Publications

[2023]

Hiroyuki Takahashi, Nao Miyoshi, Hisashi Murakami, Yuta Okamura, Naohisa Ogo, Akimitsu Takagi, Daisuke Muraoka and Akira Asai: Combined therapeutic effect of YHO-1701 with PD-1 blockade is dependent on natural killer cell activity in syngeneic mouse models. Cancer Immunol Immunother. (2023)

Asuka Shibuya, Akira Suzuki, Naohisa Ogo, Jun-ichi Sawada, Akira Asai and Hideshi Yokoyama: Crystal structure of the motor domain of centromere-associated protein E in complex with a non-hydrolysable ATP analogue. FEBS Letters, 597, 1138-1148 (2023)


[2022]

Saeko Yoshioka, Tomonori Ikeda, Sogo Fukuchi, Katsumi Ohta, Hisashi Murakami, Naohisa Ogo, Daisuke Muraoka, Osamu Takikawa, and Akira Asai: Identification and characterization of a novel dual inhibitor of indoleamine 2,3-dioxygenase 1 and tryptophan 2,3-dioxygenase. Int. J. Tryptophan Res.,15, 11786469221138456. (2022)

Eriko Hamasaki, Natsuki Wakita, Hiroki Yasuoka, Hikaru Nagaoka, Masayuki Morita, Eizo Takashima, Takayuki Uchihashi, Tetsuya Takeda, Tadashi Abe, Ji-Won Lee, Tadahiro Iimura, Moin A Saleem, Naohisa Ogo, Akira Asai, Akihiro Narita, Kohji Takei, and Hiroshi Yamada: The Lipid-Binding Defective Dynamin 2 Mutant in Charcot-Marie-Tooth Disease Impairs Proper Actin Bundling and Actin Organization in Glomerular Podocytes. Front. Cell Dev. Biol., 10, 884509, (2022)

Naohiro Yanagimura, Shinji Takeuchi, Koji Fukuda, Sachiko Arai, Azusa Tanimoto, Akihiro Nishiyama, Naohisa Ogo, Hiroyuki Takahashi, Akira Asai, Satoshi Watanabe, Toshiaki Kikuchi, Seiji Yano: STAT3 inhibition suppresses adaptive survival of ALK-rearranged lung cancer cells through transcriptional modulation of apoptosis. npj Precis Oncol. 6, 11 (2022)

Toshihiro Araki, Yuuki Watanabe, Yusuke Okada, Hisashi Murakami, Naohisa Ogo, Akira Asai: Identification of serum and glucocorticoid-regulated kinase 1 as a regulator of signal transducer and activator of transcription 3 signaling. Exp Cell Res. 413, 113079 (2022)

Yosuke Dotsu, Daisuk Muraoka, Naohisa Ogo, Yudai Sonoda, Kiyoshi Yasui, Hiroyuki Yamaguchi, Hideo Yagita, Hiroshi Mukae, Akira Asai, Hiroaki Ikeda: Chemical augmentation of mitochondrial electron transport chains tunes T cell activation threshold in tumors. J Immunother Cancer. 10, e003958 (2022)

Masaya Ono, Yoichi Sunagawa, Saho Mochizuki, Takahiro Katagiri, Hidemichi Takai, Sonoka Iwashimizu, Kyoko Inai, Masafumi Funamoto, Kana Shimizu, Satoshi Shimizu, Yasufumi Katanasaka, Maki Komiyama, Philip Hawke, Hideo Hara, Yoshiki Arakawa, Kiyoshi Mori, Akira Asai, Koji Hasegawa, Tatsuya Morimoto: Chrysanthemum morifolium Extract Ameliorates Doxorubicin-Induced Cardiotoxicity by Decreasing Apoptosis. Cancers 14, 683 (2022)


[2021]

Jun-Ichi Sawada, Kenji Matsuno, Naohisa Ogo, Akira Asai: Various effects of two types of kinesin-5 inhibitors on mitosis and cell proliferation. Biochem Pharmacol. 193, 114789 (2021)

Keisuke Taniguchi, Momomi Tsugane, Akira Asai: A Brief Update on STAT3 Signaling: Current Challenges and Future Directions in Cancer Treatment. J Cell Signal 2, 181-194 (2021)

Kenta Hayami, Yuichi Kuboki, Katsumi Ohta, Bangzhong Lin, Megumi Fumimoto, Kazuto Nunomura, Jun-Ichi Haruta, Kenichi Murai, Hiromichi Fujioka, Akira Asai, Mitsuhiro Arisawa: Design, Synthesis, Physical Properties and Indoleamine 2, 3-Dioxygenase 1 Inhibitory Activity of Substituted Indole Derivatives with N-H, N-Methoxymethyl, or N-Mehylthiomethyl Group toward Fragment-Based Drug Discovery. HETEROCYCLES 103, 511-525 (2021)

Ayuta Yamaguchi, Shinsuke Inuki, Katsumi Ohta, Shinya Oishi, Akira Asai, Hiroaki Ohno: Identification of a Novel Indoleamine 2,3-Dioxygenase Inhibitor Bearing an Eight-Membered Ring Fused Indole Scaffold and Its Structure-Activity Relationship. HETEROCYCLES 103, 331-347 (2021)

