J-GLOBAL         Last updated: Oct 12, 2019 at 14:27
Gifu University
Faculty of Engineering

Research Areas


Academic & Professional Experience

Apr 2013
Mar 2014
Department of Chemistry and Chemical Biology, Harvard University
Jun 2011
Mar 2013
Administrative Staff, Nagoya Industrial Science Research Institute

Published Papers

Sayuri L. Higashi, Aya Shibata, Yoshiaki Kitamura, Koichiro M. Hirosawa, Kenichi G. N. Suzuki, Kazunori Matsuura, Masato Ikeda
Chemistry - A European Journal   25(51) 11955-11962   Jul 2019   [Refereed]
Takuto Nogimori, Kyutatsu Nishiura, Sho Kawashima, Takahiro Nagai,Yuka Oishi, Nao Hosoda, Hiroaki Imataka, Yoshiaki Kitamura, Yukio Kitade, Shinichi Hoshino
Nucleic Acids Research   47(1) 432-449   Jan 2019   [Refereed]
Practical and reliable synthesis of 2′,3′,5′,5′′-tetradeuterated uridine derivatives
Noriko Miyamoto, Hiroki Ohno, Yoshiaki Kitamura, Kwihwan Park, Yoshinari Sawama, Hironao Sajiki, Yukio Kitade
Nucleosides, Nucleotides and Nucleic Acids      2019   [Refereed]
Masahide Hayakawa, Ayaka Ohsawa, Kumi Takeda, Ryo Torii, Yoshiaki Kitamura, Hiroshi Katagiri, Masato Ikeda
Organic & Biomolecular Chemistry   16(44) 8505-8512   Nov 2018   [Refereed]
Yoshiaki Kitamura, Shuichi Moribe, Yukio Kitade
Bioorganic and Medicinal Chemistry Letters   28(19) 3174-3176   Oct 2018   [Refereed]
Yuki Nagaya, Yoshiaki Kitamura, Aya Shibata, Masato Ikeda, Yukihiro Akao, Yukio Kitade
Bioorganic and Medicinal Chemistry Letters   27(24) 5454-5456   Oct 2017   [Refereed]
Yoshiaki Kitamura, Ryo Asakura, Koki Terazawa, Aya Shibata, Masato Ikeda, Yukio Kitade
Bioorganic and Medicinal Chemistry Letters   27(12) 2655-2658   Apr 2017   [Refereed]
Tomoya Tsuzuki, Hiroshi Katagiri, Yoshiaki Kitamura, Yukio Kitade, Masato Ikeda
Tetrahedron   72(43) 6886-6891   Oct 2016   [Refereed]
Yoshiaki Kitamura, Seiya Kito, Remi Nakashima, Katsuki Tanaka, Kumi Nagaoka, Yukio Kitade
Bioorganic&Medicinal Chemistry   24(16) 3870-3874   Aug 2016   [Refereed]
Yoshiaki Kitamura, Ryuto Sakamoto, Takao Shiraishi, Haruka Oguri, Satoshi Ohno, Yukio Kitade
Tetrahedron   72(27-28) 4016-4021   Jul 2016   [Refereed]
Ian B. Seiple, Ziyang Zhang, Pavol Jakubec, Audrey Langlois-Mercier, Peter M. Wright, Daniel T. Hog, Kazuo Yabu, Senkara Rao Allu, Takehiro Fukuzaki, Peter N. Carlsen, Yoshiaki Kitamura, Xiang Zhou, Matthew L. Condakes, Filip T. Szczypiński, William D. Green, Andrew G. Myers
Nature   533(7603) 338-345   May 2016   [Refereed]
Yuki Nagaya, Yoshiaki Kitamura, Remi Nakashima, Aya Shibata, Masato Ikeda, Yukio Kitade
Nucleosides, nucleotides & nucleic acids   35(2) 64-75   Jan 2016   [Refereed]
Yoshiaki Kitamura(Gifu University)
136 1491-1499   2016
Ziyang Zhang, Yoshiaki Kitamura, Andrew G. Myers
Synthesis   47(18) 2709-2712   Sep 2015   [Refereed]
Masato Ikeda, Keito Horio, Tomoya Tsuzuki, Ryo Torii, Aya Shibata, Yoshiaki Kitamura, Hiroshi Katagiri, Yukio Kitade
Tetrahedron Letters   56(48) 6726-6729   Aug 2015   [Refereed]
© 2015 Elsevier Ltd. Herein, we describe a new methodology for the solid phase submonomer synthesis (SPSS) of arylopeptoids using a reductive amination reaction as the key step instead of a nucleophilic substitution reaction, which is generally us...
Mahmoud Kandeel, Abdullah Al-Taher, Remi Nakashima, Tomoya Sakaguchi, Ali Kandeel, Yuki Nagaya, Yoshiaki Kitamura, Yukio Kitade
PLoS ONE   9(5) 94538   May 2014   [Refereed]
