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Related Concept Videos

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Labeling DNA Probes

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DNA probes are fragments of DNA labeled with a reporter tag to enable their detection or purification. The resulting labeled DNA probes can then hybridize to target nucleic acid sequences through complementary base-pairing, and may be used to recover or identify these regions.
Radioisotopes, fluorophores, or small molecule binding partners like biotin or digoxigenin, are the most widely used reporter tags for labeling DNA probes. These labels can be attached to the probe DNA molecule via...
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Screening Traditional Chinese Medicine Compounds for Inhibiting UCHL3 Activity Based on Molecular Docking and Deubiquitinating Enzyme Probe Technology
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Recent Developments in Cell Permeable Deubiquitinating Enzyme Activity-Based Probes.

Daniel Conole1, Milon Mondal1, Jaimeen D Majmudar2

  • 1Department of Chemistry, Imperial College London, London, United Kingdom.

Frontiers in Chemistry
|January 11, 2020
PubMed
Summary
This summary is machine-generated.

New cell-permeable activity-based probes (ABPs) enable direct study of deubiquitinating enzymes (DUBs) in live cells. This advances understanding of DUB function in health and disease, aiding drug discovery.

Keywords:
DUB activityactivity based probecell permeabilitydeubiquinating enzymesdeubiquitinasesmall moleculeubiquitin (Ub)

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Area of Science:

  • Biochemistry
  • Molecular Biology
  • Chemical Biology

Background:

  • Deubiquitinating enzymes (DUBs) regulate protein function by removing ubiquitin tags.
  • Dysregulation of DUBs is linked to various diseases, but their specific roles are often unclear.
  • Traditional ubiquitin-based activity-based probes (ABPs) are not cell-permeable, limiting in vivo studies.

Purpose of the Study:

  • To review recent advancements in cell-permeable small molecule ABPs targeting DUBs.
  • To discuss the applications of these novel probes in live-cell research.
  • To compare cell-permeable DUB ABPs with traditional ubiquitin-based probes.

Main Methods:

  • Review of recent literature on small molecule DUB activity-based probes.
  • Discussion of probe design and chemical reactivity.
  • Analysis of applications in live-cell imaging, target engagement, and biomarker discovery.

Main Results:

  • Development of cell-permeable small molecule ABPs for DUBs.
  • Demonstration of their utility in studying DUB activity within intact cells.
  • Highlighting advantages over non-permeable probes for physiological context.

Conclusions:

  • Cell-permeable DUB ABPs are crucial tools for understanding enzyme function in live systems.
  • These probes enhance translational research, including drug development and diagnostics.
  • Further development promises deeper insights into DUBs' roles in disease.