Drug Discovery and Development Laboratory

2024

1. Han-Li Su, Shu-Jung Lai, Keng-Chang Tsai, Kit-Man Fung, Tse-Lin Lung, Hsing-Mien Hsu, Yi-Chen Wu, Ching-Hui     

   Liu, Hui-Xiang Lai, Jiun-Han Lin and Tien-Sheng Tseng*. Structure-guided identification and characterization of potent

  inhibitors targeting PhoP and MtrA to combat mycobacteria. Computational and Structural Biotechnology 

   Journal  (Impact factor: 6.0, Q1), 2024. (In press)

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2. Yi-Chen Wu, Hui-Xiang Lai, Ji-Min Li, Kit-Man Fung, and Tien-Sheng Tseng* Discovery of a Potent Inhibitor, D-132, 

   Targeting AsfvPolX, via Protein-DNA Complex‐Guided Pharmacophore Screening and in vitro Molecular 

   Characterizations. Virus Research (Impact factor: 5.0, Q2). 2024 Mar 21:199359.

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3. Tien-Sheng Tseng, Chao-Chang Lee, Po-Juei Chen, Chiu-Yuen Lin, Wang-Chuan Chen, Yu-Ching Lee, Jiun-Han           Lin, Kaun-Wen Chen, and Keng-Chang Tsai. Structure-guided Discovery of PD-1/PD-L1 Interaction Inhibitors:         

     Peptide Design, Screening, and Optimization via Computation-Aided Phage Display Engineering. Journal of         

    Chemical Information and Modeling (Impact factor: 5.6, Q1), 2024, 64, 5, 1615–1627.

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2023                                                                                                            

1. Shu-Jung Lai, I-Fan Tu, Tien-Sheng Tseng, Yu-Hsuan Tsai, and Shih-Hsiung Wu. The deficiency of poly-β-1,6-N-acetyl-glucosamine deacetylase trigger A. baumannii to convert to biofilm-independent colistin-tolerant cells. Scientific reports (Impact factor 4.997). 2023 Feb 16;13(1):2800. doi: 10.1038/s41598-023-30065-5.                           

2. Lee YC, Lin TY, Lai GH, Tseng TS, Tsai TH, Chen WC, Tsai KC*. Development of anti-aflatoxin B1 nanobodies from a novel mutagenesis-derived SynaGG library for TCM and foods safety testing. Journal of Biological Engineering (2023) (Impact factor 6.248, Q1).                                                                                                                                      

2022

1. Keng-Chang Tsai, Yi-Xuan Zhang, Hsiang-Yun Kao, Kit-Man Fung, and Tien-Sheng Tseng*.Pharmacophore-driven Identification of Human Glutaminyl Cyclase Inhibitors from Foods, Plants and Herbs Unveil the Bioactive Property and Potential of Azaleatin for the Treatment of Alzheimer’s Disease. Food & Function (Impact factor: 6.317, Q1), 2022, DOI: 10.1039/D2FO02507H.                                                                                                                                      

2. Chih-Chuan Kao, Tzu-Lu Lin, Chi-Jan Lin and Tien-Sheng Tseng*. Deciphering Structure-Function Relationship Unveils Salt-Resistant Mode of Action of a Potent MRSA-Inhibiting Antimicrobial Peptide, RR14. Journal of Bacteriology (Impact factor = 3.476). 2022. Nov 15;e0031222. doi: 10.1128/jb.00312-22.                                             

3. Kit-Man Fung, Shu-Jung Lai, Tzu-Lu Lin and Tien-Sheng Tseng*. Antigen–Antibody Complex-Guided Exploration of the Hotspots Conferring the Immune-Escaping Ability of the SARS-CoV-2 RBD. Frontiers in Molecular Biosciences (impact factor: 6.12).(2022) Mar 22. doi: 10.3389/fmolb.2022.797132.                                                                           

