Lun Kelvin Tsou

Kelvin 2Lun Kelvin Tsou, Ph.D.
Investigator/Associate Director
Institute of Biotechnology and Pharmaceutical Research
Email: kelvintsou@nhri.edu.tw

 

EDUCATION

  • Ph.D. in Chemistry, Yale University (2002-2007)
  • B.S. Chemistry-Biochemistry track, and minor in Business Administration,
    University of North Carolina at Chapel Hill (1998-2002)

PROFESSIONAL EXPERIENCES

  • Associate Director, Institute of Biotechnology and Pharmaceutical Research, National Health Research Institutes (2023-present)
  • Investigator, Institute of Biotechnology and Pharmaceutical Research, National Health Research Institutes, Miaoli, Taiwan (2022-present)
  • Associate Director, Institute of Biotechnology and Pharmaceutical Research, National Health Research Institutes (2020)
  • 科技部台灣生醫與醫材轉譯加值人才培訓(SPARK Taiwan)諮詢顧問 (2018)
  • Adjunct Assistant Professor, School of Pharmacy, National Cheng Kung University (2017-present)
  • Associate Investigator, Institute of Biotechnology and Pharmaceutical Research, National Health Research Institutes, Miaoli, Taiwan (2017-2022)
  • Assistant Investigator, Institute of Biotechnology and Pharmaceutical Research, National Health Research Institutes, Miaoli, Taiwan (2012-2017)
  • Postdoctoral Fellow, Laboratory of Chemical Biology and Microbial Pathogenesis, The Rockefeller University, New York, NY (2007- 2012)

RESEARCH INTERESTS

  • Bioconjugation Chemistry
  • Chemical Biology
  • Post-Translational Modifications
  • Antivirulence and antiviral agents
  • Protein-Protein interaction inhibitors

HONORS & AWARDS

  • 2022 NSTC ​Ta-You Wu Memorial Award
  • 2020 Beyond BioMed Accelerator
  • 2019 MOST FutureTech Demo and Breakthrough Award
  • 2019 Asian Core Program Lectureship by Invitation (Japan series)
  • 2018 14th Tien Te Lee Biomedical Young Scientists Award
  • 2018 Asian Core Program Lectureship (Hong Kong series)
  • 2018 2018 NHRI Research Achievement Award-Young Scientist Award
  • 2017 2017 Tapei Biotech Award-Gold Medal for Technology Transfer Awardby Department of Economic Development, Taipei City Government
  • 2016 2016 Technology Achievement Award” by the Ministry of Economic Affairs
  • 2007  Henry and Marie-Josée Kravis Postdoctoral Fellowship, The Rockefeller University.
  • 2002  Graduated with Honors in Chemistry, University of North Carolina at Chapel Hill.