Gene silencing and RNA interference are major cellular processes that control gene expression via the cleavage of target mRNA. Eukaryotic translation initiation factor 2C2 (EIF2C2, Argonaute protein 2, Ago2) is considered to be the major player of...
Qin Ren, Kana Tsunaba, Yoshiaki Kitamura, Remi Nakashima, Aya Shibada, Masato Ikeda, Yukio Kitade
Bioorganic and Medicinal Chemistry Letters   24(6) 1519-1522   Mar 2014   [Refereed]
Positron emission tomography (PET) is a highly sensitive quantitative imaging technique for studying molecular pathways and interactions in vivo. This imaging technique plays a key role in drug discovery, pharmacokinetics, pharmacodynamics, and as...
Yoshiaki Kitamura, Yoshihito Ueno, Yukio Kitade
Current Protocols in Nucleic Acid Chemistry   4(59) 1-15   Jan 2014   [Refereed]
© 2014 by John Wiley & Sons, Inc. Conversion of dimethyl 5-aminoisophthalate into the iodoarene via the corresponding diazonium intermediate, followed by Sonogashira coupling with trimethylsilylacetylene afford the alkynylarene, which is reduced w...
Yoshiaki Kitamura, Kazumi Taniguchi, Tomohiro Maegawa, Yasunari Monguchi, Yukio Kitade, Hironao Sajiki
Heterocycles   88(1) 233-243   Jan 2014   [Refereed]
We have developed an environmentally friendly and highly efficient solvent-free Cu(I)-catalyzed azide-alkyne cycloaddition (CuAAC) reaction using a polymer-supported copper catalyst (Cu/HP20). Substrates poorly soluble in common organic solvents a...
Yoshihiro Noguchi, Yuri Yasuda, Makoto Tashiro, Tadashi Kataoka, Yoshiaki Kitamura, Mahmoud Kandeel, Yukio Kitade
Parasitology International   62(4) 368-371   Aug 2013   [Refereed]
Plasmodium falciparum thymidylate kinase (PfTMK) is a promising antimalarial target due to its unique substrate specificity. Recently, we reported that 2',3'-dideoxycarbocyclic thymidine showed moderate inhibitory activity and reported the related...
Yoshiaki Kitamura, Yuki Masegi, Shunsuke Ogawa, Remi Nakashima, Yukihiro Akao, Yoshihito Ueno, Yukio Kitade
Bioorganic and Medicinal Chemistry   21(15) 4494-4501   Aug 2013   [Refereed]
We have developed chemically modified siRNAs and miRNAs bearing urea/thiourea-bridged aromatic compounds at their 3′-end for RNAi therapy. Chemically modified RNAs possessing urea/thiourea-bridged aromatic compounds instead of naturally occurring ...
Xiong Luo, Takahiro Sugiura, Remi Nakashima, Yoshiaki Kitamura, Yukio Kitade
Bioorganic and Medicinal Chemistry Letters   23(14) 4157-4161   Jul 2013   [Refereed]
Short interfering RNA (siRNA) has been proven to be an utilizable tool for post-transcriptional gene silencing research. In this study, we designed and synthesized two glucosamine analogues and tried to modify the siRNA using these two glucosamine...
Mahmoud Kandeel, Remi Nakashima, Yoshiaki Kitamura, Mohamed Balaha, Magdy Abdelaziz, Yukio Kitade
Journal of Thermal Analysis and Calorimetry   112(2) 945-952   May 2013   [Refereed]
Among the biological parameters of chemotherapeutics, serum albumin binding is a critical factor in determining drug distribution and bioavailability. In this study, the binding properties as well as the interaction of ampicillin and streptomycin ...
Yasunari Monguchi, Kei Nozaki, Toshihide Maejima, Yutaka Shimoda, Yoshinari Sawama, Yoshiaki Kitamura, Yukio Kitade, Hironao Sajiki
Green Chemistry   15(2) 490-495   Jan 2013   [Refereed]
