Search results for: Tsu-An Hsu

Items from 1 to 19 out of 19 results

article

Design and synthesis of 1,2,3-triazole-containing N-acyl zanamivir analogs as potent neuraminidase inhibitors

Anindya Das, Avijit K. Adak, Kalyankumar Ponnapalli, Chien-Hung Lin, more

European Journal of Medicinal Chemistry > 2016 > 123 > C > 397-406

The design of potent metabolically stable neuraminidase (NA) inhibitors represents an attractive approach for treating influenza virus infection. In this study, we describe the exploitation of the 150-cavity in the active site of group 1 NA for the design, synthesis, and in vitro evaluation of new triazole-containing N-acyl derivatives related to Zanamivir. Inhibition studies with influenza virus...

article

BPR-3P0128 inhibits RNA-dependent RNA polymerase elongation and VPg uridylylation activities of Enterovirus 71

Arul Balaji Velu, Guang-Wu Chen, Po-Ting Hsieh, Jim-Tong Horng, more

Antiviral Research > 2014 > 112 > Complete > 18-25

Enterovirus 71 (EV71) infections can cause hand, foot, and mouth disease with severe neurological complications. Because no clinical drug is available for treating EV71 infections, developing an efficient antiviral medication against EV71 infection is crucial. This study indicated that 6-bromo-2-[1-(2,5-dimethylphenyl)-5-methyl-1H-pyrazol-4-yl] quinoline-4-carboxylic acid (BPR-3P0128) exhibits excellent...

article

Synthesis and biological evaluation of 2-amino-1-thiazolyl imidazoles as orally active anticancer agents

Wen-Tai Li, Der-Ren Hwang, Jen-Shin Song, Ching-Ping Chen, more

Investigational New Drugs > 2012 > 30 > 1 > 164-175

Summary Designed from a high throughput screened hit compound, novel 2-amino-1-thiazolyl imidazoles were synthesized and demonstrated cytotoxicity against human cancer cells. 1-(4-Phenylthiazol-2-yl)-4-(thiophen-2-yl)-1H-imidazol-2-amine (compound 2), a 2-amino-1-thiazolyl imidazole, inhibited tubulin polymerization, interacted with the colchicine-binding sites of tubulins, and caused cell cycle arrest...

article

Development of a whole‐cell screening system for evaluation of the human CYP1A2‐mediated metabolism

Chih‐Chieh Chu, Kao‐Lu Pan, Hsien‐Tsung Yao, John Tsu‐An Hsu

Biotechnology and Bioengineering > 108 > 12 > 2932 - 2940

Cytochrome P450 1A2 (CYP1A2) is an important member of cytochrome P450 involved in drug metabolism. In this study, a cell line, Huh7‐1A2‐I‐E, with high expression level of CYP1A2 is established based on Huh7 cells. To achieve this, we constructed a recombinant lentiviral vector, pLenti‐1A2‐I‐E, containing a single promoter encoding CYP1A2 followed by an internal ribosome entry site (IRES) to permit...

article

Isatin-β-thiosemicarbazones as potent herpes simplex virus inhibitors

Iou-Jiun Kang, Li-Wen Wang, Tsu-An Hsu, Andrew Yueh, more

Bioorganic & Medicinal Chemistry Letters > 2011 > 21 > 7 > 1948-1952

A series of isatin-β-thiosemicarbazones have been designed and evaluated for antiviral activity against herpes simplex virus type 1 (HSV-1) and type 2 (HSV-2) in a plaque reduction assay. Their cytotoxicity was examined using human rhabdomyosarcoma cells (RD cells). Several derivatives of isatin-β-thiosemicarbazone exhibited significant and selective antiviral activity with low cytotoxicity. It was...

article

Design and efficient synthesis of novel arylthiourea derivatives as potent hepatitis C virus inhibitors

Iou-Jiun Kang, Li-Wen Wang, Sheng-Ju Hsu, Chung-Chi Lee, more

Bioorganic & Medicinal Chemistry Letters > 2009 > 19 > 21 > 6063-6068

A novel class of arylthiourea HCV inhibitors bearing various functionalities, such as cyclic urea, cyclic thiourea, urea, and thiourea, on the alkyl linker were designed and synthesized. Herein we report the synthesis and structure–activity relationships (SARs) of this novel class of arylthiourea derivatives that showed potent inhibitory activities against HCV in the cell-based subgenomic HCV replicon...

