Our Contributions to the World

Chemical generation of small molecule-based bispecific antibody-drug conjugates for broadening the target scope

Aiko Yamaguchi, Yasuaki Anami, Summer Yin Yuen Ha, Travis Roeder, Wei Xiong, Jangsoon Lee, Naoto T. Ueno, Ningyan Zhang, Zhiqiang An, and Kyoji Tsuchikama* Bioorg. Med. Chem. accepted on January 4th, 2021.

Invited as part of the Therapeutic Proteins and Their Chemistry Issue

Antibody-drug conjugates with dual payloads for combating breast tumor heterogeneity and drug resistance

Chisato M. Yamazaki, Aiko Yamaguchi, Yasuaki Anami, Wei Xiong, Yoshihiro Otani, Jangsoon Lee, Naoto T. Ueno, Ningyan Zhang, Zhiqiang An, and Kyoji Tsuchikama* Manuscript under review, preprint posted on bioRxiv. DOI: 10.1101/2020.12.18.423326.

Total Synthesis of the Monomeric Unit of Lomaiviticin A

K. C. Nicolaou, K. C.*, Chen, Q., Li, R., Anami, Y., and Tsuchikama, K. J. Am. Chem. Soc. 142, 20201 (2020)

Antibody Clicking as a Strategy to Modify Antibody Functionalities on the Surface of Targeted Cells

Toru Komatsu*, Etsu Kyo, Haruki Ishii, Kyoji Tsuchikama, Aiko Yamaguchi, Tasuku Ueno, Kenjiro Hanaoka, and Yasuteru Urano* J. Am. Chem. Soc. 142, 15644 (2020)

LILRB4-Targeting Antibody–Drug Conjugates for the Treatment of Acute Myeloid Leukemia

Anami, Y., Deng, M., Gui, X., Yamaguchi, A., Yamazaki, C. M., Zhang, N., Zhang, C. C.*, An, Z.*, and Tsuchikama, K.* Mol. Cancer Ther. 19, 2330 (2020).

[JAPANESE] Next-generation Antibody-drug Conjugates (ADCs): Exploring New Frontiers with Chemical Approaches

Anami, Y., and Tsuchikama, K.* J. Syn. Org. Chem. Jpn. 78, 503 (2020)

[JAPANESE] Novel Chemical Linkers for Next-generation Antibody-drug Conjugates (ADCs)

Tsuchikama, K.* J. Pharm. Soc. Jpn. 139, 209 (2019)

Disrupting LILRB4/APOE Interaction by an Efficacious Humanized Antibody Reverses T-cell Suppression and Blocks AML Development

Gui, X., Deng, M., Song, H., Chen, Y., Xie, J., Li, Z., He, L., Huang, F., Xu, Y., Anami, Y., Yu, H., Yu, C., Li, L., Yuan, Z., Xu, X., Wang, Q., Chai, Y., Huang, T., Shi, Y., Tsuchikama, K., Liao, X. C., Xia, N., Gao, G. F., Zhang, N.*, Zhang, C. C.*, and An, Z.* Cancer Immunol. Res. 7, 1244 (2019).

Transglutaminase-Mediated Conjugations

Yasuaki Anami and Kyoji Tsuchikama In: Tumey L. (eds) Antibody-Drug Conjugates. Methods in Molecular Biology, vol 2078, pp 71-82. Humana, New York, NY (2019)

Glutamic acid–valine–citrulline linkers ensure stability and efficacy of antibody–drug conjugates in mice

Yasuaki Anami, Chisato M. Yamazaki, Wei Xiong, Xun Gui, Ningyan Zhang, Zhiqiang An, and Kyoji Tsuchikama* Nature Commun. 9:2512 (2018). DOI: 10.1038/s41467-018-04982-3.


A short article in Behind the Paper (Nature Chemistry Community)

Featured in Nature Communications Editors' Highlights

Highlighted in UTHealth McGovern Medical School News

Antibody-drug conjugates: recent advances in conjugation and linker chemistries

Kyoji Tsuchikama* and Zhiqiang An Protein Cell 9, 33–46 (2018).

