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Noncovalent Fluorescent Probes of Human Immuno- and Constitutive Proteasomes

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journal contribution
posted on 13.11.2014, 00:00 by Audrey Desvergne, Yan Cheng, Sophie Grosay-Gaudrel, Xavier Maréchal, Michèle Reboud-Ravaux, Emilie Genin, Joëlle Vidal
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.