Chemical Biology of Natural Products: Target ID and Activity Control - Scientific Research on Innovative Areas, a MEXT Grant-in-Aid Project FY2011-2015

Publication in 2012

Publication in 2012



Hiroshi Handa, A01 Group Leader
Professor, Graduate School of Bioscience and Biotechnology, Tokyo Institute of Technology
  1. G. Diamant, L. Amir-Zilberstein, Y. Yamaguchi, H. Handa, R. Dikstein, DSIF restricts NF-κB signaling by coordinating elongation with mRNA Processing of negative feedback genes, Cell Reports, 2, 1-10 (2012).
  2. T. Wada, M. Hara, T. Taneda, C. Qingfu, R. Takara, K. Moro, K. Takeda, T. Kishimoto, H. Handa, Antisense morpholino targeting just upstream from a poly(A) tail junction of maternal mRNA removes the tail and inhibits translation. Nucleic Acids Res., 40, e173 (2012).
  3. Y. Ito, T. Ito, S. Karasawa, T. Enomoto, A. Nashimoto, Y. Hase, S. Sakamoto, T. Mimori, Y. Matsumoto, Y. Yamaguchi, H. Handa, Identification of DNA-dependent protein kinase catalytic subunit (DNA-PKcs) as a novel target of Bisphenol A, PLoS ONE, 7, e50481 (2012).
  4. Lopez-Girona, D. Mendy, T. Ito, K. Miller, A. K. Gandhi, J. Kang, S. Karasawa, G. Carmel, P. Jackson, M. Abbasian, A. Mahmoudi, B. Cathers, E. Rychak, S. Gaidarova, R. Chen, P. H. Schafer, H. Handa, T. O. Daniel, J. F. Evans, R. Chopra, Cereblon is a direct protein target for immunomodulatory and antiproliferative activities of lenalidomide and pomalidomide, Leukemia, 26, 2326-2335 (2012).
  5. T. Ito, H. Handa, Deciphering the mystery of thalidomide teratogenicity, Congenit. Anom., 52, 1-7 (2012).
  6. E. Okuda-Ashitaka, T. Minami, S. Tsubouchi, H. Kiyonari, A. Iwamatsu, T. Noda, H. Handa, S. Ito, Identification of NIPSNAP1 as a nocistatin-interacting protein involving pain transmission, J. Biol. Chem., 287, 10403-10413 (2012).
  7. S. Sakamoto, M. Hatakeyama, T. Ito, H. Handa, Tools and methodologies capable of isolating and identifying a target molecule for a bioactive compound, Bioorg. Med. Chem., 20, 1990-2001 (2012).
Ryuichi Okamoto
Associate Professor, Department of Gastroenterology and Hepatology, Tokyo Medical and Dental University
  1. 1.Y. Nemoto, T. Kanai, M. Takahara, S. Oshima, T. Nakamura, R. Okamoto, K. Tsuchiya, M. Watanabe, Bone marrow-mesenchymal stem cells are a major source of interleukin-7 and sustain colitis by forming the niche for colitogenic CD4 memory T cells, Gut 62,1142-52(2013).【Epub 2012】
  2. S. Yui, T. Nakamura, T. Sato, Y. Nemoto, T. Mizutani, X. Zheng, S. Ichinose, T. Nagaishi, R. Okamoto, K. Tsuchiya, H. Clevers, M. Watanabe, Functional engraftment of colon epithelium expanded in vitro from a single adult Lgr5+ stem cell, Nat Med, 18, 618-623 (2012).
  3. O. Yamaji, T. Nagaishi, T. Totsuka, M. Onizawa, M. Suzuki, N. Tsuge, A. Hasegawa, R. Okamoto, K. Tsuchiya, T. Nakamura, H. Arase, T. Kanai, M. Watanabe, The development of colitogenic CD4+ T cells is regulated by IL-7 in collaboration with natural killer cell function in a murine model of colitis, J Immunol, 188, 2524-2536 (2012).
  4. T. Mizutani, T. Nakamura, R. Morikawa, M. Fukuda, W. Mochizuki, Y. Yamauchi, K. Nozaki, Yui S, Y. Nemoto, T. Nagaishi, R. Okamoto, K. Tsuchiya, M. Watanabe, Real-time analysis of P-glycoprotein-mediated drug transport across primary intestinal epithelium three-dimensionally cultured in vitro, Biochem Biophys Res Commun, 419, 238-243 (2012).
Hajime Watanabe
Professor, Graduate School of Engineering, Osaka University
  1. Y. Kato, T. Matsuura, H. Watanabe, Genomic integration and germline transmission of plasmid injected into crustacean Daphnia magna eggs.PloS ONE 7(3):e45318(2012).
Motomasa Kobayashi
Professor, Graduate School of Pharmaceutical Sciences, Osaka University
Co-Researcher:Masayoshi Arai, Naoyuki Kotoku
  1. M. Arai, Y. Yamano, M. Fujita, A. Setiawan, M. Kobayashi, Stylissamide X, a new proline-rich cyclic octapeptide as an inhibitor of cell migration, from an Indonesian marine sponge of Stylissa sp. Bioorg. Med. Chem. Lett., 22, 1818-1821 (2012).
  2. N. Kotoku, Y. Sumii, T. Hayashi, S. Tamura, T. Kawachi, S. Shiomura, M. Arai, M. Kobayashi, Creation of readily accessible and orally active analogue of cortistatin A. ACS Med. Chem. Lett., 3, 673-677 (2012).
  3. Y. Yamano, M. Arai, M. Kobayashi, Neamphamide B, new cyclic depsipeptide, as an anti-dormant mycobacterial substance from a Japanese marine sponge of Neamphius sp. Bioorg. Med. Chem. Lett., 22, 4877-4881 (2012).
Kenichi Nishiyama
Professor, Cryobiofrontier Research Center, Faculty of Agriculture, Iwate University
  1. Morita, K., Tokuda, H. and Nishiyama, K., Multiple SecA molecules drive protein translocation across a single translocon with SecG inversion, J. Biol. Chem., 287, 455-464 (2012)
  2. Nishiyama, K., Maeda, M., Yanagisawa, K., Nagase, R., Komura, H., Iwashita, T., Yamagaki, T., Kusumoto, S., Tokuda, H. and Shimamoto, K., MPIase is a glycolipozyme essential for membrane protein integration, Nat. Commun., 3, 1260 (2012)
Shin Hamamoto
Assistant Professor, Graduate School of Engineering, Tohoku University
  1. Y. Ishimaru, S. Hamamoto, N. Uozumi and M. Ueda, Regulatory mechanism of plant nyctinastic movement: An ion channel-related plant behavior Plant Electrophysiology, Plant Electrophysiology, pp125-142 (2012).
Kohji Fukunaga
Professor,Graduate School of Pharmaceutical Sciences, Tohoku University
  1. Y. Shinoda, K. Fujita, S. Saito, H. Matsui, Y. Kanto, Y. Nagaura, K. Fukunaga, S. Tamura, T. Kobayashi, Acyl-CoA binding domain containing 3 (ACBD3) recruits the protein phosphatase PPM1L to ER-Golgi membrane contact sites, FEBS Lett., 586(19), 3024-9 (2012).
  2. YM. Lu, RR. Tao, JY. Huang, LT. Li, MH. Liao, XM. Li, K. Fukunaga, ZH. Hong, F. Han, P2X(7) signaling promotes microsphere embolism-triggered microglia activation by maintaining elevation of Fas ligand, J Neuroinflammation, 9, 172 (2012).
  3. N. Shioda, K. Ishikawa, H. Tagashira, T. Ishizuka, H. Yawo, K. Fukunaga, Expression of a truncated form of the endoplasmic reticulum chaperone protein, σ1 receptor, promotes mitochondrial energy depletion and apoptosis, J Biol Chem, 287(28), 23318-31 (2012).
  4. K. Fukunaga, Benefit of vanadium compound in therapy for cardiovascular diseases, Yakugaku Zasshi, 132(3), 279-84 (2012).
  5. H. Tagashira, K. Fukunaga, Cardioprotective effect of fluvoxamine, sigma-1 receptor high affinity agonist, Yakugaku Zasshi, 132(2), 167-72 (2012).
  6. S. Moriguchi, N. Shioda, Y. Yamamoto, H. Tagashira, K. Fukunaga, The T-type voltage-gated calcium channel as a molecular target of the novel cognitive enhancer ST101: enhancement of long-term potentiation and CaMKII autophosphorylation in rat cortical slices, J Neurochem, 121(1), 44-53 (2012).
