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Zhen-Hua Chen,Liang-Peng Sun,Wei Zhang,Qiang Shen,Li-Xin Gao,Jia Li,Hu-Ri Piao 대한화학회 2012 Bulletin of the Korean Chemical Society Vol.33 No.5
Protein tyrosine phosphatase 1B (PTP1B) is a key factor in negative regulation of the insulin pathway, and is a promising target for the treatment of type-II diabetes, obesity and cancer. Herein, compound (4) was first observed to have moderate inhibitory activity against PTP1B with an IC50 value of 13.72 ± 1.53 μM. To obtain more potent PTP1B inhibitors, we synthesized a series of chalcone derivatives using compound (4) as the lead compound. Compound 4l (IC50 = 3.12 ± 0.18 μM) was 4.4-fold more potent than the lead compound 4 (IC50 = 13.72 ± 1.53 μM), and more potent than the positive control, ursolic acid (IC50 = 3.40 ± 0.21 μM). These results may help to provide suitable drug-like lead compounds for the design of inhibitors of PTP1B as well as other PTPs.
Chen, Zhen-Hua,Sun, Liang-Peng,Zhang, Wei,Shen, Qiang,Gao, Li-Xin,Li, Jia,Piao, Hu-Ri Korean Chemical Society 2012 Bulletin of the Korean Chemical Society Vol.33 No.5
Protein tyrosine phosphatase 1B (PTP1B) is a key factor in negative regulation of the insulin pathway, and is a promising target for the treatment of type-II diabetes, obesity and cancer. Herein, compound ($\mathbf{4}$) was first observed to have moderate inhibitory activity against PTP1B with an $IC_{50}$ value of $13.72{\pm}1.53{\mu}M$. To obtain more potent PTP1B inhibitors, we synthesized a series of chalcone derivatives using compound ($\mathbf{4}$) as the lead compound. Compound $\mathbf{4l}$ ($IC_{50}=3.12{\pm}0.18{\mu}M$) was 4.4-fold more potent than the lead compound $\mathbf{4}$ ($IC_{50}=13.72{\pm}1.53{\mu}M$), and more potent than the positive control, ursolic acid ($IC_{50}=3.40{\pm}0.21{\mu}M$). These results may help to provide suitable drug-like lead compounds for the design of inhibitors of PTP1B as well as other PTPs.
Chen, Peng,Wang, Xiu-Li,Ma, Zhong-Sen,Xu, Zhong,Jia, Bo,Ren, Jin,Hu, Yu-Xin,Zhang, Qing-Hua,Ma, Tian-Gang,Yan, Bing-Di,Yan, Qing-Zhu,Li, Yan-Lei,Li, Zhen,Yu, Jin-Yan,Gao, Rong,Fan, Na,Li, Bo,Yang, Jun Asian Pacific Journal of Cancer Prevention 2012 Asian Pacific journal of cancer prevention Vol.13 No.7
HMGN5 is a typical member of the HMGN (high mobility group nucleosome-binding protein) family which may function as a nucleosomal binding and transcriptional activating protein. Overexpression of HMGN5 has been observed in several human tumors but its role in tumorigenesis has not been fully clarified. To investigate its significance for human lung cancer progression, we successfully constructed a shRNA expression lentiviral vector in which sense and antisense sequences targeting the human HMGN5 were linked with a 9-nucleotide loop. Inhibitory effects of siRNA on endogenous HMGN5 gene expression and protein synthesis were demonstrated via real-time RT-PCR and western blotting. We found HMGN5 silencing to significantly inhibit A549 and H1299 cell proliferation assessed by MTT, BrdU incorporation and colony formation assays. Furthermore, flow cytometry analysis showed that specific knockdown of HMGN5 slowed down the cell cycle at the G0/G1 phase and decreased the populations of A549 and H1299 cells at the S and G2/M phases. Taken together, these results suggest that HMGN5 is directly involved in regulation cell proliferation in A549 and H1299 cells by influencing signaling pathways involved in cell cycle progression. Thus, our finding suggests that targeting HMGN5 may be an effective strategy for human lung cancer treatment.
