CURRICULUM VITAE
NAME
Akira Asai, Ph.D.
POSITION
Professor
Center for Drug Discovery
Graduate School of Pharmaceutical Sciences
ADDRESS52-1 Yada, Suruga-ku, Shizuoka, 422-8526, Japan
Phone: 81-54-264-5231
Fax: 81-54-264-5231
E-mail: aasai@u-shizuoka-ken.ac.jp
URL: http://w3pharm.u-shizuoka-ken.ac.jp/tansaku/
EDUCATION
Ph.D. (1996): Graduate School of Science and Technology, Keio University
M.S. (1989): Graduate School of Science and Technology, Keio University
B.S. (1987): Applied Chemistry, Keio University
PROFESSIONAL EXPERIENCE
2004 (Apr)-: Professor, Center for Drug Discovery, Graduate School of Pharmaceutical
Sciences, University of Shizuoka
2002-2004: Senior Scientist, Pharmaceutical Research Institutes, Kyowa Hakko Kogyo Co.
Ltd
2001-2002: Visiting Scientist, the Scripps Research Institute (USA)
2000-2001: Stuff Scientist, Pharmaceutical Research Institutes, Kyowa Hakko Kogyo Co.
Ltd.
1995 (Jun-Sep): Visiting Scientist, Geron Co. (USA)1989-2000: Stuff Scientist, Tokyo Research Laboratories, Kyowa Hakko Kogyo Co. Ltd.
RESEARCH INTERESTS
1) Assay development and lead discovery for new anticancer drug candidates
2) Chemical biology and medicinal chemistry for biologically active small molecules
PUBLICATIONS
1.

Yoshioka S, Ikeda T, Fukuchi S, Kawai Y, Ohta K, Murakami H, Ogo N, Muraoka D, Takikawa O, Asai
A. Identification and characterization of a novel dual inhibitor of indoleamine 2,3-dioxygenase 1 and1tryptophan 2,3-dioxygenase. Int J Tryptophan Res. 15, 11786469221138456 (2022)
2. Hamasaki E, Wakita N, Yasuoka H, Nagaoka H, Morita M, Takashima E, Uchihashi T, Takeda T, Abe T,
Lee J, Iimura T, Saleem M, Ogo N, Asai A, Narita A, Takei K, Yamada H. 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)
3. Yanagimura N, Takeuchi S, Fukuda K, Arai S, Tanimoto A, Nishiyama A, Ogo N, Takahashi H, Asai A,
Watanabe S, Kikuchi T, Yano S. npj Precis. Oncol. 6, 11 (2022)
4. Araki T, Watanabe Y, Okada Y, Murakami H, Ogo N, Asai A. Identification of serum andglucocorticoid-regulated kinase 1 as a regulator of signal transducer and activator of transcription 3
signaling. Exp. Cell Res. 413, 113079 (2022)
5. Dotsu Y, Muraoka D, Ogo N, Sonoda Y, Yasui K, Yamaguchi H, Yagita H, Mukae H, Asai A, Ikeda H.
Chemical augmentation of mitochondrial electron transport chains tunes T cell activation threshold intumors. J. Immunother. Cancer 10, e003958 (2022)
6. Ono M, Sunagawa Y, Mochizuki S, Katagiri T, Takai H, Iwashimizu S, Inai K, Funamoto M, Shimizu K,
Shimizu S, Katanasaka Y, Komiyama M, Hawke P, Hara H, Arakawa Y, Mori K, Asai A, Hasegawa K,
Morimoto T. Chrysanthemum morifolium Extract Ameliorates Doxorubicin-Induced Cardiotoxicity by
Decreasing Apoptosis. Cancers 14, 683 (2022)
7. Taniguchi K, Tsugane M, Asai A. A brief update on STAT3 signaling: current challenges and future
directions in cancer treatment. J Cell Signal. 2, 181-194 (2021)
8. Sawada J, Matsuno K, Ogo N, Asai A. Various effects of two types of kinesin-5 inhibitors on mitosis
and cell proliferation. Biochemical Pharmacol. 193, 114789 (2021)
