Publications

Selected Publications

Research Articles

  1. X. Meng, K. Fu, Y. Liu, Y. Liu, J. Z. Zhang, X. Kang, C. Wu, Y.-H. Tsai, Disulfide-directed multicyclic peptides for chimeric antigen receptors targeting solid tumors. J. Am. Chem. Soc. 2026, 148, 400. PMID: 41480930. Preprint deposit. News in X-MOL.
  2. H. Liu, L. Song, X. Meng, J. Li, S. Fan, H. Dong, X. Wang, M. Li, H. Yu, Y.-H. Tsai, Y. Yin, C. Wu, Proline-mediated enhancement in evolvability of disulfide-rich peptides for discovering protein binders. J. Am. Chem. Soc. 2025, 147, 24870. PMID: 40601296. News in American Peptide Society.
  3. Y. Huang, C. Wu, A. Lu, J. Wang, J. Liang, H. Sun, L. Yang, S. Duan, A. A. Berezin, C. Wu, B. Zhang, Y.-L. Wu, Y.-H. Tsai, A single bioorthogonal reaction for multiplex cell surface protein labelling. J. Am. Chem. Soc. 2025, 147, 1612. PMID: 39749835. News in ChemH and X-MOL.
  4. C. Xu, X. Meng, P. Chai, H. Liu, Z. Duan, Y.-H. Tsai, C. Wu, Directed evolution of multicyclic peptides using yeast display for sensitive and selective fluorescent analysis of CD28 on the cell surface. Anal. Chem. 2025, 97, 4031. PMID: 39808546.
  5. T. L. Williams, I. M. Taily, L. Hatton, A. A. Berezin, Y.-L. Wu, V. Moliner, K. Świderek, Y.-H. Tsai, L. Y. P. Luk, Secondary amine catalysis in enzyme design: broadening protein template diversity through genetic code expansion. Angew. Chem. Int. Ed. 2024, 63, e202403098. PMID: 38545954.
  6. Y. Zhai, X. Zhang, Z. Chen, D. Yan, L. Zhu, Z. Zhang, X. Wang, K. Tian, Y. Huang, X. Yang, W. Sun, D. Wang, Y.-H. Tsai, T. Luo, G. Li, Global profiling of functional histidines in live cells using small-molecule photosensitizer and chemical probe relay labelling. Nat. Chem. 2024, 16, 1546. PMID: 38834725.
  7. J. Chen, G. Dai, S. Duan, Y. Huang, Y.-L. Wu, Z. Xie, Y.-H. Tsai, Selective protein degradation through tetrazine ligation of genetically incorporated unnatural amino acids. Chem. Asian J. 2024, 19, e202400824. PMID: 39221720.
  8. S.-J. Lai, I-F. Tu, T.-S. Tseng, Y.-H. Tsai, S.-H. Wu, The deficiency of poly-β-1,6-N-acetyl-glucosamine deacetylase trigger A. baumannii to convert to biofilm-independent colistin-tolerant cells. Sci. Rep. 2023, 13, 2800. PMID: 36797306.
  9. D. Cardella, Y.-H. Tsai, L. Y. P. Luk, Towards the use of an amino acid cleavable linker for solid-phase chemical synthesis of peptides and proteins. Org. Biol. Chem. 2023, 21, 966. PMID: 36628630.
  10. L. A. Spear, Y. Huang, J. Chen, A. R. Nödling, S. Virdee, Y.-H. Tsai, Selective inhibition of cysteine-dependent enzymes by bioorthogonal tethering. J. Mol. Biol. 2022, 434, 167524. PMID: 35248542.
  11. V. L. Barlow, Y.-H. Tsai, Acetylation at lysine 86 of Escherichia coli HUβ modulates the DNA-binding capability of the protein. Front. Microbiol. 2022, 12, 809030. PMID: 35185833.
  12. D. Cardella, W. Deng, L. Y. P. Luk, Y.-H. Tsai, Effect of trimethine cyanine dye- and folate-conjugation on the in vitro biological activity of proapoptotic peptides. Biomolecules 2022, 12, 725. PMID: 35625652.
  13. R. Cruz-Samperio, R. J. Mart, L. Y. P. Luk, Y.-H. Tsai, A. T. Jones, R. K. Allemann, Spatio-temporal photo-activation of cytotoxic proteins. ChemBioChem 2022, 23, e202200115. PMID: 35420232.
