E-resources
Peer reviewed
-
de Bruin, Gerjan; Xin, Bo Tao; Kraus, Marianne; van der Stelt, Mario; van der Marel, Gijsbert A.; Kisselev, Alexei F.; Driessen, Christoph; Florea, Bogdan I.; Overkleeft, Herman S.
Angewandte Chemie (International ed.), March 18, 2016, Volume: 55, Issue: 13Journal Article
Proteasomes are therapeutic targets for various cancers and autoimmune diseases. Constitutively expressed proteasomes have three active sites, β1c, β2c, and β5c. Lymphoid tissues also express the immunoproteasome subunits β1i, β2i, and β5i. Rapid and simultaneous measurement of the activity of these catalytic subunits would assist in the discovery of new inhibitors, improve analysis of proteasome inhibitors in clinical trials, and simplify analysis of subunit expression. In this work, we present a cocktail of activity‐based probes that enables simultaneous gel‐based detection of all six catalytic human proteasome subunits. We used this cocktail to develop specific inhibitors for β1c, β2c, β5c, and β2i, to compare the active‐site specificity of clinical proteasome inhibitors, and to demonstrate that many hematologic malignancies predominantly express immunoproteasomes. Furthermore, we show that selective and complete inhibition of β5i and β1i is cytotoxic to primary cells from acute lymphocytic leukemia (ALL) patients. A cocktail of activity‐based probes enables the visualization and relative quantification of the six catalytically active subunits of the constitutive proteasome and the immunoproteasome. Proteasome inhibitors were thus characterized, and specific inhibitors for each subunit were developed. Specific inhibition of the immunoproteasome subunits β5i and β1i proved to be cytotoxic to primary cells from acute lymphocytic leukemia patients.
![loading ... loading ...](themes/default/img/ajax-loading.gif)
Shelf entry
Permalink
- URL:
Impact factor
Access to the JCR database is permitted only to users from Slovenia. Your current IP address is not on the list of IP addresses with access permission, and authentication with the relevant AAI accout is required.
Year | Impact factor | Edition | Category | Classification | ||||
---|---|---|---|---|---|---|---|---|
JCR | SNIP | JCR | SNIP | JCR | SNIP | JCR | SNIP |
Select the library membership card:
If the library membership card is not in the list,
add a new one.
DRS, in which the journal is indexed
Database name | Field | Year |
---|
Links to authors' personal bibliographies | Links to information on researchers in the SICRIS system |
---|
Source: Personal bibliographies
and: SICRIS
The material is available in full text. If you wish to order the material anyway, click the Continue button.