2014
DOI: 10.1038/cddis.2014.113
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Abstract: 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 identified several put… Show more

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Cited by 109 publications
(114 citation statements)
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“…Plasmids expressing c-myc-ITCH-WT or the enzymatically inactive ITCH-C830A mutant were kindly provided by G. Melino (Leicester University, UK) and were described previously (54). ITCH-specific or random small interfering RNAs (siRNAs) were purchased from Dharmacon.…”
Section: Methodsmentioning
confidence: 99%
“…Plasmids expressing c-myc-ITCH-WT or the enzymatically inactive ITCH-C830A mutant were kindly provided by G. Melino (Leicester University, UK) and were described previously (54). ITCH-specific or random small interfering RNAs (siRNAs) were purchased from Dharmacon.…”
Section: Methodsmentioning
confidence: 99%
“…[16][17][18][19][20][21] Here, the cellular defense to DNA damage is based on sensors and effectors that activates the cell death pathway, [22][23][24] via p53 [25][26][27][28][29] or its family members. [30][31][32][33][34][35][36][37] Like for our recent Itch inhibitor screening, 14 we believe that in a near future innovative E3 inhibitors will be developed. Here, however, we adopted a different approach to inhibit their function, based on a deeper understanding of the interaction of Itch with its substrate.…”
Section: Introductionmentioning
confidence: 99%
“…This constitutes an extension to HM of the protocol originally designed to optimize the binding site of receptors complexed with nonnative ligands [62][63][64][65][66][67]. The LSHM method was used to model the melanin concentrating hormone receptor 1 (MCH-R1), an anti-obesity GPCR target.…”
Section: Integral Binding-site Modeling and Refinementmentioning
confidence: 99%