Publications: 2000-2004

740) I. Namatame, H. Tomoda, M. Arai, and S. Ōmura: Effect of fungal metabolites cytochalasans on lipid droplet formation in mouse macrophages. J. Antibiot., 53, 19-25 (2000).

741) K. Otoguro, K. Shiomi, Y. Yamaguchi, N. Arai, T. Sunazuka, R. Masuma, Y. Iwai, and S. Ōmura: Arisugacins C and D, novel acetylcholinesterase inhibitors and their related novel metabolites produced by Penicillium sp. FO-4259-11. J. Antibiot., 53, 50-57 (2000).

742) M. Desaki, H. Takizawa, T. Ohtoshi, T. Kasama, K. Kyobayashi, T. Sunazuka, S. Ōmura, K. Yamamoto, and K. Ito: Erythromycin suppresses nuclear Factor-B and activator protein-1 activation in human bronchial epithelial cells. Biochem. Biophys. Res. Comm., 267, 124-128 (2000).

743) M. Zhao, H. Kiyoi, Y. Yamamoto, M. Ito, M. Towatari, S. Ōmura, T. Kitamura, R. Ueda, H. Saito, and T. Naoe. In vivo treatment of mutant FLT3-transformed murine leukemia with a tyrosine kinase inhibitor. Leukemia, 14, 374-378 (2000).

744) I. Namatame, H. Tomoda, and S. Ōmura. Screening for novel inhibitors of macrophage-derived foam cell formation as potential anti-atherosclerotic agents (Review article, in Japanese). Bioscience and Industry, 58, 193-194 (2000).

745) T. Sunazuka, T. Hirose, T. Shirahata, Y. Harigaya, M. Hayashi, K. Komiyama, S. Ōmura, and A. B. Smith, III: Total synthesis of (＋)-madindoline A and (-)-madindoline B, potent, selective inhibitors of interleukin 6. Determination of the relative and absolute configurations. J. Am. Chem. Soc., 122, 2122-2123 (2000).

746) T. Hirose, T. Sunazuka, T. Z.-Ming, M. Handa, R. Uchida, K. Shiomi, Y. Hariyaga, and S. Ōmura: Novel protein farnesyltransferase inhibitors, and absolute structures of kurasoins A and B. Heterocycles, 53, 777-784 (2000).

747) K. Shiomi, N. Arai, Y. Iwai, A. Turberg, H. Kolbl, and S. Ōmura: Structure of argifin, a new chitinase inhibitor produced by Gliocladium sp. Tetrahedron Lett., 41, 2141-2143 (2000).

748) R. Obata, T. Sunazuka, Y. Harigaya, M. Hayashi, M-C. Rho,. H. Tomoda, and S. Ōmura: Structure-activity relationships study of pyripyropenes: reversal of cancer cell multidrug resistance. J. Antibiot., 53, 422-425 (2000).

749) Z. Li, T. Sunazuka, R. Yamada, Y. Kato, A. Enomoto, M. Hayashi, Y. Harigaya, and S. Ōmura: Synthesis and antiangiogenic activity of staurosporine derivatives. J. Antibiot., 53, 426-429 (2000).

750) Y. Ogiso, A. Tomida, S. Lei, S. Ōmura, and T. Tsuruo: Proteasome inhibition circumvents solid tumor resistance to topoisomerase II-directed drugs. Cancer Res., 60, 2429-2434 (2000).

751) F. Sako, S. Marui, N. Inatomi, Z. Itoh, and S. Ōmura: EM-574, an erythromycin derivative, improves delayed gastric emptying of semi-solid meals in conscious dogs. European J. Pharmacol., 395, 165-172 (2000).

752) P. Masdehors, H. M.-Beral, K. Maloum, S. Ōmura, H. Magdelenat, and J. Delic: Deregulation of the ubiquitin system and p53 proteolysis modify the apoptotic response in B-CLL lymphocytes. Blood, 96, 269-274 (2000).

753) R. Obata, T. Sunazuka, K. Otoguro, H. Tomoda, Y. Harigaya, and S. Ōmura: Synthetic conversion of ACAT inhibitor to acetylcholinesterase inhibitor. Bioorg. Med. Chem. Lett., 10, 1315-1316 (2000).

754) S. Ōmura, N. Arai, Y. Yamaguchi, R. Masuma, Y. Iwai, M. Namikoshi, A. Turberg, H. Kolbl, and K. Shiomi: Argifin, a new chitinase inhibitor, produced by Gliocladium sp. FTD 0668. I. Taxonomy, fermentation, and biological activities. J. Antibiot., 53, 603-608 (2000).

755) N. Arai, K. Shiomi, Y. Iwai, and S. Ōmura: Argifin, a new chitinase inhibitor, produced by Gliocladium sp. FTD-0668. II. Isolation, physico-chemical properties, and structure elucidation. J. Antibiot., 53, 609-614 (2000).

756) H. Ostrowska, C. Wojcik, S. Wilk, S. Ōmura, L. Kozlowski, T. Stoklosa, K. Worowski, P. Radziwon: Separation of cathepsin A-like enzyme and proteasome: evidence that lactacystin/b-lactone is not a specific inhibitor of the proteasome. J. Biochem. Cell Biol., 32, 747-757 (2000).