  14. E. M. Mills, V. L. Barlow, A. T. Jones, Y.-H. Tsai, Development of mammalian cell logic gates controlled by unnatural amino acids. Cell Rep. Methods 2021, 1, 100073. PMID: 35474893.
  15. T. L. Williams, D. Iskandar, A. R. Nödling, Y. Tan, L. Y. P. Luk, Y.-H. Tsai, Transferability of N-terminal mutations of pyrrolysyl-tRNA synthetase in one species to that in another species on unnatural amino acid incorporation efficiency. Amino Acids 2021, 53, 89. PMID: 33331978.
  16. X. Zheng, Z. Li, W. Gao, X. Meng, X. Li, L. Y. P. Luk, Y. Zhao, Y.-H. Tsai, C. Wu, Condensation of 2-((alkylthio)(aryl)methylene)malononitrile with 1,2-aminothiol as a novel bioorthogonal reaction for site-specific protein modification and peptide cyclization. J. Am. Chem. Soc. 2020, 142, 5097. PMID: 32108479.
  17. T. M. S. Tang, D. Cardella, A. J. Lander, X. Li, J. S. Escudero, Y.-H. Tsai, L. Y. P. Luk, Use of an asparaginyl endopeptidase for chemo-enzymatic peptide and protein labeling. Chem. Sci. 2020, 11, 5881. PMID: 32874509.
  18. A. R. Nödling, E. M. Mills, X. Li, D. Cardella, E. J. Sayers, S.-H. Wu, A. T. Jones, L. Y. P. Luk, Y.-H. Tsai, Cyanine dye mediated mitochondrial targeting enhances the anti-cancer activity of small-molecule cargoes. Chem. Commun. 2020, 56, 4672. PMID: 32211623.
  19. V. L. Barlow, S.-J. Lai, C.-Y. Chen, C.-H. Tsai, S.-H. Wu, Y.-H. Tsai, Effect of membrane-fusion protein AdeT1 on the antimicrobial resistance of Escherichia coli. Sci. Rep. 2020, 10, 20464. PMID: 33235243.
  20. N. G. Eissa, E. J. Sayers, D. Birch, S. G. Patel, Y.-H. Tsai, H. M. Nielsen, A. T. Jones, EJP18 peptide derived from the juxtamembrane domain of epidermal growth factor receptor represents a novel membrane-active cell-penetrating peptide. Biochem. J. 2020, 477, 45. PMID: 31820794. Commented in Biochemical Journal.
  21. S. G. Patel, E. J. Sayers, L. He, R. Narayan, T. L. Williams, E. M. Mills, R. K. Allemann, L. Y. P. Luk, A. T. Jones, Y.-H. Tsai, Cell-penetrating peptide sequence and modification dependent uptake and subcellular distribution of green florescent protein in different cell lines. Sci. Rep. 2019, 9, 6298. PMID: 31000738.
  22. A. R. Nödling, K. Świderek, R. Castillo, J. W. Hall, A. Angelastro, L. C. Morrill, Y. Jin, Y.-H. Tsai, V. Moliner, L. Y. P. Luk, Reactivity and selectivity of iminium organocatalysis improved by a protein host. Angew. Chem. Int. Ed. 2018, 57, 12478.  PMID: 30027571. Recommended by F1000Prime.
  23. T. Suzuki, M. Asami, S. G. Patel, L. Y. P. Luk, Y.-H. Tsai, A. C. F. Perry, Switchable genome editing via genetic code expansion. Sci. Rep. 2018, 8, 10051. PMID: 29968790. News in Science, The Conversation, GenomeWeb and Biotechnology and Biological Sciences Research Council (BBSRC). Press releases from Cardiff University and University of Bath.
  24. K. Świderek, A. R. Nödling, Y.-H. Tsai, L. Y. P. Luk, V. Moliner, Reaction mechanism of organocatalytic Michael addition of nitromethane to cinnamaldehyde: a case study on catalyst regeneration and solvent effects. J. Phys. Chem. A 2018, 122, 451. PMID: 29256614.
