MST in Drug Discovery: Characterizing Biomolecular Interactions, Slides of Biology

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microscale thermophoresis frag

ment screening

Microscale thermophoresis (MST) has become a common

technique to detect specific target-probe interactions,

and it measures the differences in the movement rate

through a microscopic temperature gradient caused when

complexes are formed. MST can be applied to

characterize any type of biomolecular interactions, for

example, protein-DNA, protein-RNA, protein-protein,

antigen-antibody interactions, as well as the binding of a

ligand to ternary complexes.

Brief Introduction to Microscale Thermophoresis (MST)

MST is a non-immobilized technique for quantitative analysis of

biomolecular interactions in solution. The technique is based on

thermophoresis and fluorescence detection. The instrument of MST

utilizes an infrared laser for local heating to cause molecular directional

movement, and then analyze the molecular distribution ratio in the

temperature gradient field by fluorescence (fluorescence labeling or

intrinsic fluorescence). The MST technique can detect ligand binding-

caused changes in thermophoretic mobility, which rely on size, charge,

hydration shell, and conformations. Kd values can be estimated using

these changes in thermophoretic mobility.

Advantages of our MagHelix™ Microscale Thermophoresis (MST) services:

• We have many years of experience in using MST technology to study

biomolecular interactions, and our MST services have been proven to be

reliable by customers from biotech, pharmaceutical, and biopharmaceutical

industries.

• Determination of binding stoichiometries and the number of binding sites.
• Determination of thermodynamic parameters of interactions, such as ΔG G

(Gibbs free energy), ΔG H (enthalpy), and ΔG S (entropy).

• We can apply MST technology to perform

high-throughput screening of compounds/fragments and

fragment-based screening.

• By combining with other biophysical technologies, the limitations of MST are

compensated to make the results more reliable.

As an advanced contract service provider in the drug discovery phase, Creative

Biostructure can simultaneously apply a variety of established approaches and

biophysical techniques to identify, validate, classify and characterize the hit

compounds according to the goals and requirements of the project. If your

project has such needs, please feel free to contact us, and our scientists will

provide professional consultation for you.

References

1.Alexander C G.; et al. Novel microscale approaches for easy, rapid determination of protein

stability in academic and commercial settings. Biochimica et Biophysica Acta (BBA)-Proteins and

Proteomics. 2014, 1844(12): 2241-2250.

2.Bartoschik T.; et al. Microscale thermophoresis in drug discovery. Applied Biophysics for Drug

Discovery. 2017: 73-99.

3.Rainard J M.; et al. Using microscale thermophoresis to characterize hits from high-

throughput screening: a European lead factory perspective. SLAS DISCOVERY: Advancing Life

Sciences R&D. 2018, 23(3): 225-241.