|
Multiple Myeloma
|
0.100 |
Biomarker
|
disease |
BEFREE |
Immunomodulatory drugs (IMiDs) including lenalidomide and pomalidomide bind cereblon (CRBN) and activate the CRL4<sup>CRBN</sup> ubiquitin ligase to trigger proteasomal degradation of the essential transcription factors IKZF1 and IKZF3 and multiple myeloma (MM) cytotoxicity.
|
30026574 |
2019 |
|
Multiple Myeloma
|
0.100 |
AlteredExpression
|
disease |
BEFREE |
The immunomodulatory drugs (IMiDs) thalidomide and its analogs, lenalidomide and pomalidomide, all FDA approved drugs for the treatment of multiple myeloma, induce ubiquitination and degradation of the lymphoid transcription factors Ikaros (IKZF1) and Aiolos (IKZF3) via the cereblon (CRBN) E3 ubiquitin ligase for proteasomal degradation.
|
31157769 |
2019 |
|
Multiple Myeloma
|
0.100 |
AlteredExpression
|
disease |
BEFREE |
Ikaros family zinc finger protein 1 and 3 (IKZF1 and IKZF3) are transcription factors that promote multiple myeloma (MM) proliferation.
|
30760870 |
2019 |
|
Multiple Myeloma
|
0.100 |
Biomarker
|
disease |
BEFREE |
We also demonstrated that treatment with a pan-PIM kinase inhibitor resulted in increased expression of cereblon, and that knockdown of cereblon via a shRNA lentivirus abolished the effects of PIM kinase inhibition on the degradation of IKZF1 and IKZF3 and myeloma cell apoptosis, demonstrating a central role of cereblon in pan-PIM kinase inhibitor-mediated down-regulation of IKZF1 and IKZF3 and myeloma cell killing.
|
30312729 |
2019 |
|
Multiple Myeloma
|
0.100 |
Biomarker
|
disease |
BEFREE |
CONCLUSIONS Our results suggest that baicalein suppresses the growth and promotes apoptosis of myeloma U266 cells through downregulating IKZF1 and IKZF3.
|
29729093 |
2018 |
|
Multiple Myeloma
|
0.100 |
Biomarker
|
disease |
BEFREE |
The immunomodulatory drugs (IMiDs) thalidomide, lenalidomide, and pomalidomide, all approved for the treatment of multiple myeloma, induce targeted ubiquitination and degradation of Ikaros (IKZF1) and Aiolos (IKZF3) via the cereblon (CRBN) E3 ubiquitin ligase.
|
30118587 |
2018 |
|
Multiple Myeloma
|
0.100 |
AlteredExpression
|
disease |
BEFREE |
The prognostic and predictive value of IKZF1 and IKZF3 expression in T-cells in patients with multiple myeloma.
|
30288348 |
2018 |
|
Multiple Myeloma
|
0.100 |
Biomarker
|
disease |
BEFREE |
For example, UBE2G1 inactivation significantly attenuated the degradation of myeloma survival factors IKZF1 and IKZF3 induced by lenalidomide and pomalidomide, hence conferring drug resistance.
|
30234487 |
2018 |
|
Multiple Myeloma
|
0.100 |
AlteredExpression
|
disease |
BEFREE |
Our data suggest a prognostic role of IKZF1, IKZF3 and BSG expression levels in lenalidomide-treated multiple myeloma.
|
28017969 |
2017 |
|
Multiple Myeloma
|
0.100 |
AlteredExpression
|
disease |
BEFREE |
Lenalidomide (LEN) acts directly on multiple myeloma (MM) cells by inducing cereblon-mediated degradation of interferon regulatory factor 4, Ikaros (IKZF)1 and IKZF3, transcription factors that are essential for MM cell survival.
|
28643330 |
2017 |
|
Multiple Myeloma
|
0.100 |
AlteredExpression
|
disease |
BEFREE |
IKZF1 and IKZF3 are essential transcription factors in multiple myeloma.
|
24292625 |
2014 |
|
Multiple Myeloma
|
0.100 |
Biomarker
|
disease |
BEFREE |
Analysis of myeloma cell lines revealed that loss of IKZF1 and IKZF3 is both necessary and sufficient for lenalidomide's therapeutic effect, suggesting that the antitumor and teratogenic activities of thalidomide-like drugs are dissociable.
|
24292623 |
2014 |