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| 1 | Physiological levels of ATP negatively regulate proteasome function显示文摘由 ubiquitin-proteasome 系统的细胞内部的蛋白质降级是 ATP 依赖者,和最佳的 ATP 集中激活 proteasome 在 vitro 的功能是 ~ 100 渭 M。细胞内部的 ATP 层次在在这个范围以内的水平通常在低 millimolar 范围,而是 ATP 被显示在 vitro 禁止 proteasome peptidase 活动。这里,我们报导支持在生理的层次的细胞内部的 ATP 双向地调整的一个假设的新证据 26S proteasome 在房间的解朊的功能。首先,我们证实 ATP 在 vitro 在 26S proteasome 上施加了双向规定,与最佳的 ATP 集中(在 50 和 100 渭 M 之间) 刺激 proteasome 像糜蛋白酶的活动。第二,我们发现操作细胞内部的 ATP 层次也在有教养的房间在 proteasome 特定的蛋白质底层的层次导致了双向变化。最后,测量增加提高的细胞内部的 ATP,当减少的细胞内部的 ATP 稀释了导致房间死亡的 proteasome 抑制的能力时。这些数据强烈建议在生理的集中范围以内的内长的 ATP 能在 proteasome 活动施加否定影响,允许房间到很快,在应力下面的 ATP 减小上的 upregulate proteasome 活动调节。 | Hongbiao Huang Xiaoyan Zhang Shujue Li Ningning Liu Wen Elan Emily McDowell Ping Zhou Canguo Zhao Haiping Guo Change Zhang Changshan Yang Guangmei Wen Xiaoxian Dong Li Lu Ningfang Ma Weihua Dong Q Ping Dou Xuejun Wang Jinbao Liu | 2010 | Cell Research2010，20，12： | 4 |
| 2 | Shikonin extracted from medicinal Chinese herbs exerts anti-inflammatory effect via proteasome inhibition显示文摘 | Li Lu Aiping Qin Hongbiao Huang Ping Zhou Chuanyin Zhang Ningning Liu Shujue Li Guanmei Wen Change Zhang Weihua Dong Xuejun Wang Q. Ping Dou Jinbao Liu | 2011 | European Journal of Pharmacology2011，，2： | 1 |
| 3 | Recent progress in fragment-based drug discovery facilitated by NMR spectroscopy显示文摘Considerable developments have been observed in fragment-based lead/drug discovery(FBLD/FBDD)recently,with four drugs approved and many others under investigation.Nuclear magnetic resonance(NMR)has gained increasing popularity in FBLD due to its intrinsic capability in characterizing protein-ligand interactions in a large dynamic range of affinity,from weak hits to highly potent drugs.Here,we summarize NMR applications in fragment-based hit-to-lead evolution,including the construction of a fragment library,screening methods,spectra processing,and the delineation of the protein-ligand binding modes.These state-of-the-art NMR techniques have been exemplified in the discovery of inhibitors against multiple targets over the past five years,and they are expected to continue to provide new insights in the future. | Lei Wang Jia Gao Rongsheng Ma Yaqian Liu Mingqing Liu Fumei Zhong Jie Hu Shuju Li Jihui Wu Hualiang Jiang Jiahai Zhang Ke Ruan | 2022 | Magnetic Resonance Letters2022，2，2： | 0 |
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