assays Permit Quantitative Assessment of Small Molecule Ligand Binding to Smoothened.
Article in Methods in molecular biology (Clifton, N.J.), 2022. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 2 papers.
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
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2 citing papers in PubMed, 5 citations in OpenAlex.
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- Application of Fluorescence- and Bioluminescence-Based Biosensors in Cancer Drug Discovery.Biosensors · 2024Review
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Authors and funding
2 authors at 1 institution in 1 country.
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Abstract
Smoothened (SMO) is a G protein-coupled receptor (GPCR) that mediates Hedgehog (Hh) signaling. SMO activity is regulated following the binding of Hh to the transmembrane protein Patched. Overactive SMO signaling is oncogenic, and hence this receptor is a target for several marketed drugs. However, development of new SMO ligands has been hampered by the fact that current radioligand and fluorescence-based binding assays are not high-throughput scalable. Here, we demonstrate two Nanoluciferase (Nluc) bioluminescence resonance energy transfer-based ligand binding assays (NanoBRET and NanoBiT/BRET) which provide a sensitive and high-throughput-compatible tool in drug screening efforts. In the described assays, SMO is N-terminally tagged either with full-length nanoluciferase or the partial HiBiT sequence, and subsequently binding of BODIPY-cyclopamine is assessed by quantifying resonance energy transfer between the receptor and the fluorescent ligand. Additionally, the assay allows performing competition binding experiments using commercially available SMO ligands, such as the SMO agonist SAG1.3.
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