Keisuke Taniguchi, Hiroaki Konishi, Akiko Yoshinaga, Momomi Tsugane, Hiroyuki Takahashi, Fukiko Nishisaka, Yoshiyuki Shishido, and Akira Asai: Efficacy of combination treatment using YHO-1701, an orally active STAT3 inhibitor, with molecular-targeted agents on cancer cell lines. Sci Rep. 11, 6685 (2021)

Ryota Fukai, Naohisa Ogo, Taiki Ichida, Masayoshi Yamane, Jun-ichi Sawada, Nao Miyoshi, Hisashi Murakami, Akira Asai: Design, synthesis, and evaluation of a novel prodrug, a S-trityl-L-cysteine derivative targeting kinesin spindle protein. Eur J Med Chem. 215, 113288 (2021)

Asuka Shibuya, Naohisa Ogo, Jun-ichi Sawada, Akira Asai and Hideshi Yokoyama: Structure and comparison of the motor domain of centromere-associated protein E. Acta Cryst. D77, 280-287 (2021)

Miyuki Kumazawa, Manabu Tejima, Miwa Fukuda, Shota Takeda, Kenji Suzuki, Yukiko Mizumoto, Kakeru Sato, Minoru Waki, Hiroyuki Miyachi, Akira Asai, Osamu Takikawa, Tomoko Hashimoto, Osamu Ohno, and Kenji Matsuno: Discovery of carbono(di)thioates as indoleamine 2,3-dioxygenase 1 inhibitors. ACS Med Chem Lett. 12, 211-216 (2021)


[2020]

Fukiko Nishisaka, Keisuke Taniguchi, Momomi Tsugane, Genya Hirata, Akimitsu Takagi, Naoyuki Asakawa, Akinobu Kurita, Hiroyuki Takahashi, Naohisa Ogo, Yoshiyuki Shishido, Akira Asai: Antitumor activity of a novel oral STAT3 inhibitor YHO-1701. Cancer Sci. 111, 1774-1784 (2020)

Yumiko Suzuki, Ayana Otake, Satoshi Ueno, Kensuke Hayashi, Hirosuke Ishii, Nao Miyoshi, Kenta Kuroiwa, Masashi Tachikawa, Yuki Fujimaki, Kotaro Nishiyama, Kei Manabe, Ryuta Yamazaki, and Akira Asai: Discovery of a potent anticancer agent PVHD303 with in vivo activity. ACS Med Chem Lett. 11, 1287−1291 (2020)

Matteo Mori, Ettore Gilardoni, Luca Regazzoni, Alessandro Pedretti, Diego Colombo, Gary Parkinson, Akira Asai, Fiorella Meneghetti, Stefania Villa, Arianna Gelain: Towards the inhibition of protein-protein interactions (PPIs) in STAT3: insights into a new class of benzothiadiazole derivatives. Molecules 25, 3509 (2020)

Kouki Makitani, Naohisa Ogo, and Akira Asai: STX-0119, a novel STAT3 dimerization inhibitor, prevents fibrotic gene expression in a mouse model of kidney fibrosis by regulating Cxcr4 and Ccr1 expression. Physiol Rep. 8, e14627 (2020)


[2019]

Daisuke Muraoka, Naohiro Seo, Tae Hayashi, Yoshiro Tahara, Keisuke Fujii, Isao Tawara, Yoshihiro Miyahara, Kana Okamori, Hideo Yagita, Seiya Imoto, Rui Yamaguchi, Mitsuhiro Komura, Satoru Miyano, Masahiro Goto, Shin-ichi Sawada, Akira Asai, Hiroaki Ikeda, Kazunari Akiyoshi, Naozumi Harada, and Hiroshi Shiku: Antigen delivery targeted to tumor-associated macrophages overcomes tumor immune resistance. J Clin Invest. 129, 1278-1294 (2019)

Gelain Arianna, Mori Matteo, Meneghetti Fiorella, Porta Federica, Basil Livia e, Marverti Gaetano, Asai Akira, Hyeraci Mariafrancesca, García-Argá ez Aída Nelly, Via Lisa Dalla, Guccione Salvatore, Villa Stefania: Exploring the biological activity of a library of 1,2,5-oxadiazole derivatives endowed with antiproliferative activity. Anticancer Res. 39, 135-144 (2019)

Tastuya Koseki, Naoya Suehiro, Yoshiaki Masuda, Nao Miyoshi, Daisuke Muraoka, Naohisa Ogo, Akira Asai: Discovery of a new STAT3 inhibitor acting on the linker domain. Biol Pharm Bull. 42, 792-800 (2019)

Liujie Wu, Ayan Sadhukhan, Yuriko Kobayashi, Naohisa Ogo, Mutsutomo Tokizawa, Raj Kishan Agrahari, Hiroki Ito, Satoshi Iuchi, Masatomo Kobayashi, Akira Asai, Hiroyuki Koyama: Involvement of phosphatidylinositol metabolism in aluminum-induced malate secretion in Arabidopsis. J Exp Bot. 70, 3329-3342 (2019)

Jun-ichi Sawada, Hirosuke Ishii, Kenji Matsuno, Masayuki Sato, Yumiko Suzuki, and Akira Asai: Selective Inhibition of Spindle Microtubules by a Tubulin-Binding Quinazoline Derivative. Mol Pharmacol. 96, 609-618 (2019)