Enzymatic conjugation using branched linkers for constructing homogeneous antibody-drug conjugates with high potency

Yasuaki Anami, Wei Xiong, Xun Gui, Mi Deng, Cheng Cheng Zhang, Ningyan Zhang, Zhiqiang An, and Kyoji Tsuchikama* Org. Biomol. Chem. 15, 5635–5642 (2017).

Truncated autoinducing peptide conjugates selectively recognize and kill Staphylococcus aureus

Kyoji Tsuchikama,* Yasuhiro Shimamoto, and Yasuaki Anami ACS Infect. Dis. 3, 406–410 (2017).


  1. Shibata, T.; Takami, K.; Arai, Y.; Tsuchikama, K.; Maekawa, S. “The Reaction of Butatrienolates with Aldehydes for the Syntheses of α-Vinylidene Acylsilanes”, Bull. Chem. Soc. Jpn. 2004, 77, 1937–1938.

  2. Shibata, T.; Tsuchikama, K. “Ir-catalyzed almost perfect enantioselective synthesis of helical polyaryls based on an axially-chiral sequence”, Chem. Commun. 2005, 6017–6019. Highlighted in Synfacts 2006, 183.

  3. Shibata, T.; Tsuchikama, K.; Otsuka, M. “Enantioselective intramolecular [2+2+2] cycloaddition of triynes for the synthesis of atropisomeric chiral ortho-diarylbenzene derivatives”, Tetrahedron: Asymmetry 2006, 17, 614–619. Ranked in the Top-50 most cited articles in Tetrahedron: Asymmetry in the period of 2006-2009.

  4. Tsuchikama, K.; Kuwata, Y.; Shibata, T. “Highly Enantioselective Construction of a chiral Spirocyclic Structure by the [2 + 2 + 2] Cycloaddition of Diynes and exo-Methylene Cyclic Compounds”, J. Am. Chem. Soc. 2006, 128, 13686–13687. Highlighted in Synfacts 2007, 183.

  5. Shibata, T.; Arai, Y.; Takami, K.; Tsuchikama, K.; Fujimoto, T.; Takebayashi, S.; Takagi, K. “Iridium-Catalyzed Enantioselective [2+2+2] Cycloaddition of Diynes and Monoalkynes for the Generation of Axial Chiralities”, Adv. Synth. Catal. 2006, 348, 2475–2483.

  6. Tsuchikama, K.; Yoshinami, Y.; Shibata, T. “Rhodium Complex-Catalyzed [2+2+2] Cycloaddition of Diynes and Carbonyl Compounds”, Synlett 2007, 1395–1398.

  7. Tsuchikama, K.; Kuwata, Y.; Tahara, Y.; Yoshinami, Y.; Shibata, T. “Rh-Catalyzed Cyclization of Diynes and Enynes Initiated by Carbonyl-Directed Activation of Aromatic and Vinylic C–H Bonds”, Org. Lett. 2007, 9, 3097–3099. Highlighted in Synfacts 2007, 1071.

  8. Shibata, T.; Kawachi, A.; Ogawa, M.; Kuwata, Y.; Tsuchikama, K.; Endo, K. “Rhodium-catalyzed enantioselective [2+2+2] cycloaddition of diynes with unfunctionalized alkene”, Tetrahedron 2007, 63, 12853–12859.

  9. Tsuchikama, K.; Kasagawa, M.; Hashimoto, Y.; Endo, K.; Shibata, T. “Cationic iridium-BINAP complex-catalyzed addition of aryl ketones to alkynes and alkenes via directed C-H bond cleavage”, J. Organomet. Chem. 2008, 693, 3939–3942.

  10. Shibata, T.; Tsuchikama, K. “Recent advances in enantioselective [2+2+2] cycloaddition”, Org. Biomol. Chem. 2008, 6, 1317–1323. Selected as a Hot Article and ranked in the Top 10 most downloaded OBC articles in April 2008.

  11. Tsuchikama, K.; Kasagawa, M.; Endo, K.; Shibata, T. “Cationic Ir(I)-Catalyzed sp3 C-H Bond Alkenylation of Amides with Alkynes”, Org. Lett. 2009, 11, 1821–1823. Highlighted in Synfacts 2009, 782.