Copper catalysts supported on chelate resins bearing iminodiacetate moieties (DIAION CR11) or polyamine moieties (DIAION CR20) as chelating functional groups (12% Cu/CR11 and 7% Cu/CR20, respectively) were developed. 12% Cu/CR11 effectively cataly...
Yoshiaki Kitamura, Kana Edayoshi, Yukio Kitade
Tetrahedron Letters   53(51) 6987-6989   Dec 2012   [Refereed]
We have developed an efficient stereoselective synthesis of 1-deoxy-1-ethynyl-β-d-ribofuranose (RE), via the β-selective cyanation of the anomeric position of 1-O-acetyl-2,3,5-tri-O- benzoyl-β-d-ribofuranose. Under conditions for copper(I)-catalyz...
Aya Kato, Yuri Yasuda, Yoshiaki Kitamura, Mahmoud Kandeel, Yukio Kitade
Parasitology International   61(3) 501-503   Sep 2012   [Refereed]
During the course of our research into new anti-malaria drugs, Plasmodium falciparum thymidylate kinase (PfTMK) has emerged as an important drug target because of its unique substrate specificity. Compared with human thymidylate kinase (HsTMK), Pf...
Waleed Osman, Satoshi Endo, Kentaro Oh-hashi, Yoshiaki Kitamura, Yukio Kitade
Biological and Pharmaceutical Bulletin   35(7) 1191-1196   Jul 2012   [Refereed]
Asymmetrical diadenosine 5′,5″-P1,P 4-tetraphosphate hydrolase (EC from human malaria parasite Plasmodium falciparum was expressed in Escherichia coli, purified to homogeneity, and characterized for the first time as a biological target ...
Kazumi Taniho, Remi Nakashima, Mahmoud Kandeel, Yoshiaki Kitamura, Yukio Kitade
Bioorganic and Medicinal Chemistry Letters   22(7) 2518-2521   Apr 2012   [Refereed]
To elucidate the role of the sugar moiety in the two natural nucleotides of the 3′-overhang region of small interfering RNA (siRNA), we synthesized siRNAs that incorporated two abasic nucleosides, 1-deoxy-d-ribofuranose (R H). We improved the meth...
Kinji Furukawa, Mayumi Hattori, Tokimitsu Ohki, Yoshiaki Kitamura, Yukio Kitade, Yoshihito Ueno
Bioorganic and Medicinal Chemistry   20(1) 16-24   Jan 2012   [Refereed]
The development of a reliable and simple method for detecting single nucleotide polymorphisms (SNPs), common genetic variations in the human genome, is currently an important research area because SNPs are important for identifying disease-causing...
Takao Shiraishi, Yoshiaki Kitamura, Yoshihito Ueno, Yukio Kitade
Chemical Communications   47(9) 2691-2693   Mar 2011   [Refereed]
We synthesised aryl acetylene derivatives as versatile probes for labelling of oligonucleotides. RNA oligomers bearing an aryl acetylene molecule rapidly reacted with benzylazide derivatives under ligand-free click reaction conditions. © 2011 The ...
Yoshiaki Kitamura, Satoko Sako, Azusa Tsutsui, Yasunari Monguchi, Tomohiro Maegawa, Yukio Kitade, Hironao Sajiki
Advanced Synthesis and Catalysis   352(4) 718-730   Mar 2010   [Refereed]
A ligand-free and heterogeneous palladium on carbon (Pd/C)-catalyzed hetero-SuzukiMiyaura coupling reaction has been developed. The protocol enables the construction of both heterocyclic-alicyclic and heterocyclic-heterocyclic biaryl derivatives i...
Kumi Nagaoka, Yoshiaki Kitamura, Yoshihito Ueno, Yukio Kitade
Bioorganic and Medicinal Chemistry Letters   20(3) 1186-1188   Feb 2010   [Refereed]
Human ribonuclease L (RNase L), an interferon-induced endoribonuclease, becomes enzymatically active after binding to 2-5A. The 5′-phosphoryl group of 2-5A is reportedly necessary for the conformational change leading to RNase L activation. Howeve...
