Preferred Label : Ets-family Transcription Factor Inhibitor TK216;
NCIt definition : A proprietary biologic that inhibits the transcriptional-promoting activity of E26
transformation-specific (Ets, E-twenty-six) family transcription factors, with potential
antineoplastic activity. Although the exact mechanism(s) of action through which this
agent exerts its effect has yet to be fully elucidated, upon administration, Ets-family
transcription factor inhibitor TK216 inhibits transcriptional activation mediated
by Ets family proteins, including the oncogenic Ewing sarcoma breakpoint region 1/Friend
leukemia virus integration 1 (EWSR1/FLI1; EWS/FLI1) fusion protein. This agent may
both inhibit the malignant downstream effects mediated by genomic rearrangements that
result in the overexpression of Ets family transcription factors and decrease tumor
cell growth and proliferation. A chromosomal translocation t(11;22)(q24;q12) fuses
the EWSR1 gene and the FLI1 gene and encodes the EWSR1/FLI1 fusion protein, which
is an oncoprotein expressed by peripheral primitive neuroectodermal (pPNET) tumors.;
Molecule name : TK-216;
NCI Metathesaurus CUI : CL504343;
Origin ID : C125657;
UMLS CUI : C4086267;
Semantic type(s)
- concept_is_in_subset
- has_target
