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eeyarestatin I
- Development stage
- Unknown
- Modality
- Small Molecules
01
Overview
Eeyarestatin I (EerI) is a synthetic small-molecule inhibitor of endoplasmic reticulum-associated degradation (ERAD) and protein translocation. It acts by directly binding to the AAA ATPase p97 (also known as valosin-containing protein, VCP), specifically targeting the p97-associated deubiquitinating process (PAD) and inhibiting ataxin-3 (atx3)-dependent deubiquitination. Additionally, eeyarestatin I inhibits Sec61-mediated protein translocation at the endoplasmic reticulum. It is widely used as a research tool to study ER stress, protein degradation, and cellular homeostasis, and has demonstrated cytotoxic activity preferentially against cancer cells by inducing cell death via the proapoptotic protein NOXA.
- Other names
- EERSTIEerIeeyarestatin 1eeyarestatin1eeyarestatin-1
02
Targets
SEC61A1 (Sec61 subunit alpha-1)MELTF (Melanotransferrin)
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