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Shigeki Sasaki Last modified date:2019.12.13

Professor / Department of Chemo-Pharmaceutical Sciences
Department of Chemo-Pharmaceutical Sciences
Faculty of Pharmaceutical Sciences

Graduate School
Undergraduate School

Home page of Bioorganic and Synthetic Chemistry at Graduate School of Pharmaceutical Sciences .
Academic Degree
Doctor of Pharmaceutical Sciences
Field of Specialization
Bioorganic and Synthetic Chemistry
Research Interests
  • Application of the intelligent functional oligonucleotides and nano-DDS to innovative molecular therapy
    keyword : genome, chemistry, regulation of gene expression, therapeutic oligonucleotide, medicinal chemistry, drug delivery, molecular therapy
  • Development of recognition molecule for 8-nitroguanosine
    keyword : 8-nitroguanosine, chemistry
  • Development of self-assemblying molecules mediated by complexation of metal cations on the long DNA
    keyword : genome, chemistry, synthesis, medicina chemistry, long DNA repeat
    2008.04~2016.03New type of DNA-binding molecules has been investigated, which may assemble on the DNA by mediation of complex formation with magnesium cation. The self assembling molecules are expected to be useful for recognition of the repeated sequence of DNA..
  • Development of smart nano-medicine for the specific targeting of the genome.
    keyword : genome, chemistry, regulation of gene expression
    2005.04~2016.04For development of smart, nano-medicine, the genome-targeting molecules were investigated by using chemically-reactive oligonucleotides, and the following new functions have been exhibited. (1) Functionality-transfer reaction to the target RNA, (2) New non-natural nucleoside analogs for the foramtion of stable triplex DNA, (3) Multi-functional molecules for nano-medicine, (4) New chemical probes for detection of damaged DNA..
  • Study on innovative medicines for targeting genes
    keyword : genome, chemistry, regulation of gene expression, point mutation, repair, synthesis of natural product, medicinal chemistry
    1993.03~2016.04Site-directed reaction with high efficiency and specificity to DNA or RNA has become of great interest, because of potential applications to modulation of gene expression at the site of reaction. The cross-linking within complementary duplex or triplex is a tool for such a site-directed modification. The objective of the present research is to establish the new concept of 者synchronous activation謝 to develop new bio-functional molecules that exhibit highly selective and efficient reaction toward the target DNA sequence. When reactive oligonucleotides will be applied in vivo, reactive molecules should have high reactivity together with high stability. Therefore, a reactive group should have inducible reactivity to be activated in proximity with a target base within duplex. Thus, a new strategy was designed so as to induce the reactive vinyl group of 2-amino-6-vinylpurine within complementary duplex. In the new strategy, the vinyl group is first protected by a phenylsulfide and incorporated into the oligonucleotides. Phenylsulfide can be oxidized to sulfoxide, and subsequent elimination would re-generate the vinyl group. Especially, it was anticipated that duplex formation with complementary strand might work as a trigger for this activation process, that is, the vinyl group would be regenerated by auto-activation within duplex..
Academic Activities
1. Daichi Jitsuzaki, Kazumitsu Onizuka, Atsushi Nishimoto, Ikuya Oshiro, Yosuke Taniguchi, Shigeki Sasaki, Remarkable acceleration of a DNA/RNA inter-strand functionality transfer reaction to modify a cytosine residue: the proximity effect via complexation with a metal cation , Nulceic Acids Research, 10.1093/nar/gku538 , 42, 13, 8808-8815, 2014.06.
1. 佐々木 茂貴, Design of non-natural nucleosides for the formation of stable triplexes toward the duplex DNA having CG or TA interrupting sites, Asian Three Round Table Meeting on Nucleic Acids 2015 (A3RONA), 2015.09.
Membership in Academic Society
  • Nucleic Acids Therapeutics Society of Japan
  • Oligonucleotide Therapeutic Society
  • International Pharmaceutical Federation (FIP)
  • Development of the novel functional molecules targeting DNA and RNA
  • ortho-Methyl substituted W-shaped nucleoside analog accelerates the DNA strand displacement reaction
Professional and Outreach Activities
・Vice President of the Pharmaceutical Society of Japan
・Member of the FIP-BPS (Board of Pharmaceutical Sciences-International Pharmaceutical Federation)
・A major member of the founders of the Nucleic Acids Therapeutics Society of Japan, and the first President of this Society
・A member of the Foresight Program, A3 Chemical Probe Research Hub.