Participated projects

Molecular functional screening using macromolecular library

Chen, S. H. et al. Engineering transaldolase in Pichia stipitis to improve bioethanol production. ACS Chem. Biol. 2012, 7, 481-486. (PMID: 22148723)

Tsai, T. I. et al. An effective bacterial fucosidase for glycoprotein remodeling. ACS Chem. Biol. 2017, 12, 63-72. (PMID: 28103685)


Molecular functional screening using GRC and user-provided small molecule library

Lin, C. Y. et al. Small-molecule PIK-93 modulates the tumor microenvironment to improve immune checkpoint blockade response. Sci. Adv. 2023, 9, eade9944. (PMID: 37027467)

Tseng, Y.W. et al. Dual-targeting compounds possessing enhanced anticancer activity via microtubule disruption and histone deacetylase inhibition. Eur. J. Med. Chem. 2024 265, 116042. (PMID: 38141287)

Huang, C. Y. et al. Population-based high-throughput toxicity screen of human iPSC-derived cardiomyocytes and neurons. Cell Rep. 2022 39, 110643. (PMID: 35385754)

Nicholson, M. W. et al. Cardio- and neurotoxicity of selected anti-COVID-19 drugs. Pharmaceuticals (Basel) 2022,15, 765. (PMID: 35745684)

Tsai, T. Y. et al. SIGLEC-3 (CD33) serves as an immune checkpoint receptor for HBV infection. J. Clin. Invest.2021, 131, e141965. (PMID: 34060491)

Peng, C. et al. Inhibitor development of MTH1 via high-throughput screening with fragment-based library and MTH1 substrate binding cavity. Bioorg. Chem. 2021, 110, 104813. (PMID: 33774493)

Jan, J. T. et al. Identification of existing pharmaceuticals and herbal medicines as inhibitors of SARS-CoV-2 infection. Proc. Natl. Acad. Sci. U. S. A. 2020, 118, e2021579118. (PMID: 33452205)

Lin, C. Y. et al. Suppression of drug-resistant non-small-cell lung cancer with inhibitors targeting minichromosomal maintenance protein. J. Med. Chem. 2020, 63, 3172-3187. (PMID: 32125853)

Wang, Y. Y. et al. Orabase-formulated gentian violet effectively improved oral potentially malignant disorder in vitro and in vivo. Biochem. Pharmacol. 2020, 171, 113713. (PMID: 31733192)

Woodring, J. L. et al. Disrupting the conserved salt bridge in the trimerization of influenza A nucleoprotein. J. Med. Chem. 2020, 63, 205-215. (PMID: 31769665)

Chang, Y. H. et al. Design and synthesis of glyco-peptides as anti-cancer agents targeting thrombin-protease activated receptor-1 interaction. Chem. Commun. 2020, 56, 5827-5830. (PMID: 32329494)

Lin, M. S. et al. 4(1H)-quinolone derivatives overcome acquired resistance to anti-microtubule agents by targeting the colchicine site of β-tubulin. Eur. J. Med. Chem. 2019, 181, 111584. (PMID: 31419740)

Huang, M. R. et al. Structure-guided development of purine amide, hydroxamate, and amidoxime for the inhibition of non-small cell lung cancer. Eur. J. Med. Chem. 2019, 181, 111551. (PMID: 31376567)

Tu, L. H. et al. Rationally designed divalent caffeic amides inhibit amyloid-β fibrillization, induce fibril dissociation, and ameliorate cytotoxicity. Eur. J. Med. Chem. 2018, 158, 393-404. (PMID: 30227353)

Yu, J. Y. et al. Structure-based design of bacterial transglycosylase inhibitors incorporating biphenyl, amine linker and 2-alkoxy-3-phosphorylpropanoate moieties. Eur. J. Med. Chem. 2018, 150, 729-741. (PMID: 29574202)

Cheng, H. W. et al. 2-anilino-4-amino-5-aroylthiazole-type compound AS7128 inhibits lung cancer growth through decreased iASPP and p53 interaction. Cancer Sci. 2018, 109, 832-842. (PMID: 29285847)

Wang, X. et al. Towards new antibiotics targeting bacterial transglycosylase: Synthesis of a Lipid II analog as stable transition-state mimic inhibitor. Bioorg. Med. Chem. Lett. 2018, 28, 2708-2712. (PMID: 29602680)

Chi, Y. H. et al. Lung cancer-targeting peptides with multi-subtype indication for combinational drug delivery and molecular imaging. Theranostics 2017, 7, 1612-1632. (PMID: 28529640

Huang, Y. W.; Yang, H. I.; Wu, Y. T.; Hsu, T. L.; Lin, T. W.; Kelly, J. W.; Wong, C. H. Residues comprising the enhanced aromatic sequon influence protein N-glycosylation efficiency. J. Am. Chem. Soc. 2017, 139, 12947-12955. (PMID: 28820257)

Zhai, Y. et al. An Automatic quality control pipeline for high-throughput screening hit identification. J. Biomol. Screen. 2016, 21, 832-841. (PMID: 27313114)

Kuo, T. C. et al. Purine-type compounds induce microtubule fragmentation and lung cancer cell death through interaction with katanin. J. Med. Chem. 2016, 59, 8521-8534. (PMID: 27536893)

Lin, M. I. et al. Synthesis and inhibitory effects of novel pyrimido-pyrrolo-quinoxalinedione analogues targeting nucleoproteins of influenza A virus H1N1. Eur. J. Med. Chem. 2015, 102, 477-486. (PMID: 26310893)

Wang, S. H. et al. HotLig: a molecular surface-directed approach to scoring protein-ligand interactions. J. Chem. Inf. Model. 2013, 53, 2181-2195. (PMID: 23862697)

Bryk, R. et al. Lipoamide channel-binding sulfonamides selectively inhibit mycobacterial lipoamide dehydrogenase. Biochemistry 2013, 52, 9375-9384. (PMID: 24251446)

Huang, S. H. et al. New continuous fluorometric assay for bacterial transglycosylase using Förster resonance energy transfer. J. Am. Chem. Soc. 2013, 135, 17078-17089. (PMID: 24131464)

Cheng, H. et al. Design, synthesis, and in vitro biological evaluation of 1H-1,2,3-triazole-4-carboxamide derivatives as new anti-influenza A agents targeting virus nucleoprotein. J. Med. Chem. 2012, 55, 2144-2153. (PMID: 22332894)

Shen, Y. F. et al. E339...R416 salt bridge of nucleoprotein as a feasible target for influenza virus inhibitors. Proc. Natl. Acad. Sci. U. S. A. 2011, 108, 16515-16520. (PMID: 21930946)

Cheng, T. J. et al. High-throughput identification of antibacterials against methicillin-resistant Staphylococcus aureus (MRSA) and the transglycosylase. Bioorg. Med. Chem. 2010, 18, 8512-29. (PMID: 21075637)

Su, C. Y. et al. High-throughput identification of compounds targeting influenza RNA-dependent RNApolymerase activity. Proc. Natl. Acad. Sci. U. S. A. 2010, 107, 19151-19156. (PMID: 20974907)

Wang, S. Y. et al. HA-pseudotyped retroviral vectors for influenza antagonist screening. J. Biomol. Screen. 2009, 14 (3), 294-302. (PMID: 19211776)

Cheng, T. J. et al. Domain requirement of moenomycin binding to bifunctional transglycosylases and development of high-throughput discovery of antibiotics. Proc. Natl. Acad. Sci. U. S. A. 2008, 105 (2), 431-436. (PMID: 18182485)