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ETS transcription factors as emerging drug targets in cancer.

08:00 EDT 29th March 2019 | BioPortfolio

Summary of "ETS transcription factors as emerging drug targets in cancer."

The ETS family of proteins consists of 28 transcription factors, many of which have been implicated in development and progression of a variety of cancers. While one family member, ERG, has been rigorously studied in the context of prostate cancer where it plays a critical role, other ETS factors keep emerging as potential hallmark oncodrivers. In recent years, numerous studies have reported initial discoveries of small molecule inhibitors of ETS proteins and opened novel avenues for ETS-directed cancer therapies. This review summarizes the state of the art data on therapeutic targeting of ETS family members and highlights the corresponding drug discovery strategies.

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Name: Medicinal research reviews
ISSN: 1098-1128
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Medical and Biotech [MESH] Definitions

A family of basic helix-loop-helix transcription factors that control expression of a variety of GENES involved in CELL CYCLE regulation. E2F transcription factors typically form heterodimeric complexes with TRANSCRIPTION FACTOR DP1 or transcription factor DP2, and they have N-terminal DNA binding and dimerization domains. E2F transcription factors can act as mediators of transcriptional repression or transcriptional activation.

Maf transcription factors are a family of basic-leucine zipper transcription factors that are closely related to V-MAF ONCOGENE PROTEIN. The C-MAF PROTO-ONCOGENE PROTEIN was the first mammalian Maf transcription factor identified, and now the family is known to include a variety of other Maf proteins such as MAFB TRANSCRIPTION FACTOR; MAFF TRANSCRIPTION FACTOR; MAFG TRANSCRIPTION FACTOR; and MAFK TRANSCRIPTION FACTOR.

A family of transcription factors that contain a single cut domain and a divergent homeodomain. They regulate gene networks by controlling the expression of other transcription factors and they play an important role in CELL DIFFERENTIATION and METABOLISM.

A family of histone acetyltransferases that is structurally-related to CREB-BINDING PROTEIN and to E1A-ASSOCIATED P300 PROTEIN. They function as transcriptional coactivators by bridging between DNA-binding TRANSCRIPTION FACTORS and the basal transcription machinery. They also modify transcription factors and CHROMATIN through ACETYLATION.

Transcription factors that form transcription initiation complexes on DNA, bind to specific DNA-DIRECTED RNA POLYMERASES and are required to initiate transcription. Although their binding may be localized to distinct sequence and structural motifs within the DNA they are considered non-specific with regard to the specific gene being transcribed.

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