  7. K. Fukunaga, N. Shioda, Novel dopamine D2 receptor signaling through proteins interacting with the third cytoplasmic loop, Mol Neurobiol, 45(1), 144-52 (2012).
  8. S. Moriguchi, Y. Yabuki, K. Fukunaga, Reduced calcium/calmodulin-dependent protein kinase II activity in the hippocampus is associated with impaired cognitive function in MPTP-treated mice, J Neurochem, 120(4), 541-51 (2012).
  9. RR. Tao, YL. Ji, YM. Lu, K. Fukunaga, F. Han, Targeting nitrosative stress for neurovascular protection: new implications in brain diseases, Curr Drug Targets, 13(2), 272-84 (2012).
  10. GS. Zhang, WF. Ye, RR. Tao, YM. Lu, GF. Shen, K. Fukunaga, JY. Huang, YL. Ji, F. Han, Expression profiling of Ca2+/calmodulin-dependent signaling molecules in the rat dorsal and ventral hippocampus after acute lead exposure, Exp Toxicol Pathol, 64(6), 619-24 (2012).
  11. N. Shioda, S. Moriguchi, T. Oya, Y. Ishii, J. Shen, T. Matsushima, H. Nishijo, M. Sasahara, K. Fukunaga, Aberrant hippocampal spine morphology and impaired memory formation in neuronal platelet-derived growth factor β-receptor lacking mice, Hippocampus, 22(6), 1371-8 (2012).
Kazuhisa Sekimizu
Professor, Graduate School of Pharmaceutical Sciences, The University of Tokyo
  1. Inagaki Y, Matsumoto Y, Kataoka K, Matsuhashi N, Sekimizu K. Evaluation of drug-induced tissue injury by measuring alanine aminotransferase (ALT) activity in silkworm hemolymph. BMC pharmacology & toxicology., 13, 13 (2012).
  2. Paudel A, Hamamoto H, Kobayashi Y, Yokoshima S, Fukuyama T, Sekimizu K. Identification of novel deoxyribofuranosyl indole antimicrobial agents. J Antibiot (Tokyo). 65, 53-57 (2012).
  3. Tomoda H, Sekimizu K. Recent advance in research of new anti-infectious agents-discovery chemical biology and development-. Yakugaku Zasshi., 132, 35-36 (2012).
  4. Hamamoto H, Urai M, Paudel A, Horie R, Murakami K, Sekimizu K. Identification of novel therapeutically effective antibiotics using silkworm infection model. Yakugaku Zasshi., 132, 79-84 (2012).
Maiko Okada
Assistant Professor, St.Marianna University School of Medicine.
Nobuaki Matsumori
Associate Professor, Graduate School of Science, Osaka Univeristy
  1. Y. Manabe, M. Ebine, N. Matsumori, M. Murata, T. Oishi, Confirmation of the Absolute Configuration at C45 of Amphidinol 3. J. Nat. Prod., 75, 2003-2006 (2012).
  2. N. Matsumori, T. Yasuda, H. Okazaki, T. Suzuki, T. Yamaguchi, H. Tsuchikawa, M. Doi, T. Oishi, M. Murata, Comprehensive molecular motion capture for sphingomyelin by site-specific deuterium labeling. Biochemistry, 51, 8363-8370 (2012).
  3. Y. Umegawa, T. Adachi, N. Matsumori, M. Murata, Possible conformation of amphotericin B dimer in membrane-bound assembly as deduced from solid-state NMR. Bioorg. Med. Chem., 20, 5699-5704 (2012).
  4. S. A. Goretta, M. Kinoshita, S. Mori, H. Tsuchikawa, N. Matsumori, M. Murata, Effects of chemical modification of sphingomyelin ammonium group on formation of liquid-ordered phase. Bioorg. Med. Chem., 20, 4012-4019 (2012).
  5. T. Oishi, K. Konoki, R. Tamate, K. Torikai, F. Hasegawa, N. Matsumori, M. Murata, Artificial ladder-shaped polyethers that inhibit maitotoxin-induced Ca2+ influx in rat glioma C6 cells. Bioorg. Med. Chem. Lett., 22, 3619-3622 (2012).
  6. T. Yamaguchi, T. Suzuki, T. Yasuda, T. Oishi, N. Matsumori, M. Murata, NMR-based conformational analysis of sphingomyelin in bicelles. Bioorg. Med. Chem., 20, 270-278 (2012).
  7. Y. Umegawa, Y. Nakagawa, K. Tahara, H. Tsuchikawa, N. Matsumori,T. Oishi, M. Murata, Head-to-tail interaction between amphotericin B and ergosterol occurs in hydrated phospholipid membrane. Biochemistry, 51, 83-89 (2012).
Toshiaki Okuno
Associate Professor, Juntendo University School of Medicine
  1. Sasaki F, Okuno T, Saeki K, Min L, Onohara N, Kato H, Shimizu T and Yokomizo T. A high-affinity monoclonal antibody against the FLAG tag useful for G-protein coupled receptor study. Analytical Biochemistry, 425, p. 157-165, (2012).
  2. Aratake Y, Okuno T, Matsunobu T, Saeki K, Takayanagi R, Furuya S, Yokomizo T. Helix 8 of leukotriene B4 receptor 1 inhibits ligand-induced internalization. FASEB Journal, 26 (10), p. 4068-4078 (2012).
Akihiro Sugawara
Assistant Professor,
Kitasato Institute for Life Sciences &Graduate School of Infection Control Sciences, Kitasato University
  1. A. Sugawara, A. Sueki, T. Hirose, H. Shima, K. S. Akagawa, S. Ōmura, T. Sunazuka, Novel 12-membered non-antibiotic macrolides, EM900 series with anti-inflammatory and/or immunomodulatory activity; synthesis, structure–activity relationships and in vivo study, J. Antibiotic., 65, 487-490, (2012).
  2. A. Kimishima, T. Hirose, A. Sugawara, T. Matsumaru, K. Nakamura, K. Katsuyama, M. Toda, H. Takada, R. Masuma, S. Ōmura, T. Sunazuka, Toward the total synthesis of Luminamicin: construction of 14-membered lactone framework possessing versatile enol ether moiety Tetrahedron Lett., 53, 2813-2816, (2012).
  3. H. Gouda, Y. Kobayashi, T. Yamada, T. Ideguchi, A. Sugawara, T. Hirose, S. Omura, T. Sunazuka, S. Hirono, Three-dimensional solution structure of bottromycin A2: a potent antibiotic active against methicillin-resistant Staphylococcus aureus and vancomycin-resistant Enterococci. Chem. Pharm. Bull., 60, 169-171, (2012).
Shuichi Sakamoto
Senior Researcher, Institute of Microbial Chemistry
  1. S. Sakamoto, F. Kojima, I. Momose, M. Kawada, H. Adachi, Y. Nishimura, Decalpenic acid induces early osteoblastic markers in pluripotent mesenchymal cells via activation of retinoic acid receptor γ, Biochem Biophys Res Commun, 422, 751-757 (2012).
Soichi Kojima
Unit Leader, RIKEN Center for Life Science Technology
  1. T.-F. Kuo, H. Tatsukawa, S. Kojima, Regulation of transglutaminase-mediated hepatic cell death in alcoholic steatohepatitis and non-alcoholic steatohepatitis, J Gastro Hepatol 27(suppl 2), 52-57 (2012).
Koichi Watashi
Senior Researcher, National Institute of Infectious Diseases
  1. L. Weng, X. Tian, Y. Gao, K. Watashi, K. Shimotohno, T. Wakita, M. Kohara, T. Toyoda, Different mechanisms of hepatitis C virus RNA polymerase activation by cyclophilin A and B in vitro, Biochim Biophys Acta, 1820, 1886-1892 (2012).
  2. A. Murayama, N. Sugiyama, K. Watashi, T. Masaki, R. Suzuki, H. Aizaki, T. Mizuochi, T. Wakita, T. Kato, Different mechanisms of hepatitis C virus RNA polymerase activation by cyclophilin A and B in vJapanese reference panel of blood specimens for evaluation of hepatitis C virus RNA and core antigen quantitative assays, J Clin Microbiol, 50, 1943-1949 (2012).


Kazuhiro Irie, A02 Group Leader
Professor, Graduate School of Agriculture, Kyoto Universiy
  1. K. Irie, R. C. Yanagita, Y. Nakagawa, Development of New Anticancer Drugs Based on the Activation Mechanism of Protein Kinase C, Med. Res. Rev., 32, 518-535 (2012).
