A panel of subunit-selective activity-based proteasome probes.
Mammals express seven different catalytically active proteasome subunits. In order to determine the roles of the different proteolytically active subunits in antigen presentation and other cellular processes, highly specific inhibitors and activity-based probes that selectively target specific active sites are needed. In this work we present the development of fluorescent activity-based probes that selectively target the beta1 and beta5 sites of the constitutive proteasome.
Verdoes
Martijn
M
Leiden Institute of Chemistry, Gorlaeus Laboratories, Leiden University, PO Box 9502, 2300 RA Leiden, The Netherlands.
Willems
Lianne I
LI
van der Linden
Wouter A
WA
Duivenvoorden
Boudewijn A
BA
van der Marel
Gijsbert A
GA
Florea
Bogdan I
BI
Kisselev
Alexei F
AF
Overkleeft
Herman S
HS
D001665:Binding Sites; D002478:Cells, Cultured; D004791:Enzyme Inhibitors / Q000737:chemistry; D005456:Fluorescent Dyes / Q000737:chemistry*; D006801:Humans; D008958:Models, Molecular; D046988:Proteasome Endopeptidase Complex / Q000737:chemistry / Q000378:metabolism*; D061988:Proteasome Inhibitors; D021122:Protein Subunits / Q000037:antagonists & inhibitors / Q000737:chemistry* / Q000378:metabolism; D013379:Substrate Specificity
D004791:Enzyme Inhibitors; D005456:Fluorescent Dyes; D061988:Proteasome Inhibitors; D021122:Protein Subunits; D046988:Proteasome Endopeptidase Complex
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