Kagoshima University · Graduate School of Science and Engineering · 教授

Research keywordsProtein Engineering・Therapeutic Antibody・ペプチド・ファージディスプレイ・抗体・蛋白質工学・遺伝子工学・Gene Engineering

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• Tsuji K., Miura Y., Kuwata T., Matsuzaki R., Kobayakawa T., Matsumoto K., Ito Y., Yoshiya T., Matsushita S., Tamamura H. . CD4 Mimic-Neutralizing Antibody Conjugates Synthesized by Site-Specif2025 · 記述言語： 日本語 出版者・発行元： Chemmedchem Antibody-drug conjugates (ADCs) that equip multiple cytotoxic drugs on an antibody have been developed, particularly in cancer chemotherapy. In the treatment of viral infectious diseases, there are dominantly fewer examples of ADCs. Recently, we developed double-warhead ADCs targeting the entry of human immunodeficiency virus type 1 (HIV-1) into host cells. One is a small molecule CD4 mimic, which is a competitive inhibitor against the interaction between a viral envelop protein, gp120, and a primary receptor, CD4, and the other is neutralizing antibodies, which recognize the regions of gp120, exposed by its conformational change after the interaction between gp120 and CD4. The conformational changes are also triggered by the binding of gp120 and a CD4 mimic, and therefore, the ADCs show positive effects on anti-HIV-1 activity compared to the combinational use of CD4 mimics with neutralizing antibodies. Herein, we synthesized novel ADCs containing a CD4 mimic and a neutralizing antibody, KD-247, using tCAP chemistry, which is based on a site-specific modification method for IgG antibodies, and evaluated their anti-HIV-1 and antibody-dependent cellular cytotoxicity (ADCC) activities. As a result, the KD-247-adopted ADCs demonstrated enhanced anti-HIV-1 activities, whereas all of the ADCs reduced their ADCC activities. DOI： 10.1002/cmdc.202500820 Scopus PubMed
• Muguruma Kyohei, Fukuda Akane, Shida Hayate, Osawa Rento, Harigaya Soichiro, Ito Mayu, Sato Nana, Kuroda Aya, Kobayashi Atsuki, Kishimoto Satoshi, Taguchi Akihiro, Takayama Kentaro, Taniguchi Atsuhiko, Ito Yuji, Hayashi Yoshio2025 · 記述言語： 英語 出版者・発行元： (公社)日本薬学会
• Kawakami H., Rafique A., Tsuda S., Nagashima A., Nohara Y., Dozono N., Sakamoto K., Masuda S., Kiyoshi M., Shibata H., Ishii-Watabe A., Yoshiya T., Ito Y. . Development of tCAP(N3): Affinity P2025 · 記述言語： 日本語 出版者・発行元： Chemistry A European Journal Direct modification of native antibodies with affinity peptides remains a significant challenge, primarily because the affinity peptide often stays bound to the antibody and blocks its interaction with key receptors. In this study, we developed tCAP(N3), a novel traceless chemical conjugation method that employs an affinity peptide. tCAP(N3) can be stored for over a year at refrigerated temperature, as it contains an active ester precursor that can be spontaneously activated under neutral conditions. When tCAP(N3) was mixed with a target native IgG, Ac-Lys(N<inf>3</inf>)-Gly-Gly was site-selectively transferred onto Lys248, yielding divalently azidated IgG that can be further modified with DBCO compounds. The resulting antibody conjugates retained Fc receptor binding and antigen recognition comparable to the parent IgG. DOI： 10.1002/chem.202503144 Scopus PubMed
• Hichiwa G., Rafique A., Nagashima A., Wang Y., Kazuki K., Ogihara R., Jatnika M.F., Shimamoto R., Iwai Y., Uno N., Satofuka H., Tomizuka K., Ito Y., Kazuki Y. . Targeting of bowel tissue by fu2025 · 記述言語： 日本語 出版者・発行元： Biomedicine and Pharmacotherapy Monoclonal antibodies are indispensable therapeutic agents for various diseases, including cancer, autoimmune disorders, and infectious diseases. Glycoprotein A33 (GPA33), a cell surface antigen highly expressed in colorectal cancer, provides a compelling therapeutic target; however, the species-specificity of anti-GPA33 antibodies has limited their utility in preclinical models, thus inhibiting their development. Here, we generated and characterized fully human, cross-reactive anti-GPA33 antibodies using phage-display technology with transchromosomic antibody-producing animals. The resulting single-chain variable fragment and single-chain variable fragment crystallizable antibodies exhibited high specificity and affinity for both human and mouse GPA33. In vivo imaging confirmed their targeted retention in mouse intestine, indicating their potential for developing targeted therapeutic approaches. The ability of these antibodies to recognize both human and murine GPA33 enhances their applicability in preclinical models, improving their translation from experimental to clinical applications. These results highlight the feasibility of developing cross-reactive, fully human antibodies and support the advancement of GPA33-targeted diagnostic approaches and the exploration of novel therapeutic strategies for relevant gastrointestinal diseases. DOI： 10.1016/j.biopha.2025.118336 Scopus PubMed

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