Tatsumi, T.; Zhao, S.; Kasahara, A.; Aoki, M.; Nishijima, K.; Ukon, N.; Kodama, T.; Takahashi, K.; Sugiyama, A.*; Washiyama, K.*; Yamatsugu, K.*; Kanai, M.*

“In Vivo-Stable Bis-Iminobiotin for Targeted Radionuclide Delivery with the Mutant Streptavidin”

Bioorg. Med. Chem. Lett. 2024, 108, 129803.

DOI: 10.1016/j.bmcl.2024.129803


Shimazoe, K.*; Donghwan, K.; Mineo, T.; Sato, T.; Ohta, S.; Tatsumi, T.; Sugiyama, A.; Yamatsugu, K.; Nomura, S.; Terabayashi, R.; Tomita, H.; Sonoda, T.; Shigekawa, Y.; Yokokita, T.; Uenomachi, M.

“pH dependence of perturbed angular correlation in DOTA chelated 111In measured with ring-shape gamma-ray detectors”

Interactions 2024, 245, 22.

DOI: 10.1007/s10751-024-01864-7


Fujimura, A.; Ishida, H.; Nozaki, T.; Terada, S.; Azumaya, Y.; Ishiguro, T.; Kamimura, Y. R.; Kujirai, T.; Kurumizaka, H.; Kono, H.; Yamatsugu, K.; Kawashima, S. A.*; Kanai, M.*

“Designer Adaptor Proteins for Functional Conversion of Peptides to Small-Molecule Ligands toward In-Cell Catalytic Protein Modification”

ACS Cent. Sci. 2023, 9, 11, 2115-2128.

DOI: 10.1021/acscentsci.3c00930


Sakata, J.; Tatsumi, T.; Sugiyama, A.*; Shimizu, A.; Inagaki, Y.; Katoh, H.; Yamashita, T.; Takahashi, K.; Aki, S.; Kaneko, Y.; Kawamura, T.; Miura, M.; Ishii, M.; Osawa, T.; Tanaka, T.; Ishikawa, S.; Tsukagoshi, M.; Chansler, M.; Kodama, T.; Kanai, M.; Tokuyama, H.*; Yamatsugu, K.*

“Antibody-mimetic drug conjugate with efficient internalization activity using anti-HER2 VHH and duocarmycin”

Protein Expr. Purif. 2023, 106375.

DOI: 10.1016/j.pep.2023.106375


Habazaki, M.; Mizumoto, S.; Kajino, H.; Kujirai, T.; Kurumizaka, H.; Kawashima, S. A.*; Yamatsugu, K.*; Kanai, M.*

“A chemical catalyst enabling histone acylation with endogenous acyl-CoA”

Nat. Commun. 2023, 14, 5790.



Mauro, E.; Lapaillerie, D.; Tumiotto, C.; Charlier, C.; Martins, F.; Sousa, S.; Métifiot, M.; Weigel, P.; Yamatsugu, K.; Kanai, M.; Munier-Lehmann, H.; Richetta, C.; Maisch, M.; Dutrieux, J.; Batisse, J.; Ruff, M.; Delelis, O.; Lesbats, P.; Parissi, V.*

“Modulation of the functional interfaces between retroviral intasomes and the human nucleosome”

mBio 2023, 14, 4, e01083-23.



Yamatsugu, K.*; Kanai, M.*

“Catalytic Approaches to Chemo- and Site-Selective Transformation of Carbohydrates”

Chem. Rev. 2023, 123, 10, 6793-6838.

DOI: 10.1021/acs.chemrev.2c00892


Kaneko, Y.; Yamatsugu, K.; Yamashita, T.; Takahashi, K.; Tanaka, T.; Aki, S.; Tatsumi, T.; Kawamura, T.; Miura, M.; Ishii, M.; Ohkubo, K.; Osawa, T.; Kodama, T.; Ishikawa, S.; Tsukagoshi, M.; Chansler, M.; Sugiyama, A.*; Kanai, M.*; Katoh, H.*

“Pathological complete remission of relapsed tumor by photo-activating antibody–mimetic drug conjugate treatment”

Cancer Sci. 2022, 113, 4350-4362.

DOI: 10.1111/cas.15565


Yamatsugu, K.; Katoh, H.; Yamashita, T.; Takahashi, K.; Sho, A.; Tatsumi, T.; Kaneko, Y.; Kawamura, T.; Miura, M.; Ishii, M.; Ohkubo, K.; Osawa, T.; Kodama, T.; Ishikawa, S.; Kanai, M.; Sugiyama, A.*

“Antibody mimetic drug conjugate manufactured by high-yield Escherichia coli expression and non-covalent binding system”

Protein Expr. Purif. 2022, 192, 106043.