PUBLICATIONS

  1. Lo CF, Chiu TY, Liu YT, Pan PY, Liu KL, Hsu CY, Fang MY, Huang YC, Yeh TK, Hsu TA, Chen CT*, Huang LR*, Tsou LK*. ”Targeting the Phosphatidylserine-Immune Checkpoint with a Small-Molecule Maytansinoid Conjugate.”J Med Chem. 2022 ASAP. doi: 10.1021/acs.jmedchem.2c00631.
  2. Lo CF, Chiu TY, Liu YT, Huang LR, Yeh TK, Huang KH, Liu KL, Hsu CY, Fang MY, Huang YC, Hsu TA, Chen CT, Tsou LK*. ”Synthesis and Evaluation of Small Molecule Drug Conjugates Harnessing Thioester-Linked Maytansinoids” Pharmaceutics. 2022 Jun 21;14(7):1316. doi: 10.3390/pharmaceutics14071316
  3. Huang KH, Liu YT, Pan PY, Lo CF, Liu KL, Yeh TK, Huang L.R.*, Tsou L. K.* “Rejuvenating hepatic tumor microenvironment immunity with a phosphatidylserine-targeting small molecule drug conjugate” Biomedicine & Pharmacotherapy. 2022 May 11; 151: 113084.
  4. Click Chemistry and Multicomponent Reaction for Linker Diversification of Zinc Dipicolylamine-Based Drug Conjugates.
    Tsai CH, Chiu TY, Chen CT, Hsu CY, Tsai YR, Yeh TK, Huang KH, Tsou LK. Front Chem. 2022 Feb 15;9:822587. doi: 10.3389/fchem. 2021.822587.
  5. BPRDP056, a novel small molecule drug conjugate specifically targeting phosphatidylserine for cancer therapy.Chen YY, Lo CF, Chiu TY, Hsu CY, Yeh TK, Chen CP, Huang CL, Huang CY, Wang MH, Huang YC, Ho HH, Chao YS, Shih JC, Tsou LK, Chen CT. Transl Oncol. 2021 Jan;14(1):100897. doi: 10.1016/j.tranon.2020.100897. Epub 2020 Oct 14.
  6. Chemoproteomic profiling reveals cellular targets of nitro-fatty acids.
    Fang MY, Huang KH, Tu WJ, Chen YT, Pan PY, Hsiao WC, Ke YY, Tsou LK, Zhang MM. Redox Biol. 2021 Oct;46:102126. doi: 10.1016/j.redox.2021.102126. Epub 2021 Sep 7.
  7. Briarenols W-Z: Chlorine-Containing Polyoxygenated Briaranes from Octocoral Briareum stechei (Kükenthal, 1908).Chen YY, Zhang YL, Lee GH, Tsou LK, Zhang MM, Hsieh HP, Chen JJ, Ko CY, Wen ZH, Sung PJ. Mar Drugs. 2021 Jan 31;19(2):77. doi: 10.3390/md19020077.
  8. Comparative study between deep learning and QSAR classifications for TNBC inhibitors and novel GPCR agonist discovery. Tsou LK, Yeh SH, Ueng SH, Chang CP, Song JS, Wu MH, Chang HF, Chen SR, Shih C, Chen CT, Ke YY. Sci Rep. 2020 Oct 8;10(1):16771. doi: 10.1038/s41598-020-73681-1.
  9. Liu YW, Chen YY, Hsu CY, Chiu TY, Liu KL, Lo CF, Fang MY, Huang YC, Yeh TK, Pak KY, Gray BD, Hsu TA, Huang KH, Shih C, Shia KS, Chen CT*, Tsou LK.* “Linker Optimization and Therapeutic Evaluation of Phosphatidylserine-Targeting Zinc Dipicolylamine-based Drug Conjugates.” J Med Chem. 2019 Jul 11;62(13):6047-6062.
  10. Rosenberg EM Jr, Harrison RES, Tsou LK, Drucker N, Humphries B, Rajasekaran D, Luker KE, Wu CH, Song JS, Wang CJ, Murphy JW, Cheng YC, Shia KS, Luker GD, Morikis D, Lolis EJ. “Characterization, Dynamics, and Mechanism of CXCR4 Antagonists on a Constitutively Active Mutant.” Cell Chem. Biol. 2019  16;26(5):662-673.
  11. Tsou, L. K.; Huang, Y. H.; Song, J. S.; Ke, Y. Y.; Huang, J. K.; Shia, K. S.“Harnessing CXCR4 Antagonists in Stem Cell Mobilization, Ischemic Diseases and Oncology.” Med. Res. Rev. 2018, doi: 10.1002/med.21464. (2016 IF: 8.76, ranking: 2/60 (3.3 %) in Chemistry, Medicinal)