9. Taniguchi K, Konishi H, Yoshinaga A, Tsugane M, Takahashi H, Nishisaka F, Shishido Y, Asai A.
Efficacy of combination treatment using YHO-1701, an orally active STAT3 inhibitor, withmolecular-targeted agents on cancer cell lines. Sci Rep. 11, 6685 (2021)
10. Fukai R, Ogo N, Ichida T, Yamane M, Sawada J, Miyoshi N, Murakami H, Asai A. 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)
11. Shibuya A, Ogo N, Sawada J, Asai A, Yokoyama H. Structure and comparison of the motor domain ofcentromere-associated protein E. Acta Cryst. D77, 280-287 (2021)
12. Yamaguchi A, Inuki S, Ohta K, Oishi S, Asai A, Ohno H. 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)
13. Hayami K, Kuboki Y, Ohta K, Lin B, Fumimoto M, Nunomura K, Haruta J, Murai K, Fujioka H, Asai A,
and Arisawa M. Design, synthesis, physical properties and indoleamine 2, 3-dioxygenase 1 inhibitory
activity of substitued indole derivatives with N-H, N-metohymethyl, or N-mehylthiomethyl group
toward fragment-based drug discovery. Heterocycles 103, 511-525 (2021)
14. Kumazawa M, Tejima M, Fukuda M, Takeda S, Suzuki K, Mizumoto Y, Sato K, Waki M, Miyachi H,
Asai A, Takikawa O, Hashimoto T, Ohno O, Matsuno K. Discovery of carbono(di)thioates as
indoleamine 2,3-dioxygenase 1 inhibitors. ACS Med Chem Lett. 12, 211–216 (2021)
15. Makitani K, Ogo N, Asai A. 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.
2

8, e14627 (2020)
16. Mori M, Gilardoni E, Regazzoni L, Pedretti A, Colombo D, Parkinson G, Asai A, Meneghetti F, Villa S,
Gelain A. Towards the inhibition of protein-protein interactions (PPIs) in STAT3: insights into a newclass of benzothiadiazole derivatives. Molecules 25, 3509 (2020)
17. Suzuki Y, Otake A, Ueno S, Hayashi K, Ishii H, Miyoshi N, Kuroiwa K, Tachikawa M, Fujimaki Y,
Nishiyama K, Manabe K, Yamazaki R, Asai A. Discovery of a potent anticancer agent PVHD303 within vivo activity. ACS Med Chem Lett. 11, 1287−1291 (2020)
18. Nishisaka F, Taniguchi K, Tsugane M, Hirata G, Takagi A, Asakawa N, Kurita A, Takahashi H, Ogo N,
Shishido Y, Asai A. Antitumor activity of a novel oral STAT3 inhibitor YHO-1701. Cancer Sci. 111,
1774-1784 (2020)
19. Ashizawa T, Iizuka A, Maeda C, Tanaka E, Kondou R, Miyata H, Sugino T, Kawata T, Deguchi S,
Mitsuya K, Hayashi N, Asai A, Ito M, Yamaguchi K, Akiyama Y. 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)20. Yamane M, Sawada JI, Ogo N, Ohba M, Ando T, Asai A. Identification of
benzo[d]pyrrolo[2,1-b]thiazole derivatives as CENP-E inhibitors. Biochem Biophys Res Commun. 519,
505-511 (2019)21. Sawada JI, Ishii H, Matsuno K, Sato M, Suzuki Y, Asai A. Selective Inhibition of Spindle Microtubules
by a Tubulin-Binding Quinazoline Derivative. Mol Pharmacol. 96, 609-618 (2019)
22. Wu L, Sadhukhan A, Kobayashi Y, Ogo N, Tokizawa M, Agrahari RK, Ito H, Iuchi S, Kobayashi M,
Asai A, Koyama H. Involvement of phosphatidylinositol metabolism in aluminum-induced malate
secretion in Arabidopsis. J Exp Bot. 70, 3329-3342 (2019)23. Muraoka D, Seo N, Hayashi T, Tahara Y, Fujii K, Tawara I, Miyahara Y, Okamori K, Yagita H, Imoto S,
Yamaguchi R, Komura M, Miyano S, Goto M, Sawada SI, Asai A, Ikeda H, Akiyoshi K, Harada N,
