ArticleNature communications2018
Rapid measurement of inhibitor binding kinetics by isothermal titration calorimetry.
Article in Nature communications, 2018. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 22 papers.
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Who cites it
22 citing papers in PubMed, 67 citations in OpenAlex.
- Graph neural network modeling of receptor interaction kinetics from single-molecule imaging data.bioRxiv : the preprint server for biology · 2026Article
- Decoding Enzyme-Inhibitor Kinetic Mechanisms by Isothermal Titration Calorimetry: The Case of SARS-CoV-2 3CLAnalytical chemistry · 2026Article
- Molecular and Analytical Understanding of Resveratrol Interactions for Advanced Biotechnological Applications.Molecules (Basel, Switzerland) · 2026Review
- Efficient acrylamide adduct formation suggests dual applications of ReAIV L-asparaginase.Amino acids · 2026Article
- In-Solution Characterization of Biomolecular Interaction Kinetics under Native Conditions.Analytical chemistry · 2025Article
- Characterization of antiviral compounds using Bio-Layer Interferometry.bioRxiv : the preprint server for biology · 2025Article
- FAP inhibitors: are we really using the best method to evaluate the residence time?European journal of nuclear medicine and molecular imaging · 2025Article
- Rapid Determination of Kinetic Constants for Slow-Binding Inhibitors and Inactivators of Human Histone Deacetylase 8.International journal of molecular sciences · 2024Article
- Article
- The feasibility of determining kinetic constants from isothermal titration calorimetry data.Biophysical journal · 2022Article
- Disentangling the recognition complexity of a protein hub using a nanopore.Nature communications · 2022Article
- Design, synthesis and in vitro evaluation of novel SARS-CoV-2 3CLEuropean journal of medicinal chemistry · 2022Article
- Bayesian regression and model selection for isothermal titration calorimetry with enantiomeric mixtures.PloS one · 2022Article
- A novel assay based on pre-equilibrium titration curves for the determination of enzyme inhibitor binding kinetics.European biophysics journal : EBJ · 2021Article
- Enzyme Kinetics by Isothermal Titration Calorimetry: Allostery, Inhibition, and Dynamics.Frontiers in molecular biosciences · 2020Review
- Estimation of non-constant variance in isothermal titration calorimetry using an ITC measurement model.PloS one · 2020Article
- Inhibitors of Brassinosteroid Biosynthesis and Signal Transduction.Molecules (Basel, Switzerland) · 2019Review
- Drug-Target Residence Time AffectsACS central science · 2019Article
- Quantifying the Interactions between Biomolecules: Guidelines for Assay Design and Data Analysis.ACS infectious diseases · 2019Article
- Empirical Scoring Functions for Structure-Based Virtual Screening: Applications, Critical Aspects, and Challenges.Frontiers in pharmacology · 2018Review
Corrections and comments
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Authors and funding
7 authors at 2 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Although drug development typically focuses on binding thermodynamics, recent studies suggest that kinetic properties can strongly impact a drug candidate's efficacy. Robust techniques for measuring inhibitor association and dissociation rates are therefore essential. To address this need, we have developed a pair of complementary isothermal titration calorimetry (ITC) techniques for measuring the kinetics of enzyme inhibition. The advantages of ITC over standard techniques include speed, generality, and versatility; ITC also measures the rate of catalysis directly, making it ideal for quantifying rapid, inhibitor-dependent changes in enzyme activity. We used our methods to study the reversible covalent and non-covalent inhibitors of prolyl oligopeptidase (POP). We extracted kinetics spanning three orders of magnitude, including those too rapid for standard methods, and measured sub-nM binding affinities below the typical ITC limit. These results shed light on the inhibition of POP and demonstrate the general utility of ITC-based enzyme inhibition kinetic measurements.
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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.