Inhibition of Melanoma Growth by Small Molecules that Promote the Mitochondrial Localization of ATF2

ABSTRACT: Effective therapy for malignant melanoma, the leading cause of death from skin cancer, remains an area of significant unmet need in oncology. Increased expression of PKC? in advanced metastatic melanoma, results in the phosphorylation of the transcription factor ATF2 on threonine 52, which causes its nuclear localization and confers its oncogenic activities. The nuclear-to-mitochondrial translocation of ATF2 following genotoxic stress promotes apoptosis, a function that is largely lost in melanoma cells, due to its confined nuclear localization. Therefore, promoting the nuclear export of ATF2, which sensitizes melanoma cells to apoptosis, offers a novel therapeutic modality. We conducted a pilot high-throughput screen of 3,800 compounds to identify small molecules that promote melanoma cel

ORGANISM(S): Homo sapiens

SUBMITTER: Eric Lau 

PROVIDER: E-GEOD-43135 | biostudies-arrayexpress |

REPOSITORIES: biostudies-arrayexpress