4. Jangam Vikram Kumar, Tien-Sheng Tseng, Yuan-Chao Lou, Shu-Yi Wei, Tsung-Han Wu, Hao-Cheng Tang, Yi-Chih Chiu, Chun-Hua Hsu*, Chinpan Chen*. Structural insights into DNA binding domain of vancomycin-resistance-associated response regulator in complex with its promoter DNA from Staphylococcus aureus. Protein science (Impact factor: 6.75). (2022) 2022 May;31(5):e4286. doi: 10.1002/pro.4286.                                                      

  2021

1. Min-Che Tung, Kit-Man Fung, Hsin-Mie Hsuc and Tien-Sheng Tseng*. Discovery of 8-Prenylnaringenin from Hop (Humulus lupulus L.) as a potent Monoacylglycerol Lipase Inhibitor for Treatments of Neuroinflammation and Alzheimer’s Disease. RSC Adv (Impact factor: 4.036). (2021). 11, 31062-31072. (RSC Advances HOT Article Collection)                                                                                                                                                                        

2. Keng-Chang Tsai, Yu-Ching Lee and Tien-Sheng Tseng*.Comprehensive deep mutational scanning reveals the immune-escaping hotspots of SARS-CoV-2 receptor-binding domain targeting neutralizing antibodies. Frontiers in Microbiology (Impact factor: 6.064). (2021) 12:698365. doi: 10.3389/fmicb.2021.698365.                                             

3. Min-Che Tung, Keng-Chang Tsai, Kit-Man Fung , Ming-Jaw Don and Tien-Sheng Tseng* Characterizing the Structure-Activity Relationships of Natural Products, Tanshinones, Reveals their Mode of Action in Inhibiting Spleen Tyrosine Kinase. RSC Adv (Impact factor: 4.036), (2021), 11, 2453-2460. (Impact factor: 4.036)

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 2020

1. Ping-Sheng Wu,  Shu-Jung Lai,  Kit-Man Fung  and  Tien-Sheng Tseng*. Characterization of the structure–function relationship of a novel salt-resistant antimicrobial peptide, RR12. RSC Adv (Impact factor: 4.036), (2020), 10, 23624.

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 2019

1. Keng-Chang Tsai, Po-Pin Hung, Ching-Feng Cheng, Chinpan Chen and Tien-Sheng Tseng*. Exploring the mode of action of inhibitors targeting the PhoP response regulator of Salmonella enterica through comprehensive pharmacophore approaches.RSC Adv (Impact factor: 4.036), (2019), 9, 9308-9312. 

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 Before ​2019

1. Tien-Sheng Tseng, I-Fan Tu, Hsiao-Ting Chen, Lie-Chwen Lin, Keng-Chang Tsai, Shih-Hsiung Wu and Chinpan Chen. Protein–DNA complex-guided discovery of the antibacterial lead E1 for restoring the susceptibility of Klebsiella Pneumoniae to polymyxin B by targeting the response regulator PmrA. Chemical Communications. (2018) 54, 6372 – 6375.(Impact factory: 6.22)                                                                                                                   

2. Tien-Sheng Tseng, Keng-Chang Tsai, and Chinpan Chen. Characterizing structure–function relationship reveals mode of action of a novel antimicrobial peptide, P1, from jumper ant Myrmecia pilosula. Molecular BioSystems. (2017) Jun 1;13(6):1193-1201.                                                                                                                                         

3. Tien-Sheng Tseng, Shih-Han Wang, Ting-Wei Chang, Hung-Mu Wei, Yu-June Wang, Keng-Chang Tsai, You-Di Liao and Chinpan Chen. Sarkosyl-induced helical structure of an antimicrobial peptide GW-Q6 plays an essential role in the binding of surface receptor OprI in Pseudomonas aeruginosa. PLoS One (2016) Oct 11;11(10):e0164597.                                                                                                                                                          

4. Tien-Sheng Tseng, Show-Mei Chuang, Nai-Wan Hsiao, Yi-Wen, Chen, Yu-Ching Lee, Chi-Chen Lin, Huang C and Keng-Chang Tsai. Discovery of a potent cyclooxygenase-2 inhibitor, S4, through docking-based pharmacophore screening, in vivo and in vitro estimations. Molecular BioSystems (2016) Jul 19;12(8):2541-51. doi: 10.1039/c6mb00229c.                                                                                                                                                       