Hetero-Suzuki-Miyaura Cross-Coupling Using Palladium on Carbon
Kitamura Yoshiaki, Sako Satoko, Tsutsui Azusa, Monguchi Yasunari, Maegawa Tomohiro, Kitade Yukio, Sajiki Hironao
7 844-844   2010
Mahmoud Kandeel, Aya Kato, Yoshiaki Kitamura, Yukio Kitade
Nucleic acids symposium series (2004)   283-284   Dec 2009
Here we highlight the unusual substrate specificity of Plasmodium falciparum thymidylate kinase (PfTMK) and the validity of the enzyme as a new drug target. Furthermore, we predict that the Anaplasma marginale enzyme has attractive domain constitu...
Mahmoud Kandeel, Yoshiaki Kitamura, Yukio Kitade
Nucleic acids symposium series (2004)   39-40   Dec 2009
In Plasmodium falciparum, deoxyguanylate was found to be a substrate for several DNA metabolizing enzymes. Guanylate kinase utilizes dGMP with very low specificity, which is estimated to be the lowest among well-known prokaryotic and eukaryotic en...
Yoshihito Ueno, Shinji Komatsuzaki, Keiji Takasu, Yoshiaki Kitamura, Yukio Kitade
Nucleic acids symposium series (2004)   27-28   Dec 2009
We describe the synthesis and properties of oligonucleotides (ONs) containing biaryl units, which are composed of a bis(hydroxymethyl)benzene residue and a naphthalene or pyrene moiety. We found that by introducing the biaryl units into the ONs, t...
Kumi Nagaoka, Seiya Kito, Yoshiaki Kitamura, Yoshihito Ueno, Yukio Kitade
Nucleic acids symposium series (2004)   123-124   Dec 2009
The 2',5'-oligoadenylate (2-5A) system is an interferon (IFN)-regulated RNA decay pathway that provides innate immunity against viral infections. The biological action of the 2-5A system is mediated by RNase L, an endoribonuclease that becomes enz...
Yoshihito Ueno, Shinji Komatsuzaki, Keiji Takasu, Satoru Kawai, Yoshiaki Kitamura, Yukio Kitade
European Journal of Organic Chemistry   (28) 4763-4769   Oct 2009   [Refereed]
We describe the synthesis and properties of oligonucleotides (ONs) containing biaryl units, which are composed of a bis(hydroxymethyl)benzene residue and a naphthalene or pyrene moiety. We found that by introducing the biaryl units into the ONs, t...
Yoshihito Ueno, Akihiro Kawamura, Keiji Takasu, Shinji Komatsuzaki, Takumi Kato, Satoru Kuboe, Yoshiaki Kitamura, Yukio Kitade
Organic and Biomolecular Chemistry   7(13) 2761-2769   Jun 2009   [Refereed]
This paper describes the synthesis and properties of a novel molecular beacon (MB) containing a benzene-phosphate backbone at its stem moiety. The fluorescence intensity of MBs was found to stabilize by the introduction of the benzene-phosphate ba...
Yoshihito Ueno, Kayo Yoshikawa, Yoshiaki Kitamura, Yukio Kitade
Bioorganic and Medicinal Chemistry Letters   19(3) 875-877   Feb 2009   [Refereed]
Unintended (off-target) transcript silencing is a critical problem associated with RNA interference (RNAi)-based therapeutic applications. This paper shows that the incorporation of appropriate alkyl linkers at the center of the sense strands can ...
Mahmoud Kandeel, Takayuki Ando, Yoshiaki Kitamura, Magdy Abdelaziz, Yukio Kitade
Parasitology   136(1) 11-25   Jan 2009   [Refereed]
Plasmodium falciparum thymidylate kinase (PfTMK) can tolerate a range of substrates, which distinguishes it from other thymidylate kinases. The enzyme not only phosphorylates TMP and dUMP but can also tolerate bulkier purines, namely,dGMP, GMP, an...