Shiku H. Antigen delivery targeted to tumor-associated macrophages overcomes tumor immune
resistance. J Clin Invest. 129, 1278-1294 (2019)24. Gelain A, Mori M, Meneghetti F, Porta F, Basile L, Marverti G, Asai A, Hyeraci M, García-Argáez AN,
Via LD, Guccione S, Villa S. Exploring the biological activity of a library of 1,2,5-oxadiazole
derivatives endowed with antiproliferative activity. Anticancer Res. 39, 135-144 (2019)
25. Koseki T, Suehiro N, Masuda Y, Miyoshi N, Muraoka D, Ogo N, Asai A. Discovery of a new STAT3
inhibitor acting on the linker domain. Biol. Pharm. Bull. 42, 792-800 (2019)26. Okada Y, Watanabe T, Shoji T, Taguchi K, Ogo N, Asai A. Visualization and quantification of dynamic
STAT3 homodimerization in living cells using homoFluoppi. Sci Rep. 8, 2385 (2018)27. Yokoyama H, Sawada J, Sato K, Ogo N, Kamei N, Ishikawa Y, Hara K, Asai A, Hashimoto H.
Structural and Thermodynamic Basis of the enhanced interaction between kinesin spindle protein Eg5
and STLC-type inhibitors. ACS Omega. 3, 12284–12294 (2018)
28. Fukuda M, Sasaki T, Hashimoto T, Miyachi H, Waki M, Asai A, Takikawa O, Ohno O, Matsuno K.
Cyclic analogue of S-benzylisothiourea that suppresses kynurenine production without inhibiting
indoleamine 2,3-dioxygenase activity. Bioorg Med Chem Lett. 28, 2846-2849 (2018)
29. Gabriele E, Brambilla D, Ricci C, Regazzoni L, Taguchi K, Ferri N, Asai A, Sparatore A. New
sulfurated derivatives of cinnamic acids and rosmaricine as inhibitors of STAT3 and NF-κB
3

transcription factors. J Enzyme Inhib Med Chem. 32, 1012-1028 (2017)30. Akiyama Y, Nonomura C, Ashizawa T, Iizuka A, Kondou R, Miyata H, Sugino T, Mitsuya K, Hayashi N,
Nakasu Y, Asai A, Ito M, Kiyohara Y, Yamaguchi K. The anti-tumor activity of the STAT3 inhibitor
STX-0119 occurs via promotion of tumor-infiltrating lymphocyte accumulation intemozolomide-resistant glioblastoma cell line. Immunol Lett. 190, 20-25 (2017)31. Suzuki Y, Sawada JI, Hibner P, Ishii H, Matsuno K, Sato M, Witulski B, Asai A. 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)32. Hato SV, Figdor CG, Takahashi S, Pen AE, Halilovic A, Bol KF, Vasaturo A, Inoue Y, de Haas N,
Verweij D, Van Herpen CML, Kaanders JH, van Krieken JHJM, Van Laarhoven HWM, Hooijer GKJ,
Punt CJA, Asai A, de Vries IJM, Lesterhuis WJ. Direct inhibition of STAT signaling by platinum drugs
contributes to their anti-cancer activity. Oncotarget 8. 54443 (2017)
33. Gabriele E, Ricci C, Ferri N, Asai A, Sparatorea A. Methanethiosulfonate derivatives as ligands of the
STAT3-SH2 domain. J Enzyme Inhib Med Chem. 32, 337-344 (2017)34. Porta F, Facchetti G, Ferri N, Gelain A, Meneghetti F, Villa S, Barlocco D, Masciocchi D, Asai A,
Miyoshi N, Marchianò S, Kwon BM, Gandin V, Marzano C, Rimoldi I. 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)35. Ohba M, Oka T, Ando T, Arahata S, Ikegaya A, Takagi H, Ogo N, Zhu C, Owada K, Kawamori F, Wang
Q, Saif LJ, Asai A. Antiviral effect of theaflavins against caliciviruses. J Antibiot. 70, 443-447 (2017)
36. Carbajales C, Sawada JI, Marzaro G, Sotelo E, Escalante L, Sánchez-Díaz Marta A, García-Mera X,
