High throughput screening for inhibitors of the HECT ubiquitin E3 ligase ITCH identifies antidepressant drugs as regulators of autophagy

@inproceedings{Rossi2014HighTS,
  title={High throughput screening for inhibitors of the HECT ubiquitin E3 ligase ITCH identifies antidepressant drugs as regulators of autophagy},
  author={Matteo Rossi and Barak Rotblat and Keith Ansell and Ivano Amelio and Michele Caraglia and Gabriella Misso and Francesca Bernassola and Claudio N. Cavasotto and Richard A Knight and Aaron Ciechanover and Gerry Melino},
  booktitle={Cell Death and Disease},
  year={2014}
}
Inhibition of distinct ubiquitin E3 ligases might represent a powerful therapeutic tool. ITCH is a HECT domain-containing E3 ligase that promotes the ubiquitylation and degradation of several proteins, including p73, p63, c-Jun, JunB, Notch and c-FLIP, thus affecting cell fate. Accordingly, ITCH depletion potentiates the effect of chemotherapeutic drugs, revealing ITCH as a potential pharmacological target in cancer therapy. Using high throughput screening of ITCH auto-ubiquitylation, we… CONTINUE READING
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