ArticleACS medicinal chemistry letters2013
Discovery of β2 Adrenergic Receptor Ligands Using Biosensor Fragment Screening of Tagged Wild-Type Receptor.
Article in ACS medicinal chemistry letters, 2013. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 19 papers.
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The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
19 citing papers in PubMed, 65 citations in OpenAlex.
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- Anti-nanodisc antibodies specifically capture nanodiscs and facilitate molecular interaction kinetics studies for membrane protein.Scientific reports · 2023Article
- Protein Interaction Analysis by Surface Plasmon Resonance.Methods in molecular biology (Clifton, N.J.) · 2023Article
- Surface Plasmon Resonance Screening to Identify Active and Selective Adenosine Receptor Binding Fragments.ACS medicinal chemistry letters · 2022Article
- Artificial intelligence and machine learning approaches for drug design: challenges and opportunities for the pharmaceutical industries.Molecular diversity · 2022Review
- Application of Artificial Intelligence in Discovery and Development of Anticancer and Antidiabetic Therapeutic Agents.Evidence-based complementary and alternative medicine : eCAM · 2022Review
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- A live cell NanoBRET binding assay allows the study of ligand-binding kinetics to the adenosine APurinergic signalling · 2019Article
- Reprogramming G protein coupled receptor structure and function.Current opinion in structural biology · 2018Review
- Emerging Paradigm of Intracellular Targeting of G Protein-Coupled Receptors.Trends in biochemical sciences · 2018Review
- Enabling STD-NMR fragment screening using stabilized native GPCR: A case study of adenosine receptor.Scientific reports · 2018Article
- High-throughput identification of G protein-coupled receptor modulators through affinity mass spectrometry screening.Chemical science · 2018Article
- SPR-based fragment screening with neurotensin receptor 1 generates novel small molecule ligands.PloS one · 2017Article
- Biophysics in drug discovery: impact, challenges and opportunities.Nature reviews. Drug discovery · 2016Review
- Article
- The receptor concept in 3D: from hypothesis and metaphor to GPCR-ligand structures.Neurochemical research · 2014Review
- Recent advances in bioprinting and applications for biosensing.Biosensors · 2014Review
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Authors and funding
18 authors at 5 institutions in 2 countries.
Funding
Abstract
G-protein coupled receptors (GPCRs) are the primary target class of currently marketed drugs, accounting for about a quarter of all drug targets of approved medicines. However, almost all the screening efforts for novel ligand discovery rely exclusively on cellular systems overexpressing the receptors. An alternative ligand discovery strategy is a fragment-based drug discovery, where low molecular weight compounds, known as fragments, are screened as initial starting points for optimization. However, the screening of fragment libraries usually employs biophysical screening methods, and as such, it has not been routinely applied to membrane proteins. We present here a surface plasmon resonance biosensor approach that enables, cell-free, label-free, fragment screening that directly measures fragment interactions with wild-type GPCRs. We exemplify the method by the discovery of novel, selective, high affinity antagonists of human β2 adrenoceptor.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.