Asai A, Coelho A. Multicomponent assembly of the kinesin spindle protein inhibitor CPUYJ039 andanalogues as antimitotic agents. ACS Comb Sci. 19, 153–160 (2017)37. Iwamoto K, Uehara Y, Inoue Y, Taguchi K, Muraoka D, Ogo N, Matsuno K, Asai A. Inhibition of
STAT3 by Anticancer Drug Bendamustine. PLoS One 12, e0170709 (2017)38. Miyata H, Ashizawa T, Iizuka A, Kondou R, Nonomura C, Sugino T, Urakami K, Asai A, Hayashi N,
Mitsuya K, Nakasu Y, Yamaguchi K, Akiyama Y. Combination of a STAT3 Inhibitor and an mTOR
Inhibitor Against a Temozolomide-resistant Glioblastoma Cell Line. Cancer Genomics Proteomics 14,
83-91 (2017)
39. Gabriele E, Porta F, Facchetti G, Galli C, Gelain A, Meneghetti F, Rimoldi I, Romeo S, Villa S, Ricci C,
Ferri N, Asai A, Barlocco D, Sparatore A. Synthesis of new dithiolethione and methanethiosulfonate
systems endowed with pharmaceutical interest. Arkivoc. part ii, 235-250 (2017)
40. Asai A, Takakuma K. Expression and purification of soluble STAT5b/STAT3 proteins for SH2 domainbinding assay. SH2 Domains: Methods and Protocols, Machida K, Liu BA (Eds) Springer, New York,
p351-356 (2017) book (chapter)
41. Asai A, Takakuma K. 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)
42. Takamiya M, Sakurai M, Teranishi F, Ikeda T, Kamiyama T, Asai A. Lead discovery for mammalianelongation 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)4

43. Sawada JI, Osawa A, Takeuchi T, Kaneda M, Oishi S, Fujii N, Asai A, Tanino K, Namba K. Functional
1,3a,6a-triazapentalene scaffold: Design of fluorescent probes for kinesin spindle protein (KSP). Bioorg
Med Chem Lett. 26, 5765-5769 (2016)
44. Kashima H, Momose F, Umehara H, Miyoshi N, Ogo N, Muraoka D, Shiku H, Harada N, Asai A.
Epirubicin, identified using a novel luciferase reporter assay for Foxp3 inhibitors, inhibits regulatory T
cell activity. PLoS One 11, e0156643 (2016)
45. Okada IR, Takahashi Y, Watanabe Y, Ishida H, Saito J, Nakai R, Asai A. The discovery andcharacterization of K-756, a novel Wnt/β-catenin pathway inhibitor targeting tankyrase. Mol Cancer
Ther. 15, 1525-1534 (2016)
46. Ohba M, Oka T, Ando T, Arahata S, Ikegaya A, Takagi H, Ogo N, Owada K, Kawamori F, Wang Q, Saif
LJ, Asai A. Discovery and synthesis of heterocyclic carboxamide derivatives as potent anti-norovirus
agents. Chem Pharm Bull. 64, 465-475 (2016)
47. Hayashi K, Michiue H, Yamada H, Takata K, Nakayama H, Wei FY, Fujimura A, Tazawa H, Asai A,
Ogo N, Miyachi H, Nishiki T, Tomizawa K, Takei K, Matsui H. Fluvoxamine, an anti-depressant,inhibits human glioblastoma invasion by disrupting actin polymerization. Sci Rep. 6, 23372 (2016)
48. Poli G, Gelain A, Porta F, Asai A, Martinelli A, Tuccinardi T. Identification of a new STAT3
dimerization inhibitor through a pharmacophore-based virtual screening approach. J Enzyme Inhib Med
Chem. 31, 1011-1017 (2016)
49. Ogo N, Ishikawa Y, Sawada J, Matsuno K, Hashimoto A, Asai A. Structure-guided design of novel
L-Cysteine derivatives as potent KSP inhibitors. ACS Med Chem Lett. 6,1004-1009 (2015)
50. Meneghetti F, Villa S, Masciocchi D, Barlocco D, Toma L, Han DC, Kwon BM, Ogo N, Asai A,
Legnani L, Gelain A. Ureido-pyridazinone derivatives: Insights into the structural and conformational
properties for STAT3 inhibition. Eur J Org Chem. 22, 4907–4912 (2015)