757) M. F.-Irie, M. Ito, Y. Amaya, N. Amizuka, H. Ozawa, S. Ōmura, Y. Ikehara, and K. Oda: Possible interference between tissue-non-specific alkaline phosphatase with an Arg54→Cyc substitution and a counterpart with an Asp277→Ala substitution found in a compound heterozygote associated with severe hypophosphatasia. Biochem. J., 348, 633-642 (2000).

758) F. Tokunaga, S. Takeuchi, S. Ōmura, P. Arvan, and T. Koide: Secretion, γ-carboxylation, and endoplasmic reticulum-associated degradation of chimeras with mutually exchanged Gla domain between human protein C and prothrombin. Thrombosis Res., 33, 511-521 (2000).

759) N. Arai, K. Shiomi, Y. Yamaguchi, R. Masuma, Y. Iwai, A. Turberg, H. Kolbl, and S. Ōmura: Argadin, a new chitinase inhibitor, produced by Clonostachys sp. FO-7314. Chem. Pharm. Bull., 48, 1442-1446 (2000).

760) H. Tomoda and S. Ōmura: Lactacystin, a proteasome inhibitor: Discovery and its application in cell biology (Review article in Japanese).Yakugaku Zasshi, 120, 935-949 (2000).

761) M.-C. Rho, M. Hayashi, A. Fukami, R. Obata, T. Sunazuka, H. Tomoda, K. Komiyama, and S. Ōmura: Reversal of multidrug resistance by 7-O-benzoylpyripyropene A in multidrug-resitant tumor cells. J. Antibiot., 53, 1202-1206 (2000).

762) A Fukami, T. Nakamura, K. Kawaguchi, M.-C. Roh, A. Matsumoto, Y. Takahashi, K. Shiomi, M. Hayashi, K. Komiyama, and S. Ōmura; A new antimicrobial antibiotic from Actinoplanes capillaceus sp. K95-5561T. J. Antibiot., 53, 1212-1214 (2000).

763) A. Fukami, T. Nakamura, Y.-P. Kim, K. Shiomi, M. Hayashi, T. Nagai, H. Yamada, K. Komiyama, and S. Ōmura: A new antiinfluenza virus antibiotic, 10-norparvulenone, from Microsphaeropsis sp. FO-5050. J. Antibiot., 53, 1215-1218 (2000).

764) M. Oohori, K. Otoguro, T. Sunazuka, K. Suzuki, Y. Iwai, and S. Ōmura: Effect of 14-membered ring macrolide compounds on rat leucocyte chemotaxis and the structure-activity relationships. J. Antibiot., 53, 1219-1222 (2000).

765) H. Gouda, T. Sunazuka, S. Ōmura, and S. Hirono: Three-dimensional structure-activity relationship analysis between motilin and motilide using conformational analysis and a novel molecular superimposing method. Chem. Pharm. Bull., 48, 1835-1837 (2000).

766) S. Ōmura, M. Hayashi, and H. Tomoda: Recent progress of the research on novel microbial metabolites (Review article). Pure Appl. Chem., 71, 1673-1681 (1999).

767) A. Matsumoto, Y. Takahashi, T. Kudo, A. Seino, Y. Iwai, and S. Ōmura: Actinoplanes capillaceus sp. nov., a new species of the genus Actinoplanes. Antoie van Leewenhock 78, 107-115 (2000).

768) S. Ōmura, H. Miyadera, H. Ui, K. Shiomi, Y. Yamaguchi, R. Masuma, T. Nagamitsu, D. Takano, T. Sunazuka, A, Harder, H. Kolbl, M. Namikoshi, H. Sakamoto, and K. Kita: An anthelmintic compound, nafuredin, shows selective inhibition of complex I in helminth mitochondria. Proc. Natl. Acad. Sci., USA, 98, 60-62 (2001).

769) L. Chen, L. Smith, M. A. Accavitti-Loper, S. Ōmura, J. B. Smith: Ubiquitylation and destruction of endogenous c-MycS by the proteasome: Are Myc boxes dispensable? Arch. Biochem. and Biophys., 374, 306-312 (2000).

770) L. Smith, L. Chen, M. E. Reyland, T. A. DeVries, R. V. Talanian, S. Ōmura, and J. B. Smith: Activation of a typical protein kinase Cz by caspase processing and degradation by the ubiquitin-proteasome system. J. Biol. Chem., 275, 40620-40627 (2000).

771) B.Wojcik, M. Bury, T. Stoklosa, A. Giermasz, W. Feleszko, I. Mlynarczuk, E. Pleban, G. Basak, S. Ōmura, and M. Jakobisiak: Lovastatin and simvastatin are modulators of the proteasome. J. Biochem. & Cell Biol., 32, 957-965 (2000).

772) H. Ui, K. Shiomi, Y. Yamaguchi, R. Masuma, T. Nagamitsu, D. Takano, T. Sunazuka, M. Namikoshi, and S. Ōmura: Nafuredin, a novel inhibitor of NADH-fumarate reductase, produced by Aspergillus niger FT-0554. J. Antibiot., 54, 234-238 (2001).

