Sentrin-specific protease 1 (SENP1) (SENP1)

Sentrin-specific protease 1 (SENP1) is a cysteine protease that plays a pivotal role in the small ubiquitin-like modifier (SUMO) pathway by regulating the reversible post-translational modification of proteins [UniProt]. It is responsible for both the maturation of SUMO precursors (SUMO1, SUMO2, and SUMO3) and the deconjugation of SUMO from target proteins, thereby influencing their stability, localization, and activity [UniProt, NIH]. SENP1 is a critical regulator of various transcription factors and signaling molecules, including hypoxia-inducible factor 1-alpha (HIF-1α), the androgen receptor, and c-Myc [PubMed, NIH]. In many human malignancies, such as prostate, pancreatic, and liver cancers, SENP1 is frequently overexpressed, where it promotes tumor growth, angiogenesis, and metastasis by stabilizing oncogenic proteins [PubMed]. Due to its central role in cancer progression and its ability to modulate drug resistance, SENP1 is considered a promising therapeutic target [NIH, PubMed]. Current research focuses on the development of small molecule inhibitors and natural products, such as Momordin Ic and Ursolic acid, which aim to inhibit SENP1 activity and sensitize tumors to conventional therapies [PubMed, NIH].

Other names

SUMO-specific protease 1Sentrin/SUMO-specific protease SENP1SUMO1-specific protease 1Sentrin-specific peptidase 1

Inhibition of the catalytic cysteine protease activity of SENP1, which prevents the deSUMOylation of oncogenic substrates and the maturation of SUMO precursors [PubMed, NIH].