奥马鲁利德和振动内酯：蛋白酶体-β-内酯-γ-内酰胺结合支架的差异改变了靶标偏好。
Omuralide and vibralactone: differences in the proteasome- β-lactone-γ-lactam binding scaffold alter target preferences.
机构信息
Center for Integrated Protein Science Munich, Department Chemie, Technische Universität München, Lichtenbergstrasse 4, 85747 Garching (Germany).
出版信息
Angew Chem Int Ed Engl. 2014 Jan 7;53(2):571-4. doi: 10.1002/anie.201308567. Epub 2013 Nov 28.
Despite their structural similarity, the natural products omuralide and vibralactone have different biological targets. While omuralide blocks the chymotryptic activity of the proteasome with an IC50 value of 47 nM, vibralactone does not have any effect at this protease up to a concentration of 1 mM. Activity-based protein profiling in HeLa cells revealed that the major targets of vibralactone are APT1 and APT2.
尽管结构相似，但天然产物 omuralide 和 vibralactone 的生物靶标不同。omuralide 以 47 nM 的 IC50 值阻断蛋白酶体的糜蛋白酶活性，而 vibralactone 在此蛋白酶上即使在 1 mM 的浓度下也没有任何作用。在 HeLa 细胞中的基于活性的蛋白质谱分析表明，vibralactone 的主要靶标是 APT1 和 APT2。
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