Masayoshi Yamane, Jun-ichi Sawada, Naohisa Ogo, Mai Ohba, Takayuki Ando, and Akira Asai: Identification of benzo[d]pyrrolo[2,1-b]thiazole derivatives as CENP-E inhibitors. Biochem Biophys Res Commun. 519, 505-511 (2019)

Tadashi Ashizawa, Akira Iizuka, Chie Maeda, Emiko Tanaka, Ryota Kondou, Haruo Miyata, Takashi Sugino, Takuya Kawata, Shoichi Deguchi, Koichi Mitsuya, Nakamasa Hayashi, Akira Asai, Mamoru Ito, Ken Yamaguchi, Yasuto Akiyama: Impact of combination therapy with anti-PD-1 blockade and a STAT3 inhibitor on the tumor-infiltrating lymphocyte status. Immunol Lett. 216, 43-50 (2019)


[2018]

Yusuke Okada, Taku Watanabe, Toru Shoji, Kyoko Taguchi, Naohisa Ogo, and Akira Asai: Visualization and quantification of dynamic STAT3 homodimerization in living cells using homoFluoppi. Sci Rep. 8, 2385 (2018)

Miwa Fukuda, Tomomi Sasaki, Tomoko Hashimoto, Hiroyuki Miyachi, Minoru Waki, Akira Asai, Osamu Takikawa, Osamu Ohno, and Kenji Matsuno: Cyclic analogue of S-benzylisothiourea that suppresses kynurenine production without inhibiting indoleamine 2,3-dioxygenase activity. Bioorg Med Chem Lett. 28, 2846-2849 (2018)

Hideshi Yokoyama, Jun-ichi Sawada, Kohei Sato, Naohisa Ogo, Nanami Kamei, Yoshinobu Ishikawa, Kodai Hara, Akira Asai, and Hiroshi Hashimoto: Structural and Thermodynamic Basis of the Enhanced Interaction between Kinesin Spindle Protein Eg5 and STLC-type Inhibitors. ACS Omega. 3, 12284–12294 (2018)


[2017]

Stanleyson V. Hato, Carl G. Figdor, Susumu Takahashi, Anja E. Pen, Altuna Halilovic, Kalijn F. Bol, Angela Vasaturo, Yukie Inoue, Nienke de Haas, Dagmar Verweij, Carla M.L. Van Herpen, Johannes H. Kaanders, Johan H.J.M. van Krieken, Hanneke W.M. Van Laarhoven, Gerrit K.J. Hooijer, Cornelis J.A. Punt, Akira Asai, I. Jolanda M. de Vries, and W. Joost Lesterhuis: Direct inhibition of STAT signaling by platinum drugs contributes to their anti-cancer activity. Oncotarget. 8, 54434-54443 (2017)

Daisuke Muraoka, Naohiro Seo, Tae Hayashi, Chisaki Hyuga-Amaike, Kana Okamori, Isao Tawara, Naozumi Harada, and Hiroshi Shiku: Signal-transducing adaptor protein-2 promotes generation of functional long-term memory CD8+ T cells by preventing terminal effector differentiation. Oncotarget. 8, 30766-30780 (2017)

Keisuke Fujii, Yoshihiro Miyahara, Naozumi Harada, Daisuke Muraoka, Mitsuhiro Komura, Rui Yamaguchi, Hideo Yagita, Junko Nakamura, Sahoko Sugino, Satoshi Okumura, Seiya Imoto, Satoru Miyano, and Hiroshi Shiku: Identification of an immunogenic neo-epitope encoded by mouse sarcoma using CXCR3 ligand mRNAs as sensors. OncoImmunology. e1306617 (2017)

Federica Porta, Giorgio Facchetti, Nicola Ferri, Arianna Gelain, Fiorella Meneghetti, Stefania Villa, Daniela Barlocco, Daniela Masciocchi, Akira Asai, Nao Miyoshi, Silvia Marchianò, Byoung-Mog Kwon, Yena Jin, Valentina Gandin, Cristina Marzano, and Isabella Rimoldi: An in vivo active 1,2,5-oxadiazole Pt(II) complex: a promising anticancer agent endowed with STAT3 inhibitory properties. Eur J Med Chem. 131, 196-206 (2017)

Mai Ohba, Tomoichiro Oka, Takayuki Ando, Saori Arahata, Asaka Ikegaya, Hirotaka Takagi, Naohisa Ogo, Chelsea Zhu, Kazuhiro Owada, Fumihiko Kawamori, Qiuhong Wang, Linda J Saif and Akira Asai: Antiviral effect of theaflavins against caliciviruses. J Antibiot. 70, 443-447 (2017)

Carlos Carbajales, Jun-ichi Sawada, Giovanni Marzaro, Eddy Sotelo, Luz Escalante, Antonio Sánchez-Díaz Marta, Xerardo García-Mera, Akira Asai, and Alberto Coelho: Multicomponent assembly of the kinesin spindle protein inhibitor CPUYJ039 and analogues as antimitotic agents. ACS Comb Sci. 19, 153-160 (2017)

Kazunori Iwamoto, Yutaka Uehara, Yukie Inoue, Kyoko Taguchi, Daisuke Muraoka, Naohisa Ogo, Kenji Matsuno, and Akira Asai: Inhibition of STAT3 by Anticancer Drug Bendamustine. PLoS One 12, e0170709 (2017)

