Noncovalent Fluorescent Probes of Human Immuno- and Constitutive Proteasomes

We report here the synthesis and biological evaluation of fluorescent probes functioning as inhibitors that noncovalently block human immuno- and constitutive proteasomes. These cell-penetrating linear analogues of the natural cyclopeptide TMC-95A were efficient on cells at the nanomolar level and a...

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Bibliographic Details
Published in:Journal of medicinal chemistry 2014-11, Vol.57 (21), p.9211-9217
Main Authors: Desvergne, Audrey, Cheng, Yan, Grosay-Gaudrel, Sophie, Maréchal, Xavier, Reboud-Ravaux, Michèle, Genin, Emilie, Vidal, Joëlle
Format: Article
Language:English
Subjects:
Chemical Sciences
Flow Cytometry
Fluorescent Dyes
HEK293 Cells
Humans
Medicinal Chemistry
Microscopy, Confocal
Peptides, Cyclic
Proteasome Endopeptidase Complex - metabolism
Proteasome Inhibitors - metabolism
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Summary:We report here the synthesis and biological evaluation of fluorescent probes functioning as inhibitors that noncovalently block human immuno- and constitutive proteasomes. These cell-penetrating linear analogues of the natural cyclopeptide TMC-95A were efficient on cells at the nanomolar level and assessed by confocal microscopy and flow cytometry. They may constitute an alternative to previously reported fluorescent probes that all bind covalently to proteasomes.
ISSN:0022-2623
1520-4804
DOI:10.1021/jm5011429