  25. T. L. Williams, A. R. Nödling, Y.-H. Tsai, L. Y. P. Luk, Carbapenems as water soluble organocatalysts. Wellcome Open Res. 2018, 3, 107. PMID: 30410999.
  26. J.-H. Liao, C.-H. Tsai, S. G. Patel, J.-T. Yang, I-F. Tu, M. Lo Cicero, M. Lipka-Lloyd, W.-L. Wu, W.-J. Shen, M.-R. Ho, C.-C. Chou, G. R. Sharma, H. Okanishi, L. Y. P. Luk, Y.-H. Tsai, S.-H. Wu, Acetylome of Acinetobacter baumannii SK17 reveals a highly-conserved modification of histone-like protein HU. Front. Mol. Biosci. 2017, 4, 77. PMID: 29230394. News in The Conversation.
  27. S.-J. Lai, I-F. Tu, W.-L. Wu, J.-T. Yang, L. Y. P. Luk, M.-C. Lai, Y.-H. Tsai, S.-H. Wu, Site-specific His/Asp phosphoproteomic analysis of prokaryotes reveals putative targets for drug resistance. BMC Microbiol. 2017, 17, 123. PMID: 28545444.
  28. Y.-H. Tsai, S. Essig, J. R. James, K. Lang, J. W. Chin, Selective, rapid and optically switchable regulation of protein function in live mammalian cells. Nat. Chem. 2015, 7, 554. PMID: 26100803. News in Chemical & Engineering News. Highlighted in Nature Methods and ACS Chemical Biology.
  29. S. Götze, A. Reinhardt, A. Geißner, N. Azzouz, Y.-H. Tsai, R. Kurucz, D. Varon Silva, P. H. Seeberger, Investigation of the protective properties of glycosylphosphatidylinositol-based vaccine candidates in a Toxoplasma gondii mouse challenge model. Glycobiology 2015, 25, 984. PMID: 26044798.
  30. S. Götze, N. Azzouz, Y.-H. Tsai, U. Groß, A. Reinhardt, C. Anish, P. H. Seeberger, D. Varon Silva, Diagnosis of toxoplasmosis using a synthetic glycosylphosphatidylinositol glycan. Angew. Chem. Int. Ed. 2014, 53, 13701. PMID: 25323101.
  31. Y.-H. Tsai, S. Götze, I. Vilotijevic, M. Grube, D. Varon Silva, P. H. Seeberger, A general and convergent synthesis of diverse glycosylphosphatidylinositol glycolipids. Chem. Sci. 2013, 4, 468.
  32. Y.-H. Tsai, S. Götze, N. Azzouz, H. S. Hahm, P. H. Seeberger, D. Varon Silva, A general method for synthesis of GPI anchors illustrated by the total synthesis of the low molecular weight antigen from Toxoplasma gondii. Angew. Chem. Int. Ed. 2011, 50, 9961. PMID: 21898727.
  33. M. Oberli, M. Tamborrini, Y.-H. Tsai, D. B. Werz, T. Horlacher, A. Adibekian, D. Gauss, H. M. Möller, G. Pluschke, P. H. Seeberger, Molecular analysis of carbohydrate-antibody interactions: case study using a Bacillus anthracis tetrasaccharide. J. Am. Chem. Soc. 2010, 132, 10239. PMID: 20614885.
  34. R. Kikkeri, X. Liu, A. Adibekian, Y.-H. Tsai, P. H. Seeberger, Facile synthesis of size dependent Ru(II)–carbohydrate dendrimers via click chemistry. Chem. Commun. 2010, 46, 2197. PMID: 20234904.
  35. M.-L. Hecht, Y.-H. Tsai, X. Liu, C. Wolfrum, P. H. Seeberger, Synthetic inositol phosphoglycans related to GPI lack insulin-mimetic activity. ACS Chem. Biol. 2010, 5, 1075. PMID: 20825209.
  36. Y.-L. Yang, F.-L. Yang, Z.-Y. Huang, Y.-H. Tsai, W. Zou, S.-H. Wu, Structural variation of glycolipids from Meiothermus taiwanensis ATCC BAA-400 under different growth temperatures. Org. Biomol. Chem. 2010, 8, 4252. PMID: 20668750.
  37. C.-T. Ren, Y.-H. Tsai, Y.-L. Yang, W. Zou, S.-H. Wu, Synthesis of a tetrasaccharide glycosyl glycerol. Precursor to glycolipids of Meiothermus taiwanensis ATCC BAA-400. J. Org. Chem. 2007, 72, 5427. PMID: 17579454.