  2. K. Irie, M. Kikumori, H. Kamachi, K. Tanaka, R. C. Yanagita, H. Tokuda, N. Suzuki, H. Nagai, K. Suenaga, Y. Nakagawa, Synthesis and Structure-activity Studies of Simplified Analogs of Aplysiatoxin with Anti-proliferative Activity like Bryostatin-1, Pure Appl. Chem., 84, 1341-1351 (2012).
  3. S. Ueno, R. C. Yanagita, K. Murakami, A. Murakami, H. Tokuda, N. Suzuki, T. Fujiwara, K. Irie, Identification and Biological Activities of Bryostatins from Japanese Bryozoan, Biosci. Biotechnol. Biochem., 76, 1041-1043 (2012).
  4. M. Kikumori, R. C. Yanagita, H. Tokuda, N. Suzuki, H. Nagai, K. Suenaga, K. Irie: Structure–activity Studies on the Spiroketal Moiety of a Simplified Analog of Debromoaplysiatoxin with Anti-proliferative Activity, J. Med. Chem., 55, 5614-5626 (2012).
  5. Y. Shu, R. C. Yanagita, H. Tokuda, N. Suzuki, K. Irie, Synthesis of Antineoplastic Analogs of Aplysiatoxin with Various Side Chain Structures, Heterocycles, 86, 281-303 (2012).
Masaya Imoto
Professor,Faculty of Science and Technology, Keio University
Co-Researcher: Etsu Tashiro
  1. Magi S, Tashiro.E and Imoto M. A chemical genomic study identifying diversity in cell migration signaling in cancer cells. Scientific Reports, 2, 823 (2012).
  2. Kimura.T, Kanagaki S, Matsui Y, Imoto M, Watanabe T, Shibasaki M. Synthesis and Assignment of the Absolute Configuration of an Indenotryptoline Bisindole Alkaloid, BE-54017. Org. Lett., 14, 4418-4421 (2012).
  3. Ri M, Tashiro.E, Oikawa D, Shinjo S, Tokuda M, Yokouchi Y, Narita T, Masaki A, Ito A, Ding J, Kusumoto S, Ishida T, Komatsu H, Shiotsu Y, Ueda R, Iwawaki T, Imoto M, Iida S. Identification of Toyocamycin, an agent cytotoxic for multiple myeloma cells, as a potent inhibitor of ER stress-induced XBP1 mRNA splicing. Blood Cancer J., e79 (2012).
  4. Kobayashi H, Harada, H, Nakamura M, Futamura Y, Ito A, Yoshida M, Iemura S, Shin-ya K, Doi T, Takahashi T, Natsume T, Imoto M and Sakakibara Y. Comprehensive Predictions of Target Proteins Based on Protein-Chemical Interaction Using Virtual Screening and Experimental Verifications. BMC Chemical Biology, 12, 2 (2012).
  5. Sasazawa Y, Kanagaki S, Tashiro.E, Nogawa T, Muroi M, Kondoh Y, Osada H, Imoto M. Xanthohumol Impairs Autophagosome Maturation through Direct Inhibition of Valosin-Containing Protein. ACS Chemical Biology, 7, 892-900 (2012).
  6. Yamamoto K, Makino M, Watanapokasin R, Tashiro.E and Imoto M. Inostamycin enhanced TRAIL-induced apoptosis through DR5 up-regulation on the cell surface. J. Antibiot., 65, 295-300 (2012).
  7. Tashiro.E and Imoto M. Target identification of bioactive compounds. Bioorg. & Med. Chem., 20, 1910-1921 (2012).
  8. Yamamoto K, Tashiro.E, Motohashi K, Seto H and Imoto M. Napyradiomycin A1, an inhibitor of mitochondrial complexes I and II. J. Antibiot., 65, 211-214 (2012).
  9. Kiga M, Tanzawa F, Iwasaki S, Inaba F, Fujiwara K, Iwadare H, Echigo T, Nakamura Y, Shibata T, Suzuki K, Yasumatsu, I Nakayama A, Sasazawa Y, Tashiro.E, Imoto M, S. Kurakata S. Antitumor effects of novel highly hydrophilic and non-ATP-competitive MEK1/2 inhibitor, SMK-17. Anticancer Drugs., 23, 119-130 (2012).
Shigeki Matsunaga
Professor, Graduate School of Agricultural and Life Sciences, The University of Tokyo
  1. Sun, Y.; Takada, K.; Takemoto, Y.; Yoshida, M.; Nogi, Y.; Okada, S.; Matsunaga, S.;Gliotoxin analogues from a marine-derived fungus, Penicillium sp., and their cytotoxic and histone methyltransferase inhibitory activities. J. Nat. Prod., 75, 111-114 (2012).
  2. Suzuki, M.; Ueoka, R.; Takada, K.; Okada, S.; Ohtsuka, S.; Ise, Y.; Matsunaga, S.;Isolation of spirastrellolides A and B from a marine sponge Epiplasis sp. and their cytotoxic activities. J. Nat. Prod., 75, 1192-1195 (2012).
  3. Imae, Y.; Takada, K.; Okda, S.; Ise, Y.; Yoshimura, H.; Morii, Y.; Matsunaga, S.;Isolation of cilliatamide D from a marine sponge Stelletta sp. and a reinvestigation of the configuration of ciliatamide A. J. Nat. Prod., 76, 755-758 (2012).
Masami Ishibashi
Professor,Graduate School of Pharmaceutical Sciences, Chiba University
Co-Researcher:Midori Arai, Kazufumi Toume
  1. T. Minakawa, K. Toume, M. A. Arai, S. K. Sadhu, F. Ahmed, M. Ishibashi, Eudesmane-type sesquiterpenoid and guaianolides from Kandelia candel in a screening program for compounds to overcome TRAIL-resistance, J. Nat. Prod., 75, 1431-1435 (2012).
  2. K. Toume, T. Nakazawa, H. Tahmina, T. Ohtsuki, M. A. Arai, T. Koyano, T. Kowithayakorn, M. Ishibashi, Cycloartane triterpenes and ingol diterpenes isolated from Euphorbia neriifolia in a screening program for death-receptor expression-enhancing activity, Planta medica, 78, 1370-1377 (2012).
  3. M. S. Abdelfattah, K. Toume, M. A. Arai, H. Masu, M. Ishibashi, Katorazone, a novel yellow pigment with 2-azaquinone-phenylhydrazone structure produced by Streptomyces sp. IFM 11299, Tetrahedron Lett., 53, 3346-3348 (2012).
  4. M. S. Abdelfattah, K. Toume, M. Ishibashi, Yoropyrazone, a new naphthopyridazone alkaloid isolated from Streptomyces sp. IFM 11307 and evaluation of its TRAIL resistance-overcoming activity, J. Antibiot., 65, 245-248 (2012).
Tetsuro Shinada
Professor, Graduate School of Science, Osaka City University
Co-Researcher: Yasufumi Ohfune
  1. Y. Ohfune, K. Oe, K. Namba, T. Shinada, Total Synthesis of Manzacidins. An Overview and Perspective, Heterocycles, 2012, 85, 2617–2649.
  2. T. Kotaki, T. Shinada, H. Numata, Structure Determination of a Natural Juvenile Hormone Isolated from a Heteropteran Insect, Psyche, 2012, Article ID 924256, 7pages,
  3. K. Kaihara, T. Kotaki, H. Numata, Y. Ohfune, T. Shinada, Structure-activity Relationship of Novel Juvenile Hormone, JHSB3, Isolated from the Stink Bug, Plautia Stali, Tetrahedron, 68, 106–113 (2012).
  4. Manabe, Y. Ohfune, T. Shinada, Stereoselective Total Syntheses of Insect Juvenile Hormones JH 0 and JH I”, Synlett, 1213–1216 (2012).
  5. K. Oe, T. Shinada, Y. Ohfune, Efficient Total Synthesis of Manzacidin B, Tetrahedron Lett., 53, 3250–3253 (2012).
  6. H. Ahmed, M. Hamada, T. Shinada, Y. Ohfune, L. Weerasinghe, P. P. Garner, and R. E. Oswald, The Structure of (-)-Kaitocephalin Bound to the Ligand Binding Domain of the (S)-α-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic Acid (AMPA)/Glutamate Receptor, GluA2, J. Biol. Chem., 287, 41007–41013 (2012).
  7. T. Yamada, K. Okada, T. Shinada, Y. Ohfune, and H. Hashimoto, Efficient Synthesis of Anhydrorhodovibrin and Analogs, Synlett, 2980–2984 (2012).
  8. T. Okada, A. Shimoda, T. Shinada, K. Sakaguchi, Y. Ohfune, Regioselective Prins Cyclization of Allenylsilanes. Stereoselective Formation of Multi-Substituted Heterocyclic Compounds, Org. Lett., 14, 6130–6133 (2012).
