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5LAJ

Ligand-induced Lys33-Thr1 crosslinking at the yeast proteasomal subunit beta5 by sulfonate esters

Summary for 5LAJ
Entry DOI10.2210/pdb5laj/pdb
Related4R18 5CZ4
DescriptorProteasome subunit alpha type-2, Proteasome subunit beta type-4, Proteasome subunit beta type-5, ... (16 entities in total)
Functional Keywordsproteasome, fluorescent probes, binding analysis, umpolung, crosslink, hydrolase
Biological sourceSaccharomyces cerevisiae (strain ATCC 204508 / S288c) (Baker's yeast)
More
Total number of polymer chains28
Total formula weight731318.13
Authors
Groll, M.,Dubiella, C.,Cui, H. (deposition date: 2016-06-14, release date: 2017-04-26, Last modification date: 2024-01-10)
Primary citationDubiella, C.,Cui, H.,Groll, M.
Tunable Probes with Direct Fluorescence Signals for the Constitutive and Immunoproteasome.
Angew. Chem. Int. Ed. Engl., 55:13330-13334, 2016
Cited by
PubMed Abstract: Electrophiles are commonly used for the inhibition of proteases. Notably, inhibitors of the proteasome, a central determinant of cellular survival and a target of several FDA-approved drugs, are mainly characterized by the reactivity of their electrophilic head groups. We aimed to tune the inhibitory strength of peptidic sulfonate esters by varying the leaving groups. Indeed, proteasome inhibition correlated well with the pK of the leaving group. The use of fluorophores as leaving groups enabled us to design probes that release a stoichiometric fluorescence signal upon reaction, thereby directly linking proteasome inactivation to the readout. This principle could be applicable to other sulfonyl fluoride based inhibitors and allows the design of sensitive probes for enzymatic studies.
PubMed: 27709817
DOI: 10.1002/anie.201605753
PDB entries with the same primary citation
Experimental method
X-RAY DIFFRACTION (2.9 Å)
Structure validation

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