5. Jine-Yung Huang, Yi-Fang Chiu, José M Ortega, Hsing-Ting Wang, Tien-Sheng Tseng, Shyue-Chu Ke, Mercedes Roncel, Hsiu-An Chu. Mutations of Cytochrome b559 and PsbJ on and near the QC Site in Photosystem II Influence the Regulation of Short-Term Light Response and Photosynthetic Growth of the Cyanobacterium Synechocystis sp. PCC 6803. Biochemistry. (2016). DOI: 10.1021/acs.biochem.6b00133                                          

6. Tien-Sheng Tseng, Yu-Ching Lee, Nai-Wan Hsiao, Yun-Ru Liue, Keng-Chang Tsai. Comparative study between 3D-QSAR and Docking-Based Pharmacophore models for potent Plasomodium falciparum dihydroorotate dehydrogenase inhibitors. Bioorg Med Chem Lett. (2016) Jan 15;26(2):265-71                                                             

7. Tien-Sheng Tseng, Keng-Chang Tsai, Wang-Chuan Chen, Yeng-Tseng Wang, Yu-Ching Lee, Chung-Kuang Lu, Ming-Jaw Don, Chang-Yu Chang, ChingHsiao Lee, Hui-Hsiung Lin, Hung-Ju Hsu, and Nai-Wan Hsiao. Discovery of Potent Cysteine-Containing Dipeptide Inhibitors against Tyrosinase: A Comprehensive Investigation of 20 × 20 Dipeptides in Inhibiting Dopachrome Formation. J Agric Food Chem. (2015) Jul 15;63(27):6181-8.                                   

8. Wang-Chuan Chen, Tien-Sheng Tseng, Nai-Wan Hsiao, Yun-Lian Lin, Zhi-Hong Wen, Chin-Chuan Tsai, Yu-Ching Lee, Hui-Hsiung Lin & Keng-Chang Tsai. Discovery of Highly Potent Tyrosinase Inhibitor, T1, with Significant Anti-Melanogenesis Ability by zebrafish in vivo Assay and Computational Molecular Modeling. Sci Rep. (2015) Jan 23;5:7995.                                                                                                                                                                             

9. Yu-Ching Lee, Nai-Wan Hsiao, Tien-Sheng Tseng, Wang-Chuan Chen, Hui-Hsiung Lin, Sy-Jye Leu, Ei-Wen Yang, Keng-Chang Tsai. Phage Display-Mediated Discovery of Novel Tyrosinase-Targeting Tetrapeptide Inhibitors Reveals the Significance of N-Terminal Preference of Cysteine Residues and Their Functional Sulfur Atom. Mol Pharmacol. (2015) Feb;87(2):218-30.                                                                                                                                 

10. Nai-Wan Hsiao, Tien-Sheng Tseng, Yu-Ching Lee, Wang-Chuan Chen, Hui-Hsiung Lin, Yun-Ru Chen, Yeng-Tseng Wang, Hung-Ju Hsu, and Keng-Chang Tsai. Serendipitous Discovery of Short Peptides from Natural Products as Tyrosinase Inhibitors. J Chem Inf Model. (2014) Nov 24;54(11):3099-111.                                                                          

11. Tien-Sheng Tseng, Chao-Sheng Cheng, Shang-Te Danny Hsu, Min-Fang Shih, Pei-Lin He, Ping-Chiang Lyu. Residue-Specific Annotation of Disorder-to-Order Transition and Cathepsin Inhibition of a Propeptide-Like Crammer from D. melanogaster. PLoS One. (2013);8(1):e54187.                                                                                                             

12. Tien-Sheng Tseng, Chao-Sheng Cheng, Dian-Jiun Chen, Min-Fang Shih, Yu-Nan Yu, Shang-Te Danny Hsu, and Ping-Chiang Lyu. A molten globule-to-ordered structure transition of Drosophila melanogaster crammer is required for its ability to inhibit cathepsin. Biochem J. (2012) Mar 15;442(3):563-72.