Hidenori Watanabe
Professor,Graduate School of Agricultural and Life Sciences, The University of Tokyo
  1. Y. Ogura, K. Ishigami, H. Watanabe, Total synthesis of (±)-lysidicin A, Tetrahedron, 68, 1723-1728 (2012).
Kosuke Namba
Associate Professor, Hokkaido University /
Professor, Graduate School of Pharmaceutical Science The University of Tokushima
  1. K, Namba, M. Kanaki, H. Suto, M. Nishizawa, K. Tanino, K. Hg(OTf)2-Catalyzed Vinylogous Semi-Pinacol Rearrangement Leading to 1,4-Dihydroquinolines. Org. Lett. 14, 1222-1225 (2012).
  2. H. Yamamoto, N. Yamasaki, S. Yoshidome, I. Sasaki, K. Namba, H. Imagawa, M. Nishizawa, M. Carbon-Nitrogen Bond Formation Between Allyl Silyl Ether and Hydrazide Promoted by Mercuric Triflate Catalyst. Synlett, 23, 1069-1073 (2012).
  3. R. Fuchigami, K. Namba, K. Tanino. A Concese [4+3] Cycloadditions of Pyrroles Leading to Tropinone Derivatives. Tetrahedron Lett., 53, 5725-5728 (2012).
  4. Y.Ohfune, K. Oe, K. Namba, T. Shinada. Total Synthesis of Manzacidins. An Overview and Perspective. Heterocycles, 85, 2617-2649 (2012).
  5. K. Namba, A. Mera, A. Osawa, E. Sakuda, N. Kitamura, K. Tanino. One-pot Synthesis of Highly Fluorescent 2,5-Disubstituted-1,3a,6a-triazapentalene. Org. Lett. 14, 5554-5557 (2012).
Satoshi Ichikawa 
Associate Professor,  Faculty of Pharmaceutical Science, Hokkaido University
  1. K. Okamoto, M. Sakagami, F. Fei, F. Takahashi, K. Uotani, H. Togame, H. Takemoto, S. Ichikawa, A. Matsuda, Synthesis of Pacidamycin Analogues via an Ugi-multicomponent Reaction, Bioorg. Med. Chem. Lett., 22, 4810-4815 (2012).
  2. K. Okamoto, M. Sakagami, F. Fei, K. Uotani, H. Togame, H. Takemoto, S. Ichikawa, A. Matsuda, Total Synthesis and Biological Evaluation of Pacidamycin D and Its 3’-Hydroxy Analogue, J. Org. Chem., 77, 1367-1377 (2012).
Haruhiko Fuwa
Associate Professor, Graduate School of Life Sciences, Tohoku University
  1. H. Fuwa, N. Ichinokawa, K. Noto, M. Sasaki, Stereoselective synthesis of 2,6-cis-substituted tetrahydropyrans: Brønsted acid-catalyzed intramolecular oxa-conjugate cyclization of α, β-unsaturated ester surrogates, J. Org. Chem., 77, 2588–2607 (2012).
  2. E. Alonso, H. Fuwa, C. Vale, Y. Suga, T. Goto, Y. Konno, M. Sasaki, F. M. LaFerla, S. Pérez, M. R. Vieytes, L. Giménez-Llort, *L. M. Botana, Design and synthesis of skeletal analogues of gambierol: Attenuation of amyloid β and tau pathology with voltage-gated potassium channel and N-methyl-D-aspartate receptor implications, J. Am. Chem. Soc., 134, 7467–7479 (2012).
  3. H. Fuwa, K. Ishigai, K. Hashizume, *M. Sasaki, Total synthesis and complete stereostructure of gambieric acid A, J. Am. Chem. Soc., 134, 11984–11987 (2012).
  4. M. Nakajima, H. Fuwa, *M. Sasaki, Stereoselective synthesis of the C1–C16 fragment of goniodomin A, Bull. Chem. Soc. Jpn., 85, 948–956 (2012).
  5. S. Pérez, C. Vale, E. Alonso, H. Fuwa, M. Sasaki, Y. Konno, T. Goto, Y. Suga, M. R. Vieytes, *L. M. Botana, Effect of gambierol and its heptacyclic and tetracyclic analogues in cultured cerebellar neurons: A structure–activity relationships study, Chem. Res. Toxicol., 25, 1929–1937 (2012).
  6. H. Fuwa, T. Noguchi, K. Noto, M. Sasaki, Tandem catalysis in domino olefin cross-metathesis/intramolecular oxa-conjugate cyclization: Concise synthesis of 2,6-cis-substituted tetrahydropyrans, Org. Biomol. Chem., 10, 8108–8112 (2012).
  7. H. Fuwa, K. Hirota, *M. Sasaki, A concise synthesis of the AB-ring fragment of (–)-gambierol, Heterocycles, 86, 127–132 (2012).
  8. H. Fuwa, Total synthesis of tetrahydropyran-containing natural products exploiting intramolecular oxa-conjugate cyclization, Heterocycles, 85, 1255–1298 (2012).
Hideyuki Shigemori 
Professor, Graduate School of Life and Environmental Sciences, University of Tsukuba
  1. P. Yamada, T. Ono, H. Shigemori, J. Han, and H. Isoda, Inhibitory Effect of Tannins from Galls of Carpinus tschonoskii on the Degranulation of RBL-2H3 Cells, Cytotechnology, 64, 349-356 (2012).
  2. R. Furuya, H. Hu, Z. Zhang, and H. Shigemori, Suffruyabiosides A and B, Two New Monoterpene Diglycosides from Moutan Cortex, Molecules, 17, 4915-4923 (2012).
  3. Y. Miyamae, M. Kurisu, K. Murakami, J. Han, H. Isoda, K. Irie, and H. Shigemori, Protective Effects of Caffeoylquinic Acids on the Aggregation and Neurotoxicity of the 42-residue Amyloid β-protein, Bioorg. Med. Chem., 20, 5844-5849 (2012).
  4. K. Sasaki, J. Han, H. Shigemori, and H. Isoda, Caffeoylquinic Acid Induces ATP Production and Energy Metabolim in Human Neurotypic SH-SY5Y Cells, Nutrition and Aging, 1, 141-150 (2012).
Hirokazu Kawagishi
Professor, Research Institute of Green Science and Technology, Shizuoka University
  1. J. Wang, H. Hirai, and H. Kawagishi, Biotransformation of acetamiprid by the white-rot fungus Phanerochaete sordida YK-624 , Appl. Microbiol. Biotechnol., 93, 831–835 (2012)
  2. 【Co-Study】Y. Imai, S. Hirono, H. Matsuba, H., T. Suzuki, Y. Kobayashi, H. Kawagishi, D. Takahashi, and K. Toshima Degradation of target oligosaccharides by anthraquinone-lectin hybrids with light switching, Chemistry-An Asian J., 7, 97–104 (2012).
  3. K. Fushimi, K. Anzai, S. Tokuyama, Y. Kiriiwa, M. Matsumoto, A. Sekiya, D. Hashizume, K. Nagasawa, H. Hirai, and H. Kawagishi, Agrocybynes A to E from the culture broth of Agrocybe praecox, Tetrahedron, 68, 1262-1265 (2012).
  4. J. Wang, N. Majima, H. Hirai, H., and H. Kawagishi, Effective removal of endocrine disrupting compounds by lignin peroxidase from the white-rot fungus Phanerochaete sordida YK-624, Current Microbiology, 64, 300-303 (2012).
  5. T. Suzuki, K. Sugiyama, H. Hirai, H. Ito, T. Morita, H. Dohra, T. Murata, T. Usui, H. Tateno, J. Hirabayashi, Y. Kobayashi, and H. Kawagishi, Mannose-specific lectin from the mushroom Hygrophorus russula, Glycobiology, 22, 616-629 (2012)
  6. 【Co-Study】Y. Qu, K. Sun, L. Gao, Y. Sakagami, H. Kawagishi, M. Ojika, and J. Qi, Termitomycesphins G and H, additional cerebrosides from the edible Chinese mushroom Termitomyces albuminosus, Biosci. Biotechnol. Biochem., 76, 791-793 (2012).
  7. S. Nakaya, S. Mizuno, S., Ishigami, H., Y. Yamakawa, H. Kawagishi, and T. Ushimaru, New rapid screening system for anti-aging compounds using budding yeast and identification of beauveriolide I as a potent active compound, Biosci. Biotechnol. Biochem., 76, 1226-1228 (2012).