773) Y. Enomoto, K. Shiomi, A. Matsumoto, Y. Takahashi, Y. Iwai, A. Harder, H. Kolbl, H. Boyd Woodruff, and S. Ōmura: Isolation of a new antibiotic oligomycin G produced by Streptomyces sp. WK-6150. J. Antibiot., 54, 308-313 (2001).

774) J. Inokoshi, H. Chiba, S. Asanuma, A. Takahashi, S. Ōmura, and H. Tanaka: Molecular cloning of actinohivin, a novel anti-HIV protein from an actinomycete, and its expression in Escherichia coli. Biochem. Biophys. Res. Comm., 281, 1261-1265 (2001).

775) H. Chiba, J. Inokoshi, M. Okamoto, S. Asanuma, K. Matsuzaki, M. Iwama, K. Mizumoto, H. Tanaka, M. Oheda, K. Fujita, H. Nakashima, M. Shinose, Y. Takahashi, and S. Ōmura: Actinohivin, a novel anti-HIV protein from an actinomycete that inhibits syncytium formation: isolation, characterization, and biological activities. Biochem. Biophys. Res. Comm., 282, 5601 (2001).

776) D. Takano, T. Nagamitsu, H. Ui, K. Shiomi, Y. Yamaguchi, R. Masuma, I. Kuwajima, and S. Ōmura: Absolute configuration of nafuredin, a new specific NADH-fumarate reductase inhibitor. Tetrahedron Lett., 42, 3017-3020 (2001).

777) M. Handa, T. Sunazuka, K. Nagai, R. Kimura, T. Shirahata, Z.-M. Tian, K. Otoguro, Y. Harigaya, and S. Ōmura: Convergent synthesis of arisugacin skeletons and their acetyl-cholinesterase inhibitory activity. J. Antibiot., 54, 382-385 (2001).

778) M. Handa, T. Sunazuka, K. Nagai, R. Kimura, K. Otoguro, Y. Harigaya, and S. Ōmura: Determination of absolute stereochemistries of arisugacin F and Territrem B, novel acetylcholinestarase inhibitor. J. Antibiot., 54, 386-391 (2001).

779) H. Inazawa, K. Akagawa, M. Ohori, T. Sunazuka, K. Otoguro, and S. Ōmura: Action of macrolide antibiotics on human immunocompetent cells. Jap. J. Antibiot., 54, Suppl. A, 139-142 (2001).

780) L. Kozlowski, T. Stoklosa, S. Ōmura, C. Wojcik, M. Z. Wojtukiewicz, K. Worowski, H. Ostrowska: Lactacystin inhibits cathepsin A activity in melanoma cell lines. Tumor Biology, 22, 211-215 (2001).

781) M. Arai, H. Tomoda, A. Matsumoto, Y. Takahashi, H. B. Woodruff, N. Ishiguro , S. Kobayashi, and S. Ōmura: Deacetyl- ravidomycin M, a new inhibitor of IL-4 signal transduction, produced by Streptomyces sp. WK-6326. I. Taxonomy, fermentation, isolation and biological activities. J. Antibiot., 54, 554-561 (2001).

782) M. Arai, H. Tomoda, N. Tabata, N. Ishiguro, S. Kobayashi, and S. Ōmura: Deacetyl- ravidomycin M, a new inhibitor of IL-4 signal transduction, produced by Streptomyces sp. WK-6326. II. Structure elucidation. J. Antibiot., 54, 562-566 (2001).

783) A.Tournu, A. Obled, M.-P. Roux, M. Ferrara, S. Ōmura, and M. Bechet: Glucose regulates protein catabolism in ras-transformed fibroblasts through a lysosomal-dependent proteolytic pathway. Biochem. J., 357, 255-261(2001).

784) K. Takeuchi, S. Shibamoto, K. Nagamine, I. Shigemori, S. Ōmura, N. Kitamura, and F. Ito: Signaling pathways leading to transcription and translation cooperatively regulate the transient increase in expression of c-Fos protein. J. Biol. Chem., 276, 26077-26083 (2001).

785) K. Shiomi, H. Ui, and S. Ōmura: Nafuredin, a new anthelmintic antibiotic and its target, complex I (Review Article). Bioscience and Industry, 59, 37-38 (2001).

786) H. Tomoda and S. Ōmura: Screening for inhibitors of lipid metabolism. In Enzyme Technologies for Pharmaceutical and Biotechnological Applications (Review article). (eds. H. A. Kirst and Wu-Kuang Yeh, M. J. Zmijewski, Jr.), Marcel Dekker, Inc., 343-378 (2001).

787) D. Takano, T. Nagamitsu H. Ui, K. Shiomi, Y. Yamaguchi, R. Masuma, I. Kuwajima, and S. Ōmura: Total synthesis of nafuredin, a selective NADH-fumarate reductase inhibitor. Org. Lett., 3, 2289-2291 (2001).

788) H. Zhang, H. Tomoda, N. Tabata, H. Miura, M. Namikoshi, Y. Yamaguchi, R. Masuma, and S. Ōmura: Cladospolide D, a new 12-membered macrolide antibiotic, produced by Cladosporium sp. FT-0012. J. Antibiot., 54, 635-641 (2001).

