Laboratory of Advanced Chemical Biology

Research Theme
Rational drug discovery based on a theory of dynamic epitope and innovative glycotechnology platform
Research Keywords

Chemical biology, Medicinal chemistry, Glycomedicine, Automated glycosynthesis, Glycomics, Glycotyping, Glycobiology, Biomarker discovery, Dynamic epitope, Glycopeptide, Antibody drug, Glycoconjugates probe, Microarray, Mass Spectrometry


Overview of Research and Education

Research Contents: Toward personalized medicine, our goal is to establish a promising strategy for the rational drug discovery system from disease-relevant “dynamic epitopes” based on the specific posttranslational modification of the key glycoproteins. Our new glycotechnology platform, notably glycoblotting-based high throughput glycomics and microarray displaying robust synthetic glycopeptides library, allowed for the development of epitope-defined antibodies showing potent anti-cancer activities.
At the core of our focused library construction technology, we are continuing to innovate molecular-based life technology such as microarrays and absolute quantification technology of specific key structures in life.

Laboratory of Advanced Chemical Biology (pdf)



N21, W11, Kita-ku, Sapporo, Hokkdido
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Representative Publications

Villones Lareno L, Ludwig A-K., Kumeta H., Kikuchi S., Ochi R., Aizawa T., Nishimura S-I., Gabius H-J., Hinou H, “Exploring the In situ pairing of human galectins toward synthetic O-mannosylated core M1 glycopeptides of α-dystroglycan”, Sci. Rep. 12, 17800 (2022)

Otaki M., Hirane N., Natsume-Kitatani Y., Nogami Itoh M., Shindo M., Kurebayashi Y., Nishimura S-I., “Mouse tissue glycome atlas 2022 highlights inter-organ variation in major N-glycan profiles”, Sci. Rep. 12, 17804 (2022)

Shiratori K., Yokoi Y., Wakui H., Hirane N., Otaki M., Hinou H., Yoneyama T., Hatakeyama T., Kimura S., Ohyama C., Nishimura Shin-Ichiro, “Selective reaction monitoring approach using structure-defined synthetic glycopeptides for validating glycopeptide biomarkers pre-determined by bottom-up glycoproteomics” RSC Adv. 12, 21385-21393 (2022)

Pablo A. Guillen-Poza, Elena Matilde Sánchez-Fernández, Gerard Artigas, José Manuel García Fernández, Hinou H., Carmen Ortiz Mellet, Nishimura S-I., Fayna Garcia-Martin, “Amplified detection of breast cancer autoantibodies using MUC1-based Tn antigen mimics” J. Med. Chem. 63, 8524-8533 (2020)

Koide R., Hirane N., Kambe D., Yokoi Y., Otaki M., Nishimura S-I., “Antiadhesive nanosome elicits role of glycocalyx of tumor cell-derived exosomes in the organotropic cancer metastasis” Biomaterials 280, 121314

Yokoi Y., Nishimura S-I. “Effect of Site‐specific O-Glycosylation on the Structural Behavior of NOTCH1 Receptor Extracellular EGF‐like Domains 11 and 10” Chem. Eur. J. 26, 12363-12372 (2020)

Wakui H., Tanaka Y., Ose T., Matsumoto I., Kato K., Yao M., Tachibana T., Sato M., Naruchi K., García-Martín F., Hinou H., Nishimura S-I. “A straightforward approach to antibodies recognising cancer specific glycopeptidic neoepitopes” Chem. Sci. 11, 4999-5006 (2020)

Hayakawa A., Matsushita T., Yokoi Y., Wakui H., Fayna Garcia-Martin, Hinou H., Matsuoka K., Nouso H., Kamiyama T., Taketomi A, Nishimura S-I. “Impaired O-Glycosylation at Consecutive Threonine TTX Motifs in Mucins Generates Conformationally Restricted Cancer Neoepitopes” Biochemistry 59, 1221-1241 (2020)

Koide R., Nishimura S-I., “Antiadhesive nanosomes facilitate targeting of lysosomal GlcNAc salvage pathway through derailed cancer endocytosis” Angew. Chem. Int. Ed. 58, 14513-14518 (2019)

Somovilla V.J., Bermeijo I.A., Albuquerque I.S., Martínez-S. N., Castro-Lopez J., Garcia-Martin F., Companon I.., Hinou H., Nishimura S-I., Jimenez-Barbero J., Asensio J.L, Avenoza G., Busto J.H., Hurtado-Guerrero. R., Peregrina J.M., Bernardes G.J.L., Corzana F., “The use of fluoroproline in MUC1 antigen enables efficient detection of antibodies in patients with prostate cancer”, J. Am. Chem. Soc. 129, 18255-18261 (2017)

Ohyabu N, Kakiya K., Yokoi Y., Hinou H., Nishimura S-I., “Convergent solid-phase synthesis of macromolecular MUC1 models truly mimicking serum glycoprotein biomarkers of interstitial lung diseases”, J. Am. Chem. Soc. 138, 8392-8395(2016)