DOI: 10.1016/j.pep.2021.106043


Adamson, C.; Kajino, H.; Kawashima, S. A.*; Yamatsugu, K.*; Kanai, M.*

“Live-Cell Protein Modification by Boronate-Assisted Hydroxamic Acid Catalysis”

J. Am. Chem. Soc. 2021, 143, 14976-14980.

DOI: 10.1021/jacs.1c07060


Fujiyoshi, K.; Kawashima, S. A.; Yamatsugu, K.*; Kanai, M.*

“A Single-Step Asymmetric Phosphodiester Synthesis from Alcohols with Phosphoenolpyruvate Phosphodiester”

Synlett 2021, 32, 1135-1140.

DOI: 10.1055/a-1509-9275


Takahashi, K.; Sugiyama, A.; Ohkubo, K.; Tatsumi, T.; Kodama, T.; Yamatsugu, K.*; Kanai, M.*

“Axially-substituted silicon phthalocyanine payloads for antibody-drug conjugates”

Synlett 2021, 32, 1098-1103.

DOI: 10.1055/a-1503-6425


Fujiwara, Y.; Yamanashi, Y.; Fujimura, A.; Sato, Y.; Kujirai, T.; Kurumizaka, H.; Kimura, H.; Yamatsugu, K.*; Kawashima, S. A.*; Kanai, M.*

“Live-Cell Epigenome Manipulation by Synthetic Histone Acetylation Catalyst System”

Proc. Natl. Acad. Sci. USA 2021, 118, 4, e2019554118.

DOI: 10.1073/pnas.2019554118


Fujiyoshi, K.; Yamatsugu, K.; Kanai, M.


Encyclopedia of Reagents for Organic Synthesis rn02368.


Kajino, H.; Nagatani, T.; Oi, M.; Kujirai, T.; Kurumizaka, H.; Nishiyama, A.; Nakanishi, M.; Yamatsugu, K.*; Kawashima, S. A.*; Kanai, M.*

“Synthetic hyperacetylation of nucleosomal histones”

RSC Chem. Biol. 2020, 1, 2, 56-59.

DOI: 10.1039/D0CB00029A


Ohkawachi, K.; Kobayashi, D.; Morimoto, K.; Shigenaga, A.; Denda, M.; Yamatsugu, K.; Kanai, M.; Otaka, A.*

“Sulfanylmethyldimethylaminopyridine as a Useful Thiol Additive for Ligation Chemistry in Peptide/Protein Synthesis”

Org. Lett. 2020, 22, 14, 5289-5293.

DOI: 10.1021/acs.orglett.0c01383


Mizumoto, S.; Xi, S.; Fujiwara, Y.; Kawashima, S. A.; Yamatsugu, K.*; Kanai, M.*

“Hydroxamic Acid-Piperidine Conjugate is an Activated Catalyst for Lysine Acetylation under Physiological Conditions”

Chem. Asian J. 2020, 15. 6, 833-839.

DOI: 10.1002/asia.201901737


Domon, K.; Puripat, M.; Fujiyoshi, K.; Hatanaka, M.; Kawashima, S. A.; Yamatsugu, K.*; Kanai, M.*

“Catalytic Chemoselective O-Phosphorylation of Alcohols”

ACS Cent. Sci. 2020, 6, 2, 283-292.

DOI: 10.1021/acscentsci.9b01272


Ito, K.; Tatsumi, T.; Takahashi, K.; Shimizu, Y.; Yamatsugu, K.; Kanai, M.*

“A Stable and Cleavable O-Linked Spacer for Drug Delivery Systems”

Chem. Pharm. Bull. 2020, 68, 3, 212-215.

DOI: 10.1248/cpb.c19-00376


Sugiyama, A; Kawamura, T.; Tanaka, T.; Doi, H.; Yamashita, T.; Shinoda, K.; Fujitani, H.; Yamatsugu, K.; Shimizu, Y.; Tatsumi, T.; Takahashi, K.; Kanai, M.; Mizohata, E.; Kawato, T.; Doi, T.; Inoue, T.; Kodama, T.*

“Cupid and Psyche system for the diagnosis and treatment of advanced cancer”

Proc. Jpn. Acad. Ser. B 2019, 95, 10, 602-611.

DOI: 10.2183/pjab.95.041


Hamajima, W.; Fujimura, A.; Fujiwara, Y.; Yamatsugu, K.*; Kawashima, S. A.*; Kanai, M.*

“Site-selective synthetic acylation of a target protein in living cells promoted by a chemical catalyst/donor system”

ACS Chem. Biol. 2019, 14, 6, 1102-1109.

