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Related Concept Videos

Drug Discovery: Overview01:26

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Drug discovery is a multifaceted process involving extensive screening, testing, and optimization of lead compounds to identify potential new drugs for therapeutic use. It combines several approaches, including screening large numbers of natural products, chemical modification of known active molecules, identification of new drug targets, and rational design based on biological mechanisms and drug-receptor structure. These approaches are carried out in both academic research laboratories and...
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X-ray diffraction or XRD is an analytical tool that utilizes X-rays to study ordered structures such as crystalline organic and inorganic samples, polycrystalline materials, proteins, carbohydrates, and drugs.
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Nuclear magnetic resonance (NMR) spectroscopy is a very valuable analytical technique for researchers. It has been used for more than 50 years as an analytical tool. F. Bloch and E. Purcell formulated NMR in 1946 and won the 1952 Nobel Prize in Physics  for their work. Biological macromolecules such as proteins, nucleic acids, lipids, and organic molecules including pharmaceutical compounds, can be studied using this versatile tool that exploits the magnetic properties of certain nuclei.
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Related Experiment Video

Updated: Jan 12, 2026

Biosensor-based High Throughput Biopanning and Bioinformatics Analysis Strategy for the Global Validation of Drug-protein Interactions
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Drug discovery through biophysical techniques: Methods and applications.

Yinhao Zhou1, Haiyun Hu1, Qiuyan Huang1

  • 1Jiangsu Key Laboratory of Drug Discovery and Translational Research for Brain Diseases, Jiangsu Province Engineering Research Center of Precision Diagnostics and Therapeutics Development, Suzhou International Joint Laboratory for Diagnosis and Treatment of Brain Diseases, College of Pharmaceutical Sciences, Soochow University, Suzhou, Jiangsu 215123, China.

Pharmacology & Therapeutics
|November 8, 2025
PubMed
Summary

Biophysical techniques are essential for modern drug discovery, offering insights into molecular interactions and protein behavior. This review details key methods like SPR, NMR, and MS to accelerate therapeutic development.

Keywords:
BLIBiophysical technologyCETSADrug discoveryFPFRETHDX-MSITCMSTNMRSPRTSAX-ray crystallographyXL-MS

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Area of Science:

  • Biophysics
  • Drug Discovery
  • Analytical Chemistry

Background:

  • Modern drug discovery requires precise characterization of molecular dynamics and protein behavior.
  • Biophysical techniques are crucial for investigating protein-ligand interactions, structural basis, and cellular mechanisms in rational drug design.

Purpose of the Study:

  • To systematically review pivotal biophysical technologies used in contemporary drug discovery.
  • To trace the historical development, fundamental principles, and innovations of these techniques.
  • To evaluate the strengths, limitations, and emerging trends of each method for advancing therapeutic innovation.

Main Methods:

  • Förster resonance energy transfer (FRET)
  • Fluorescence polarization (FP)
  • Thermal shift assays (TSA/CETSA)
  • Surface plasmon resonance (SPR)
  • Bio-layer interferometry (BLI)
  • Microscale thermophoresis (MST)
  • Isothermal titration calorimetry (ITC)
  • Nuclear magnetic resonance (NMR)
  • X-ray crystallography
  • Mass spectrometry (MS)-based approaches (HDX-MS, XL-MS)

Main Results:

  • The review systematically summarizes key biophysical techniques essential for drug discovery.
  • Each method's historical development, principles, and innovations are detailed.
  • Strengths, limitations, and emerging trends like improved sensitivity and automation are discussed.

Conclusions:

  • Biophysical techniques are indispensable tools in pharmaceutical development, accelerating the discovery of innovative therapeutic agents.
  • Advancements in sensitivity, automation, and high-throughput implementation will ensure these methods remain pivotal in biomedical research and precision medicine.
  • These techniques are vital for addressing complex drug targets and the growing need for personalized therapeutic solutions.