  12. Wu, C. H.; Song, J. S.; Kuan, H. H.; Wu, S. H.; Chou, M. C.; Jan, J. J.; Tsou, L. K.; Ke, Y. Y.; Chen, C. T.; Yeh, K. C.; Wang, S. Y.; Yeh, T. K.; Tseng, C. T.; Huang, C. L.; Wu, M. H.; Kuo, P. C.; Lee C. J.; Shia, K. S. “Development of Stem-Cell-Mobilizing Agents Targeting CXCR4 Receptor for Peripheral Blood Stem Cell Transplantation and Beyond.” J. Med. Chem. 2018, 61(3), 818-833. (2016 IF: 6.26, ranking: 3/60 (5.0 %) in Chemistry, Medicinal)
  13. Liu, Y. W.;Shia, K. S.; Wu, C. H.;Liu,K. L.;Yeh, Y. C.;Lo, C. F.;Chen, C. T.; Chen, Y. Y.; Yeh, T. K.; Chen, W. H.;Jan, J. J.; Huang, Y. C.;Huang, C. L.;Fang, M. Y.; Gray, B. D.; Pak, K. Y.;Hsu, T. A.;Huang, K. H.; Tsou, L. K. * “Targeting Tumor Associated Phosphatidylserine with New Zinc Dipicolylamine-Based Drug Conjugates.” Bioconjugate Chem. 2017, doi:10.1021/acs.bioconjchem. (*Corresponding author). (2016 IF: 4.82, ranking: 10/77 (12.9 %) in Biochemical Research Methods)
  14. Yeh, T. K.; Kuo, C. C.; Lee, Y. Z.; Ke, Y. Y.; Chu, K. F.; Hsu, H. Y.; Chang, H. Y.; Liu, Y. W.; Song, J. S.; Yang, C. W.; Lin, L. M.; Sun, M.; Wu, S. H.; Kuo, P. C.; Shih, C.; Chen, C. T.; Tsou, L. K. *; Lee, S. J. *“Design, Synthesis, and Evaluation of Thiazolidine-2,4-dione Derivatives as a Novel Class of Glutaminase Inhibitors.” .” J. Med. Chem. 2017, 60(13), 5599-5612. (*Co-corresponding author). (2016 IF: 6.26, ranking: 3/60 (5.0 %) in Chemistry, Medicinal)
  15. Tsou, L. K.; Yount,J. S.; Hang, H. C. “Epigallocatechin-3-gallate inhibits bacterial virulence and invasion of host cells.” Bioorg. Med. Chem.2017, 25 (11): 2883-2887. (2016 IF: 2.93, ranking: 16/59 (27.1 %) in Chemistry, Organic)
  16. Cheng, C. Y.; Chang, C. P.; Lauderdale, T. Y.; Yu, G. Y.; Lee, J. C.; Jhang, Y. W.; Wu, C. H.; Ke, Y. Y.; Sadani, A. A.; Yeh, C. F.; Huang, I. W.; Kuo, Y. P.; Tsai, D. J.; Yeh, T. K.; Tseng, C. T.; Song, J. S.; Liu, Y. W.; Tsou, L. K. *; Shia, K. S.*“Bromomethylthioindole Inspired Carbazole Hybrids as Promising Class of Anti-MRSA Agents.” ACS Med. Chem. Lett. 2016;7(12):1191-1196. (*Co-corresponding author) (2016 IF: 3.75, ranking: 9/60 (15.0 %) in Chemistry, Medicinal)
  17. Tsou, L. K.; Lara-Tejero, M.; Zhang, Z. J.; RoseFigura, J.; Wang Y-C.; Yount, J. S.; Lefebre, M.; Dossa, P. D.; Kato, J.; Guan, F.; Lam, W.; Cheng, Y-C.; Galán, J. E.; Hang, H. C. “Antibacterial Flavonoids from Medicinal Plants Covalently Inactivate Type III Protein Secretion Substrates.” J.  Am. Chem. Soc., 2016, ASAP.
  18. Wu, C. H.; Song, J. S.; Chang, K. H.; Jan, J. J.; Chen, C. T.; Chou, M. C.; Yeh, K. C.; Wong, Y. C.; Tseng, C. T,; Wu, S. H.; Yeh, C. F.; Huang, C. Y.; Wang, M. H.; Sadani, A. A.; Chang, C. P.; Cheng, C. Y.; Tsou, L. K.; Shia, K. S. “Stem cell mobilizers targeting chemokine receptor CXCR4: renoprotective application in acute kidney injury.” J Med Chem. 2015, 58(5), 2315-25
  19. Wu, C. H.; Wang, C. J.; Chang, C. P.; Cheng, Y. C.; Song, J. S.; Jan, J. J.; Chou, M. C.; Ke, Y. Y.; Ma, J.; Wong, Y. C.; Hsieh, T. C.; Tien, Y. C.; Gullen, E. A.; Lo, C. F.; Cheng, C. Y.; Liu, Y. W.; Sadani, A. A.; Tsai, C. H.; Hsieh, H. P.; Tsou, L. K. *; Shia, K. S * “Function-oriented development of CXCR4 antagonists as selective human immunodeficiency virus (HIV)-1 entry inhibitors.” J Med Chem. 2015, 58(3), 1452-65 (*Co-corresponding author).
  20. Tsou, L. K.; Dossa, P. D.; Hang, H. C. “Small molecules aimed at type III secretion systems to inhibit bacterial virulence.” MedChem Comm. 2013, 4(1), 68-79