  8. 【Co-Study】J-H. Choi, K. Maeda, H. Hirai, E. Harada, M. Kawade, J. Qi, M. Ojika, and H. Kawagishi, A novel cerebroside, termitomycesphin I from the mushroom Termitomyces titanicus, Biosci. Biotechnol. Biochem., 76, 1407-1409 (2012).
  9. T. Sugiura, T. Mori, I. Kamei, H. Hirai, H. Kawagishi, and R. Kondo, Improvement of ligninolytic properties in the hyper lignin-degrading fungus Phanerochaete sordida YK-624 using a novel gene promoter, FEMS Microbiol. Lett., 331, 81-83 (2012).
  10. T. Suzuki, T., J-H.Choi, T. Kawaguchi, K. Yamashita, A. Morita, H. Hirai, K. Nagai, K., T. Hirose, S. Omura, T. Sunazuka, and H. Kawagishi, Makomotindoline from Makomotake, Zizania latifolia infected with Ustilago esculenta, Bioorg. Med. Chem. Lett., 22, 4246–4248 (2012).
  11. Y. Kobayashi, H. Tateno, H. Dohra, K. Moriwaki, K., E. Miyoshi, J. Hirabayashi, and H. Kawagishi, A novel core fucose-specific lectin from the mushroom Pholiota squarrosa, J. Biol. Chem., 287, 33973-33978 (2012).
  12. J. Wu, S. Tokuyama, K. Nagai, N. Yasuda, K. Noguchi, T. Matsumoto, H. Hirai, and H. Kawagishi, Strophasterols A to D with an unprecedented steroid skeleton: from the mushroom Stropharia rugosoannulata, Angew. Chem., Int. Ed., 51, 10820 -10822 (2012).
Makoto Ojika
Professor, Graduate School of Bioagricultural Sciences, Nagoya University
  1. 【Co-Study】J.-H. Choi, K. Maeda, H. Hirai, E. Harada, M. Kawade, J. Qi, M. Ojika, H. Kawagishi, Novel cerebroside, termitomycesphin I, from the mushroom, Termitomyces titanicus, Biosci. Biotechnol. Biochem. 76, 1407-1409 (2012).
  2. 【Co-Study】Y. Qu, K. Sun, L. Gao, Y. Sakagami, H. Kawagishi, M. Ojika, Jianhua Qi, Termitomycesphins G and H, Additional Cerebrosides from the Edible Chinese Mushroom Termitomyces albuminosus, Biosci. Biotechnol. Biochem. 76(4), 791-793 (2012).
Shinichi Nishimura
Assistant Professor, Graduate School of Pharmaceutical Sciences, Kyoto University
  1. Kishimoto, S., Tsunematsu, Y., Nishimura, S., Hayashi, Y., Hattori, A. & Kakeya, H. Tumescenamide C, an antimicrobial cyclic lipodepsipeptide from Streptomyces sp. Tetrahedron, 68, 5572-5578 (2012).
Katsunori Tanaka
Associate Chief Scientist, RIKEN
Co-Researcher  Takayuki Iwata, Masataka Kitadani.
  1. K. Tanaka, E. R. O. Siwu, S. Hirosaki, T. Iwata, R. Matsumoto, Y. Kitagawa, A. R. Pradipta, M. Okumura, K. Fukase, Efficient Synthesis of 2,6,9-Triazabicyclo [3.3.1]nonanes through Amine-Mediated Formal [4+4] Reaction of Unsaturated Imines, Tetrahedron Lett., 53, 5899-5902 (2012).
  2. K. Fukase, K. Tanaka, Bio-Imaging and Cancer Targeting with Glycoproteins and N-Glycans, Curr. Opin. Chem. Biol., 16, 614-621 (2012).
  3. K. Tanaka, Development of Azaelectrocyclization-Based Labeling and Application to Noninvasive Imaging and Targeting Using N-Glycan Derivatives -In pursuit of N-Glycan Functions on Proteins, Dendrimers, and Living Cells-, Trends in Glycoscience and Glycotechnology, 24, 47-64 (2012).
  4. K. Tanaka, S. Shirotsuki, C. Kageyama, T. Tahara, S. Nozaki, E. R. O. Siwu, T. Iwata, S. Tamura, S. Douke, N. Murakami, H. Onoe, Y. Watanabe, K. Fukase, Template-Assisted and Self-Activating Clicked Peptide as a Synthetic Mimic of the SH2 Domain, ACS Chem. Biol., 7, 637-645 (2012).
  5. K. Tanaka, S. Yokoi, K. Morimoto, T. Iwata, Y. Nakamoto, K. Nakayama, K. Koyama, T. Fujiwara, K. Fukase, Cell Surface Biotinylation by Azaelectrocyclization: Easy-Handling and Versatile Approach for Living Cell Labeling, Bioorg. Med. Chem., 20, 1865–1868 (2012).
  6. K. Tanaka, K. Mazumder, E. R. O. Siwu, S. Nozaki, Y. Watanabe, K. Fukase, Auxiliary-Directed Oxidation of Ursolic Acid by “Ru”-Porphyrins: Chemical Modulation of Cytotoxicity against Tumor Cell Lines, Tetrahedron Lett., 53, 1756–1759 (2012).
  7. K. Tanaka, S. Katsumura, K. Fukase, Discovery and application of 6π-Azaelectrocyclization to natural product synthesis & synthetic biology, Sci. China Chem., 55, 19-30 (2012).
  8. T. Kobayashi, F. Hasegawa, Y. Hirose, K. Tanaka, H. Mori, S. Katsumura, Stereocontrolled Synthesis of Substituted Chiral Piperidines via One-Pot Asymmetric 6π-Azaelectrocyclization: Asymmetric Syntheses of (−)-Dendroprimine, (+)-7-Epidendroprimine, (+)-5-Epidendroprimine, and (+)-5,7-Epidendroprimine, J. Org. Chem., 77, 1812–1832 (2012).
  9. K. Tanaka, K. Fukase, Oligosaccharide Synthesis on Solid-supports, In Solid-Phase Organic Synthesis Book, P. Toy (ed), Wiley, 489-530 (2012).
Kazunobu Toshima
Professor, Faculty of Science and Technology Keio University
  1. M. Nishibu, D. Takahashi, K. Toshima, Carbohydrate recognition and photodegradation by an anthracene-Kemp’s acid hybrid, Organic & Biomolecular Chemistry, 10, 8393-8395 (2012).
  2. D. Takahashi, T. Miura, K. Toshima, Photodegradation of lipopolysaccharides and the inhibition of macrophage activation by anthraquinone-boronic acid hybrids, Chemical Communications, 48, 7595-7597 (2012).
  3. S. Tanimoto, S. Sakai, E. Kudo, S. Okada, S. Matsumura, D. Takahashi, K. Toshima, Target-selective photodegradation of HIV-1 protease and inhibition of HIV-1 replication in living cells by designed fullerene-sugar hibrids, Chemistry-An Asian Journal, 7, 911-914 (2012).
  4. D. Takahashi, K. Toshima, Chemistry based approach for degradation of target-oligosaccharides using photo-activatable organic small molecules, Trends in Glycoscience and Glycotechnology, 24, 258-276 (2012).
  5. K. Toshima, D.Takahashi, S. Tanimoto, Creation of novel biofunctional molecules for target-selective photodegradation of proteins and carbohydrates: a synthetic and chemical, biological study for the post-genome era, Journal of Synthetic Organic Chemistry, 70, 1187-1195 (2012).
  6. K. Toshima, Design, synthesis and evaluation of light-activatable organic molecules that target-selectively degrade DNA, proteins and carbohydrates; an interdisciplinary challenge for a synthetic organic chemist, Synlett, 23, 2025-2052 (2012).
  7. S. Tanimoto, D. Takahashi, K. Toshima, Chemical methods for degradation of target proteins using designed light-activatable organic molecules, Chemical Communications, 48, 7659-7671 (2012).
  8. D. Takahashi, K. Toshima, Chemical methods for degradation of target oligosaccharides using designed light-activatable organic molecules, Chemical Communications, 48, 4397-4407 (2012).
  9. Y. Imai, S. Hirono, H. Matsuba, T. Suzuki, Y. Kobayashi, H. Kawagishi, D. Takahashi, K. Toshima, Degradation of target oligosaccharides by anthraquinone-lectin hybrids with light switching, Chemistry-An Asian Journal, 7, 97-104 (2012).
Yoko Saikawa
Lecture, Faculty of Science and Technology, Keio University
  1. M. Yamada, N. Tokumitsu, Y. Saikawa, M. Nakata, J. Asano, K. Miyairi, T. Okuno, K. Konno, K. Hashimoto, Molybdophyllysin, a toxic metalloendopeptidase from the tropical toadstool, Chlorophyllum molybdites, Bioorg. Med. Chem. 20, 6583-6588 (2012).
