ETS proto-oncogene 1, transcription factor (ETS1) (ETS1)

ETS proto-oncogene 1 (ETS1) is the founding member of the ETS family of transcription factors, characterized by a highly conserved eighty-five amino acid DNA-binding domain [1]. It plays a pivotal role in regulating genes involved in cellular proliferation, differentiation, and tissue remodeling, and is essential for the development and function of immune cells such as T, B, and NK cells [2]. In oncology, ETS1 is frequently overexpressed and acts as a driver of tumor progression by promoting angiogenesis, invasion, and the epithelial-mesenchymal transition (EMT) [3]. Furthermore, genetic variants and overexpression of ETS1 are strongly linked to autoimmune disorders, particularly systemic lupus erythematosus (SLE), where it influences inflammatory cytokine production [4]. While transcription factors like ETS1 have historically been considered difficult to target with small molecules, current therapeutic strategies focus on disrupting its DNA-binding capacity or its interaction with essential co-activators to suppress its oncogenic and pro-inflammatory activities [5].

Other names

Protein C-ets-1p54EWSR2ETS-1V-ets erythroblastosis virus E26 oncogene homolog 1

Inhibition of DNA binding activity at the ETS domain, disruption of protein-protein interactions with transcriptional co-activators like CBP/p300, or targeted protein degradation using PROTACs.