789) K. Otoguro, A. Kohana, C. Manabe, A. Ishiyama, H. Ui, K. Shiomi, H. Yamada, and S. Ōmura: Potent antimalarial activities of polyether antibiotic, X-206. J. Antibiot., 54, 658-663 (2001).

790) H. Ikeda, T. Nonomiya, and S. Ōmura: Organization of biosynthetic gene cluster for avermectin in Streptomyces avermitilis: analysis of enzymatic domains in four polyketide synthases. J. Ind. Microbiol. & Biotechnol., 27, 170-176 (2001).

791) S. Ōmura, H. Ikeda, J. Ishikawa, A. Hanamoto, C. Takahashi, M. Shinose, Y. Takahashi, H. Horikawa, H. Nakazawa, T. Osonoe, H. Kikuchi, T. Shiba, Y. Sakaki, and M. Hattori : Genome sequence of an industrial microorganism, Streptomyces avermitilis: deducing the ability of producing secondary metabolites. Proc. Natl. Acad. Sci., USA, 98, 12215-12220 (2001).

792) K. Tajima, Y. Takahashi, A. Seino, Y. Iwai, and S. Ōmura: Description of two novel species of the genus Kitasatosporia, Kitasatospora cineracea sp. nov. and Kitasatospora niigatensis sp. Nov. Int. J. Syst. and Evol. Microbiol., 51, 1765-1771 (2001).

793) R. Masuma, Y. Yamaguchi, M. Noumi, S. Ōmura, and M. Namikoshi: Effect of sea water concentration on hyphal growth and antimicrobial metabolilte production in marine fungi. Mycoscience, 42, 455-459 (2001).

794) H. Chiba, S. Asanuma, M. Okamoto, J. Inokoshi, H. Tanaka, K. Fujita, and S. Ōmura: A simple screening system for anti-HIV drugs: syncytium formation assay using T-cell line tropic and macrophage tropic HIV env expressing cell lines-establishment and validation- J. Antibiot., 54, 818-826 (2001).

795) R. Uchida, H. Tomoda, M. Arai, and S. Ōmura: Chlorogentisylquinone, a new neutral sphingomyelinase inhibitor, produced by a marine fungus. J. Antibiot., 54, 882-889 (2001).

796) R. Blaise, P. Masdehors. A. Lauge, D. S.-Lyonnet, C. Alapetite, H. Merle-Beral, J.-L. Binet, S. Ōmura, H. Magdelenant, L. Sabatier, and J. Delic: Chromosomal DNA and p53 stability, ubiquitin system and apoptosis in B-CLL lymphocytes. Leukemia and Lymphoma, 42, 1173-1180 (2001).

797) T. Sunazuka, M. Handa, K. Nagai, T. Shirahata, Y. Harigaya, K. Otoguro, I. Kuwajima, and S. Ōmura: The first total synthesis of (+)-arisugasin A, a potent, orally bioavailable inhibitor of acetylcholinesterase. Org. Lett., 4, 367-369 (2002).

798) T. Sunazuka, T. Shirahata, K. Yoshida, D. Yamamoto, Y. Harigaya, T. Nagai, H. Kiyohara, H. Yamada, I. Kuwajima, and S. Ōmura: Total synthesis of pinellic acid, a potent oral adjuvant for nasal influenza vaccine. Determination of the relative and absolute configuration. Tetrahedron Lett., 43, 1265-1268 (2002).

799) T. Hirose, T. Sunazuka, T. Shirahata, D.Yamamoto, Y. Harigaya, I. Kuwajima, and S. Ōmura: Short total synthesis of (+)-madindolines A and B. Org. Lett., 4, 501-503 (2002).

800) H. Tomoda, T. Okuda, H. Wang, N. Tabata, R. Masuma, Y. Yamaguchi, and S. Ōmura: Funicone-related compounds, potentiators of antifungal miconazole activity, produced by Talaromyces flavus FKI-0076. J. Antibiot., 55, 172-180 (2002).

801) A. Fukami, K. Iijima, M. Hayashi, K. Komiyama, and S. Ōmura: Macrosphelide B suppressed metastasis through inhibition of adhesion of sLex/E-selectin molecules. Biochem. Biophys. Res. Comm., 291, 1065-1070 (2002).

802) I. Namatame, H. Tomoda, D. Matsuda, N. Tabata, S. Kobayashi, and S. Ōmura: K97-0239A and B, new inhibitors of macrophage foam cell formation, produced by Streptomyces sp. K97-0239. Proc. Japan Acad., 78, 45-50 (2002).

803) Y. Tsuchihashi, K. Oishi, H. Yoshimine, S. Suzuki, A. Kumatori, T. Sunazuka, S. Ōmura, K. Matsushima, and T. Nagatake: Fourteen-member macrolides suppress interleukin-8 production but do not promote apoptosis of activated neutrophils. Antimicrob. Agents and Chemother., 46, 1101-1104 (2002).

804) Y. Yamaguchi, R. Masuma, R. Uchida, M. Arai, H. Tomoda, and S. Ōmura: Phoma sp. FOM-8108, a producer of gentisylquinones, isolated from sea sand. Mycoscience, 43, 127-133 (2002).