Mahmoud Kandeel, Takayuki Ando, Yoshiaki Kitamura, Magdy Abdel-Aziz, Yukio Kitade
Heterocycles   77(1) 521-532   Jan 2009   [Refereed]
A polymer-supported copper catalyst (Cu/HP20) is easily prepared in water and effectively catalyzed the Huisgen cycloaddition between azides and terminal alkynes. © 2009 The Japan Institute of Heterocyclic Chemistry All rights reserved.
Yoshihito Ueno, Miki Hirai, Kayo Yoshikawa, Yoshiaki Kitamura, Yoko Hirata, Yoko Hirata, Kazutoshi Kiuchi, Yukio Kitade
Tetrahedron   64(49) 11328-11334   Dec 2008   [Refereed]
Short interfering RNAs (siRNAs) containing P3′→N5′ phosphoramidate linkages were successfully synthesized by introducing 2′-deoxy-2′-fluororibonucleoside and 5′-amino-2′,5′-dideoxy-2′α-fluororibonucleoside in succession. It was found that the intr...
Yoshihito Ueno, Takumi Inoue, Mahito Yoshida, Kayo Yoshikawa, Aya Shibata, Yoshiaki Kitamura, Yukio Kitade
Bioorganic and Medicinal Chemistry Letters   18(19) 5194-5196   Oct 2008   [Refereed]
We describe the synthesis and silencing activities of siRNA possessing N 1-[3,5-bis(hydroxymethyl)phenyl]thymine (b t) in their 3′-overhang regions. We found that an siRNA possessing b t in the 3′-overhang region was more effective than an siRNA w...
Monguchi Yasunari(Gifu Pharmaceutical University ),Kitamura Yoshiaki(Gifu University),Maegawa Tomohiro(Gifu Pharmaceutical University ),Sajiki Hironao(Gifu Pharmaceutical University )
53 256-261   2008
Yoshiaki Kitamura, Satoko Sako, Takahiro Udzu, Azusa Tsutsui, Tomohiro Maegawa, Yasunari Monguchi, Hironao Sajiki
Chemical Communications   5069-5071   Dec 2007   [Refereed]
We have developed a mild and efficient protocol for the ligand-free and heterogeneous Pd/C-catalyzed hetero Suzuki-Miyaura coupling reaction that allows for the synthesis of both heteroaryl-aryl and heteroaryl-heteroaryl derivatives in good to exc...
Yoshiaki Kitamura, Ai Sakurai, Takahiro Udzu, Tomohiro Maegawa, Yasunari Monguchi, Hironao Sajiki
Tetrahedron   63(43) 10596-10602   Oct 2007   [Refereed]
Heterogeneous Pd/C-catalyzed Suzuki-Miyaura cross-coupling reaction of aryl boronic esters with aryl bromides was successfully carried out in aqueous media at room temperature without the use of a ligand such as phosphine derivatives. © 2007 Elsev...
Tomohiro Maegawa, Yoshiaki Kitamura, Satoko Sako, Takahiro Udzu, Ai Sakurai, Asami Tanaka, Yusuke Kobayashi, Koichi Endo, Utpal Bora, Takanori Kurita, Atsushi Kozaki, Yasunari Monguchi, Hironao Sajiki
Chemistry - A European Journal   13(20) 5937-5943   Aug 2007   [Refereed]
A mild and efficient ligand-free Suzuki-Miyaura coupling reaction catalyzed by heterogeneous Pd/C was developed. Aryl bromides and triflates undergo the cross-coupling with aryl boronic acids in excellent yields without the presence of any additiv...
Yoshiaki Kitamura, Asami Tanaka, Mutsumi Sato, Keiji Oono, Takashi Ikawa, Tomohiro Maegawa, Yasunari Monguchi, Hironao Sajiki
Synthetic Communications   37(22) 4381-4388   Jan 2007   [Refereed]
A practical and efficient preparation method of palladium-fibroin (Pd/Fib),
silk-fibroin-supported Pd(0) by means of sonication, has been developed. The Pd/Fib
catalyst could be prepared within 12 h at room temperature starting from commercial
Hironao Sajiki, Takanori Kurita, Atsushi Kozaki, Guolin Zhang, Guolin Zhang, Yoshiaki Kitamura, Tomohiro Maegawa, Kosaku Hirota
Journal of Chemical Research   344   May 2005

