Key Laboratory of Chemical Biology

Jinan, China

Key Laboratory of Chemical Biology

Jinan, China
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Su Z.,Nanjing Agricultural University | Chen H.,Nanjing Agricultural University | Wang P.,Nanjing Agricultural University | Shen Y.,Key Laboratory of Chemical Biology | And 2 more authors.
Molecular Microbiology | Year: 2017

Heat-stable antifungal factor (HSAF) produced by Lysobacter enzymogenes is a potential lead compound for developing new antibiotics. Yet, how L. enzymogenes regulates the HSAF biosynthesis remains largely unknown. Here, we show that 4-hydroxybenzoic acid (4-HBA) serves as a diffusible factor for regulating HSAF biosynthesis. The biosynthesis of 4-HBA involved an oxygenase, LenB2, and mutation of lenB2 almost completely abolished 4-HBA production, leading to significantly impaired HSAF production. Introduction of a heterologous gene coding for 4-HBA biosynthetic enzyme into the lenB2 mutant restored the production of 4-HBA and HSAF to their corresponding wild-type levels. Exogenous addition of 0.5-1 μM 4-HBA was sufficient to restore HSAF production in the lenB2 mutant. Furthermore, the shikimate pathway was found to regulate the biosynthesis of HSAF via 4-HBA. Finally, we identified a LysR-family transcription factor (LysRLe) with activity directed to HSAF production. LysRLe could bind to the HSAF promoter and, as a result, regulates expression of HSAF biosynthesis genes. The 4-HBA could bind to LysRLe and appeared to partly enhance formation of the LysRLe-DNA complex. Collectively, our findings suggest that L. enzymogenes produces 4-HBA to serve as an adaptor molecule to link the shikimate pathway to the biosynthesis of a unique antifungal metabolite (HSAF). © 2017 John Wiley & Sons Ltd.


Chen X.,Key Laboratory of Chemical Biology | Chen X.,Universities of Hunan Province | Chen X.,Hunan Normal University | Shi Y.-Y.,Key Laboratory of Chemical Biology | And 17 more authors.
Chinese Journal of Inorganic Chemistry | Year: 2012

The phosphors designed as Sr 2-mMg 1-nSi 2O 7:mTb 3+,nLi +(m=0.03~0.50, n=m)were prepared by the high temperature solid state reaction. Crystallization and optical properties were investigated by using powder X-ray diffraction and fluorescence spectrophotometer, respectively. Under the excitation of ultraviolet (377 nm), the emission spectra of these phosphors exhibit sharp multi-emission lines peaked at about 490 nm, 542 nm, 590 nm and 613 nm corresponding to 5D 4→ 7F J,(j=6,5,4,3)typical transitions of Tb 3+respectively. The luminescence color can be tuned from blue to white, yellow and green by adjusting the doping concentration of Tb 3+ ions. It had been found that the nominal composition Sr 1.95Mg 0.95Si 2O 7:0.05Tb 3+,0.05Li +phosphor provides a white emission (0.322, 0.311) that is very close to the standard white (i=0.33, y=0.33), which shows that it is a potential singlephased white phosphor for LED-based UV-chip.


Deng S.-Z.,Key Laboratory of Chemical Biology | Deng S.-Z.,Universities of Hunan Province | Deng S.-Z.,Hunan Normal University | Liu C.,Key Laboratory of Chemical Biology | And 20 more authors.
Chinese Journal of Inorganic Chemistry | Year: 2015

Ba1.97Zn1-xMgxSi2O7: 0.03Eu and Ba1.97-yZn0.9Mg0.1Si2O7: 0.03Eu,yCe3+ phosphors were synthesized in air condition by a high temperature solid-state reaction. Crystallization and optical properties were investigated by using powder X-ray diffraction and fluorescence spectrophotometer, respectively. Under the excitation of ultraviolet (330~360 nm), the emission spectra of these solid-solution phosphors exhibit multi-emission bands peaked at about 360 nm (blue-purple color), 500 nm (green color) and 590~725 nm (red color), the two formers are corresponding to the 4f65d1-4f7 transition of Eu2+, the latter is originated from the5D0-7FJ(J=1,2,3,4) transitions of Eu3+. The investigated results indicate that part of Eu3+ can be self-reduced to Eu2+ in the matrix and will reach the maximum when x =0.1 mol. When co-doping Ce3+ ions, the luminescent colors of the phosphors Ba1.97-yZn0.9Mg0.1Si2O7: 0.03Eu,yCe3+ can be tunable from green to white to orange area. It had been found that the nominal composition Ba1.96Zn0.9Mg0.1Si2O7: 0.03Eu,0.01Ce3+ phosphor provides a white emission (0.323, 0.311) that is very close to the standard white (x=0.33, y=0.33), which shows that it is a potential white phosphor for LED-based UV-chip. The energy transfer processes among rare earths and the luminescent mechanism were discussed. © 2015, Chinese Chemical Society.All Rights Reserved.


