ArticleMolecules (Basel, Switzerland)2020
Competition NMR for Detection of Hit/Lead Inhibitors of Protein-Protein Interactions.
Article in Molecules (Basel, Switzerland), 2020. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 11 papers.
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Who cites it
11 citing papers in PubMed.
- Biophysical Assays for Investigating Modulators of Macromolecular Complexes: An Overview.ACS omega · 2024Review
- Structural and biological characterization of pAC65, a macrocyclic peptide that blocks PD-L1 with equivalent potency to the FDA-approved antibodies.Molecular cancer · 2023Article
- In Vivo Protein-Protein Binding Competition Assay Based on Split-GFP Reassembly: Proof of Concept.Biomolecules · 2023Article
- Computer- and NMR-Aided Design of Small-Molecule Inhibitors of the Hub1 Protein.Molecules (Basel, Switzerland) · 2022Article
- Exploring the Surface of the Ectodomain of the PD-L1 Immune Checkpoint with Small-Molecule Fragments.ACS chemical biology · 2022Article
- Driving force of biomolecular liquid-liquid phase separation probed by nuclear magnetic resonance spectroscopy.Biophysics reports · 2022Article
- Fragment-to-Lead Medicinal Chemistry Publications in 2020.Journal of medicinal chemistry · 2022Review
- Small Molecule Agents Targeting PD-1 Checkpoint Pathway for Cancer Immunotherapy: Mechanisms of Action and Other Considerations for Their Advanced Development.Frontiers in immunology · 2022Review
- Design, Synthesis, and Biological Evaluation of Imidazopyridines as PD-1/PD-L1 Antagonists.ACS medicinal chemistry letters · 2021Article
- Small molecule inhibitors against PD-1/PD-L1 immune checkpoints and current methodologies for their development: a review.Cancer cell international · 2021Review
- Di-bromo-Based Small-Molecule Inhibitors of the PD-1/PD-L1 Immune Checkpoint.Journal of medicinal chemistry · 2020Article
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Authors and funding
7 authors.
Funding
Abstract
Screening for small-molecule fragments that can lead to potent inhibitors of protein-protein interactions (PPIs) is often a laborious step as the fragments cannot dissociate the targeted PPI due to their low μM-mM affinities. Here, we describe an NMR competition assay called w-AIDA-NMR (weak-antagonist induced dissociation assay-NMR), which is sensitive to weak μM-mM ligand-protein interactions and which can be used in initial fragment screening campaigns. By introducing point mutations in the complex's protein that is not targeted by the inhibitor, we lower the effective affinity of the complex, allowing for short fragments to dissociate the complex. We illustrate the method with the compounds that block the Mdm2/X-p53 and PD-1/PD-L1 oncogenic interactions. Targeting the PD-/PD-L1 PPI has profoundly advanced the treatment of different types of cancers.
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Registered trials
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