805) D. R. Houston, K. Shiomi, N. Arai, S. Ōmura, M. G. Peter, A. Turberg, B. Synstad, V. G. H. Eijsink, and D. M. F. van Alten: High-resolution structures of a chitinase complexed with natural product cyclopentapeptide inhibitors: Mimicry of carbohydrate substrate. Proc. Natl. Acad. Sci., USA, 99, 9127-9132 (2002).

806) L. Yu, Y. Takahashi, A. Matsumoto, A. Seino, Y. Iwai, and S. Ōmura: Application of PCR for selection of Gram-positive bacteria with high DNA G+C content among new isolates. Actinomycetologica., 16, 1-5 (2002).

807) K. Shiomi and S. Ōmura: Discovery of new macrolides. In “Macrolide Antibiotics-Chemistry, Biology, and Practice”, ed., S. Omura, Academic Press, pp. 1-56 (2002).

808) T. Sunazuka, S. Iwasaki, and S. Ōmura: Chemical modification of macrolides (Review article). In “Macrolide Antibiotics-Chemistry, Biology, and Practice”, ed., S. Omura, Academic Press, pp.99-180 (2002).

809) H. Ikeda and S. Omura: Biosynthesis, regulation, and genetics of macrolide production (Review article). In “Macrolide Antibiotics-Chemistry, Biology, and Practice”, ed., S. Ōmura, Academic Press, pp. 285-326 (2002).

810) N. Inatomi, F. Sato, Z. Itoh, and S. Omura: Mode of action of macrolides with motilin agonistic activity-motilides (Review article). In “Macrolide Antibiotics-Chemistry, Biology, and Practice”, ed., S. Ōmura, Academic Press, pp. 501-531 (2002).

811) S. Ōmura: Mode of action of avermectin (Review article). In “Macrolide Antibiotics-Chemistry, Biology, and Practice”, ed., S. Omura, Academic Press, pp.571-576 (2002).

812) K. Otoguro, A. Ishiyama, H. Ui, M. Kobayashi, C. Manabe, G. Yan, Y. Takahashi, H. Tanaka, H. Yamada, and S. Ōmura: In vitro and in vivo antimalarial activities of the monoglycoside polyether antibiotic, K-41 against drug resistant strains of Plasmodia. J. Antibiot., 55, 832-834 (2002).

813) M. Hayashi, M.-C. Rho, A. Enomoto, A. Fukami, Y.-P. Kim, Y. Kikuchi, T. Sunazuka, T. Hirose, K. Komiyama, and S. Ōmura: Suppression of bone resportion by madindoline A, a novel nonpeptide antagonist to gp130. Proc. Natl. Acad. Sci., USA, 99, 14728-14739 (2002).

814) H. Uciro, K.Nagasawa, T. Sawa, J. Hasegawa, T. Kotake, Y.Sugiura, S. Kobayashi, K. Otoguro, and S. Ōmura: Remarkable influence of the aromatic substructure in 9-methoxy-strobilurin derivatives on their antifungal activity. Bioorg. Med. Chem. Lett., 13, 2699-2702 (2002).

815) H. Koga, H. Takanashi, Z. Ito, and S. Ōmura: Design, SAR and pharmacology of GM-611, the first acid-stable nonpeptide motilin receptor agonist (Review article). Drugs of the Future, 27, 255-272 (2002).

816) H. Tomoda, I. Namatame, and S. Ōmura: Microbial metabolites with inhibitory activity against lipid metabolism (Review article). Proc. Jap. Acad., 78, 217-240 (2002).

817) H. Tomoda, S. Kobayashi, and S. Ōmura: New antibiotics miyakamides produced by a fungus. J. Antibiot., 55, 952-961 (2002).

818) H. Tomoda, M. Arai, N. Koyama, H. Matsui, S. Ōmura, R. Obata, and Y. C. Lee: Accelerated degradation of mislocalized UDP-glucuronosyl- transferase family 1 (UGT1) protein in Gunn rat hepatocytes. Arch. Biochem. Biophys., 405, 163-169 (2002).

819) Y. Emi, S. Ōmura, S. Ikushiro, and T. Iyanagi: Purification of Shiga-like toxin 1 by pigeon egg white glycoproteins immobilized on Sepharose gels. Analytical Biochem., 311, 50-56 (2002).

820) I. Namatame, D. Matsuda, H. Tomoda, Y. Yamaguchi, R. Masuma, S. Kobayashi, and S. Omura: Selective production of fungal beauveriolide I or III by fermentation in amino acid-supplemented media. J. Antibiot., 55, 1048-1052 (2002).

821) Y. Takahashi, A. Matsumoto, A. Seino, J. Ueno, Y. Iwai, and S. Ōmura: Streptomyces avermectinius sp. nov., an avermectin-producing strain. Int. J. Syst. Evol. Microbiol., 52, 2163-2168 (2002).

822) Tomoda, N. Tabata, Y. Ohyama and S. Ōmura: Core structure in roselipins essential for eliciting inhibitory activity against diacylglycerol acyltransferase. J. Antibiot., 56, 24-29 (2003).