Chen X.,Key Laboratory of Chemical Biology | Meng Q.,Key Laboratory of Chemical Biology | Qiu L.,Shandong University | Zhan P.,Key Laboratory of Chemical Biology | And 4 more authors.
Chemical Biology and Drug Design | Year: 2015

A novel series of triazine derivatives targeting the entrance channel of the HIV-1 non-nucleoside reverse transcriptase inhibitor binding pocket (NNIBP) were designed and synthesized on the basis of our previous work. The results of a cell-based antiviral screening assay indicated that most compounds showed good-to-moderate activity against wild-type HIV-1 with EC50 values within the concentration range of 0.0078-0.16 μm (compound DCS-a4, EC50 = 7.8 nm). Some compounds displayed submicromolar activity against the K103N/Y181C resistant mutant strain (such as compound DCS-a4, EC50 = 0.65 μm). Molecular modeling studies confirmed that the new compounds could bind into the NNIBP similarly as the lead compound, and the newly introduced flexible heterocycles could occupy the entrance channel effectively. In addition, the preliminary structure-activity relationship and the RT inhibitory assay are presented in this study. A novel series of triazine derivatives targeting the entrance channel of NNRTI were designed by combining the pharmacophoric groups of the drug etravirine and the pDAPY derivatives, which showed promising activity against HIV-1 in MT-4 cell line. © 2014 John Wiley & Sons A/S.


Wang Y.-Y.,Key Laboratory of Chemical Biology | Liu J.-Z.,Key Laboratory of Chemical Biology | Yu X.-Y.,Key Laboratory of Chemical Biology | Yang D.-Z.,Key Laboratory of Chemical Biology | And 2 more authors.
Chemical Research in Chinese Universities | Year: 2013

A series of hydrazine and oxadiazole analogs of Sorafenib was designed, synthesized and characterized by proton nuclear magnetic resonance(1H NMR) spectrometry and high resolution mass spectrometry(HRMS). The antiproliferative activities of these compounds against human colorectal carcinoma(HCT-116) and human breast cancer (MDA-MB-231) tumor cell lines were evaluated in vitro by MTT method[MTT=3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide]. The bioassay results suggest that most of the synthesized compounds have antitumor potential to HCT-116 cell line compared with MDA-MB-231 cell line. Compounds 8a, 8b, 8d, 8e, 9f and 9j competitive with Sorafenib demonstrated antiproliferative activities on HCT-116 cell line. © 2013 Jilin University, The Editorial Department of Chemical Research in Chinese Universities and Springer-Verlag GmbH.


Wang X.,Key Laboratory of Chemical Biology | Huang B.,Key Laboratory of Chemical Biology | Suzuki T.,Kyoto Prefectural University of Medicine | Suzuki T.,Japan Science and Technology Agency | And 2 more authors.
Epigenomics | Year: 2015

LSD1 is an epigenetic modulator associated with transcriptional regulation of genes involved in a broad spectrum of key cellular processes, and its activity is often altered under pathological conditions. LSD1 inhibitors are considered to be candidates for therapy of cancer, viral diseases and neurodegeneration. Many LSD1 inhibitors with various scaffolds have been disclosed, and a few potent molecules are in different stages of clinical development. In this review, we summarize recent biological findings on the roles of LSD1 and the current understanding of the clinical significance of LSD1, and focus on the medicinal chemistry strategies used in the design and development of LSD1 inhibitors as drug-like epigenetic modulators since 2012, including a brief consideration of structure-activity relationships. © 2015 Future Medicine Ltd.