article

Design and synthesis of indole, 2,3-dihydro-indole, and 3,4-dihydro-2H-quinoline-1-carbothioic acid amide derivatives as novel HCV inhibitors

Iou-Jiun Kang, Li-Wen Wang, Sheng-Ju Hsu, Chung-Chi Lee, more

Bioorganic & Medicinal Chemistry Letters > 2009 > 19 > 15 > 4134-4138

An efficient synthetic methodology to provide indole, 2,3-dihydro-indole, and 3,4-dihydro-2H-quinoline-1-carbothioic acid amide derivatives is described. These conformationally restricted heterobicyclic scaffolds were evaluated as a novel class of HCV inhibitors. Introduction of an acyl group at the NH ₂ of the thiourea moiety has been found to enhance inhibitory activity. The chain length...

article

Design, synthesis, and anti-HCV activity of thiourea compounds

Iou-Jiun Kang, Li-Wen Wang, Chung-Chi Lee, Yen-Chun Lee, more

Bioorganic & Medicinal Chemistry Letters > 2009 > 19 > 7 > 1950-1955

A series of thiourea derivatives were synthesized and their antiviral activity was evaluated in a cell-based HCV subgenomic replicon assay. SAR studies revealed that the chain length and the position of the alkyl linker largely influenced the in vitro anti-HCV activity of this class of potent antiviral agents. Among this series of compounds synthesized, the thiourea derivative with a six-carbon alkyl...

article

Structural Basis for the Structure−Activity Relationships of Peroxisome Proliferator-Activated Receptor Agonists

Neeraj Mahindroo, Yi-Hui Peng, Chia-Hui Lin, Uan-Kang Tan, more

Journal of Medicinal Chemistry > 2006 > 49 > 21 > 6421 - 6424

article

Novel Indole-Based Peroxisome Proliferator-Activated Receptor Agonists: Design, SAR, Structural Biology, and Biological Activities

Neeraj Mahindroo, Chien-Fu Huang, Yi-Huei Peng, Chiung-Chiu Wang, more

Journal of Medicinal Chemistry > 2005 > 48 > 26 > 8194 - 8208

article

Papain-Like Protease 2 (PLP2) from Severe Acute Respiratory Syndrome Coronavirus (SARS-CoV): Expression, Purification, Characterization, and Inhibition ^†

Yu-San Han, Gu-Gang Chang, Chiun-Gung Juo, Hong-Jen Lee, more

Biochemistry > 2005 > 44 > 30 > 10349 - 10359

article

Design, synthesis, and structure-activity relationships of pyrazolo[3,4-d]pyrimidines: a novel class of potent enterovirus inhibitors

Jyh-Haur Chern, Kak-Shan Shia, Tsu-An Hsu, Chia-Liang Tai, more

Bioorganic & Medicinal Chemistry Letters > 2004 > 14 > 10 > 2519-2525

A series of pyrazolo[3,4-d]pyrimidines were synthesized and their antiviral activity was evaluated in a plaque reduction assay. It is very interesting that this class of compounds provide remarkable evidence that they are very specific for human enteroviruses, in particular, coxsackieviruses. Some derivatives proved to be highly effective in inhibiting enterovirus replication at nanomolar concentrations...

article

Purification and characterization of human prolyl dipeptidase DPP8 in Sf9 insect cells

Yuan-Shou Chen, Chia-Hui Chien, Chandra M. Goparaju, John Tsu-An Hsu, more

Protein Expression and Purification > 2004 > 35 > 1 > 142-146

DPP8 is a new member of the prolyl dipeptidases, many of which have important biological functions in vivo. DPP8 catalyzes the cleavage at the carboxyl side of the proline residue at the penultimate position. To study its structure and biochemical properties, we have overexpressed the human DPP8 protein in baculovirus infected Sf9 cells. The protein is soluble and can be purified to homogeneity. Using...

article

Sequential expression of recombinant proteins and their separate recovery from a Pichia pastoris cultivation