51. Yokoyama H, Sawada J, Katoh S, Matsuno K, Ogo N, Ishikawa Y, Hashimoto H, Fujii S, Asai A.
Structural basis of new allosteric inhibition in Kinesin spindle protein Eg5. ACS Chem Biol. 10,
1128-1136 (2015)
52. Kuroiwa K, Ishii H, Matsuno K, Asai A, Suzuki Y. Synthesis and structure-activity relationship studyof 1-phenyl-1-(quinazolin-4-yl)ethanols as anticancer agents. ACS Med Chem Lett. 6, 287-291 (2015)
53. Dell'Orto S, Masciocchi D, Villa S, Meneghetti F, Celentano G, Barlocco D, Colombo D, Legnani L,
Toma L,. Jeon YJ, Kwon BM, Asai A, Gelain A. Modeling, synthesis and NMR characterization ofnovel chimera compounds targeting STAT3. Med Chem Commun. 5, 1651-1657 (2014)
54. Ashizawa T, Akiyama Y, Miyata H, Iizuka A, Komiyama M, Kume A, Omiya M, Sugino T, Asai A,
Hayashi N, Mitsuya K, Nakasu Y, Yamaguchi K. Effect of the STAT3 inhibitor STX-0119 on the
proliferation of a temozolomide-resistant glioblastoma cell line. Int J Oncol. 45, 411-418 (2014)
55. Kawamura S, Unno Y, Asai A, Arisawa M, Shuto S. 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)
56. Takeuchi T, Oishi S, Kaneda M, Misu R, Ohno H, Sawada JI, Asai A, Nakamura S, Nakanishi I, Fujii N.
Optimization of diaryl amine derivatives as kinesin spindle protein inhibitors. Bioorg Med Chem. 22,
3171-3179 (2014)
57. Takeuchi T, Oishi S, Kaneda M, Ohno H, Nakamura S, Nakanishi I, Yamane M, Sawada J, Asai A,
5

Fujii N. Kinesin spindle protein inhibitors with diaryl amine scaffolds: crystal packing analysis for
improved aqueous solubility. ACS Med Chem Lett. 5, 566-571 (2014)
58. Kawamura S, Unno Y, Asai A, Arisawa M, Shuto S. Structurally Novel highly potent proteasome
inhibitors created by the structure-based hybridization of nonpeptidic belactosin derivatives and peptideboronates. J Med Chem. 57, 2726-2735 (2014)
59. Kawamura S, Unno Y, Hirokawa T, Asai A, Arisawa M, Shuto S. Rational hopping of a peptidic
scaffold into non-peptidic scaffolds: structurally novel potent proteasome inhibitors derived from anatural product, belactosin A. Chem Commun. 50, 2445-2447 (2014)
