KinITC: Transforming the ITC roles in Drug Discovery.

Since the kinetic information is the more relevant thing to look at in drug discovery, a typical question comes to our minds:

Which technique should we choose to get kinetic information?

This question doesn´t have an easy answer because many factors should be taken into account to make this decision, but lately, one technique is rising up: Isothermal titration calorimetry and more specifically, the KinITC method developed by P Duma et al [1].

 

In AFFINImeter we have implemented the KinITC method that is making possible the measurement of binding kinetics, kon and koff rate constants, through the analysis of the thermogram (s) obtained from a traditional ITC experiment (s).

 

Try our KinITC tool

 

We want to share the following article as an example of how some researchers are exploring kinetics of molecular interaction with KinITC. In this article, the authors used KinITC to analyzed 29 ITC data of mannosides binding to the bacterial adhesin FimH and they validated those kinetic values obtained with the KinITC method with Surface Plasmon Resonance experiments [2].

 

 

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Here are few recommendations though if you are planning to perform new ITC experiments, focused on getting high-quality data for kinetic analysis:

[1] Dumas et al. (2016) Extending ITC to Kinetics with KinITC, Methods in Enzymology, Vol. 567, Chap. 7, A. Feig Ed.
[2] Ernst et al. (2018) KinITC—One Method Supports both Thermodynamic and Kinetic SARs as Exemplified on FimH Antagonists, Chemistry A European Journal. 10.1002/chem.201802599