Abstract
Bromodomain and PHD finger-containing protein 1 (BRPF1) is an essential component of histone acetyltransferase complexes, where it acts as a scaffold to facilitate their assembly and enzymatic activity, thereby playing a key role in chromatin remodeling and transcriptional regulation. Emerging evidence indicates that BRPF1 is frequently dysregulated in cancer and contributes to tumorigenesis by modulating key oncogenic pathways. Its overexpression has been associated with poor prognosis in multiple malignancies, highlighting its relevance as a candidate for targeted therapy. Specifically, BRPF1 is particularly implicated in cancers of gastrointestinal and genitourinary systems, as well as in brain, skin, breast, and hematological tumors. The development of selective BRPF1 bromodomain inhibitors has opened new therapeutic avenues, with preclinical models showing notable anticancer effects. Moreover, combinatorial strategies involving BRPF1 inhibitors and other targeted therapies have shown promise in enhancing treatment efficacy. This review provides a comprehensive overview of BRPF1 structure and function, its oncogenic role, and the therapeutic targeting strategies. We also examined current advancements in drug development, highlighting the challenges in BRPF1 inhibition, and proposed future research directions to elucidate its role in cancer epigenetics and translate these insights into improved clinical outcomes.