  21. Tsou, L. K.; Cheng, Y.; Cheng, Y. C. “Therapeutic development in targeting protein-protein interactions with synthetic topological mimetics.” Curr Opin Pharmacol. 2012, 12(4), 403-7
  22. Tsou, L. K.; Chen, C.H.; Dutschman, G.E.; Cheng, Y.C.; Hamilton, A.D. “Blocking HIV-1 entry by a gp120 surface binding inhibitor.” Bioorg Med Chem Lett. 2012, 22(9), 3358-61
  23. Charron, G.; Tsou, L. K.; Maguire, W.; Yount, J. S.; Hang, H. C.  “Alkynyl-farnesol reporters for detection of protein S-prenylation in cells.”    Molecular BioSystems. 2011, 7(1), 67-73.
  24. Yount, J. S.; Tsou, L. K.; Dossa, P. D.; Kullas, A. L.; van der Velden, A. W. M.; Hang, H. C.  “Visible Fluorescence Detection of Type III Protein Secretion from Bacterial Pathogens.” J. Am. Chem. Soc., 2010, 132(24), 8244-8245.
  25. Zhang, M. M.*; Tsou, L. K.*; Charron, G.; Raghavan, A. S.; Hang, H. C. “Tandem fluorescence imaging of dynamic S-acylation and protein turnover.”    Proc.  Nat.  Acad.  Sci. USA. 2010, 107(19), 8627-8632. (*M.M.Z. and L.K.T. contribute equally to this work.)
  26. Tsou L. K.; Dutschman G.E.; Gullen E.A.; Telpoukhovskaia M.; Cheng Y.-C.; Hamilton A.D. “Discovery of a synthetic dual inhibitor of HIV and HCV infection based on a tetrabutoxy-calix[4]arene scaffold.” Bioorg. Med. Chem. Lett. 2010, 20(7), 2137-2139.
  27. Cheng, Y.; Tsou, L. K.; Cai, J.; Aya, T.; Dutschman, G. E.; Gullen, E. A.; Grill, S. P.; Chen, A. P.-C.; Lindenbach, B. D.; Hamilton, A. D.; Cheng, Y.-C. “A novel class of meso-Tetrakis-porphyrin derivatives exhibits potent activities against hepatitis C virus genotype 1b replicons in vitro.” Antimicrobial Agents and Chemotherapy. 2010, 54(1), 197-206.
  28. Tsou, L. K.; Zhang, M. M.; Hang, H. C. “Clickable fluorescent dyes for multimodal biorthogonal imaging.”    Organic & Biomolecular Chemistry. 2009, 7(24), 5055-5058.
  29. Margulies, D.; Opatowsky, Y.; Fletcher, S.; Saraogi, I.; Tsou, L. K.; Saha, S.; Lax, I.; Schlessinger, J.; Hamilton, A. D.  “Surface binding inhibitors of the SCF-KIT protein-protein interaction.”    ChemBioChem, 2009, 10(12), 1955-1958.
  30. Jain, Rishi K.; Tsou, L. K.; Hamilton, A. D., “Combined solid/solution phase synthesis of large surface area scaffolds derived from aminomethyl-benzoates.”   Tet. Lett. 2009, 50(23), 2787-2789.
  31. Jayawickramarajah, J.; Tagore, D.; Tsou, L. K.; Hamilton, A. D., “Allosteric control of self-assembly: Modulating the formation of guanine quadruplexes through orthogonal aromatic interactions”, Angew. Chem. Int. Ed., 2007, 46, 7583-7586.
  32. Davis, J. M.; Tsou, L. K.; Hamilton, A. D. “Synthetic non-peptide mimetics of alpha-helices.” Chem. Soc. Rev., 2007, 36, 326-334.
  33. Park, K. K.; Tsou, L. K.; Hamilton, A. D. “Facile and selective aerobic oxidation of arylalkanes to aryl ketones using cesium carbonate.” Synthesis, 2006, 21, 3617-3620.
  34. Jain, R. K.; Tsou, L. K.; Hamilton, A. D. “Recognition of Cytochrome C by Tetraphenylporphyrin-based Protein Surface Receptors.” Macrocyclic Chemistry, 2005, Kluwer, Editor: Carsten Gloe.
  35. Tsou, L. K.; Jain, R. K.; Hamilton, A. D. “Protein surface recognition by porphyrin-based receptors.” J. Porph. Phthalocyan. 2004, 8, 141-147.
  36. Tsou, L. K.; Tatko, C. D.; Waters, M. L. “A Simple Cation-π Interaction Between a Phenyl Ring and a Protonated Amine Stabilizes an Alpha-Helix in Water.” J. Am. Chem. Soc., 2002, 124, 14917-1492

