English
 
User Manual Privacy Policy Disclaimer Contact us
  Advanced SearchBrowse

Item

ITEM ACTIONSEXPORT
  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.

Item is

Basic

show hide
Item Permalink: http://hdl.handle.net/11858/00-001M-0000-002E-55CA-5 Version Permalink: http://hdl.handle.net/11858/00-001M-0000-002E-9B29-7
Genre: Journal Article

Files

show Files
hide Files
:
2505339.pdf (Publisher version), 2MB
 
File Permalink:
-
Name:
2505339.pdf
Description:
-
Visibility:
Restricted (Max Planck Institute for Biophysical Chemistry (Karl Friedrich Bonhoeffer Institute), Göttingen; )
MIME-Type / Checksum:
application/pdf
Technical Metadata:
Copyright Date:
-
Copyright Info:
-
License:
-
:
2505339_Suppl.docx (Supplementary material), 2MB
Name:
2505339_Suppl.docx
Description:
-
Visibility:
Public
MIME-Type / Checksum:
application/vnd.openxmlformats-officedocument.wordprocessingml.document / [MD5]
Technical Metadata:
Copyright Date:
-
Copyright Info:
-
License:
-

Locators

show

Creators

show
hide
 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              

Content

show
hide
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.

Details

show
hide
Language(s): eng - English
 Dates: 2017-11-162017-12
 Publication Status: Published in print
 Pages: -
 Publishing info: -
 Table of Contents: -
 Rev. Method: Peer
 Identifiers: DOI: 10.1007/s10858-017-0150-5
 Degree: -

Event

show

Legal Case

show

Project information

show

Source 1

show
hide
Title: Journal of Biomolecular NMR
Source Genre: Journal
 Creator(s):
Affiliations:
Publ. Info: -
Pages: - Volume / Issue: 69 (4) Sequence Number: - Start / End Page: 229 - 235 Identifier: -