Seijiro Hosokawa
Professor, Faculry of Science and Engineering, Waseda University
Co-Researcher:Mayumi Okamoto, Isao Shimizu
  1. Yuki Mukaeda, Takuya Kato, and Seijiro Hosokawa, Syn-selective Kobayashi aldol reaction using the E, E-vinylketene N,O-acetal. Organic Letters, 14 (20), 5298-5301 (2012).
  2. Takayuki Nakajima, Keiko Seto, Fumihiro Horikawa, Isao Shimizu; Andreas Scheurer; Bunsho Kure; Takashi Kajiwara; Tomoaki Tanase; Masahiro Mikuriya. Wheel-Shaped Icosanuclear Homo- and Heterometallic Complexes of Ni II, Co II, and Cu II ions supported by unsymmetrical aminoalcohol ligands. Inorganic Chemistry. 51(22):12503-12510 (2012).
  3. Mayumi Okamoto, Shun Kobayashi, Hiroshi Ikeuchi, Shunji Yamada, Korehito Yamanouchi, Kazumichi Nagasawa, Shun Maekawa, Takashi Kato, Isao Shimizu. Synthesis and bioassay of a boron-dipyrromethene derivative of estradiol for fluorescence imaging in vivo. Steroids, 77, 845-849 (2012).
  4. Kuniaki Tatsuta, Tomohiro Fukuda, Tatsuya Ishimori, Rearu Yachi, Shinpei Yoshida, Hiroshi Hashimoto, and Seijiro Hosokawa, The first total synthesis of hibarimicinone, a potent v-Src tyrosine kinase inhibitor, Tetrahedron Letters, 53 (4), 422-425 (2012).
Go Hirai
Senior Research Scientist, RIKEN
  1. A. Tsuchiya, G. Hirai, Y. Koyama, K. Oonuma, Y. Otani, H. Osada, and M. Sodeoka, Dual-specificity Protein Phosphatase CDC25A/B Inhibitor Identified from a Focused Library with Non-electrophilic Enamine Core Structure, ACS Med. Chem. Lett., 3, 294-298 (2012).
  2. M. Morita, G. Hirai, M. Ohkubo, H. Koshino, D. Hashizume, K. Maruoka, and M. Sodeoka, Kinetically Controlled One-Pot Formation of DEFGH-Rings of Type B Physalins through Domino-Type Transformations, Org, Lett., 14, 3434-3437 (2012).


Minoru Ueda , A03 Group Leader
Professor, Graduate School of Science, Tohoku University
  1. M. Ueda, Chemical Biology of Natural Products on the Basis of Identification of Target Proteins (Highlight Review), Chem. Lett., 41, 658-666 (2012).
  2. M. Ueda, G. Yang, Y. Ishimaru, S. Tamura, T. Itabashi, K. Kiyota, S. Kuwahara, S. Inomata, M. Shoji, T. Sugai, Hybrid Stereoisomers of Compact Molecular Probes Based on Jasmonic Acid Glucoside: Syntheses and Biological Evaluations, Bioorg. Med. Chem., 20, 5832-5843 (2012).
  3. H. Kasai, T. Murakami, Y. Ikuta, Y. Koseki, K. Baba, H. Oikawa, H. Nakanishi, M. Okada, M. Shoji, M. Ueda, H. Imahori, M. Hashida, Creation of Pure Nanodrugs and Their Anticancer Properties, Angew. Chem. Int. Ed., 51, 10315-10318 (2012).
  4. Y. Ishimaru, S. Hamamoto, N. Uozumi, and M. Ueda, Regulatory Mechanism of Plant Nyctinastic Movement: An Ion Channel-Regulated Plant Behavior, in A. Volkov eds. “Plant Electrophysiology Signaling and Responses”, Springer-Verlag, pp. 125-142 (2012).
Naoki Kanoh
Associate Professor, Graduate School of Pharmaceutical Sciences, Tohoku University
  1. H. Fukuda, Y. Nishiyama, S. Nakamura, Y. Ohno, T. Eguchi, Y. Iwabuchi, T. Usui, and N. Kanoh, Synthesis and Structure-Activity Relationship of Vicenistatin, a Cytotoxic 20-Membered Macrolactam Glycoside, Chem. Asian J. 7, 2872-2881 (2012)
Hideo Kigoshi
Professor, Faculty of Pure and Applied Sciences, University of Tsukuba
Co-Researcher: Ichiro Hayakawa
  1. M. Ojika, H. Kigoshi, K. Suenaga, Y. Imamura, K. Yoshikawa, T. Ishigaki, A. Sakakura, T. Mutou, K. Yamada, Aplyronines D-H from the sea hare Aplysia kurodai: isolation, structures, and cytotoxicity, Tetrahedron, 68, 982-987 (2012).
  2. K. Kobayashi, Y. Fujii, Y. Hirayama, S. Kobayashi, I. Hayakawa, H. Kigoshi, Design, Synthesis, and Biological Evaluations of Aplyronine A-Mycalolide B Hybrid Compound, Org. Lett., 14, 1290-1293 (2012).
  3. Y. Satoh, D. Kawamura, M. Yamaura, Y. Ikeda, Y. Ochiai, I. Hayakawa, H. Kigoshi, Synthetic studies towards biselides. Part 1: Synthesis of the core carbon framework of biselides A, B, and E using Stille coupling, Tetrahedron Lett., 53, 1390-1392 (2012).
  4. Y. Satoh, T. Yamada, Y. Onozaki, D. Kawamura, I. Hayakawa, H. Kigoshi, Synthetic studies toward biselides. Part 2: Synthesis of the macrolactone part of biselides A and B using allylic oxidation, Tetrahedron Lett., 53, 1393-1396 (2012).
  5. T. Ohyoshi, S. Funakubo, Y. Miyazawa, K. Niida, I. Hayakawa, H. Kigoshi, Total Synthesis of (-)-13-Oxyingenol and its Natural Derivative, Angew. Chem. Int. Ed., 51, 4972-4975 (2012).
  6. T. Takemura, I. Hayakawa, E. Fukasawa, T. Sengoku, H. Kigoshi, Toward the synthesis of γ-pyrone-containing natural products: diastereoselective aldol-type reaction of a γ-pyrone, Tetrahedron, 68, 6477-6484 (2012).
  7. M. Kita, K. Yoneda, Y. Hirayama, K. Yamagishi, Y. Saito, Y. Sugiyama, Y. Miwa, O. Ohno, M. Morita, K. Suenaga, H. Kigoshi, Fluorescent Aplyronine A: Intracellular Accumulation and Disassembly of Actin Cytoskeleton in Tumor Cells, ChemBioChem, 13, 1754-1758 (2012).
  8. I. Hayakawa, T. Takemura, E. Fukasawa, Y. Ebihara, N. Sato, T. Nakamura, K. Suenaga, H. Kigoshi, Total synthesis and biological evaluation of auripyrones A and B, Bull. Chem. Soc. Jpn., 85, 1077-1092 (2012).
  9. M. Kita, H. Oka, A. Usui, T. Ishitsuka, Y. Mogi, H. Watanabe, H. Kigoshi, Synthesis and biological activities of the tris-oxazole macrolactone analogs of mycalolides, Tetrahedron, 68, 8753-8760 (2012).
  10. I. Hayakawa, A. Ikedo, T. Chinen, T. Usui, H. Kigoshi, Design, synthesis, and biological evaluation of the analogues of glaziovianin A, a potent antitumor isoflavone, Bioorg. Med. Chem., 20, 5745-5756 (2012).
  11. M. Kita, Y. Hirayama, K. Yamagishi, K. Yoneda, R. Fujisawa, H. Kigoshi, Interactions of the Antitumor Macrolide Aplyronine A with Actin and Actin-Related Proteins Established by Its Versatile Photoaffinity Derivatives, J. Am. Chem. Soc., 134, 20314-20317 (2012).
  12. O. Ohno, M. Morita, K. Kitamura, T. Teruya, K. Yoneda, M. Kita, H. Kigoshi, K. Suenaga, Apoptosis-inducing activity of the actin- depolymerizing agent aplyronine A and its side-chain derivatives, Bioorg. Med. Chem. Lett., 23, 1467-1471 (2012).