DOI: 10.1021/acschembio.9b00102


Yamatsugu, K.*

“How My Experiences in Asymmetric Catalysis and Glycobiology Led to My Current Research in Synthetic Post-translational Modifications by Chemical Catalysts”

Yakugaku Zasshi 2019, 139, 2, 187-198.

DOI: 10.1248/yakushi.18-00169-1


Yamatsugu, K.*; Furuta, M.; Xi, S.; Amamoto, Y.; Liu, J.; Kawashima, S. A.; Kanai, M.*

“Kinetic analyses and structure-activity relationship studies of synthetic lysine acetylation catalysts”

Bioorg. Med. Chem. 2018, 26, 19, 5359-5367.

DOI: 10.1016/j.bmc.2018.07.009


Yamatsugu, K.*; Kawashima, S. A.*; Kanai, M.*

“Leading approaches in synthetic epigenetics for novel therapeutic strategies”

Curr. Opin. Chem. Biol. 2018, 46, 10-17.

DOI: 10.1016/j.cbpa.2018.03.011


Tanabe, K.; Liu, J.; Kato, D.; Kurumizaka, H.; Yamatsugu, K.; Kanai, M.*; Kawashima, S. A.*

“LC-MS/MS-based quantitative study of the acyl group- and site-selectivity of human sirtuins to acylated nucleosomes”

Sci. Rep. 2018, 8, 2656.

DOI: 10.1038/s41598-018-21060-2


Ishiguro, T.; Amamoto, Y.; Tanabe, K.; Liu, J.; Kajino, H.; Fujimura, A.; Aoi, Y.; Osakabe, A.; Horikoshi, N.; Kurumizaka, H.; Yamatsugu, K.; Kawashima, S. A.*; Kanai, M.*

“Synthetic Chromatin Acylation by an Artificial Catalyst System”

Chem 2017, 2, 6, 840-859.

DOI: 10.1016/j.chempr.2017.04.002


Amamoto, Y.; Aoi, Y.; Nagashima, N.; Suto, H.; Yoshidome, D.; Arimura, Y.; Osakabe, A.; Kato, D.; Kurumizaka, H.; Kawashima, S. A.; Yamatsugu, K.*; Kanai, M.*

“Synthetic Posttranslational Modifications: Chemical Catalyst-Driven Regioselective Histone Acylation of Native Chromatin”

J. Am. Chem. Soc. 2017, 139, 22, 7568-7576.

DOI: 10.1021/jacs.7b02138


Yamatsugu, K.; Splain, R. A; Kiessling, L. L.*

“Fidelity and Promiscuity of a Mycobacterial Glycosyltransferase”

J. Am. Chem. Soc. 2016, 138, 29, 9205-9211.

DOI: 10.1021/jacs.6b04481


Takemoto, A.*; Kawashima, S. A.; Li, J.-J.; Jeffery, L.; Yamatsugu, K.; Elemento, O.; Nurse, P.

“Nuclear envelope expansion is crucial for proper chromosomal segregation during a closed mitosis”

J. Cell Sci. 2016, 129, 1250-1259.

DOI: 10.1021/jacs.6b04481


Kimura, Y.; Saito, N.; Hanada, K.; Liu, J.; Okabe, T.; Kawashima, S. A.*; Yamatsugu, K.*; Kanai, M.*

“Supramolecular Ligands for Histone Tails by Employing a Multivalent Display of Trisulfonated Calix[4]arenes”

ChemBioChem 2015, 16, 18, 2599-2604.

DOI: 10.1002/cbic.201500448


Alagiri, K.; Furutachi, M.; Yamatsugu, K.; Kumagai, N.; Watanabe, T.*; Shibasaki, M.*

“Two Approaches toward the Formal Total Synthesis of Oseltamivir Phosphate (Tamiflu): Catalytic Enantioselective Three-Component Reaction Strategy and l-Glutamic Acid Strategy”

J. Org. Chem. 2013, 78, 8, 4019-4026.

DOI: 10.1021/jo400360j


Komatsu, H.; Shindo, Y.; Kawashima, S. A.; Yamatsugu, K.; Oka K.; Kanai, M.*

“Intracellular activation of acetyl-CoA by an artificial reaction promoter and its fluorescent detection”

Chem. Commun. 2013, 49, 28, 2876-2878.

DOI: 10.1039/C3CC40616D


Shibasaki, M.*; Kanai, M.; Yamatsugu, K.

“Recent Development in Synthetic Strategies for Oseltamivir Phosphate”

Israel J. Chem. 2011, 51, 3-4, 316-328.

DOI: 10.1002/ijch.201100001


Kimura, Y.; Yamatsugu, K.; Kanai, M.*; Echigo, N.; Kuzuhara, T.; Shibasaki, M.*

“Design and Synthesis of Resin-Conjugated Tamiflu Analogs for Affinity Chromatography”

Bull. Korean. Chem. Soc. 2010, 31, 3, 588-594.