823) H. Miyadera, K. Shiomi, H. Ui, Y. Yamaguchi, R. Masuma, H. Tomoda, H. Miyoshi, A. Osanai, K. Kita, and S. Ōmura: Atpenins, potent and specific inhibitors of mitochondrial complex II (succinate-ubiquinone oxidoreductase). Proc. Natl. Acad. Sci., USA, 100, 473-477 (2003).

824) H. Ikeda and S. Ōmura: Studies on microbial products after the completion of genome sequence of Streptomyces –Diversity of genes involving secondary metabolite biosynthesis (Review article, in Japanese). Pharmacia 38, 829-833 (2002).

825) H. Ikeda, J. Ishikawa, and S. Ōmura: The genome sequence of soil bacterium Streptomyces (Review article, in Japanese). Tanpakushitu Kakusan Koso 47, 1845-1850 (2002).

826) H. Ikeda and S. Ōmura: Streptomyces (Review article, in Japanese). Kagaku to Seibutsu, 40, 694-700 (2002).

827) T. Shirahata, T. Sunazuka, K. Yoshida, D. Yamamoto, Y. Harigaya,T. Nagai, H. Kiyohara, H. Yamada, I. Kuwajima, and S. Ōmura: Total synthesis and adjuvant activity of all stereoisomers of pinellic acid. Bioorg. Med. Chem. Lett., 13, 937-941 (2003).

828) M. Handa, H. Ui, D. Yamamoto, S. Monma, Y. Iwai, T. Sunazuka, and S. Ōmura: Structure determination of lustromycin, an antibiotic against anaerobic bacteria. Heterocycle, 59, 497-500 (2003).

829) K. Otoguro, H. Ui, A. Ishiyama, N. Aria, M. Kobayashi,Y. Takahashi, R. Masuma, K. Shiomi, H. Yamada, and S. Ōmura: In vitro antimalarial activities of the microbial metabolites. J. Antibiot., 56, 322–324 (2003).

830) S. M. Gantt, J. M. Myung, M. R. S. Briones, W. D. Li, E. J. Corey, S. Omura, V. Nussenzweig, and P. Sinnis: Proteasome inhibitors block development of Plasmodium spp. Antimicrob. Agents Chemother., 42, 2731-2738 (1998)

831) A. Fukami, Y. Taniguchi, T. Nakamura, M.-C. Rho, K. Kawaguchi, M. Hayashi, K. Komiyama, and S. Ōmura: New members of the macrosphelides from Microsphaeropsis sp. FO-5050IV. J. Antibiot., 52, 501-504 (1999).

832) H. Ikeda, J. Ishikawa, A. Hanamoto, M. Shinose, H. Kikuchi, T. Shiba, Y. Sakaki, M. Hattori, and S. Ōmura: Complete genome sequence and comparative analysis of the industrial microorganism Streptomyces avermitilis. Nature Biotechnol., 21, 526-531 (2003).

833) Y.-P. Kim, H. Tomoda, K. Lizima, T. Fukuda, A. Matsumoto, Y. Takahashi, and S. Ōmura: Takanawaenses, novel antifungal antibiotics produced by Streptomyces sp. K99-5278. I. Taxonomy, fermentation, isolation and biological properties. J. Antibiot., 56, 448-453 (2003).

834) T. Fukuda, Y.-P. Kim, K. Iizima, H. Tomoda, and S. Ōmura: Takanawaenses, novel antifungal antibiotics produced by Streptomyces sp. K99-5278. II. Structure elucidation. J. Antibiot., 56, 454-458 (2003).

835) M. Arai, K. Yamamoto, I. Namatame, H. Tomoda, and S. Ōmura: New monordens produced by amidepsine-producing fungus Humicola sp. FO-2942. J. Antibiot., 56, 526-532 (2003).

836) K. Yamamoto, H. Hatano, M. Arai, K. Shiomi, H. Tomoda, and S. Ōmura: Structure elucidation of new monordens produced by Humicola sp. FO-2942. J. Antibiot., 56, 533-538 (2003).

837) T. Nagamitsu, D. Takano, K. Shiomi, H. Ui, Y. Yamaguchi, r. Masuma, Y. Harigaya, I. Kuwajima, and S. Ōmura: Total synthesis of nafuredin-γ, a γ-lactone related to nafuredin with selective inhibitory activity against NADH-fumarate reductase. Tetrahedron Lett., 44, 6441-6444 (2003).

838) T. Sunazuka, K. Yoshida, M. Oohori, K. Otoguro, Y. Harigaya, Y. Iwai, K. S. Akagawa, and S. Ōmura: Effect of 14-membered macrolide compounds on monocyte to macrophage differentiation. J. Antibiot., 56, 721-724 (2003).

839) K. Otoguro, H. Ui, A. Ishiyama, M. Kobayashi, H. Togashi, Y. Takahashi, R. Masuma, H. Tanaka, H. Tomoda, H. Yamada, and S. Ōmura: In vitro and in vivo antimalarial activities of a non-glycoside 18-membered macrolide antibiotic, borrelidin, against drug-resistant strains of Plasmodia. J. Antibot., 56, 727-729 (2003).