Elena Gabriele, Chiara Ricci, Fiorella Meneghetti, Nicola Ferri, Akira Asai, and Anna Sparatore: Methanethiosulfonate derivatives as ligands of the STAT3-SH2 domain. J Enzyme Inhib Med Chem. 32, 337-344 (2017)

Haruo Miyata, Tadashi Ashizawa, Akira Iizuka, Ryota Kondou, Chizu Nonomura, Takashi Sugino, Kenichi Urakami, Akira Asai, Nakamasa Hayashi, Koichi Mitsuya, Yoko Nakasu, Ken Yamaguchi, And Yasuto Akiyama: Combination of a STAT3 Inhibitor and an mTOR Inhibitor Against a Temozolomide-resistant Glioblastoma Cell Line. Cancer Genomics Proteomics 14, 83-91 (2017)

Elena Gabriele, Federica Porta, Giorgio Facchetti, Corinna Galli, Arianna Gelain, Fiorella Meneghetti, Isabella Rimoldi, Sergio Romeo, Stefania Villa, Chiara Ricci, Nicola Ferri, Akira Asai, Daniela Barlocco, and Anna Sparatore: Synthesis of new dithiolethione and methanethiosulfonate systems endowed with pharmaceutical interest. Arkivoc. part ii, 235-250 (2017)

Elena Gabriele, Dario Brambilla, Chiara Ricci, Luca Regazzoni, Kyoko Taguchi, Nicola Ferri, Akira Asai, and Anna Sparatore: New sulfurated derivatives of cinnamic acids and rosmaricine as inhibitors of STAT3 and NF-κB transcription factors. J Enzyme Inhib Med Chem. 32, 1012-1028 (2017)

Yasuto Akiyama, Chizu Nonomura, Tadashi Ashizawa, Akira Iizuka, Ryota Kondou, Haruo Miyata, Takashi Sugino, Koichi Mitsuya, Nakamasa Hayashi, Yoko Nakasu, Akira Asai, Mamoru Ito, Yoshio Kiyohara, and Ken Yamaguchi: The anti-tumor activity of the STAT3 inhibitor STX-0119 occurs via promotion of tumor-infiltrating lymphocyte accumulation in temozolomide-resistant glioblastoma cell line. Immunol Lett. 190, 20-25 (2017)

Yumiko Suzuki, Jun-ichi Sawada, Paulina Hibner, Hirosuke Ishii, Kenji Matsuno, Masayuki Sato, Bernhard Witulski, and Akira Asai: Fluorescent anticancer quinazolines as molecular probes for β-tubulin colchicine site competition assay and visualization of microtubules as intracellular targeting sites. Dyes and Pigments 145, 233-238 (2017)

Akira Asai, and Kazuyuki Takakuma: Expression and purification of soluble STAT5b/STAT3 proteins for SH2 domain binding assay. SH2 Domains: Methods and Protocols, Machida K, Liu BA (Eds) Springer, New York, p351-356 (2017) book (chapter 9)

Akira Asai, and Kazuyuki Takakuma: Alpha-based Multiplexed Assay for Identifying SH2 Domain Antagonists. SH2 Domains: Methods and Protocols, Machida K, Liu BA (Eds) Springer, New York, p163-172 (2017) book (chapter 19)

浅井章良 新薬のためのコンセプトデザイン Biophilia 6 No.1, 22-28 (2017)


[2016]

Ryoko Okada-Iwasaki, Yuichi Takahashi, Yasuo Watanabe, Hiroshi Ishida, Jun-Ichi Saito, Ryuichiro Nakai, and Akira Asai: The discovery and characterization of K-756, a novel Wnt/β-catenin pathway inhibitor targeting tankyrase. Mol Cancer Ther. 15, 1525-1534 (2016)

Hajime Kashima, Fumiyasu Momose, Hiroshi Umehara, Nao Miyoshi, Naohisa Ogo, Daisuke Muraoka, Hiroshi Shiku, Naozumi Harada, and Akira Asai: Epirubicin, identified using a novel luciferase reporter assay for Foxp3 inhibitors, inhibits regulatory T cell activity. PLoS One. 11, e0156643 (2016)

Keiichiro Hayashi, Hiroyuki Michiue, Hiroshi Yamada, Katsuyoshi Takata, Hiroki Nakayama, Fan-Yan Wei, Atsushi Fujimura, Hiroshi Tazawa, Akira Asai, Naohisa Ogo, Hiroyuki Miyachi, Tei-ichi Nishiki, Kazuhito Tomizawa, Kohji Takei, and Hideki Matsui: Fluvoxamine, an anti-depressant, inhibits human glioblastoma invasion by disrupting actin polymerization. Sci Rep. 6, 23372 (2016)

Mai Ohba, Tomoichiro Oka, Takayuki Ando, Saori Arahata, Asaka Ikegaya, Hirotaka Takagi, Naohisa Ogo, Kazuhiro Owada, Fumihiko Kawamori, Qiuhong Wang, Linda J. Saif, and Akira Asai: Discovery and synthesis of heterocyclic carboxamide derivatives as potent anti-norovirus agents. Chem. Pharm. Bull. 64, 465-475 (2016)

