title: Noncovalent fluorescent probes of human immuno- and constitutive proteasomes.
abstract: 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.
authors.affiliation: Sorbonne Universités, UPMC Univ Paris 06, UMR 8256, Biological Adaptation and Ageing (B2A), Integrated Cellular Ageing and Inflammation , 7 Quai St Bernard, 75005 Paris, France.
authors.forename: Audrey
authors.initials: A
authors.lastname: Desvergne
authors.forename: Yan
authors.initials: Y
authors.lastname: Cheng
authors.forename: Sophie
authors.initials: S
authors.lastname: Grosay-Gaudrel
authors.forename: Xavier
authors.initials: X
authors.lastname: Maréchal
authors.forename: Michèle
authors.initials: M
authors.lastname: Reboud-Ravaux
authors.forename: Emilie
authors.initials: E
authors.lastname: Genin
authors.forename: Joëlle
authors.initials: J
authors.lastname: Vidal
mesh_terms: D005434:Flow Cytometry; D005456:Fluorescent Dyes; D057809:HEK293 Cells; D006801:Humans; D018613:Microscopy, Confocal; D010456:Peptides, Cyclic; D046988:Proteasome Endopeptidase Complex / Q000378:metabolism*; D061988:Proteasome Inhibitors / Q000378:metabolism*
chemical_list: D005456:Fluorescent Dyes; D010456:Peptides, Cyclic; D061988:Proteasome Inhibitors; C408291:TMC-95A; D046988:Proteasome Endopeptidase Complex