840) M. Handa, T. Sunazuka, A. Sugawara, Y. Harigaya, K. Otoguro, and S. Ōmura: Total synthesis of the AchE inhibitors (+)-arisugacins F and G. J. Antibiot., 56, 730-733 (2003).

841) Y. Takahashi and S. Ōmura: Isolation of new actinomycetes strains for the screening of new bioactive compounds (Review article). J. Gen. Appl. Microbiol., 49, 141-154 (2003).

842) Y. Takahashi, S. Katoh, N. Shikura, H. Tomoda, and S. Ōmura: Superoxide dismutase produced by soil bacteria increases bacterial colony growth from soil samples. J. Gen. Appl. Microbiol., 49, 263-266 (2003).

843) T. Takahashi, S. Kusaka, T. Doi, T. Sunazuka, and S. Ōmura: A combinatorial synthesis of a macrosphelide library utilizing a palladium-catalyzed carbonylation on a polymer support. Angew. Chem. Int. Ed., 42, 5230-5234 (2003).

844) A. Matsumoto, Y. Takahashi, M. Shinose, A. Seino, Y. Iwai, and S. Omura: Longispora albida gen. nov. sp. nov., a new genus of the family Micromonosporaceae. Int. J. Sys. Evol. Microbiol., 53, 1553-1559 (2003).

845) D. C. Lamb, H. Ikeda, D. R. Nelson, J. Ishikawa, T. Skaug, C. Jackson, S. Ōmura, M. R. Waterman, and S. L. Kelly: Cytochrome P450 complement (CYPome) of the avermectin-producer Streptomyces avermitilis and comparison to that of Streptomyces coelicolor A3(2). Biochem. Biophys. Res. Comm., 307, 610-619 (2003).

846) Y. Sakano, M. Shibuya, A. Matsumoto, Y. Takahashi, H. Tomoda, S. Ōmura, and Y. Ebizuka: Lanopylins, A1, B1, A2 and B2, novel lanosterol synthase inhibitors from Streptomyces sp. K99-5041. J. Antibiot., 56, 817-826 (2003).

847) K. Nagai, T. Sunazuka, K. Shiomi, A. Harder, A. Turberg, and S. Ōmura: Synthesis and biological activities of novel 4”-alkylidene avermectin derivatives. Bioorg. & Med. Chem. Lett., 13, 3943-3946 (2003).

848) K. Kumamoto, T. Ishikawa, and S. Ōmura: Chemistry of structurally confused kinamysins (Review article in Japanese). J. Synthetic Organic Chem. Japan, 62, 49-58 (2004).

849) D. Matsuda, I. Namatame, H. Tomoda, S. Kobayashi, R. Zocher, H. Kleinkauf, and S. Ōmura: New beauveriolides produced by amino acid-supplemented fermentation of Beauveria sp. FO-6979. J. Antibiot., 57, 1-9 (2004).

850) I. Namatame, H. Tomoda, S. Ishibashi, and S. Ōmura: Antiatherogenic activity of fungal beauveriolides, inhibitors of lipid droplet accumulation in macrophages. Proc. Natl. Acad. Sci., USA, 101, 737-742 (2004).

851) T. Fukuda, M. Arai, Y. Yamaguchi, R. Masuma,H. Tomoda, and S. Ōmura: New beauvericins, potentiators of antifungal miconazole activity, produced by Beauveria sp. FKI-1366. I. Taxonomy, fermentation, isolation and biological properties. J. Antibiot., 57, 110-116 (2004).

852) T. Fukuda, M. Arai, H. Tomoda, and S. Ōmura: New beauvericins, potentiators of antifungal miconazole activity, produced by Beauveria sp. FKI-1366. II. Structure elucidation. J. Antibiot., 57, 117-124 (2004).

853) S. Iwasaki and S. Ōmura: Cell-based screening strategy in the search for bioactive microbial secondary metabolites (Review article). Proc. Japan Acad. Ser. B, 80, 54-73 (2004).

854) K. Nagai, T. Sunazuka, and S. Ōmura: Synthesis of 4”-alkoxy avermectin derivatives using rhodium carbenoid mediated O-H insertion reaction. Tetrahedron lett., 45, 2507-2509 (2004).

855) Y. Yamaguchi, R. Masuma, Y.-P. Kim, R. Uchida, H. Tomoda, and S. Ōmura: Taxonomy and secondary metabolites of Pseudobotrytis sp. FKA-25. Mycoscience, 45, 9-16 (2004).

856) S. Nunome, A. Ishiyama, M. Kobayashi, K. Otoguro, H. Kiyohara, H. Yamada, and S. Ōmura: In vitro antimalarial activity of biflavonoids from Wikstroemia indica. Planta Med., 70, 77-79 (2004).

857) H. Chiba, J. Inokoshi, H. Nakshima, S. Ōmura, and H. Tanaka: Actinohivin, a novel anti-human immunodeficiency virus protein from an actinomycete, inhibits viral entry to cells by binding high-mannose type sugar chains of gp120. Biocem. Biophys. Res. Commun., 316, 203-210 (2004).

