biostudies-otherUnknownSchoen MargareteHomo sapienshttps://www.ebi.ac.uk/biostudies/studies/S-ECPF-GEOD-8772EurocanPlatformInterference 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-κB-1), a highly selective small-molecule IKKβ inhibitor, as a potent suppressor of both constitutive and induced NF-κB activity in melanoma cells. While KINK-1 profoundly diminished various NF-κB-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-κB activation, a mechanism implicated in chemoresistance, was abrogated by KINK-1. In addition, wbiostudies-othertranscription profiling by arrayEurocanPlatformSchoen MargaretefalseTranscription profiling of human melanoma cells reveals KINK-1 a novel small-molecule inhibitor of IKK, enhances susceptibility of melanoma cells to antitumoral treatmentInterference 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-κB-1), a highly selective small-molecule IKKβ inhibitor, as a potent suppressor of both constitutive and induced NF-κB activity in melanoma cells. While KINK-1 profoundly diminished various NF-κB-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-κB activation, a mechanism implicated in chemoresistance, was abrogated by KINK-1. In addition, w2016-04-14T14:44:41Z2016-04-14T14:44:41Z2016-04-14T14:44:41ZS-ECPF-GEOD-8772GSE8772E-GEOD-8772EFO_0000756EFO_0000322E-GEOD-8772