Jyh-Ming Wu, Lieng-Lung Chieng, Tsu-An Hsu, Cheng-Kang Lee

Biochemical Engineering Journal > 2003 > 16 > 1 > 9-16

Pichia pastoris strains with capability to sequentially express two recombinant proteins under control of the constitutive glyceraldehydes-3-phosphate dehydrogenase (GAP) and the methanol-induced alcohol oxidase (AOX1) promoters have been constructed. The intracellular β-galactosidase (β-gal), secreted human serum albumin (hSA) and human granulocyte-macrophage colony-stimulating factor (hGM-CSF) are...

article

Generation of chimeric baculovirus with histidine-tags displayed on the envelope and its purification using immobilized metal affinity chromatography

Yu-Chen Hu, Chien-Tai Tsai, Yao-Chi Chung, Jen-Te Lu, more

Enzyme and Microbial Technology > 2003 > 33 > 4 > 445-452

Baculovirus/insect cell system has been widely used for recombinant protein production. Since the finding that baculovirus is capable of transducing hepatocytes in 1995, success to utilize baculovirus as a gene delivery vehicle into mammalian cells has been reported. Due to the high transduction efficiency and the non-replication nature in mammalian cells, baculovirus has emerged as a vector for in...

article

Formation of enterovirus-like particle aggregates by recombinant baculoviruses co-expressing P1 and 3CD in insect cells

Yu-Chen Hu, John Tsu-An Hsu, Jen-Huang Huang, Mei-Shang Ho, more

Biotechnology Letters > 2003 > 25 > 12 > 919-925

The assembly of enterovirus requires the cleavage of P1 polyprotein by protease 3CD into individual structural proteins. Two recombinant baculoviruses were constructed to encode P1 and 3CD of enterovirus 71 (EV71), respectively. The expressed 3CD successfully cleaved P1 in vitro and in vivo. Also, the co-infection in insect cells resulted in crystalline virus-like particle structures morphologically...

article

Expression of the gene coding for bacterial hemoglobin improves β-galactosidase production in a recombinant Pichia pastoris

Jyh-Ming Wu, Tsu-An Hsu, Cheng-Kang Lee

Biotechnology Letters > 2003 > 25 > 17 > 1457-1462

Genes coding for Vitreoscilla hemoglobin (VHb) with peroxisome targeting signal (PTS1) tag and β-galactosidase were co-expressed in Pichia pastoris under the alcohol oxidase1 (AOX1) promoter. The expression of VHb-PTS1 had no positive effect on cell growth but significantly enhanced the whole cell β-galactosidase activity to 4-fold higher than that of VHb-free cell in yeast extract/peptone/methanol...

article

The 3C Protease Activity of Enterovirus 71 Induces Human Neural Cell Apoptosis

Mei-Ling Li, Tsu-An Hsu, Tzu-Chun Chen, Shih-Cheng Chang, more

Virology > 2002 > 293 > 2 > 386-395

The human glioblastoma SF268 cell line was used to investigate the induction of apoptosis by the 3C protease of enterovirus 71 (EV71). Transient expression in these cells of the wild-type 3C protein encoded by EV71 induced morphological alterations typical of apoptosis, including generation of apoptotic bodies. Degradation of cellular DNA in nucleosomes was also observed. When two of the amino acids...

article

Rescue of Immunoglobulins from Insolubility Is Facilitated by PDI in the Baculovirus Expression System

Tsu-An Hsu, Sarah Watson, Joseph J. Eiden, Michael J. Betenbaugh

Protein Expression and Purification > 1996 > 7 > 3 > 281-288

A substantial fraction of immunoglobulin heavy and light chain polypeptides were insoluble when expressed in the baculovirus–insect cell expression system. In the presence of coexpressed heterologous protein disulfide isomerase (PDI), however, the solubility of the immunoglobulins was enhanced and IgG was secreted at higher levels from baculovirus-infectedTrichoplusia niinsect cells. Pulse-chase experiments...

Filter options

Publication date

Set your own date range

INFONA - science communication portal

Search results for: Tsu-An Hsu

Add recipient

Sending message cancelled

Are you sure you want to cancel sending this message?

Send message

Filter options

Publication date

Date range setting

Set the date range to filter the displayed results. You can set a starting date, ending date or both. You can enter the dates manually or choose them from the calendar.

Keywords

Data set

Journal

Reporting an error / abuse

Sending the report failed

Accessibility options