ArticlePloS one2017
SPR-based fragment screening with neurotensin receptor 1 generates novel small molecule ligands.
Article in PloS one, 2017. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 14 papers.
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Who cites it
14 citing papers in PubMed, 32 citations in OpenAlex.
- Latest surface plasmon resonance advances for G protein-coupled receptors.Journal of pharmaceutical analysis · 2026Review
- Fab-Induced Stabilization of an Ion Channel Receptor Enables Mechanistic Characterization of Small-Molecule Therapeutics.Analytical chemistry · 2025Article
- The Nature of Nanodisc Lipids Influences Fragment-Based Drug Discovery Results.Chemical biology & drug design · 2025Article
- Identification of a Novel Subtype-Selective αACS chemical neuroscience · 2024Article
- Surface Plasmon Resonance Screening to Identify Active and Selective Adenosine Receptor Binding Fragments.ACS medicinal chemistry letters · 2022Article
- GPCR systems pharmacology: a different perspective on the development of biased therapeutics.American journal of physiology. Cell physiology · 2022Review
- A Review on the Role of TRP Channels and Their Potential as Drug Targets_An Insight Into the TRP Channel Drug Discovery Methodologies.Frontiers in pharmacology · 2022Review
- Directed evolution for high functional production and stability of a challenging G protein-coupled receptor.Scientific reports · 2021Article
- Neurotensin: A novel mediator of ovulation?FASEB journal : official publication of the Federation of American Societies for Experimental Biology · 2021Article
- Engineering of Challenging G Protein-Coupled Receptors for Structure Determination and Biophysical Studies.Molecules (Basel, Switzerland) · 2021Review
- Complexes of the neurotensin receptor 1 with small-molecule ligands reveal structural determinants of full, partial, and inverse agonism.Science advances · 2021Article
- Assays and technologies for developing proteolysis targeting chimera degraders.Future medicinal chemistry · 2020Review
- Theory and applications of differential scanning fluorimetry in early-stage drug discovery.Biophysical reviews · 2020Review
- Article
Corrections and comments
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Authors and funding
8 authors at 2 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
The neurotensin receptor 1 represents an important drug target involved in various diseases of the central nervous system. So far, the full exploitation of potential therapeutic activities has been compromised by the lack of compounds with favorable physicochemical and pharmacokinetic properties which efficiently penetrate the blood-brain barrier. Recent progress in the generation of stabilized variants of solubilized neurotensin receptor 1 and its subsequent purification and successful structure determination presents a solid starting point to apply the approach of fragment-based screening to extend the chemical space of known neurotensin receptor 1 ligands. In this report, surface plasmon resonance was used as primary method to screen 6369 compounds. Thereby 44 hits were identified and confirmed in competition as well as dose-response experiments. Furthermore, 4 out of 8 selected hits were validated using nuclear magnetic resonance spectroscopy as orthogonal biophysical method. Computational analysis of the compound structures, taking the known crystal structure of the endogenous peptide agonist into consideration, gave insight into the potential fragment-binding location and interactions and inspires chemistry efforts for further exploration of the fragments.
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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.