Reviews

  1. J. Chen, Y.-H. Tsai*, Applications of genetic code expansion in studying protein post-translational modification. J. Mol. Biol. 2022, 434, 167424. PMID: 34971673.
  2. Y.-H. Tsai, T. Doura, S. Kiyonaka, Tethering-based chemogenetic approaches for the modulation of protein function in live cells. Chem. Soc. Rev. 2021, 50, 7909. PMID: 34114579.
  3. H. C. Hayes, L. Y. P. Luk, Y.-H. Tsai, Approaches for peptide and protein cyclisation. Org. Biomol. Chem. 2021, 19, 3983. PMID: 33978044.
  4. E. M. Mills, V. L. Barlow, L. Y. P. Luk, Y.-H. Tsai, Applying switchable Cas9 variants to in vivo gene editing for therapeutic applications. Cell Biol. Toxicol. 2020, 36, 17. PMID: 31418127.
  5. A. R. Nödling, N. Santi, T. L. Williams, Y.-H. Tsai, L. Y. P. Luk, Enabling protein-hosted organocatalytic transformations. RSC Adv. 2020, 10, 16147. PMID: 33184588.
  6. A. R. Nödling, L. A. Spear, T. L. Williams, L. Y. P. Luk, Y.-H. Tsai, Using genetically incorporated unnatural amino acids to control protein functions in mammalian cells. Essays Biochem. 2019, 63, 237. PMID: 31092687.
  7. Y.-H. Tsai, X. Liu, P. H. Seeberger, Chemical biology of glycosylphosphatidylinositol anchors. Angew. Chem. Int. Ed. 2012, 51, 11438. PMID: 23086912.
  8. Y.-H. Tsai, M. Grube, P. H. Seeberger, D. Varon Silva, Glycosylphosphatidylinositols of protozoan parasites. Trends Glycosci. Glycotechnol. 2012, 24, 231.

Editorial

  1. L. Wang, S. Yao, Y.-H. Tsai, Peptide passports: programmable import fuels novel protein building blocks. Cell Chem. Biol. 2025, 32, 1432. PMID: 41418760.
  2. Y.-H. Tsai, H. Iwaï, K. Pors, Editorial: chemical biology tools for peptide and protein research, Front. Chem. 2022, 10, 861699. PMID: 35252123.

Protocols

  1. J. Chen, Y. Huang, W.-B. Gan, Y.-H. Tsai. (2023) Selective inhibition of kinase activity in mammalian cells by bioorthogonal ligand tethering. In: Y.-H. Tsai & S. J. Elsässer (eds) Genetically Incorporated Non-Canonical Amino Acids. Methods in Molecular Biology, Vol 2676, 215 (Humana New York, NY). PMID: 37277636
  2. H. Sun, Y. Huang, Y.-H. Tsai. (2023) Genetically encoded 1,2-aminothiol for site-specific modification of a cellular membrane protein via TAMM condensation. In: Y.-H. Tsai & S. J. Elsässer (eds) Genetically Incorporated Non-Canonical Amino Acids. Methods in Molecular Biology, Vol 2676, 191 (Humana New York, NY). PMID: 37277634.
  3. E. J. Sayers, V. L. Barlow, Y.-H. Tsai, A. T. Jones. (2022) Quantitative subcellular analysis of cyclic cell-penetrating peptide EJP18 in nonadherent cells. In: Ü Langel (eds) Cell Penetrating Peptides. Methods in Molecular Biology, Vol 2383, 211 (Humana New York, NY). PMID: 34766292.