Mari Takamiya, Masaaki Sakurai, Fumie Teranishi, Tomoko Ikeda, Tsutomu Kamiyama, and Akira Asai: Lead discovery for mammalian elongation of long chain fatty acids family 6 using a combination of high-throughput fluorescent-based assay and RapidFire mass spectrometry assay. Biochem Biophys Res Commun. 480, 721-726 (2016)

Jun-ichi Sawada, Ayumi Osawa, Tomoki Takeuchi, Masato, Kaneda, Shinya Oishi, Nobutaka Fujii, Akira Asai, Keiji Tanino and Kosuke Namba: Functional 1,3a,6a-triazapentalene scaffold: Design of fluorescent probes for kinesin spindle protein (KSP). Bioorg.Med. Chem Lett., 26, 5765-5769 (2016)

Giulio Poli, Arianna Gelain, Akira Asai, Adriano Martinelli, and Tiziano Tuccinardi: Identification of a new STAT3 dimerization inhibitor through a pharmacophore-based virtual screening approach. J Enzyme Inhib Med Chem. 31, 1011-1017 (2016)


[2015]

Naohisa Ogo, Yoshinobu Ishikawa, Jun-ichi Sawada, Kenji Matsuno, Akihiro Hashimoto, and Akira Asai: Structure-Guided Design of Novel L Cysteine Derivatives as Potent KSP Inhibitors. ACS Med. Chem. Lett., 6, 1004-1009 (2015)

Hideshi Yokoyama, Jun-ichi Sawada, Shiori Katoh, Kenji Matsuno, Naohisa Ogo, Yoshinobu Ishikawa, Hiroshi Hashimoto, Satoshi Fujii, and Akira Asai: Structural basis of new allosteric inhibition in kinesin spindle protein Eg5. ACS Chem. Biol., 10, 1128-1136 (2015)

Kenta Kuroiwa, Hirosuke Ishii, Kenji Matsuno, Akira Asai, and Yumiko Suzuki: Synthesis and Structure–Activity Relationship Study of 1-Phenyl-1-(quinazolin-4-yl)ethanols as Anticancer Agents. ACS Med. Chem. Lett., 6, 287-291 (2015)

Fiorella Meneghetti, Stefania Villa, Daniela Masciocchi, Daniela Barlocco, Lucio Toma, Dong-Cho Han, Byoung-Mog Kwon, Naohisa Ogo, Akira Asai, Laura Legnani, and Arianna Gelain: Ureido-Pyridazinone Derivatives: Insights into the Structural and Conformational Properties for STAT3 Inhibition. Eur. J. Org. Chem., 2015, 22, 4907-4912, (2015)

Giulio Polia, Arianna Gelain, Federica Porta, Akira Asai, Adriano Martinelli, and Tiziano Tuccinardi: Identification of a new STAT3 dimerization inhibitor through a pharmacophore-based virtual screening approach. J. Enzyme. Inhib. Med. Chem., Aug 26, 1-7 (2015)

浅井章良 がんの免疫逃避機構を標的とする新しい抗がん剤の開発 化学工業66 No.12, 13-21 (2015)

小郷尚久、浅井章良 新規KSP阻害剤の創製―システイン誘導体の合成と構造活性相関― MEDCHEM NEWS 25, 88-94 (2015)


[2014]

Silvia Dell'Orto, Daniela Masciocchi, Stefania Villa, Fiorella Meneghetti, Giuseppe Celentano, Daniela Barlocco, Diego Colombo, Laura Legnani, Lucio Toma, Yoon Jung Jeon, Byoung-Mog Kwon, Akira Asai, Arianna Gelain. Modeling, synthesis and NMR characterization of novel chimera compounds targeting STAT3. Med Chem Commun. 5, 1651-1657 (2014)

adashi Ashizawa, Yasuto Akiyama, Haruo Miyata, Akira Iizuka, Masaru Komiyama, Akiko Kume, Maho Omiya, Takashi Sugino, Akira Asai, Nakamasa Hayashi, Koichi Mitsuya, Yoko Nakasu, Ken Yamaguchi. Effect of the STAT3 inhibitor STX-0119 on the proliferation of a temozolomide-resistant glioblastoma cell line. Int J Oncol. 411-418 (2014)

Shuhei Kawamura, Yuka Unno, Akira Asai, Mitsuhiro Arisawa, Satoshi Shuto. Development of a new class of proteasome inhibitors with an epoxyketone warhead: Rational hybridization of non-peptidic belactosin derivatives and peptide epoxyketones. Bioorg Med Chem. 22, 3091-3095 (2014)

Tomoki Takeuchi, Shinya Oishi, Masato Kaneda, Ryosuke Misu, Hiroaki Ohno, Jun-ichi Sawada, Akira Asai, Shinya Nakamura, Isao Nakanishi, Nobutaka Fujii. Optimization of diaryl amine derivatives as kinesin spindle protein inhibitors. Bioorg Med Chem. 22, 3171-3179 (2014)

Tomoki Takeuchi, Shinya Oishi, Masato Kaneda, Hiroaki Ohno, Shinya Nakamura, Isao Nakanishi, Masayoshi Yamane, Jun-ichi Sawada, Akira Asai, Nobutaka Fujii. Kinesin spindle protein inhibitors with diaryl amine scaffolds: crystal packing analysis for improved aqueous solubility. ACS Med Chem Lett. 5, 566-571 (2014)

