yk-4-279 and Lymphoma

Transcription factors are commonly deregulated in cancer, and they have been widely considered as difficult to target due to their nonenzymatic mechanism of action. Altered expression levels of members of the ETS-transcription factors are often observed in many different tumors, including lymphomas. Here, we characterized two small molecules, YK-4-279 and its clinical derivative, TK-216, targeting ETS factors via blocking the protein-protein interaction with RNA helicases, for their antilymphoma activity.. The study included preclinical. YK-4-279 and TK-216 demonstrated an antitumor activity across several lymphoma cell lines, which we validated. The ETS inhibitor YK-4-279 and its clinical derivative TK-216 represent a new class of agents with

Topics: Animals; Antineoplastic Agents; Apoptosis; Biomarkers, Tumor; Cell Line, Tumor; Cell Proliferation; Disease Models, Animal; Drug Synergism; Gene Expression Profiling; Humans; Immunohistochemistry; Indoles; Lymphoma; Mice; Prognosis; Protein Binding; Protein Kinase Inhibitors; Proto-Oncogene Proteins c-ets; Transcriptome; Xenograft Model Antitumor Assays