Zheng H.,Key Laboratory of Chemical Biology | Li L.,Key Laboratory of Chemical Biology | Sun B.,Key Laboratory of Chemical Biology | Sun B.,Shandong University | And 2 more authors.
Journal of Medicinal Chemistry | Year: 2016

Paraptosis is nonapoptotic cell death characterized by massive endoplasmic reticulum (ER)- or mitochondria-derived vacuoles. Induction of paraptosis offers significant advantages for the treatment of chemotherapy-resistant tumors compared with anticancer drugs that rely on apoptosis. Because some natural alkaloids induce paraptotic cell death, a novel series of benzo[a]quinolizidine derivatives were synthesized, and their antiproliferative activity and ability to induce cytoplasmic vacuolation were analyzed. Structural optimization led to the identification of the potent compound 22b, which inhibited cancer cell proliferation in vitro and in vivo and profoundly facilitated paraptosis-like cell death and induced caspase-dependent apoptosis. Further investigation revealed that 22b-mediated vacuolation originated from persistent ER stress and upregulation of LC3B. Paraptosis induced by benzo[a]quinolizidine derivatives thus represents an alternative strategy for cancer chemotherapy. © 2016 American Chemical Society.


Zhao Y.,Hebei University | Zhao Y.,Key Laboratory of Analytical Science and Technology | Zhao Y.,Key Laboratory of Chemical Biology | Liu L.,Hebei University | And 8 more authors.
Chinese Journal of Chromatography (Se Pu) | Year: 2013

An analytical method for the simultaneous determination of 18α-glycyrrhizic acid, 18β-glycyrrhizinic acid, related substances A and B and drug quality standard by reversed-phase high performance liquid chromatography (RP-HPLC) was established. The assay was carried out on a Durashell-Cl8 column (250 mm ×4. 6 mm, 5 μm) with 10 mmol/L ammonium perchlo-rate (the pH value was adjusted to 8.20 with ammonia)-methanol (48: 52, v/v) as mobile phase at a flow rate of 0. 80 mL/min, and the detection wavelength was set at 254 nm. The column temperature was 50 °C and the injection volume was 10 (xL. Under the separation conditions, the calibration curves of the analytes showed good linearities within the mass concentrations of 0. 50 - 100 mg/L (r >0. 999 9). The detection limits for 18α-glycyrrhizic acid, 18β-gly-cyrrhizinic acid, related substances A and B were 0. 15, 0. 10, 0. 10, 0. 15 mg/L, respectively. The average recoveries were between 97. 32% and 99. 33% (n = 3) with the relative standard deviations (RSDs) between 0. 05% and 1. 06%. The method is sensitive, reproducible, and the results are accurate and reliable. The method can be used for the determination of principal components and related substances of ammonium glycyrrhizinate for the quality control of raw material drug of ammonium glycyrrhizinate.


Xiao R.,Key Laboratory of Chemical Biology | Xiao R.,Shanxi University | Gao Y.,Key Laboratory of Chemical Biology | Gao Y.,Shanxi University | And 7 more authors.
Cell Biology International | Year: 2013

The eukaryotic class II polypeptide chain release factor (eRF3) is an eRF1- and ribosome-dependent GTPase involved in translation termination of protein biosynthesis. eRF3 is a multifunctional protein that is also involved in chromosomal segregation and cytokinesis during mitosis. Survivin is a member of the inhibitor of apoptosis protein (IAP) family that is involved in the organisation of spindle and cell apoptosis. Interaction between survivin and eRF3a-F3 or eRF3b, encoded by the GSPT1 and GSPT2 genes, respectively, was confirmed using yeast two-hybrid (Y2H) and pull-down assays in vitro, and coimmunoprecipitation in vivo. The domains involved in the formation of the survivin-eRF3s complex have been identified. The sites on survivin that interact with eRF3 are located in the baculovirus IAP repeat domain (residues 65-76), which forms a betastrand structure with an overall negative charge. The sites on eRF3 that interact with survivin were localised to the N-terminal domain(NTD; residues 131-200). Cell localisation experiments indicate that both factors are in the nucleus, suggesting that they cooperatively function in nuclear processes. © 2013 International Federation for Cell Biology.

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