Shuhei Kawamura, Yuka Unno, Akira Asai, Mitsuhiro Arisawa, Satoshi Shuto. Structurally Novel highly potent proteasome inhibitors created by the structure-based hybridization of nonpeptidic belactosin derivatives and peptide boronates. J Med Chem. 57, 2726-2735 (2014)

Shuhei Kawamura, Yuka Unno, Takatsugu Hirokawa, Akira Asai, Mitsuhiro Arisawa, Satoshi Shuto. Rational hopping of a peptidic scaffold into non-peptidic scaffolds: structurally novel potent proteasome inhibitors derived from a natural product, belactosin A. Chem Commun. 2445-2447 (2014)

Hiroshi Yamada, Tadashi Abe, Shun-Ai Li, Shota Tago, Peng Huang, Masami Watanabe, Satoru Ikeda, Naohisa Ogo, Akira Asai, Kohji Takei. N’-[4-(dipropylamino)benzylidene]-2-hydroxybenzohydrazide is a dynamin GTPase inhibitor that suppresses cancer cell migration and invasion by inhibiting actin polymerization. Biochem Biophys Res Commun. 443, 511-517 (2014)

浅井章良 アカデミア創薬における特許出願と学術発表はジレンマとなるか? 実験医学 32, 120-125 (2014)


[2013]

Kazuyuki Takakuma, Naohisa Ogo, Yutaka Uehara, Susumu Takahashi, Hao Miyoshi, Akira Asai. Novel multiplexed assay for identifying SH2 domain antagonists of STAT family proteins. PLoS ONE 8, e71646 (2013)

Shuhei Kawamura, Yuka Unno, Akira Asai, Mitshiro Arisawa, Satoshi Shuto. Deisign and synthesis of the stabilized analog of belactosin A with the unnatural cis-cyclopropane structure. Org Biomol Chem. 6615-6622 (2013)

Daniela Masciocchi, Arianna Gelain, Federica Porta, Fiorella Meneghetti, Alessandro Pedretti, Giuseppe Celentano, Daniela Barlocco, Laura Legnani, Lucio Toma, Byoung-Mog Kwon, Akira Asai, Stefania Villa. New tricyclic pyridazinone derivatives as potential STAT3 inhibitors. Med Chem Commun. 4, 1181-1188 (2013)

Tadashi Ashizawa, Haruo Miyata, Akira Iizuka, Masaru Komiyama, Chie Oshita, Akiko Kume, Masahiro Nogami, Mika Yagoto, Ichiro Ito, Takuma Oishi, Reiko Watanabe, Koichi Mitsuya, Kenji Matsuno, Toshio Furuya, Tadashi Okawara, Masami Otsuka, Naohisa Ogo, Akira Asai, Yoko Nakasu, Ken Yamaguchi, Yasuto Akiyama. Effect of the STAT3 inhibitor STX-0119 on the proliferation of cancer stem-like cells derived from recurrent glioblastoma. Int J Oncol. 43, 219-227 (2013)

Shuhei Kawamura, Yuka Unno, Motohiro Tanaka, Takuma Sasaki, Akihito Yamano, Takatsugu Hirokawa, Tomoshi Kameda, Akira Asai, Mitsuhiro Arisawa, Satoshi Shuto. Investigation of the noncovalent binding mode of covalent proteasome inhibitors around the transition state by combined use of cyclopropylic strain-based conformational restriction and computational modeling. J Med Chem. 56, 5829-5842 (2013)

Shuhei Kawamura, Yuka Unno, Anja List, Akirai Mizuno, Motohiro Tanaka, Takuma Sasaki, Mitsuhiro Arisawa, Akira Asai, Michael Groll, Satoshi Shuto. Potent proteasome inhibitors derived from the unnatural
cis-cyclopropane isomer of belactosin A: synthesis, biological activity, and mode of action. J Med Chem. 56, 3689−3700 (2013)

Takashi Sato, Miho Iwase, Motoki Miyama, Masato Komai, Etsuo Ohshima, Akira Asai, Hiroshi Yano, Ichiro Miki. Internalization of CCR4 and Inhibition of Chemotaxis by K777, a Potent and Selective CCR4 Antagonist. Pharmacology 91, 305-313 (2013)

浅井章良、小郷尚久 創薬研究における点と線 ドラッグライクとドラッガブルの接点を探る 細胞工学 32, 644-648 (2013)


[2012]

Daniela Masciocchi, Stefania Villa, Fiorella Meneghetti, Alessandro Pedretti, Daniela Barlocco, Laura Legnani, Lucio Toma, Byoung-Mog Kwon, Shintaro Nakano, Akira Asai, Arianna Gelain. Biological and computational evaluation of an oxadiazole derivative (MD77) as a new lead for direct STAT3 inhibitors. Med Chem Commun. 3, 592-599 (2012)

Hiroshi Umehara, Akira Asai. Tributylhexadecylphosphonium bromide, a novel nuclear factor of activated T cells signaling inhibitor, blocks interleukin-2 induction associated with inhibition of p70 ribosomal protein S6 kinase phosphrylation. Biol Pharm Bull. 35, 805-809 (2012)

