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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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Detection of Bacteria Using Fluorogenic DNAzymes
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Fluorescent Probes for Ecto-5'-nucleotidase (CD73).

Constanze C Schmies1, Georg Rolshoven1, Riham M Idris1

  • 1PharmaCenter Bonn, Pharmaceutical Institute, Department of Pharmaceutical & Medicinal Chemistry, University of Bonn, An der Immenburg 4, D-53121 Bonn, Germany.

ACS Medicinal Chemistry Letters
|November 20, 2020
PubMed
Summary
This summary is machine-generated.

Researchers developed novel fluorescent CD73 inhibitors. These high-affinity probes, derived from PSB-12379, are valuable for studying the immunosuppressive enzyme ecto-5'-nucleotidase (CD73) in biological and diagnostic applications.

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Area of Science:

  • Biochemistry
  • Medicinal Chemistry
  • Immunology

Background:

  • Ecto-5'-nucleotidase (CD73) generates adenosine, an immunosuppressive molecule.
  • CD73 is prevalent in cancer cells, promoting an immunosuppressive tumor microenvironment.

Purpose of the Study:

  • To design and synthesize novel fluorescent inhibitors of CD73.
  • To create high-affinity probes for CD73 for biological and diagnostic use.

Main Methods:

  • Chemical synthesis of fluorescent-labeled CD73 inhibitors based on N-benzyl-α,β-methylene-ADP (PSB-12379).
  • Characterization of inhibitor affinity and selectivity for CD73.

Main Results:

  • Developed fluorescent CD73 inhibitors with low nanomolar affinity.
  • Identified PSB-18332 (2.98 nM) and PSB-19416 (12.6 nM) as high-affinity probes.
  • Achieved high selectivity for CD73.

Conclusions:

  • The synthesized fluorescent probes are effective tools for CD73 research.
  • These compounds can be utilized in biological studies, drug screening, and diagnostics.