STD NMR in Drug Discovery: Saturation Transfer Difference at Creative Biostructure, Slides of Biology

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std-nmr drug discovery

Various nuclear magnetic resonance (NMR) spectroscopy applications have been developed for the

identification and validation of hit compounds and lead optimization. NMR has many advantages, such as the

ability to directly observe target proteins and compounds and can be used for protein-based and ligand-

based approaches. NMR spectroscopy can also offer significant information about the interactions in the

protein-ligand complex, such as structure, affinity, and kinetics, especially in cases where the interactions are

too weak to be detected by other approaches or where high-quality crystals of protein-ligand complex

cannot be obtained. Among them, the saturation transfer difference (STD) NMR has become a popular

ligand-based approach for studying protein-ligand interactions and it has been shown to be particularly

effective in fragment screening.

Creative Biostructure applies expertise and experience in NMR spectroscopy technology to lead compound

discovery and optimization. We provide STD NMR services to help you directly identify a ligand against the

specific target from a mixture of compounds and determine its pharmacophoric groups.

Advantages of our MagHelix™ Saturation Transfer Difference (STD) NMR services:

• There is no requirement for the molecular weight of the protein and this approach does not require

stable isotope or radioisotope to label the target protein.

• Epitope maps of ligands binding to target proteins at the atomic level can be obtained without

crystallized protein-ligand complexes.

• Suitable for the screening of ligands with medium-weak affinity (high nm to low mm).
• Customers only need to provide a small number of samples, since this approach is extremely sensitive to

detect ligand binding at low protein concentration.

• We can rapidly and reliably obtain high-quality structural information and the values including KD,

association and dissociation kinetics from STD NMR experiments.

• By improving the STD NMR method, we can perform fragment screening against soluble therapeutic

targets and membrane proteins, such as GPCRs.

• We overcome the lack of conventional STD NMR to obtain information about the amino acids

surrounding the ligand in the binding site and can get pharmacophore information on the target protein.

Creative Biostructure is confident to provide STD NMR services to assist you in solving ligand screening

and binding site characterization in drug discovery programs. Before performing the STD NMR

experiment, our scientists will design an experimental strategy according to specific research purposes.

Our standard operating procedures ensure the reliability of experimental data. And we will offer all the

raw data and analysis reports. Furthermore, a variety of mainstream

biophysical techniques for the validation and characterization of hits can be found here.

Thank you!

Excerpt from:

https://drug-discovery.creative-biostructure.com/maghelix-

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