Shintaro Nakano, Kazushige Takai, Yoshinobu Isaka, Susumu Takahashi, Yuka Unno, Naohisa Ogo, Kenji Matsuno, Osamu Takikawa, Akira Asai. Identification of novel kynurenine production-inhibiting benzenesulfonamide derivatives in cancer cells. Biochem Biophys Res Commun. 419, 556-561 (2012)

Kenji Matsuno, Hiroshi Yamazaki, Yoshinobu Isaka, Kazushige Takai, Yuka Unno, Naohisa Ogo, Yoshinobu Ishikawa, Satoshi Fujii, Osamu Takikawa, Akira Asai. Novel candesartan derivatives as indoleamine 2,3-dioxygenase inhibitors. Med Chem Commun. 3, 475-479 (2012)

浅井章良, 松野研司 創薬標的としての転写因子STAT3, ファルマシア 48,673-677 (2012)


[2011]

Tomoki Takeuchi, Shinya Oishi, Toshiaki Watanabe, Hiroki Ohno, Jun-ichi Sawada, Kenji Matsuno, Akira Asai, Naoya Asada, Kazuo Kitaura, Nobutaka Fujii. Structure-Activity Relationships of Carboline and Carbazole Derivatives as a Novel Class of ATP-Competitive Kinesin Spindle Protein Inhibitors. J Med Chem. 54, 4839-4846 (2011)

Tadashi Ashizawa, Haruo Miyata, Hidee Ishii, Chie Oshita, Kenji Matsuno, Yoshiaki Masuda, Toshio Furuya, Tadashi Okawara, Masami Otsuka, Naohisa Ogo, Akira Asai, Yasuto Akiyama. Antitumor activity of a novel small molecule STAT3 inhibitor against a human lymphoma cell line with high STAT3 activation. Int. J. Oncol. 38, 1245-1252 (2011)


[2010]

Makiko Shimizu, Hirosuke Ishii, Naohisa Ogo, Yuka Unno, Kenji Matsuno, Jun-ichi Sawada, Yasuto Akiyama, Akira Asai. S-trityl-L-cysteine derivative induces caspase-independent cell death in K562 human chronic myeloid leukemia cell line. Cancer Lett. 298, 99-106 (2010)

Kenji Matsuno, Kazushige Takai, Yoshinobu Isaka, Yuka Unno, Masayuki Sato, Osamu Takikawa and Akira Asai. S-Benzylisothiourea derivatives as small-molecule inhibitors of indoleamine-2,3-dioxygenase. Bioorg. Med. Chem. Lett. 20, 5126-5129 (2010)

Shinya Oishi, Kentaro Watanabe, Saori Ito, Michinori Tanaka, Hiroki Nishikawa, Hiroaki Ohno, Kazuki Shimane, Kazuki Izumi, Yasuko Sakagami, Eiichi N. Kodama, Masao Matsuoka, Akira Asai and Nobutaka Fujii. Affinity selection and sequence-activity relationships of HIV-1 membrane fusion inhibitors directed at the drug-resistant variants. Med. Chem. Commun. 1, 276-281 (2010)

Shinya Oishi, Toshiaki Watanabe, Jun-ichi Sawada, Akira Asai: Hiroaki Ohno and Nobutaka Fujii. Kinesin spindle protein (KSP) inhibitors with 2,3-fused indole scaffolds. J. Med. Chem. 53, 5054-5058 (2010)

Kenji Matsuno, Yoshiaki Masuda, Yutaka Uehara, Hiroshi Sato, Ayumu Muroya, Osamu Takahashi, Takane Yokotagawa, Toshio Furuya, Tadashi Okawara, Masami Otsuka, Naohisa Ogo, Tadashi Ashizawa, Chie Oshita, Sachie Tai, Hidee Ishii, Yoshito Akiyama and Akira Asai. Identification of a new series of STAT3 inhibitors by virtual screening. ACS Med. Chem. Lett. 1, 371-375 (2010)

Makiko Shimizu, Hirosuke Ishii, Naohisa Ogo, Kenji Matsuno, Akira Asai. Biochemical analysis of cellular target of S-trityl-L-cysteine derivatives using affinity matrix. Bioorg. Med. Chem. Lett. 20, 1578-1580 (2010)

Tsuyoshi Oikawa, Yuka Unno, Kenji Matsuno, Jun-ichi Sawada, Naohisa Ogo, Kiyoshi Tanaka, Akira Asai Identification of a small-molecule inhibitor of the interaction between Survivin and Smac/DIABLO. Biochem. Biophys. Res. Commun. 393, 253-258 (2010)

Kenji Matsuno, Yutaka Uehara, Hiroshi Sato, Yoshiaki Masuda, Ayumu Muroya, Osamu Takahashi, Takane Yokotagawa, Toshio Furuya, Tadashi Okawara, Masami Otsuka, Naohisa Ogo, Tadashi Ashizawa, Chie Oshita, Sachie Tai, Hidee Ishii, Yoshito Akiyama, Akira Asai. Discovery of novel STAT3 dimerization inhibitors. Drugs of the Future 35 (Suppl. A) 111 (2010) [Proceeding]
Nobuyuki Suzuki, Naohisa Ogo, Yumie Maeda, Kazunori Takahashi, Akira Asai. Study on construction and the use of Shizuoka chemical library for the drug discovery in Fuji pharma valley. Bulletin of Shizuoka Institute of Environ. and Hyg. 53, 53-57 (2010)


