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  Label-free NMR-based dissociation kinetics determination.

Trigo-Mourino, P., Griesinger, C., & Lee, D. (2017). Label-free NMR-based dissociation kinetics determination. Journal of Biomolecular NMR, 69(4), 229-235. doi:10.1007/s10858-017-0150-5.

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 Creators:
Trigo-Mourino, P.1, Author           
Griesinger, C.1, Author           
Lee, D., Author
Affiliations:
1Department of NMR Based Structural Biology, MPI for Biophysical Chemistry, Max Planck Society, ou_578567              

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Free keywords: Ligand binding; NMR; Relaxation dispersion
 Abstract: Understanding the dissociation of molecules is the basis to modulate interactions of biomedical interest. Optimizing drugs for dissociation rates is found to be important for their efficacy, selectivity, and safety. Here, we show an application of the high-power relaxation dispersion (RD) method to the determination of the dissociation rates of weak binding ligands from receptors. The experiment probes proton RD on the ligand and, therefore, avoids the need for any isotopic labeling. The large ligand excess eases the detection significantly. Importantly, the use of large spin-lock fields allows the detection of faster dissociation rates than other relaxation approaches. Moreover, this experimental approach allows to access directly the off-rate of the binding process without the need for analyzing a series of samples with increasing ligand saturation. The validity of the method is shown with small molecule interactions using two macromolecules, bovine serum albumin and tubulin heterodimers.

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Language(s): eng - English
 Dates: 2017-11-162017-12
 Publication Status: Issued
 Pages: -
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 Table of Contents: -
 Rev. Type: Peer
 Identifiers: DOI: 10.1007/s10858-017-0150-5
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Title: Journal of Biomolecular NMR
Source Genre: Journal
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Pages: - Volume / Issue: 69 (4) Sequence Number: - Start / End Page: 229 - 235 Identifier: -