DOI: 10.5012/bkcs.2010.31.03.588


Yamatsugu, K.; Kanai, M.*; Shibasaki, M.*

“An alternative synthesis of Tamiflu: a synthetic challenge and the identification of a ruthenium-catalyzed dihydroxylation route”

Tetrahedron 2009, 65, 31, 6017-6024.

DOI: 10.1016/j.tet.2009.05.077


Tomita, D.; Yamatsugu, K.; Kanai, M.*; Shibasaki, M.*

“Enantioselective synthesis of SM-130686 based on the development of asymmetric Cu(I)F catalysis to access 2-oxindoles containing a tetrasubstituted carbon”

J. Am. Chem. Soc. 2009, 131, 20, 6946-6948.

DOI: 10.1021/ja901995a


Kimura, Y.; Yamatsugu, K.; Kanai, M.*; Echigo, N.; Kuzuhara, T.; Shibasaki, M.*

“Design and synthesis of immobilized Tamiflu analog on resin for affinity chromatography” 

Tetrahedron Lett. 2009, 50, 26, 3205-3208.

DOI: 10.1016/j.tetlet.2009.01.142


Yamatsugu, K.; Yin, L.; Kamijo, S.; Kimura, Y.; Kanai, M.*; Shibasaki, M.*

“A synthesis of Tamiflu based on a barium-catalyzed Diels-Alder-type reaction”

Angew. Chem. Int. Ed. 2009, 48, 6, 1070-1076.

DOI: 10.1002/anie.200804777


Ose, A.; Ito, M.; Kusuhara, H.; Yamatsugu, K.; Kanai, M.; Shibasaki, M.; Hosokawa, M.;  Schuetz, J. D.; Sugiyama, Y.*

“Limited brain distribution of Ro 64-0802, a pharmacologically active form of oseltamivir, by active efflux across the blood–brain barrier mediated by organic anion transporter 3 (Oat3/Slc22a8) and multidrug resistance-associated protein 4 (Mrp4/Abcc4)”

Drug. Metab. Dispos. 2009, 37, 2, 315-321.

DOI: 10.1124/dmd.108.024018


Usami, A.; Sasaki, T.; Satoh, N.; Akiba, T.; Yokosima, S.; Fukuyama, T.; Yamatsugu, K., Kanai, M.; Shibasaki, M.; Matsuki, N.; Ikegaya, Y.*

“Oseltamivir enhances hippocampal network synchronization”

J. Pharmacol. Sci. 2008, 106, 4, 659-662.

DOI: 10.1254/jphs.SC0070467


Ose, A.; Kusuhara, H.; Yamatsugu, K.; Kanai, M.; Shibasaki, M.; Fujita, T.; Yamamoto, A.; Sugiyama, Y.*

“P-glycoprotein restricts the penetration of oseltamivir across the blood-brain barrier”

Drug. Metab. Dispos. 2008, 36, 2, 427-434.

DOI: 10.1124/dmd.107.018556


Ishii, K.; Hamamoto, H.; Sasaki, T.; Ikegaya, Y.; Yamatsugu, K.; Kanai, M.; Shibasaki, M.; Sekimizu, K.*

“Pharmacologic action of oseltamivir on the nervous system”

Drug Discoveries & Therapeutics 2008, 2, 1, 24-34.


Morita, M.; Sone, T.; Yamatsugu, K.; Sohtome, Y.; Matsunaga, S.; Kanai, M.*; Yasuyosi, W.; Shibasaki, M.*

“A method for the synthesis of an oseltamivir PET tracer”

Bioorg. Med. Chem. Lett. 2008, 18, 2, 600-602.

DOI: 10.1016/j.bmcl.2007.11.079


Yamatsugu, K.; Kamijo, S.; Suto, Y.; Kanai, M.*; Shibasaki, M.*

“A concise synthesis of Tamiflu: third generation route via the Diels-Alder reaction and the Curtius rearrangement”

Tetrahedron Lett. 2007, 48, 8, 1403-1406.

DOI: 10.1016/j.tetlet.2006.12.093


Yamatsugu, K.; Motoki, R.; Kanai, M.*; Shibasaki, M.*

“Identification of potent, selective protein kinase C inhibitors based on a phorbol skeleton”

Chem. Asian. J. 2006, 1, 3, 314-321.

DOI: 10.1002/asia.200600185


Kuramochi, A.; Usuda, H.; Yamatsugu, K.; Kanai, M.*; Shibasaki, M.*

“Total synthesis of (+/−)-garsubellin A”

J. Am. Chem. Soc. 2005, 127, 41, 14200-14201.

DOI: 10.1021/ja055301t


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