60. Yamada H, Abe T, Li S, Tago S, Huang P, Watanabe M, Ikeda S, Ogo N, Asai A, Takei K.
N’-[4-(dipropylamino)benzylidene]-2-hydroxybenzohydrazide is a dynamin GTPase inhibitor thatsuppresses cancer cell migration and invasion by inhibiting actin polymerization. Biochem Biophys Res
Commun. 443, 511-517 (2014)
61. Takakuma K, Ogo N, Uehara Y, Takahashi S, Miyoshi N, Asai A. Novel multiplexed assay for
identifying SH2 domain antagonists of STAT family proteins PLoS One 8, e71646 (2013)
62. Kawamura S, Unno Y, Asai A, Arisawa M, Shuto S. Design and synthesis of the stabilized analogs ofbelactosin A with the unnatural cis-cyclopropane structure. Org Biomol Chem. 11, 6615-6622 (2013)
63. Masciocchi D, Gelain A, Porta F, Meneghetti F, Pedretti A, Celentano G, Barlocco D, Legnani L, Toma
L, Kwon B, Asai A, Villa S. Synthesis, structure–activity relationships and stereochemical
investigations of new tricyclic pyridazinone derivatives as potential STAT3 inhibitors Med Chem
Commun. 4, 1181-1188 (2013)
64. Ashizawa T, Miyata H, Iizuka A, Komiyama M, Oshita C, Kume A, Nogami M, Yagoto M, Ito I, Oishi
T, Watanabe R, Mitsuya K, Matsuno K, Furuya T, Okawara T, Otsuka M, Ogo N, Asai A, Nakasu Y,
Yamaguchi K, Akiyama Y. Effect of the STAT3 inhibitor STX-0119 on the proliferation of cancer
stem-like cells derived from recurrent glioblastoma. Int J Oncol. 43, 219-217 ( 2013)
65. Kawamura S, Unno Y, Tanaka M, Sasaki T, Yamano A, Hirokawa T, Kameda T, Asai A, Arisawa M,
Shuto S. Investigation of the non-covalent binding mode of covalent proteasome inhibitors around thetransition state by combined use of cyclopropylic strain-based conformational restriction andcomputational modeling. J Med Chem. 56, 5829-5842 (2013)
66. Sato T, Iwase M, Miyama M, Komai M, Ohshima E, Asai A, Yano H, Miki I. Internalization of CCR4and Inhibition of Chemotaxis by K777, a Potent and selective CCR4 antagonist. Pharmacology 91,
305-313 (2013)
67. Kawamura S, Unno Y, List A, Mizuno A, Tanaka M, Sasaki T, Arisawa M, Asai A, Groll M, Shuto S.
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)
68. Masciocchi D, Villa S, Meneghetti F, Pedretti A, Barlocco D, Legnani L, Toma L, Kwon B, Nakano S,
Asai A, Gelain A. Biological and computational evaluation of an oxadiazole derivative (MD77) as a
new lead for direct STAT3 inhibitors. Med Chem Commun.3, 592-599 (2012)
69. Umehara H, Asai A. 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)
70. Nakano S, Takai K, Isaka Y, Takahashi S, Unno Y, Ogo N, Matsuno K, Takikawa O, Asai A.
6

Identification of novel kynurenine production-inhibiting benzenesulfonamide derivatives in cancer cells.
Biochem Biophys Res Commun. 419, 556-561 (2012)
71. Matsuno K, Yamazaki H, Isaka Y, Takai K, Unno Y, Ogo N, Ishikawa Y, Fujii S, Takikawa O Asai A.
Novel candesartan derivatives as indoleamine 2,3-dioxygenase inhibitors. Med Chem Commun. 3,
475-479 (2012)
72. Takeuchi T, Oishi S, Watanabe T, Ohno H, Sawada JI, Matsuno K, Asai A, Asada N, Kitaura K, Fujii N.
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)
73. Ashizawa T, Miyata H, Ishii H, Oshita C, Matsuno K, Masuda Y, Furuya T, Okawara T, Otsuka M,
Ogo N, Asai A, Akiyama Y. Antitumor activity of a novel small molecule STAT3 inhibitor against ahuman lymphoma cell line with high STAT3 activation. Int J Oncol. 38, 1245-1252 (2011)
74. Matsuno K, Masuda Y, Uehara Y, Sato H, Muroya A, Takahashi O, Yokotagawa T, Furuya T, Okawara
T, Otsuka M, Ogo N, Ashizawa T, Oshita C, Tai S, Ishii H, Akiyama Y, Asai A. Identification of a
new series of STAT3 inhibitors by virtual screening. ACS Med Chem Lett. 1, 371-375 (2010)
75. Oishi S, Watanabe K, Ito S, Tanaka M, Nishikawa H, Ohno H, Shimane K, Izumi K, Sakagami Y,
Kodama NE, Matsuoka M, Asai A, Fujii N. 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).