SELECTED PRESENTATIONS

  1. 14th Asian Core Program on Cutting-Edge Organic Chemistry in Asia. Hokkaido, September/2019
  2. 2019 Asian Chemical Congress
  3. 18th Consortium for Globalization of Chinese Medicine (CGCM) Shanghai, China. August/2019
  4. “Apoptotic Signal Amplifying Drug Conjugates for Cancer Therapy”, Invited talk. 2018中國化學年會. Taiwan. December/2018
  5. “Apoptotic Signal Amplifying Drug Conjugates for Cancer Therapy”, Keynote talk. 4th Advanced Research Network on Cutting-Edge Organic Chemistry in Asia (ARNCEOCA-4). Singapore. October/2018
  6. “Antibacterial flavonoids from medicinal plants covalently inactivate type III protein secretion substrates” invited talk. 11th世界華人藥物化學研討會(International Symposium for Chinese Medicinal Chemists, ISCMC)鄭州, China. August/2018
  7. “Antibacterial flavonoids from medicinal plants covalently inactivate type III protein secretion substrates” invited talk. 11th世界華人藥物化學研討會(International Symposium for Chinese Medicinal Chemists, ISCMC)鄭州, China. August/2018
  8. “Chemical Toolbox for Dissecting Bacterial Pathogenesis and Beyond” Invited talk. 清華大學化學系 September/2017
  9. “Antibacterial Flavonoids from Medicinal Plants Covalently Inactivate Type III Protein Secretion Substrates.” Invited talk, The Fourth Asian Chemical Biology Conference, Taiwan, November/2016.
  10. “Chemical toolbox for dissecting bacterial pathogenesis and beyond,” Invited talk, Institute of Chemistry, Academia Sinica, Taiwan, April/2016.
  11. “Zinc-dipicolylamine directed pharmaceutical delivery system (ZAPS) as an innovative cancer drug delivery platform” Invited talk, 10th International Symposium for Chinese Medicinal Chemists, Taiwan, January/2016.
  12. “Chemical toolbox for dissecting bacterial pathogenesis and beyond,” Invited talk, Institute of Biological Chemistry, Academia Sinica, Taiwan, January/2016.
  13. “Small molecule drug conjugate technology as an innovative modular precision-therapeutic platform,” Invited talk, 精準醫療 (藥物+診斷)的現況與趨勢–小分子藥物開發產業聯盟, Taiwan, 2015
  14. “Zinc-dipicolylamine directed pharmaceutical delivery system (ZAPS) as an innovative cancer drug delivery platform,” Invited talk, Golden Jubilee Chemistry Conference, Kent Ridge, Singapore, 2015.
  15. “Chemical toolbox for dissecting bacterial pathogenesis and beyond,” Invited talk, Department of medicinal and applied chemistry, Kaohsiung Medical University, Taiwan, 2015.
  16. “Chemical toolbox for dissecting bacterial pathogenesis and beyond,” Invited talk, Agricultural Biotechnology Research Center (ABRC), Academia Sinica, Taiwan, 2014.
  17. “Mining traditional Chinese medicine for bacterial virulence inhibitors,” Invited talk, 12th Meeting of Consortium for Globalization of Chinese Medicine, Graz, Belgium, 2013.

