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| 1 | Discovery and identification of EIF2AK2 as a direct key target of berberine for anti-inflammatory effects显示文摘Using chemoproteomic techniques,we first identified EIF2AK2,eEF1A1,PRDX3 and VPS4B as direct targets of berberine(BBR)for its synergistically anti-inflammatory effects.Of them,BBR has the strongest affinity with EIF2AK2 via two ionic bonds,and regulates several key inflammatory pathways through EIF2AK2,indicating the dominant role of EIF2AK2.Also,BBR could subtly inhibit the dimerization of EIF2AK2,rather than its enzyme activity,to selectively modulate its downstream pathways including JNK,NF-κB,AKT and NLRP3,with an advantage of good safety profile.In EIF2AK2 gene knockdown mice,the inhibitory IL-1β,IL-6,IL-18 and TNF-a secretion of BBR was obviously attenuated,confirming an EIF2AK2-dependent anti-inflammatory efficacy.The results highlight the BBR's network mechanism on anti-inflammatory effects in which EIF2AK2 is a key target,and inhibition of EIF2AK2 dimerization has a potential to be a therapeutic strategy against inflammationrelated disorders. | Wei Wei Qingxuan Zeng Yan Wang Xixi Guo Tianyun Fan Yinghong Li Hongbin Deng Liping Zhao Xintong Zhang Yonghua Liu Yulong Shi Jingyang Zhu Xican Ma Yanxiang Wang Jiandong Jiang Danqing Song | 2023 | Acta Pharmaceutica Sinica B2023，13，5： | 2 |
| 2 | Author correction to‘Discovery and identification of EIF2AK2 as a direct key target of berberine for anti-inflammatory effects’[Acta Pharmaceutica Sinica B 13(2023)2138-2151]显示文摘The authors regret that there are some misplaced figure numbers in the body of this article due to negligence in the layout and proofreading of the figures.Although it does not affect the conclusion,it is an obvious error.The authors have now modified as below.The authors apologize for any inconvenience caused to the journal and readers. | Wei Wei Qingxuan Zeng Yan Wang Xixi Guo Tianyun Fan Yinghong Li Hongbin Deng Liping Zhao Xintong Zhang Yonghua Liu Yulong Shi Jingyang Zhu Xican Ma Yanxiang Wang Jiandong Jiang Danqing Song | 2024 | Acta Pharmaceutica Sinica B2024，14，3： | 0 |
| 3 | Evolution and development of potent monobactam sulfonate candidate IMBZ18g as a dual inhibitor against MDR Gram-negative bacteria producing ESBLs显示文摘A series of new monobactam sulfonates is continuously synthesized and evaluated for their antimicrobial efficacies against Gram-negative bacteria.Compound 33a(IMBZ18G)is highly effective in vitro and in vivo against clinically intractable multi-drug-resistant(MDR)Gram-negative strains,with a highly druglike nature.The checkerboard assay reveals its significant synergistic effect withβ-lactamase inhibitor avibactam,and the MIC values against MDR enterobacteria were reduced up to 4—512folds.X-ray co-crystal and chemoproteomic assays indicate that the anti-MDR bacteria effect of 33a results from the dual inhibition of the common PBP3 and some class A and Cβ-lactamases.Accordingly,preclinical studies of 33a alone and 33a-avibactam combination as potential innovative candidates are actively going on,in the treatment ofβ-lactamase-producing MDR Gram-negative bacterial infections. | Zhiwen Li Zhihao Guo Xi Lu Xican Ma Xiukun Wang Rui Zhang Xinxin Hu Yanxiang Wang Jing Pang Tianyun Fan Yonghua Liu Sheng Tang Haigen Fu Jingpu Zhang Yinghong Li Xuefu You Danqing Song | 2023 | Acta Pharmaceutica Sinica B2023，13，7： | 0 |
| 4 | N-(2-Phenoxy)ethyl imidazo[1,2-a]pyridine-3-carboxamides containing various amine moieties:Design,synthesis and antitubercular activity显示文摘Seven 2,6-disubstituted N-(2-phenoxy)ethyl imidazo[1,2-a]pyridine-3-carboxamide series containing various amine moieties were designed and synthesized as new anti-TB agents.Many of them show excellent in vitro activity against both drug-sensitive MTB strain H37Rv and two MDR-MTB clinical isolates(MIC:<0.002-0.030 μg/mL).Compounds 2f,5e and 5g display acceptable safety and pharmacokinetic profiles,opening a new direction for further development. | Linhu Li Apeng Wang Bin Wang Mingliang Liu Kai Lv Zeyu Tao Chao Ma Xican Ma Bing Han Aoyu Wang Yu Lu | 2020 | Chinese Chemical Letters2020，31，2： | 0 |
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