|
Multiple Myeloma
|
0.400 |
AlteredExpression
|
disease |
BEFREE |
We showed that ectopic MCL1 expression rescued apoptosis of MM.
|
31653349 |
2020 |
|
Multiple Myeloma
|
0.400 |
Biomarker
|
disease |
BEFREE |
Preclinical evaluation of the simultaneous inhibition of MCL-1 and BCL-2 with the combination of S63845 and venetoclax in multiple myeloma.
|
31320555 |
2020 |
|
Multiple Myeloma
|
0.400 |
Biomarker
|
disease |
BEFREE |
This work led to the discovery of <b>1</b>, a potent Mcl-1 inhibitor (IC<sub>50</sub> = 19 nM in an OPM-2 cell viability assay) with good pharmacokinetic properties and excellent in vivo efficacy in an OPM-2 multiple myeloma xenograft model.
|
31736296 |
2019 |
|
Multiple Myeloma
|
0.400 |
PosttranslationalModification
|
disease |
BEFREE |
Co-culture experiments resulted in MDSC-induced AMPK phosphorylation in MM cells, which was associated with an increase in the anti-apoptotic factors MCL-1 and BCL-2, and the autophagy-marker LC3II.
|
30419344 |
2019 |
|
Malignant neoplasm of lung
|
0.400 |
AlteredExpression
|
disease |
BEFREE |
Using the Mcl-1-binding PH domain of Akt as a docking site, we identified a novel small molecule, PH-687, that directly targets the PH domain and disrupts Mcl-1/Akt binding, leading to suppression of Akt activity and growth inhibition of lung cancer <i>in vitro</i> and <i>in vivo</i>.
|
31662324 |
2019 |
|
Malignant neoplasm of lung
|
0.400 |
Biomarker
|
disease |
BEFREE |
The CUL5 ubiquitin ligase complex mediates resistance to CDK9 and MCL1 inhibitors in lung cancer cells.
|
31294695 |
2019 |
|
Malignant neoplasm of lung
|
0.400 |
GeneticVariation
|
disease |
BEFREE |
Degradation of MCL-1 by bufalin reverses acquired resistance to osimertinib in EGFR-mutant lung cancer.
|
31301315 |
2019 |
|
Malignant neoplasm of lung
|
0.400 |
PosttranslationalModification
|
disease |
BEFREE |
Thus, nicotine-induced cell survival and chemoresistance may occur in a mechanism by stimulating Mcl-1 phosphorylation and its interaction with Bak, which may contribute to improving the efficacy of chemotherapy in the treatment of human lung cancer.
|
30741422 |
2019 |
|
Malignant neoplasm of lung
|
0.400 |
Biomarker
|
disease |
BEFREE |
In this study, we characterize the MCL-1 inhibitor maritoclax alone or in combination with a BCL-2/xL inhibitor in a panel of lung cancer cell lines.
|
31150457 |
2019 |
|
Multiple Myeloma
|
0.400 |
AlteredExpression
|
disease |
BEFREE |
In myeloma, in vitro sensitivity to venetoclax is mainly observed in plasma cells harboring the t(11;14) translocation, a molecular subgroup associated with high Bcl-2 and low Mcl-1/Bcl-XL expression.
|
30076373 |
2018 |
|
Multiple Myeloma
|
0.400 |
Biomarker
|
disease |
BEFREE |
Multiple myeloma is considered to be a disease dependent mainly on MCL1 for survival, based mostly on studies using cell lines.
|
30309889 |
2018 |
|
Multiple Myeloma
|
0.400 |
AlteredExpression
|
disease |
BEFREE |
ABT-199 is a specific Bcl-2 inhibitor in clinical trials for MM; however, its activity as a single agent was limited to myeloma patients with the t(11;14) translocation who acquire resistance due to co-expression of Mcl-1 and Bcl-xL.
|
29761903 |
2018 |
|
Multiple Myeloma
|
0.400 |
Biomarker
|
disease |
BEFREE |
Our studies demonstrate that AZD5991 binds directly to Mcl-1 and induces rapid apoptosis in cancer cells, most notably myeloma and acute myeloid leukemia, by activating the Bak-dependent mitochondrial apoptotic pathway.