PATENT GRANTED

  1. Chiung-Tong Chen, Kak-Shan Shia, Chien-Huang Wu, Lun Kelvin Tsou, Yu-Sheng Chao. Dipicolyamine derivatives and their pharmaceutical uses. United States. US 9,388,193(B2)
  2. Chiung-Tong Chen, Kak-Shan Shia, Chien-Huang Wu, Lun Kelvin Tsou, Yu-Sheng Chao. 二甲基吡啶胺衍生物及其醫藥用途, Taiwan, ROC. TWI600644
  3. Chiung-Tong Chen, Kak-Shan Shia, Chien-Huang Wu, Lun Kelvin Tsou, Yu-Sheng Chao. Dipicolyamine derivatives and their pharmaceutical uses. Singapore. 11201609786X
  4. Kak-Shan Shia, Jiing-Jyh Jan, Lun Kelvin Tsou, Chiung-Tong Chen, Yu-Sheng Chao. 雜環化合物及其用途, Taiwan, ROC. TWI598348
  5. Chiung-Tong Chen, Kak-Shan Shia, Chien-Huang Wu, Lun Kelvin Tsou, Yu-Sheng Chao. Dipicolyamine derivatives and their pharmaceutical uses. Russia. 領證中
  6. Kak-Shan Shia, Jiing-Jyh Jan, Lun Kelvin Tsou, Chiung-Tong Chen, Yu-Sheng Chao. Heterocyclic compounds and use thereof. Russia. 領證中
  7. Chiung-Tong Chen, Kak-Shan Shia, Chien-Huang Wu, Lun Kelvin Tsou, Yu-Sheng Chao. Dipicolyamine derivatives and their pharmaceutical uses. Australia. AU2015264409(B2)
  8. Chiung-Tong Chen, Kak-Shan Shia, Chien-Huang Wu, Lun Kelvin Tsou, Yu-Sheng Chao. Dipicolyamine derivatives and their pharmaceutical uses. South Africa. 領證中
  9. Kak-Shan Shia, Jiing-Jyh Jan, Lun Kelvin Tsou, Chiung-Tong Chen, Yu-Sheng Chao. Heterocyclic compounds and use thereof. United States. US 9926298(B2)
  10. Chiung-Tong Chen, Kak-Shan Shia, Chien-Huang Wu, Lun Kelvin Tsou, Yu-Sheng Chao. Dipicolyamine derivatives and their pharmaceutical uses. Japan. 領證中

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