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Figure 7
Occupation of the selectivity pocket of Sirt2 with large hydrophobic moieties such as EX243 or the DMP group of SirReal2 induces a conformational shift of the hinge loop and consequently significantly enlarges the selectivity pocket, which leads to an isotype-selective inhibition of Sirt2. Exploiting this binding pocket and the flexibility of the hinge loop of Sirt2 with large hydrophobic moieties presents a potential strategy for the development of Sirt2-selective inhibitors.

ISSN: 2053-230X
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