| + |
carfilzomib | down-regulates activity 
chemical inhibition
|
PSMB9 |
0.8 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-259311 |
|
|
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 |
| + |
carfilzomib | down-regulates activity
chemical inhibition
|
PSMB10 |
0.8 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-259308 |
|
|
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 |
| + |
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 |
| + |
carfilzomib | down-regulates activity
chemical inhibition
|
PSMB5 |
0.8 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-257818 |
|
|
Homo sapiens |
MOLT-4 Cell |
| pmid |
sentence |
| 19348473 |
Carfilzomib selectively inhibits the CT-L activity of the 20S proteasome and displays equivalent potency against β5 and LMP7 with minimal cross reactivity to other protease classes. |
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| + |
carfilzomib | down-regulates activity
chemical inhibition
|
PSMB8 |
0.8 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-257819 |
|
|
Homo sapiens |
MOLT-4 Cell |
| pmid |
sentence |
| 19348473 |
Carfilzomib selectively inhibits the CT-L activity of the 20S proteasome and displays equivalent potency against β5 and LMP7 with minimal cross reactivity to other protease classes. |
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| + |
carfilzomib | down-regulates activity
chemical inhibition
|
PSMB1 |
0.8 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-259307 |
|
|
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 |
3.0
carfilzomib