|
30559424 |
2018 |
|
Multiple Myeloma
|
0.400 |
Biomarker
|
disease |
BEFREE |
Members of MCL1-M captured both MM cell-intrinsically acting signals and the signals regulating the interaction between MM cells with bone marrow microenvironment.
|
29696703 |
2018 |
|
Multiple Myeloma
|
0.400 |
Biomarker
|
disease |
BEFREE |
Expression of pro-survival BCL-2 family protein MCL-1 is essential for survival of malignant PC in multiple myeloma (MM).
|
30524962 |
2018 |
|
Multiple Myeloma
|
0.400 |
AlteredExpression
|
disease |
BEFREE |
MCL-1 ectopic expression or knockdown in MM cells significantly diminished or increased ABT-199 sensitivity, respectively.
|
29241222 |
2018 |
|
Multiple Myeloma
|
0.400 |
Biomarker
|
disease |
BEFREE |
In conclusion, the NEAT1/miR-193a/MCL1 pathway is closely associated with the development of DEX resistance in myeloma cells, and knockdown of NEAT1 can significantly improve DEX sensitivity in MM.
|
29205703 |
2018 |
|
Malignant neoplasm of lung
|
0.400 |
Biomarker
|
disease |
BEFREE |
Caenepeel and colleagues and Ramsey and colleagues have developed two novel, potent, and selective MCL1 inhibitors that are effective against many hematologic malignancies, and Nangia and colleagues describe how one of these inhibitors can be successfully combined with BCL-xL and MEK inhibition to treat KRAS-mutated lung cancer.<i>See related article by Ramsey et al., p. 1566</i>.<i>See related article by Caenepeel et al., p. 1582</i>.<i>See related article by Nangia et al., p. 1598</i>.
|
30510014 |
2018 |
|
Malignant neoplasm of lung
|
0.400 |
Biomarker
|
disease |
BEFREE |
MALAT1/miR-101-3p/MCL1 axis mediates cisplatin resistance in lung cancer.
|
29484127 |
2018 |
|
Malignant neoplasm of lung
|
0.400 |
Biomarker
|
disease |
BEFREE |
Imperatorin Targets MCL-1 to Sensitize CD133+ Lung Cancer Cells to γδ-T Cell-Mediated Cytotoxicity.
|
30138935 |
2018 |
|
Malignant neoplasm of lung
|
0.400 |
Biomarker
|
disease |
BEFREE |
Mechanistically, DTCs undergo a protein biosynthesis enrichment resulting in increased mTORC1-mediated mRNA translation of MCL-1, revealing a novel mechanism in which lung cancer cells adapt to short-term pressures of apoptosis-inducing kinase inhibitors.
|
30087143 |
2018 |
|
Multiple Myeloma
|
0.400 |
Biomarker
|
disease |
BEFREE |
We used the Bcl-2/Bcl-x<sub>L</sub> inhibitor ABT-737 to study the factors regulating whether myeloma is Mcl-1 dependent, and thus resistant to ABT-737-induced apoptosis, or Bcl-2/Bcl-x<sub>L</sub> codependent, and thus sensitive to ABT-737.
|
28151428 |
2017 |
|
Multiple Myeloma
|
0.400 |
AlteredExpression
|
disease |
BEFREE |
Mcl-1 was up-regulated in all MM lines tested, including bortezomib-resistant lines, human MM xenograft mouse models, and primary CD138<sup>+</sup> MM cells.
|
28938651 |
2017 |
|
Multiple Myeloma
|
0.400 |
Biomarker
|
disease |
BEFREE |
The antiapoptotic proteins BCL-2 and myeloid cell leukemia sequence 1 (MCL-1) promote multiple myeloma (MM) cell survival.
|
28847998 |
2017 |
|
Multiple Myeloma
|
0.400 |
AlteredExpression
|
disease |
BEFREE |
Venetoclax is a selective, orally bioavailable BCL-2 inhibitor that induces cell death in multiple myeloma (MM) cells, particularly in those harboring t(11;14), which express high levels of BCL-2 relative to BCL-X<sub>L</sub> and MCL-1.
|
29018077 |
2017 |