  12. Tsuchikama, K.; Hashimoto, Y.; Endo, K.; Shibata, T. “Iridium-Catalyzed Selective Synthesis of 4-Substituted Benzofurans and Indoles via Directed Cyclodehydration”, Adv. Synth. Catal. 2010, 351, 2850–2854. Highlighted in Synfacts 2010, 153.

  13. Tsuchikama, K.; Kasagawa, M.; Endo, K.; Shibata, T. “Sequential Catalytic Reactions for the Synthesis of Benzofulvenes Using an Iridium Complex with Dual Function”, Synlett 2010, 97–100. Highlighted in Synfacts 2010, 294.

  14. Shibata, T.; Hashimoto, Y.; Otsuka, M.; Tsuchikama, K.; Endo, K. “Ir(III)-Catalyzed Room-Temperature Synthesis of Multisubstituted Benzofurans Initiated by C–H Activation of α-Aryloxy Ketones”, Synlett 2011, 2075–2079.

  15. Shibata, T.; Hirashima, H.; Kasagawa, M.; Tsuchikama, K.; Endo, K. “Cationic Ir(I)-Catalyzed sp3 C-H Bond Alkenylation of Ureas with Alkynes for the Synthesis of 2,3-Disubstituted Indoles”, Synlett 2011, 2171–2176.

  16. Shibata, T.; Uchiyama, T.; Yoshinami, Y.; Takayasu, S.; Tsuchikama, K.; Endo, K. “Highly enantioselective synthesis of silahelicenes using Ir-catalyzed [2+2+2] cycloaddition” Chem. Commun. 2012, 48, 1311–1313.

  17. Salzameda, N. T.; Eubanks, L. M.; Zakhari, J. S.; Tsuchikama, K.; DeNunzio, N.; Allen, K. N.; Hixon, M. S.; Janda, K. D. “A Cross-over Inhibitor of the Botulinum Neurotoxin Light Chain B: A Natural Product Implicating an Exosite Mechanism of Action”, Chem. Commun. 2011, 1713–1715.

  18. Tsuchikama, K.; Lowery, C. A.; Janda, K. D. “Probing Autoinducer-2 Based Quorum Sensing: The Biological Consequences of Molecules Unable To Traverse Equilibrium States”, J. Org. Chem. 2011, 76, 6981–7294. Selected as a Featured Article and featured on the front cover of Volume 76, Issue 17.

  19. Tsuchikama, K.; Zhu, J.; Lowery, C. A.; Kaufmann, G. F.; Janda, K. D. “C4-Alkoxy-HPD: A Potent Class of Synthetic Modulators Surpassing Nature in AI-2 Quorum Sensing”, J. Am. Chem. Soc. 2012, 134, 13562–13564.

  20. Cai, X.; Tsuchikama, K.; Janda, K. D. “Modulating Cocaine Vaccine Potency Through Hapten Fluorination”, J. Am. Chem. Soc. 2013, 135, 2971–2974.

  21. Shibata, T.; Tsuchikama, K.; Pan, S. “Cationic Iridium-Catalyzed Synthesis Initiated by the Cleavage of C-H, N-H, and C-O Bonds”, J. Syn. Org. Chem. Jpn. 2013, 71, 1182–1194. (English Edition)

  22. Collins, K. C.; Tsuchikama, K.; Lowery, C. A.; Zhu, J.; Janda, K. D., "Dissecting AI-2-mediated quorum sensing through C5-analogue synthesis and biochemical analysis", Tetrahedron 2016, 72, 3593–3598.

  23. Tsuchikama, K.; Gooyit, M.; Harris, T. L.; Zhu, J.; Globisch, D.; Kaufmann, G. F.; Janda, K. D. “An Unprecedented Glycation Reactivity of a Quorum-Sensing Signaling Molecule” Angew. Chem. Intl. Ed. 2016, 55, 4002–4006. Selected as a Very Important Paper.


Seeds for Innovation


PCT/US2018/034363 filed, US-2020-0115326-A1 and EU18804968.8-1109/3630189 issued

©2018-present – Kyoji Tsuchikama. All rights reserved.

土釜 恭直 山﨑 ちさと 穴見 康昭 山口 藍子