Toshio Nishikawa
Professor,Graduate School of Bioagricultural Sciences, Nagoya University
Co-Researcher :Masaatsu Adachi, Keiichi Konoki
  1. M. Adachi, K. Higuchi, N. Thasana, H. Yamada, T. Nishikawa, Stereocontrolled Synthesis of an Indole Moiety of Sespendole and Stereochemical Assignment of the Side Chain, Org. Lett, 14, 114-117 (2012).
  2. T. Komada, M. Adachi, T. Nishikawa, A Concise Synthesis of a Highly Strained Cyclobutane in Solanoeclepin A by Radical Cyclization, Chem. Lett, 41, 287-289 (2012).
  3. N. Matsumoto, T. Tsujimoto, A. Nakazaki, M. Isobe, T. Nishikawa, Synthetic Studies on Pactamycin, a Potent Antitumor Antibiotic, RSC Advances, 2, 9448-9462 (2012).
  4. A. Nakazaki, A. Mori, S. Kobayashi, T. Nishikawa, Diastereoselective Synthesis of 3,3-Disubstituted Oxindoles from Atropisomeric N-Aryl Oxindole Derivatives, Tetrahedron Lett, 53, 7131-7134 (2012).
  5. T. Oishi, K. Konoki, R. Tamate, K. Torikai, F. Hasegawa, N. Matsumori, M. Murata, Artificial Ladder-shaped Polyethers That Inhibit Maitotoxin-induced Ca2+ Influx in Rat Gioma C6 Cells, Bioorg. Med. Chem. Lett, 22, 3619-3622 (2012).
Makoto Sasaki
Professor Graduate School of Life Sciences, Tohoku University
Co-Researcher Haruhiko Fuwa, Keiichi Konoki
  1. H. Fuwa, N. Ichinokawa, K. Noto, M. Sasaki, Stereoselective Synthesis of 2,6-cis-Substituted Tetrahydropyrans: Brønsted Acid-Catalyzed Intramolecular Oxa-Conjugate Cyclization of α,β-Unsaturated Ester Surrogates, J. Org. Chem., 77, 2558-2607 (2012).
  2. E. Alonso, H. Fuwa, C. Vale, Y. Suga, T. Goto, Y. Konno, M. Sasaki, F. M. LaFerla, M. R. Vieytes, L. Gimenez-Llort, L. M. Botana, Design and Synthesis of Skeletal Analogues of Gambierol: Attenuation of Amyloid-β and Tau Pathology with Voltage-Gated Potassium Channel and N-Methyl-D-aspartate Receptor Implications, J. Am. Chem. Soc., 134, 7467-7479 (2012).
  3. Y. Kasai, T. Ito, M. Sasaki, Total Synthesis of (–)-Polycavernoside A: Suzuki–Miyaura Coupling Approach, Org. Lett., 14, 3186-3189 (2012).
  4. H. Fuwa, K. Ishigai, K. Hashizume, M. Sasaki, Total Synthesis and Complete Stereostructure of Gambieric Acid A, J. Am. Chem. Soc., 134, 11984-11987 (2012).
  5. H. Fuwa, K. Hirota, M. Sasaki, A Convergent Synthesis of the AB-Ring Fragment of (–)-Gambierol, Heterocycles, 86, 127-132 (2012).
  6. M. Nakajima, H. Fuwa, M. Sasaki, Stereoselective Synthesis of the C1–C16 Fragment of Goniodomin A, Bull. Chem. Soc. Jpn., 85, 948-956 (2012).
  7. S. Perez, C. Vale, E. Alonso, H. Fuwa, M. Sasaki, Y. Konno, T. Goto, Y. Suga, M. R. Vieytes, L. M. Botana, Effect of Gambierol and Its Tetracyclic and Heptacyclic Analogues in Cultured Cerebellar Neurons. A Structure-Activity Relationships Study, Chem. Res. Toxicol., 25, 1929-1937 (2012).
  8. H. Fuwa, T. Noguchi, K. Noto, M. Sasaki, Tandem Catalysis in Domino Olefin Cross-Metathesis/Intramolecular Oxa-Conjugate Cyclization: Concise Synthesis of 2,6-cis-Substituted Tetrahydropyran Derivatives, Org. Biomol. Chem., 10, 8108-8112 (2012).
Fumi Nagatsugi
Professor, The Institute of Multidisciplinary Research for Advanced Materials, Tohoku University
  1. Kusano,S., Sakuraba, T., Hagihara, S., Nagatsugi, F. Synthesis of 6-amino-2-vinyl purine derivatives for cross-linking and evaluation of the reactivity, Bioorg. Med. Chem. Lett., 22, 6957–6961 (2012). 10.1016/j.bmcl.2012.08.122
  2. Imoto, S., Chikuni, T., Kansui, H, Kunieda, T. , Nagatsugi, F. Fast DNA Interstrand Cross-linking Reaction by 6-Vinylpurine, Nucleosides Nucleotides Nucleic Acids., 31, 752–762 (2012). 10.1080/15257770.2012.726756
  3. Hagihara, S., Kusano, S., Lin, W.C., Chao, X.G., Hori, T., Imoto, S., Nagatsugi, F., Production of truncated protein by the crosslink formation of mRNA with 2’-OMe oligoribonucleotide containing 2-amino-6-vinylpurine, Bioorg. Med. Chem. Lett., 22, 3870-3872 (2012). 10.1016/j.bmcl.2012.04.123
Takamitsu Hosoya
Pofessor, Institute of Biomaterials and Bioengineering Tokyo Medical and Dental University
  1. S. H. Yoshimura, S. Khan, S. Ohno, T. Yokogawa, K. Nishikawa, T. Hosoya, H. Maruyama, Y. Nakayama, K. Takeyasu, Site-Specific Attachment of a Protein to a Carbon Nanotube End without Loss of Protein Function, Bioconjugate Chem., 23, 1488–1493 (2012).
Yousuke Takaoka
Assistant Professor, Graduate School of Engineering, Kyoto University
  1. K. Mizusawa, Y. Takaoka, I. Hamachi, Specific Cell Surface Protein Imaging by Extended Self-Assembling Fluorescent Turn-on Nanoprobes, J. Am. Chem. Soc., 134, 13386-13395 (2012).
Junko Ohkanda
Associate professor, Institute for Chemical Research, Kyoto University
  1. K. Kawakami, M.Hattori, T. Inoue, Y. Maruyama, J. Ohkanda, N. Kato, M. Tongu, T. Yamada, M. Akimoto, K. Takenaga, T. Sassa, J. Suzumiya, Y. Honma, A novel fusicoccin derivative preferentially targets hypoxic tumor cells and inhibits tumor growth in xenografts, Anticancer Agents Med. Chem., 12, 791-800 (2012).
  2. Y. Yamaguchi, N. Kato, H. Azuma, T. Nagasaki, J. Ohkanda, Protein recognition of hetero-/homoleptic ruthenium (II) tris(bipyridine)s for α-chymotrypsin and cytochrome c, Bioorg. Med. Chem. Lett., 22, 2354-2358 (2012).
  3. M. Takahashi, A. Kawamura, N. Kato, T. Nishi, I. Hamachi, J. Ohkanda, Phosphopeptide-dependent labeling of 14-3-3ζ proteins by fusicoccin-based fluorescent probes, Angew. Chem. Int. Ed., 51, 509-512 (2012).
Misako Aida
Professor, Graduate School of Science, Hiroshima University
  1. Misako Aida, Dai Akase, Hideo Doi, Tomoki Yoshida, Digraphs in Chemistry: All Possible Structures and Temperature-Dependent Distribution of Water Clusters, in J. Leszczynski, M. K. Shukla eds. “Practical Aspects of Computational Chemistry II,” Springer Netherlands, pp.49-68 (2012).
  2. Shunsuke Mieda, Misako Aida, Dipole Moments of Amino Acid Residues, Gly and Ala, in α-Helix: Quantum Chemical Building Blocks for Macrodipole Moment of α-Helical Polypeptide, Chemistry Letters, 41, 1579-1580 (2012).
Akira Otaka
Professor, Institute of Health Biosciences and Graduate School of Pharmaceutical Sciences,
The University of Tokushima
  1. K. Sakamoto, K. Sato, A. Shigenaga, K. Tsuji, S. Tsuda, H. Hibino, Y. Nishiuchi, A. Otaka. Synthetic procedure for N-Fmoc amino acyl-N-sulfanylethylaniline linker as crypto-peptide thioester precursor with practical application to native chemical ligation. J. Org. Chem. 2012, 77, 6948-6958.
  2. K. Ogura, A. Shigenaga, K. Ebisuno, H. Hirakawa, A. Otaka. Fmoc-based solid phase synthesis of adenylylated peptides using diester-type adenylylated amino acid derivatives. Tetrahedron Lett. 2012, 53, 3429-3432.