858) H. Tomoda, N. Ohbayashi, Y. Morikawa, H. Kumagai, and S. Ōmura: Binding site for fungal β-lactone hymeglucin on cytosolic 3-hydroxy-3-methylglutaryl coenzyme A synthase. Biochem. Biophys. Acta, 1636, 22-28 (2004).

859) A. T. Lada, M. Davis, C. Kent, J. Chapman, H. Tomoda, S. Ōmura, and L.L. Rudel: identification of ACAT1- and ACAT2-specific inhibitors using a novel, cell-based fluorescence assay: individual ACAT uniqueness. J. Lipid Res., 45, 378-386 (2004).

860) Xu Ping, Y. Takahashi, A. Seino, Y. Iwai, and S. Ōmura: Streptomyces scabrisporus sp. nov. Int. J. Syst. And Evol. Microbiol., 54, 577-581 (2004).

861) T. Nagamitsu, D. Takano, T. Fukuda, K. Otoguro, I. Kuwajima, Y. Harigaya, and S. Ōmura: Total synthesis of (-)-borrelidin. Organic Lett., 6, 1865-1867 (2004).

862) M. Desaki, H. Okazaki, T. Sunazuka, S. Ōmura, K. Yamamoto, and H. Takizawa: Molecular mechanisms of anti-inflammatory action of erythromycin in human bronchial epithelial cells: possible role in he signaling pathway that regulates nuclear factor-kB activation. Antimicrob. Agents and Chemother., 48, 1581-1582 (2004).

863) P. Khaomek, H. Kiyohara, K. Otoguro, H. Yamada, and S. Ōmura: Chemical constituents of Erythrina suberosa. Nature Medicine, 58, 84 (2004).

864) M. Arai, H. Sato, H. Kobayashi, M. Suganuma, T. Kawabe, H. Tomoda, and S. Ōmura: Selective inhibition of bleomycin-induced G2 cell cycle checkpoint by simaomicin a. Biochem. Biophys. Res. Comm., 317, 817-822 (2004).

865) N. Arai, M. Chikaraishi, M. Ikawa, S. Ōmura, and I. Kuwajima: Enantioselective preparation of asymmetrically protected 2-propanoyl-1,3-propanediol derivatives. Tetrahedron Asymmetry, 13, 733-741 (2004).

866) K. Otoguro, A. Ishiyama, M. Kobayashi, H. Sekiguchi, T. Izuhara, T. Sunazuka, H. Tomoda, and S. Omura: In vitro and in vivo antimalarial activities of a carbohydrate antibiotic, prumycin, against drug-resistant strains of Plasmodia. J. Antibiot., 57, 400-402 (2004).

867) Y. Koizumi, M. Arai, H. Tomoda, and S. Ōmura: Fungerin: A fungal alkaloid, arrests the cell cycle in M phase by inhibition of microtubule polymerization. J. Antibiot., 57, 415-420 (2004).

868) K. Shiomi and S. Ōmura: Antiparasitic agents produced by microorganisms. (Review article) Proc. Japan Acad. Ser. B., 40, 245-258 (2004).

869) T. Sunazuka, M. Handa, K. Nagai, T. Shirahata, Y. Harigaya, K. Otoguro, I. Kuwajima, and S. Ōmura: Absolute stereochemistries and total synthesis of (+)-arisugacins A and B, potent orally bioactive and selective inhibitors of acetylcholinesterase. Tetrahedron, 60, 7845-7859 (2004).

870) K. Nagai, K. Shiomi, T. Sunazuka, A. Harder, A. Turberg, and S. Ōmura: Synthesis and biological evaluation of novel 4”-alkoxy avermectin derivatives. Bioorg. Med. Chem. Lett., 14, 4135-4139 (2004).

871) Y. Koizumi, M. Arai, H. Tomoda, and S. Ōmura: Oxaline, a fungal alkaloid, arrests the cell cycle in M phase by inhibition of tubulin polymerization. Biochim. Biophys. Acta, 1693, 47-55 (2004).

872) S. Herai, Y. Hashimoto, H. Higashibata, H. Maseda, H. Ikeda, S. Ōmura, and M. Kobayashi: Hyper-inducible expression system for streptomycetes. Proc. Natl. Acad. Sci., USA., 101, 14031-14035 (2004)

873)Y. Sakano, M. Shibuya, Y. Yamaguchi, R. Masuma, H. Tomoda, S. Ōmura, and Y. Ebizuka: Epohelmins A and B, novel lanosterol synthase inhibitors from a fungal strain FKI-0929. J. Antibiot. 57, 564-568 (2004).

874) M. Arai, Y. Koizumi, H. Sato, T. Kawabe, M. Suganuma, H. Kobayashi, H. Tomoda, and S. Ōmura: Boromycin abrogates bleomycin-induced G2 checkpoint. J. Antibiot., 57, 662-668 (2004)

875) I. Ghosh, Y. Kishi, H. Tomoda, and S. Ōmura: Use of chiral praseodymium shift reagent in predicting the complete stereostructure of glisoprenin A. Organic Lett., 6, 4719-4711 (2004).

876) S. Ōmura and A. Crump: The life and times of ivermectin-a success story (Review article). Nature Rev. Microb., 2, 984-989 (2004).