Books etc

医薬品モダリティの 特許戦略と技術開発動向
May 2019   
Kitamura Yoshiaki(Gifu Pharmaceutical University),Sajiki Hironao(Gifu Pharmaceutical University) (Part:Contributor)
Jul 2007   

Conference Activities & Talks

川出 桃歌
Mar 2017   
柴田 綾
Mar 2017   
長屋 優貴
Mar 2017   
川出 桃歌
Nov 2016   
岩井 千織
Oct 2016   
森部 修一
Oct 2016   
朝倉 領
Oct 2016   
Synthesis of chemically modified siRNAs bearing high affinity molecules for human Argonaute 2 PAZ domain and their biological properties
喜多村 徳昭
Sep 2016   
東 小百合
Jul 2016   
伊藤 卓真
May 2016   
柴田 綾
Mar 2015   
長屋 優貴
Jul 2014   
抗マラリア薬開発を指向したPlasmodium falciparum Uracil-DNA glycosylaseの性状解析
小林 昌平
Nov 2012   
Stereoselective synthesis of 1-deoxy-1-ethynyl-β-D-ribofuranose and its applications
枝吉 佳奈
Nov 2012   
枝吉 佳奈
Jul 2012   
Synthesis of oligonucleotides possessing abasic nucleosides and their biological activities
北出 幸夫
Aug 2011   
白石 孝雄
Mar 2010   
Mar 2010   
Diazirine-containing RNA photo-cross-linking probes for the study of siRNA-protein interactions
久保江 悟
Nov 2009   
Labeling of 2’,5’-oligoadenylates (2-5As) by click reaction
喜多村 徳昭
Aug 2009   
Pd/C-catalyzed, Ligand-free Suzuki-Miyaura reaction
門口 泰也
Mar 2009   
Molecular cloning, expression, characterization and mutation of Plasmodium falciparum guanylate kinase
Jul 2008   

Research Grants & Projects

Ministry of Education, Culture, Sports, Science and Technology: Grants-in-Aid for Scientific Research(若手研究(B))
Project Year: 2010 - 2012    Investigator(s): Yoshiaki KITAMURA
Small interfering RNAs (siRNAs) are considered to be attractive candidates as nucleic acid drugs, owing to their powerful regulation of gene expression in a sequence-specific manner. In this study, novel some solid supports and synthetic method of...


5871231 : エチニル基含有環状イミド化合物、並びに、それを用いたチオール基修飾剤及びそれを用いたアミノ基修飾剤