  3. A. Shigenaga, K. Ogura, H. Hirakawa, J. Yamamoto, K. Ebisuno, L. Miyamoto, K. Ishizawa, K. Tsuchiya, and A. Otaka. Development of reduction-responsive amino acid that induces peptide bond cleavage in hypoxic cells. ChemBioChem 2012, 13, 968-971.
  4. A. Otaka, K. Sato, H. Ding, and A. Shigenaga. One-pot/sequential native chemical ligation using N-sulfanylethylanilide peptide. Chem. Record 2012, 12, 479-490.
Hideo Takahashi
Professor, Graduate School of Medical Life Science, Yokohama City University
  1. T. Onizuka, H. Shimizu, Y. Moriwaki, T. Nakano, S. Kanai, I. Shimada, and H. Takahashi, NMR study of ligand release from asialoglycoprotein receptor under solution conditions in early endosomes, FEBS J. 279, 2645-2656 (2012)
  2. T. Sugiki, K. Takeuchi, T. Yamaji, T. Takano, Y. Tokunaga, K. Kumagai, K. Hanada, H. Takahashi, and I. Shimada, Structural Basis for the Golgi Association by the Pleckstrin Homology Domain of the Ceramide Trafficking Protein (CERT), J. Biol. Chem., 287, 33706-33718 (2012)
  3. T. Sugiki, O. Ichikawa, M. Miyazawa-Onami, I. Shimada, and H. Takahashi, Isotopic labeling of heterologous proteins in the yeast Pichia pastoris and Kluyveromyces lactis, Molecular Biology (Protein NMR techniques 3rd edit.), 831, 19-36 (2012)
  4. Y. Mizukoshi, A. Abe, T. Takizawa, H. Hanzawa, Y. Fukunishi, I. Shimada, and H. Takahashi, An accurate pharmacophore mapping method by NMR spectroscopy, Angew. Chem. Int. Ed. 51, 1362-1365 (2012)
Toshiyuki Kan
Professor, School of Pharmaceutical Sciences, University of Shizuoka
  1. S. Matsumoto, T. Asakawa, Y. Hamashima, T. Kan, A Short-step Asymmetric Synthesis of Dehydrodiconiferyl Alcohol via C-H Insertion Reaction, Synlett, 1082-1084 (2012).
  2. H. Ushikubo, S. Watanabe, Y. Tanimoto, K. Abe, A. Hiza, T. Ogawa, T. Asakawa, T. Kan, T. Akaishi, 3,3′,4′,5,5′-Pentahydroxyflavone is a potent inhibitor of amyloid fibril formation, Neuroscience Letters, 513, 51-56 (2012).
  3. A. Yoshida, M. Akaiwa, Y. Hamashima, S. Yokoshima, T. Fukuyama T. Kan, Total Synthesis of (-)-Lemonomycin, Chem. Eur. J. 18, 11192-11195 (2012).
  4. K. Uchida, T. Ogawa, Y. Yasuda, H. Mimura, T. Fujimoto, T. Fukuyama, T. Wakimoto, T. Asakawa, Y. Hamashima T. Kan, Stereocontrolled Total Synthesis of (+)- UCS1025A Angew. Chem. Int. Ed, 51, 12850-12853, (2012).
  5. R. Mabuchi, A. Kurita, N. Miyoshi, A. Yokoyama, T. Furuta, T. Goda, Y. Suwa, T. Kan, T. Amagai, H. Ohshima, Analysis of Nε-ethyllysine in human plasma proteins by gas chromatography-negative ion chemical ionization/mass spectrometry as a biomarker for exposure to acetaldehyde and alcohol, Alcoholism: Clinical & Experimental Research, 36, 1013-1020, (2012).
  6. K. Ikeuchi, S. Ido, S. Yoshimura, T. Asakawa, M. Inai, Y. Hamashima, T. Kan, Catalytic Desymmetrization of Cyclohexadienes by Asymmetric Bromolactonization, Org. Lett., 14, 6016-6019, (2012).
Hiroyuki Nakamura
Professor, Gakushuin Iniversity /Tokyo Institute of Technology
  1. H. Nakamura, N. Ueda, H. B. Ban, M. Ueno, S. Tachikawa, Design and synthesis of fluorescence-labeled closo-dodecaborate lipid: liposome formation and in vitro and in vivo imaging targeting to tumor for boron neutron capture therapy, Org. Biomol. Chem., 10, 1374-1380 (2012).
  2. T. Sugiishi and H. Nakamura, Zinc(II)-Catalyzed Redox Cross-Dehydrogenative Coupling of Propargylic Amines and Terminal Alkynes for Synthesis of N-Tethered 1,6-Enynes, J. Am. Chem. Soc., 134, 2504-2507 (2012).
  3. H. Nakamura, H. Kuroda, H. Minegishi, Synthesis and biological evaluation of boronic acid containing phenstatin analogues, ARKIVOC, 79-87 (2012).
  4. H. S. Ban, K. Shimizu, H. Minegishi, H. Nakamura, Identification of heat shock protein 60 as the regulator of the hypoxia-inducible factor sub-unit HIF-1α, Pure Appl. Chem., 84, 2325-2337 (2012).
  5. N. Fujimoto, M. Sakai, K. Ishii, H. Nakamura, Y. Kaneda, K. Awazu, In vitro investigation of efficient Photodynamic Therapy using non-viral vector; Hemagglutinating virus of Japan envelope, J. Biomed. Opt., 17, 078002 (2012).
  6. Y. Kim and H. Nakamura, Copper(I)-catalysed deacetylenative cross-coupling reaction of terminal alkynes with propargylic amines via C(sp)-C(sp3) bond cleavage, Synlett, 23, 1686-1690 (2012).
  7. M. Uno, Y. Koma, H. S. Ban, H. Nakamura, Discovery of 1-[4-(N-Benzylamino)phenyl]-3- phenylurea Derivatives as Non-Peptidic Selective SUMO-Sentrin Specific Protease (SENP)1 Inhibitors, Bioorg. Med. Chem. Lett., 22, 5169-5173 (2012).
  8. A. Takeuchi, M. Hori, S. Sato, H. S. Ban, T. Kuchimaru, S. Kizaka-Kondoh, T. Yamori, H. Nakamura, Synthesis and biological evaluation of furylindazoles as hypoxia inducible factor (HIF)-1α inhibitors, Med. Chem. Commun., 3, 1455-1461 (2012).
Nobuyuki Kanzawa
Associate Professor, Faculty of Science and Technology, Sophia University
  1. C.C. Chatrachatchaya, K. Wiengsamut, S. Chanthai, N. Sattayasai, T. Tamiya, N. Kanzawa, T. Tsuchiya, Fish Physiology Biochemistry 38, 1533-1543 (2012).
Yu Nakagawa
Senior Research Scientist, RIKEN
  1. Y. Nakagawa, Y. Ito, Carbohydrate-binding molecules with non-peptidic skeletons, Trends Glycosci. Glycotechnol., 24, 1-12 (2012).
  2. Y. Nakagawa, T. Doi, K. Takegoshi, Y. Igarashi, Y. Ito, Solid-state NMR analysis of calcium and D-mannose binding of BMY-28864, a water-soluble analogue of pradimicin A, Bioorg. Med. Chem. Lett., 22, 1038-1041 (2012).
  3. Y. Nakagawa, Y. Ito, Molecular architecture and therapeutic potential of lectin mimics. Adv. Carbohydr. Chem. Biochem., 68, 1-58 (2012).
Makoto Muroi
Senior Research Scientist, RIKEN
  1. Y. Futamura, M. Kawatani, S. Kazami, K. Tanaka, M. Muroi, T. Shimizu, K. Tomita, N. Watanabe and H. Osada, Morphobase, an Encyclopedic Cell Morphology Database, and Its Use for Drug Target Identification. Chem. Biol., 19, 1620-1630 (2012).
  2. Y. Asami, J. H. Jang, N. K. Soung, L. He, D. O. Moon, J. W. Kim, H. Oh, M. Muroi, H. Osada, B. Y. Kim, J. S. Ahn, Protuboxepin A, a marine fungal metabolite, inducing metaphase arrest and chromosomal misalignment in tumor cells. Bioorg. Med. Chem., 20, 3799-3806 (2012).
  3. 【Co-Study】Sasazawa Y, Kanagaki S, Tashiro E, Nogawa T, Muroi M, Kondoh Y, Osada H, Imoto M. Xanthohumol Impairs Autophagosome Maturation through Direct Inhibition of Valosin-Containing Protein. ACS Chemical Biology, 7, 892-900 (2012)

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