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GEO help: Mouse over screen elements for information. |
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| Status |
Public on Aug 09, 2008 |
| Title |
KINK-1, a novel small-molecule inhibitor of IKKbeta, enhances susceptibility of melanoma cells to antitumoral treatment |
| Organism |
Homo sapiens |
| Experiment type |
Expression profiling by array
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| Summary |
Interference with chemoresistance to enhance the efficacy of chemotherapeutics may be of great utility for cancer therapy. We have identified KINK-1 (Kinase Inhibitor of NF-kappaB-1), a highly selective small-molecule IKKkappa inhibitor, as a potent suppressor of both constitutive and induced NF-kappaB activity in melanoma cells. While KINK-1 profoundly diminished various NF-kappaB-dependent gene products regulating proliferation, cytokine production or anti-apoptotic responses, the compound by itself showed little antiproliferative or pro-apoptotic activity on the cellular level. However, its combination with some cytostatics markedly enhanced their antitumoral activities in vitro, and doxorubicin-induced NF-kappaB activation, a mechanism implicated in chemoresistance, was abrogated by KINK-1. In addition, when KINK-1 was combined with doxorubicin in an in vivo melanoma model, experimental metastasis was significantly diminished as compared to either treatment alone. Induction of chemoresistance by KINK-1 in vivo was not observed. Thus, KINK-1 or related substances might increase the susceptibility of tumors to chemotherapy.
Keywords: time-course
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| Overall design |
one control and two time point (12hrs and 24hrs) are analyzed, with one replicate each (6 arrays total)
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| Contributor(s) |
Schön M, Wienrich G, Sennefelder H, Kneitz S, Vöhringer V, Amschler K, Ziegelbauer K, Schön MP |
| Citation(s) |
18544741 |
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| Submission date |
Aug 14, 2007 |
| Last update date |
Mar 25, 2019 |
| Contact name |
Margarete Schoen |
| E-mail(s) |
[email protected]
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| Organization name |
RVZ
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| Street address |
Versbacherstr.9
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| City |
Wuerzburg |
| ZIP/Postal code |
97078 |
| Country |
Germany |
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| Platforms (1) |
| GPL570 |
[HG-U133_Plus_2] Affymetrix Human Genome U133 Plus 2.0 Array |
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| Samples (6)
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| Relations |
| BioProject |
PRJNA102059 |
| Supplementary file |
Size |
Download |
File type/resource |
| GSE8772_RAW.tar |
26.7 Mb |
(http)(custom) |
TAR (of CEL, EXP) |
| Processed data included within Sample table |
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