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Related Concept Videos

X-ray Diffraction of Biological Samples01:10

X-ray Diffraction of Biological Samples

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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.
According to Bragg's law, when X-rays strike the sample positioned on a stage, the rays are  scattered by the electron clouds around the sample atoms. The  X-ray diffraction or scattering is caused by constructive interference of the X-ray waves that reflect off the internal...
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X-ray Crystallography02:18

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The size of the unit cell and the arrangement of atoms in a crystal may be determined from measurements of the diffraction of X-rays by the crystal, termed X-ray crystallography.
Diffraction
Diffraction is the change in the direction of travel experienced by an electromagnetic wave when it encounters a physical barrier whose dimensions are comparable to those of the wavelength of the light. X-rays are electromagnetic radiation with wavelengths about as long as the distance between neighboring...
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Updated: Dec 8, 2025

Microfluidic Chips for In Situ Crystal X-ray Diffraction and In Situ Dynamic Light Scattering for Serial Crystallography
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Serial Crystallography for Structure-Based Drug Discovery.

Lan Zhu1, Xiaoyu Chen1, Enrique E Abola1

  • 1Biodesign Center for Applied Structural Discovery, Biodesign Institute, Arizona State University, Tempe, AZ 85287, USA; School of Molecular Sciences, Arizona State University, Tempe, AZ 85287, USA.

Trends in Pharmacological Sciences
|September 20, 2020
PubMed
Summary
This summary is machine-generated.

Serial crystallography (SX) advances drug discovery by enabling structural determination of challenging targets. This technique offers insights into dynamic molecular mechanisms, paving the way for novel therapeutics.

Keywords:
GPCR ligand swappingX-ray free-electron laser (XFEL)serial femtosecond crystallographystructure-based drug discovery (SBDD)synchrotron-based serial crystallographytime-resolved serial crystallography

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Area of Science:

  • Structural Biology
  • Drug Discovery
  • Biophysics

Background:

  • Structure-based drug discovery relies on 3D structural data of drug targets.
  • Experimental determination of these structures is often challenging, especially for difficult targets.
  • Serial crystallography (SX) has emerged as a powerful technique for structural determination.

Purpose of the Study:

  • To summarize recent advancements in serial crystallography (SX) technology.
  • To discuss the application of SX in structure-based drug discovery.
  • To highlight the potential of SX for elucidating dynamic molecular mechanisms.

Main Methods:

  • Serial crystallography (SX) utilizing X-ray free-electron lasers (XFELs).
  • Adaptation of SX techniques for use in synchrotron radiation facilities.
  • Time-resolved studies enabled by ultrashort X-ray pulses.

Main Results:

  • SX enables structural determination of drug targets using small crystals (micrometer/nanometer size).
  • The technology has been successfully applied to notoriously difficult-to-study targets at room temperature.
  • SX allows for time-resolved characterization of dynamic structural changes.

Conclusions:

  • Serial crystallography is a rapidly progressing technology with significant implications for drug discovery.
  • SX provides a pathway to study the molecular mechanisms of drug action through 'molecular movies'.
  • Future applications of SX promise to accelerate the development of safer and more efficacious therapeutics.