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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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Electromagnetic (EM) radiation can be considered an oscillating electric and magnetic field propagating through a medium that can interact with matter in its path. The electric field in the radiation can interact with electrical charges in the atoms or molecules in the matter. On the other hand, the magnetic field can interact with the magnetic field in the atomic nucleus. The study of the interaction between electromagnetic radiation and matter is termed spectroscopy. Spectroscopy is the study...
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Electromagnetic (EM) radiation consists of electric and magnetic field components oscillating in planes perpendicular to each other and mutually perpendicular to radiation propagation through space. EM radiation can be classified as a wave, characterized by the properties of waves such as wavelength (denoted as λ) and frequency (represented by ν).
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Cryo-electron Microscopy01:28

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Conventional electron microscopy (EM) involves dehydration, fixation, and staining of biological samples, which distorts the native state of biological molecules and results in several artifacts. Also, the high-energy electron beam damages the sample and makes it difficult to obtain high-resolution images. These issues can be addressed using cryo-EM, which uses frozen samples and gentler electron beams. The technique was developed by Jacques Dubochet, Joachim Frank, and Richard Henderson, for...
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Pharmacokinetics: Drug–Drug Interactions01:25

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Drug interactions occur when the pharmacological effect of one drug is altered by another substance, either enhancing or diminishing its activity. The drug whose activity is altered is known as the object drug, and the substance causing the alteration is called the agent drug or the precipitant. The net effects of these interactions are mostly undesirable, leading to decreased effectiveness or increased adverse effects. In rare cases, interactions can be beneficial, such as the enhanced...
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Bioequivalence of Drugs: Drugs with Multiple Indications01:09

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The concept of therapeutic equivalence (TE) in drugs with multiple indications is complex. A generic drug may be therapeutically equivalent to a brand-name product for one specific indication, but this doesn't necessarily mean it's equivalent for all other indications. Evidence of TE in one patient group and bioequivalence shown in healthy volunteers can support—but not confirm—TE for other indications. However, definitive proof requires individual clinical studies for each...
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Related Experiment Video

Updated: Jan 30, 2026

Preparation of High-Temperature Sample Grids for Cryo-EM
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Cryo-EM in drug discovery.

Tom Ceska1, Chun-Wa Chung2, Rob Cooke3

  • 1UCB Pharma, 216 Bath Road, Slough SL1 3WE, U.K. tom.ceska@ucb.com.

Biochemical Society Transactions
|January 17, 2019
PubMed
Summary

Advances in X-ray crystallography, driven by technology like GPUs, now enable high-resolution protein structure analysis. This technique is crucial for pharmaceutical drug discovery, revealing insights into ligand binding and complex protein structures.

Keywords:
cryo-EMdrug discoverypharmaceuticalstructural biology

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Area of Science:

  • Structural biology
  • Drug discovery
  • Biophysics

Background:

  • X-ray crystallography has been the primary technique in structural biology for three decades.
  • Recent technological advancements have significantly improved the resolution and analysis of protein structures.
  • These improvements include direct electron detectors, enhanced automation, and increased computing power via GPUs.

Purpose of the Study:

  • To review the impact of structural biology, specifically X-ray crystallography, on pharmaceutical drug discovery.
  • To highlight key protein structures relevant to the pharmaceutical industry.
  • To showcase the application of X-ray crystallography in analyzing challenging biological systems.

Main Methods:

  • Review of recent technological improvements in X-ray crystallography.
  • Analysis of high-resolution protein structure data.
  • Application of crystallography to study ligand-binding sites, membrane proteins, and protein complexes.

Main Results:

  • Technological advancements have enabled the acquisition and analysis of high-resolution protein structural data.
  • X-ray crystallography is effectively addressing complex targets such as membrane proteins and large molecular assemblies.
  • The technique provides detailed insights into ligand-protein interactions and structural features relevant to drug design.

Conclusions:

  • X-ray crystallography, enhanced by modern technology, is a powerful tool for pharmaceutical research and drug discovery.
  • The technique offers critical structural information for understanding disease mechanisms and developing novel therapeutics.
  • Continued advancements in crystallography will further accelerate the identification and optimization of drug candidates.