76. Matsuno K, Takai K, Isaka Y, Unno Y, Sato M, Takikawa O, Asai A. S-benzylisothiourea derivatives
as small-molecule inhibitors of indoleamine-2,3-dioxygenase. Bioorg Med Chem Lett. 20, 5126-5129(2010)
77. Shimizu M, Ishii H, Ogo N, Unno Y, Matsuno K, Sawada J, Akiyama Y, Asai A. S-trityl-L-cysteine
derivative induces caspase-independent cell death in K562 human chronic myeloid leukemia cell line.
Cancer Lett. 298, 99-106 (2010)
78. Oishi S, Watanabe T, Sawada J, Asai A, Ohno H, Fujii N. Kinesin spindle protein (KSP) inhibitors with
2,3-fused indole scaffolds. J Med Chem. 53, 5054-5058 (2010)
79. Oikawa T, Unno Y, Matsuno K, Sawada J, Ogo N, Tanaka K, Asai A. Identification of asmall-molecule inhibitor of the interaction between Survivin and Smac/DIABLO. Biochem Biophys Res
Commun. 393, 253-258 (2010)
80. Shimizu M, Ishii H, Ogo N, Matsuno K, Asai A. Biochemical analysis of cellular target of
S-trityl-L-cysteine derivatives using affinity matrix. Bioorg Med Chem Lett. 20, 1578-1580 (2010)
81. Yamada H, Abe T, Li S, Masuoka Y, Isoda M, Watanabe M, Nasu Y, Kumon H, Asai A, Takei K.
Dynasore, a dynamin inhibitor, suppresses lamellipodia formation and cancer cell invasion bydestabilizing actin filaments. Biochem Biophys Res Commun. 390, 1142-1148 (2009)
82. Matsuno K, Sawada ., Sugimoto M, Ogo N, Asai A. Bis(hetero)aryl derivatives as unique kinesin
spindle protein inhibitor. Bioorg Med Chem Lett. 19, 3405–3409 (2009)
83. Yoshida K, Yamaguchi K, Mizuno A, Unno Y, Asai A, Sone T, Yokosawa H, Matsuda A, Arisawa M,
Shuto S. Three-dimensional structure-activity relationship study of belactosin A and its stereo- andregioisomers: development of potent proteasome inhibitors by a stereochemical diversity-oriented
strategy. Org Biomol Chem. 7, 1868-1877 (2009)
84. Nakamura H, Watanabe M, Ban HS, Nabeyama W, Asai A. Synthesis and biological evaluation of7

boron peptide analogues of Belactosin C as proteasome inhibitors. Bioorg Med Chem Lett. 19,
3220-3224 (2009)
85. Uehara Y, Mochizuki M, Matsuno K, Haino T, Asai A. Novel high-throughput screening system for
identifying STAT3-SH2 antagonists. Biochem Biophys Res Commun. 380, 627-631 (2009)
86. Yoshida K, Yamguchi K, Sone T, Unno Y, Asai A, Yokosawa H, Matsuda A, Arisawa M, Shuto S.
Synthesis of 2,3- and 3,4-Methanoamino acid Equivalents with stereochemical diversity and theirconversion into the tripeptide proteasome inhibitor belactosin A and its highly potent cis-cyclopropane
stereoisomer. Organic Lett. 10, 3571-3574 (2008)
87. Yoshida M, Kabe Y, Wada T, Asai A, Handa H. 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)
88. Matsuno K, Sawada J, Asai A. Therapeutic potential of mitotic kinesin inhibitors in cancer. Expert Opin
Ther Patents. 18, 253-274 (2008) review article
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