+ |
PSMB2 | form complex
binding
|
26S Proteasome |
0.887 |
Identifier |
Residue |
Sequence |
Organism |
Cell Line |
SIGNOR-263358 |
|
|
Homo sapiens |
HEK-293 Cell |
pmid |
sentence |
29636472 |
Here, we report near-atomic resolution cryo-EM structures of the activated human proteasome|The proteasome is composed of a 28-subunit barrel-shaped core particle (CP) and two 19- subunit regulatory particles (RP)5–8 capped at both sides of the CP|Human proteasomes were purified through affinity chromatography on a large scale from a stable HEK293 cell line |
|
Publications: |
1 |
Organism: |
Homo Sapiens |
+ |
carfilzomib | down-regulates activity
chemical inhibition
|
PSMB2 |
0.8 |
Identifier |
Residue |
Sequence |
Organism |
Cell Line |
SIGNOR-259310 |
|
|
Homo sapiens |
Myeloma Cell |
pmid |
sentence |
17591945 |
Carfilzomib is a tetrapeptide epoxyketone related to epoxomicin (Figure 1A), the latter of which shows high specificity in vitro for the ChT-L proteasome activity. To evaluate the proteasomal inhibitory potential of carfilzomib in MM, extracts from ANBL-6 cells were exposed to increasing concentrations of carfilzomib. Extended exposure to carfilzomib for 5 hours saturated the β5 and β5i active sites in a dose-dependent manner and also led to increased binding to the β1, β1i, β2, and β2i subunits, with maximal binding observed at 50 nM. |
|
Publications: |
1 |
Organism: |
Homo Sapiens |
+ |
bortezomib | down-regulates activity
chemical inhibition
|
PSMB2 |
0.8 |
Identifier |
Residue |
Sequence |
Organism |
Cell Line |
SIGNOR-259309 |
|
|
Homo sapiens |
Myeloma Cell |
pmid |
sentence |
21504411 |
Proteasome inhibition is a modern and surprisingly successful approach how to cancer treatment. Bortezomib (Velcade®) is a first-in-class proteasome inhibitor and has been approved for first-line treatment of multiple myeloma and second-line treatment of mantle cell lymphoma. |
|
Publications: |
1 |
Organism: |
Homo Sapiens |