[2009]

Hiroshi Yamada, Tadashi Abe, Shun-Ai Li, Yuki Masuoka, Mihoko Isoda, Masami Watanabe, Yasutomo Nasu, Hiromi Kumon, Akira Asai and Kohji Takei. Dynasore, a dynamin inhibitor, suppresses lamellipodia formation and cancer cell invasion by destabilizing actin filaments. Biochem. Biophys. Res. Commun. 390,1142-1148 (2009)

Hiroyuki Nakamura, Mizuyoshi Watanabe, Hyun Seung Ban, Wataru Nabeyama and Akira Asai. Synthesis and biological evaluation of boron peptide analogues of Belactosin C as proteasome inhibitors. Bioorg Med Chem Lett. 19, 3220-3224 (2009)

Yutaka Uehara, Masato Mochizuki, Kenji Matsuno, Takeharu Haino and Akira Asai. Novel high-throughput screening system for identifying STAT3-SH2 antagonists. Biochem Biophys Res Commun. 380, 627-631(2009)

Kenji Matsuno, Jun-ichi Sawada, Mina Sugimoto, Naohisa Ogo and Akira Asai. Bis(hetero)aryl derivatives as unique kinesin spindle protein inhibitors. Bioorg Med Chem Lett. 19, 1058-1061 (2009)

Keisuke Yoshida, Kazuya Yamaguchi, Akira Mizuno, Yuka Unno, Akira Asai, Takayuki Sone, Hideyoshi Yokosawa, Akira Matsuda, Mitsuhiro Arisawa and Satoshi Shuto. Three-dimensional structure-activity relationship study of belactosin A and its stereo- and regioisomers: development of potent proteasome inhibitors by a stereochemical diversity-oriented strategy. Org. Biomol. Chem. 7, 1868-1877 (2009)


[2008]

Makoto Yoshida, Yasuaki Kabe, Tadashi Wada, Akira Asai, and Hiroshi Handa. A new mechanism of 6-((2-(dimethylamino)ethyl)amino)-3-hydroxy-7H-indeno(2,1-c)quinolin-7-one dihydrochloride (TAS-103) action discovered by target screening with drug-immobilized affinity beads. Mol Pharmacol. 73, 987-994 (2008)

Masafumi Suzuki, Shoichiro Furukawa, Chikanori Kuramori, Chika Sawa, Yasuaki Kabe, Mitsuhiro Nakamura, Jun-ichi Sawada, Yuki Yamaguchi, Satoshi Sakamoto, Satoshi Inouye and Hiroshi Handa. Development of a chemical screening system using aqueorin-fused protein.  Biochem. Biophys. Res. Commun. 368, 600-605 (2008)

Keisuke Yoshida, Kazuya Yamaguchi, Takayuki Sone, Yuka Unno, Akira Asai, Hideyoshi Yokosawa, Akira Matsuda, Mitsuhiro Arisawa, and Satoshi Shuto. Synthesis of 2,3- and 3,4-methanoamino acid equivalents with stereochemical diversity and their conversion into the tripeptide proteasome inhibitor belactosin a and its highly potent cis-cyclopropane stereoisomer. Org. Lett. 10, 3571-3574 (2008)

Kenji Matsuno, Jun-ichi Sawada and Akira Asai. Therapeutic potential of mitotic kinesin inhibitors in cancer. Expert Opin. Ther. Patents 18, 253-274 (2008) [Review]

Kenji Matsuno, Jun-ichi Sawada, Mina Sugimoto, Naohisa Ogo and Akira Asai. Bis(hetero)aryl derivatives as unique KSP inhibitor. Drugs of the Future 33 (Suppl. A), 288 (2008) [Proceeding]


[2007]

Naohisa Ogo, Shinya Oishi, Kenji Matsuno, Jun-ichi Sawada, Nobutaka Fujii and Akira Asai. Synthesis and biological evaluation of l-cysteine derivatives as mitotic kinesin Eg5 inhibitors. Bioorg Med Chem Lett. 17, 3921-3924 (2007)


[2006]

Ryuichiro Nakai, Hiroyuki Ishida, Akira Asai, Harumi Ogawa, Yoshihiro Yamamoto, Hideki Kawasaki, Shiro Akinaga, Tamio Mizukami, and Yoshinori Yamashita. Telomerase Inhibitors Identified by a Forward Chemical Genetics Approach Using a Yeast Strain with Shortened Telomere Length. Chemistry & Biology 13, 183-190 (2006)

Shinya Oishi, Kazuhide Miyamoto, Ayumu Niida, Mikio Yamamoto, Keiichi Ajito, Hirokazu Tamamura, Akira Otaka, Yoshihiro Kuroda, Akira Asai and Nobutaka Fujii. Application of tri- and tetrasubstituted alkene dipeptide mimetics to conformational studies of cyclic RGD peptides. Tetrahedron 62, 1416-1424 (2006)

Yuka Unno, Teruo Akuta, Yu-ichiro Sakamoto, Seikoh Horiuchi, Takaaki Akaike. Nitric Oxide-induced downregulation of leptin production by 3T3-L1 adipocytes. Nitric Oxide, Jan, 24 (2006)