IndraLab

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Farrerol activates UCHL3. 8 / 8
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"Further thorough studies on whether farrerol directly targets these proteins and the underlying mechanisms might open up new avenues for the application of farrerol when treating other types of diseases.Notably, several reports also indicated that UCHL3 is aberrantly overexpressed in different types of tumors, so caution should be taken when utilizing farrerol, as the farrerol-mediated activation of UCHL3 might be dangerous for cancer patients."
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"Experiments on both in vitro and in vivo functions indicate that farrerol promotes the catalytic activity of UCHL3, thereby leading to a reduced ubiquitination level of RAD51 and enhanced HR repair."
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"Farrerol activates the enzymatic activity of UCHL3 to promote HR repair."
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"Taken together, these data indicated that farrerol promoted DNA repair by HR in a UCHL3-dependent manner.Since the cocrystal structure of the UCHL3–farrerol complex revealed that farrerol directly binds to UCHL3 (Fig. 2a–c), a ubiquitin–AMC assay was then performed to determine whether farrerol activates UCHL3 enzymatic activity, and we found that farrerol affected both K and K , by slightly increasing K from 47.72 to 56.27 nM and significantly increasing K from 11.99 to 19.64 s (Fig. 3i), suggesting that farrerol activates UCHL3 deubiquitinase activity."
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"Moreover, we also performed a Ub-CHOP2 assay to test whether farrerol directly regulates the enzymatic activity of UCHL3."
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"Farrerol directly activates the deubiqutinase UCHL3 to promote DNA repair and reprogramming when mediated by somatic cell nuclear transfer."
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"The data indicated that farrerol at a concentration of 0.1 μM significantly increased the deubiquitinase activity of UCHL3 (Supplementary Fig. 3a)."
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"We performed in vitro and in vivo deubiquitination assay to establish that farrerol directly stimulates UCHL3 enzyme activity and promotes HR by UCHL3-RAD51 axis."
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