Wei-Rong Chen,Jia-Peng Deng,Jun Wang,Jia-Yuan Sun,Zhen-Yu He,San-Gang Wu 대한암학회 2019 Cancer Research and Treatment Vol.51 No.4
Purpose The purpose of this study was to investigate the effect of 21-gene recurrence score (RS) on predicting prognosis and chemotherapy decision in node micrometastases (N1mi) breast invasive ductal carcinoma (IDC). Materials and Methods Patients with stage T1-2N1mi and estrogen receptor-positive IDC diagnosed between 2004 and 2015 were included. The associations of 21-gene RS with breast cancer-specific survival (BCSS), chemotherapy decision, and benefit of chemotherapy were analyzed. Results We identified 4,758 patients including 1,403 patients (29.5%) treated with adjuvant chemotherapy. In the traditional RS cutoffs, 2,831 (59.5%), 1,634 (34.3%), and 293 (6.2%) patients were in the low-, intermediate-, and high-risk RS groups, respectively. In 3,853 patients with human epidermal growth factor receptor-2 (HER2) status available, most patients were HER2-negative disease (98.3%). A higher RS was independently related to chemotherapy receipt, and 14.0%, 47.7%, and 77.8% of patients in the low-, intermediate-, and high-risk RS groups received chemotherapy, respectively. The multivariate analysis indicated that a higher RS was related to worse BCSS (p < 0.001). The 5-year BCSS rates were 99.3%, 97.4%, and 91.9% in patients with low-, intermediate-, and high-risk RS groups, respectively (p < 0.001). However, chemotherapy receipt did not correlate with better BCSS in low-, intermediate-, or high-risk RS groups. There were similar trends using Trial Assigning Individualized Options for Treatment RS cutoffs. Conclusion The 21-gene RS does predict outcome and impact on chemotherapy decision of N1mi breast IDC. Large cohort and long-term outcomes studies are needed to identify the effects of chemotherapy in N1mi patients by different 21-gene RS groups.
Xing‑Quan Liu,Zhe Li,Zhen‑Jia Peng,Rui‑Xun Wang,Zhi‑Quan Liu 대한금속·재료학회 2024 METALS AND MATERIALS International Vol.30 No.1
Electroplated copper is a key electronic interconnect material in integrated circuits and printed circuits and inevitablyexposed to corrosive media in manufacturing processes. The present work reports, for the first time, that corrosion resistanceof electroplated copper in 4 wt% NaOH is enhanced via nanotwinned microstructure engineering. Nucleation and growthof oxide/hydroxide on nanotwinned copper are inhibited, attributed to existence of highly (111)-preferred grain orientationand high-density parallelly-aligned coherent twin boundaries at surface. This study unveils a novel anti-corrosion strategyof nantowinned microstructure engineering against alkaline etchant, and exhibits great application values in industrial electroplatingof copper, silver, or their alloys.
Endothelial Aquaporin-1 (AQP1) Expression Is Regulated by Transcription Factor Mef2c
Yong Jiang,He Liu,Wen-jing Liu,Hai-bin Tong,Chang-jun Chen,Fu-gui Lin,Yan-hang Zhuo,Xiao-zhen Qian,Zeng-bin Wang,Yu Wang,Peng Zhang,Hong-liang Jia 한국분자세포생물학회 2016 Molecules and cells Vol.39 No.4
Aquaporin 1 (AQP1) is expressed in most microvascula-ture endothelial cells and forms water channels that play major roles in a variety of physiologic processes. This study aimed to delineate the transcriptional regulation of AQP1 by Mef2c in endothelial cells. Mef2c cooperated with Sp1 to activate human AQP1 transcription by binding to its proximal promoter in human umbilical cord vein endothelial cells (HUVEC). Over-expression of Mef2c, Sp1, or Mef2c/Sp1 increased HUVEC migration and tube-forming ability, which can be abolished AQP1 knockdown. These data indicate that AQP1 is a direct target of Mef2c in regulating angiogenesis and vasculogenesis of endothelial cells.
Endothelial Aquaporin-1 (AQP1) Expression Is Regulated by Transcription Factor Mef2c
Jiang, Yong,Liu, He,Liu, Wen-jing,Tong, Hai-bin,Chen, Chang-jun,Lin, Fu-gui,Zhuo, Yan-hang,Qian, Xiao-zhen,Wang, Zeng-bin,Wang, Yu,Zhang, Peng,Jia, Hong-liang Korean Society for Molecular and Cellular Biology 2016 Molecules and cells Vol.39 No.4
Aquaporin 1 (AQP1) is expressed in most microvasculature endothelial cells and forms water channels that play major roles in a variety of physiologic processes. This study aimed to delineate the transcriptional regulation of AQP1 by Mef2c in endothelial cells. Mef2c cooperated with Sp1 to activate human AQP1 transcription by binding to its proximal promoter in human umbilical cord vein endothelial cells (HUVEC). Over-expression of Mef2c, Sp1, or Mef2c/Sp1 increased HUVEC migration and tube-forming ability, which can be abolished AQP1 knockdown. These data indicate that AQP1 is a direct target of Mef2c in regulating angiogenesis and vasculogenesis of endothelial cells.