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静岡県立大学教員データベース


教員情報詳細


写真:浅井 章良

氏名
浅井 章良(ASAI Akira)
所属・職名
薬学研究院(創薬探索センター) 教授
薬学部 教授(兼務)
電話番号
054-264-5231
部屋番号
一般教育棟2314号室
Eメールアドレス
aasai(ここに@を入れてください)u-shizuoka-ken.ac.jp
ホームページアドレス(URL)
http://w3pharm.u-shizuoka-ken.ac.jp/tansaku/
研究シーズ集
http://www.u-shizuoka-ken.ac.jp/file/47aasai.pdf

学歴

1987年3月 慶応義塾大学理工学部卒業
1989年3月 慶応義塾大学理工学研究科修士課程修了


学位

工学博士(慶応義塾大学・1997年)


専門分野

創薬科学、腫瘍治療学、ケミカルバイオロジー


担当科目

創薬科学、創薬探索学特論、創薬探索学演習・特別実験、化学系薬学実習


主要研究テーマ

・ケミカルジェネティクス的手法を用いた薬剤スクリーニングシステムの開発
・新規分子標的抗がん剤の創出を目的としたリード探索と構造最適化研究
・医薬品や候補物質の作用機序解析とバイオマーカーの探索
・低分子化合物を用いた細胞内ネットワークの解析と人工的制御


所属学会

日本薬学会
日本癌学会
日本分子生物学会
米国癌学会
日本ケミカルバイオロジー学会
日本がん分子標的学会
米国化学会


主な経歴

1989年4月 協和発酵工業(株)東京研究所・研究員
1995年7~9月 米国Geron社派遣
2001年7月~2002年8月 米国Scripps研究所・客員研究員
2002年4月 協和発酵工業(株)医薬総合研究所・主任研究員
2003年9月~2004年3月 東工大生命理工学部・非常勤講師兼務
2004年4月 静岡県立大学大学院・教授


主な社会活動

日本分子生物学会第32回年会実行委員(2009年)
日本ケミカルバイオロジー学会第7回年会実行委員(2011年)
日本ケミカルバイオロジー学会世話人(2011年~)
SCIENTIFICA  Editorial board member of pharmaceutics (2012年~)


主要研究業績

[2003年以降]
・Antiviral effect of theaflavins against caliciviruses. J Antibiot. 70, 443-447, 2017
・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
・Inhibition of STAT3 by Anticancer Drug Bendamustine. PLoS One 12, e0170709, 2017
・Methanethiosulfonate derivatives as ligands of the STAT3-SH2 domain. J Enzyme Inhib Med Chem. 32, 337-344, 2017
・Combination of a STAT3 Inhibitor and an mTOR Inhibitor Against a Temozolomide-resistant Glioblastoma Cell Line. Cancer Genomics Proteomics 14, 83-91, 2017
・Synthesis of new dithiolethione and methanethiosulfonate systems endowed with pharmaceutical interest. Arkivoc. part ii, 235-250, 2017
・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
・Alpha-based Multiplexed Assay for Identifying SH2 Domain Antagonists. SH2 Domains: Methods and Protocols, Machida K, Liu BA (Eds): Springer, p163-172, 2017
・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
・Design of fluorescent probes for kinesin spindle protein (KSP). Bioorg Med Chem Lett. 26, 5765-5769, 2016
・Epirubicin, identified using a novel luciferase reporter assay for Foxp3 inhibitors, inhibits regulatory T cell activity. PLoS One 11, e0156643, 2016
・The discovery and characterization of K-756, a novel Wnt/β-catenin pathway inhibitor targeting tankyrase. Mol Cancer Ther. 15, 1525-1534, 2016
・Fluvoxamine, an anti-depressant, inhibits human glioblastoma invasion by disrupting actin polymerization. Sci Rep. 6, 23372, 2016
・Discovery and synthesis of heterocyclic carboxamide derivatives as potent anti-norovirus agents. Chem Pharm Bull. 64, 465-475, 2016
・Structure-guided design of novel L-Cysteine derivatives as potent KSP inhibitors. ACS Med Chem Lett. 6, 1004-1009, 2015
・Identification of a new STAT3 dimerization inhibitor through a pharmacophore-based virtual screening approach. J Enzyme Inhib Med Chem. Aug 26, 1-7, 2015
・Ureido-pyridazinone derivatives: Insights into the structural and conformational properties for STAT3 inhibition. Eur J Org Chem. 22, 4907–4912, 2015
・Structural basis of new allosteric inhibition in Kinesin spindle protein Eg5. ACS Chem Biol. 10, 1128-1136, 2015
・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
・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 (12), 13-21, 2015
・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
・Modeling, synthesis and NMR characterization of novel chimera compounds targeting STAT3. Med Chem Commun. 5, 1651-1657, 2014
・Effect of the STAT3 inhibitor STX-0119 on the proliferation of a temozolomide-resistant glioblastoma cell line. 45, Int J Oncol. 411-418, 2014
・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
・Optimization of diaryl amine derivatives as kinesin spindle protein inhibitors. Bioorg Med Chem. 22, 3171-3179, 2014
・Kinesin spindle protein inhibitors with diaryl amine scaffolds: crystal packing analysis for improved aqueous solubility. ACS Med Chem Lett. 5, 566-571, 2014
・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
・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
・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
・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
・Novel multiplexed assay for identifying SH2 domain antagonists of STAT family proteins. PLoS ONE. 8, e71646, 2013
・Design and synthesis of the stabilized analogs of belactosin A with the unnatural cis-cyclopropane structure. Org Biomol Chem. 11, 6615-6622, 2013
・Synthesis, structure–activity relationships and stereochemical investigations of new tricyclic pyridazinone derivatives as potential STAT3 inhibitors Med Chem Commun. 4, 1181-1188, 2013
・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
・Investigation of the non-covalent 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
・Internalization of CCR4 and Inhibition of Chemotaxis by K777, a Potent and selective CCR4 antagonist. Pharmacology 91, 305-313, 2013
・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
・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
・創薬標的としての転写因子STAT3, ファルマシア, 48, 673-677, 2012
・Biological and computational evaluation of an oxadiazole derivative (MD77) as a new lead for direct STAT3 inhibitors. Med Chem Commun.3, 592-599, 2012
・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
・Identification of novel kynurenine production-inhibiting benzenesulfonamide derivatives in cancer cells. Biochem Biophys Res Commun. 419, 556-561, 2012
・Novel candesartan derivatives as indoleamine 2,3-dioxygenase inhibitors. Med Chem Commun. 3, 475-479, 2012
・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
・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
・Identification of a new series of STAT3 inhibitors by virtual screening. ACS Med Chem Lett. 1, 371-375, 2010
・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
・S-benzylisothiourea derivatives as small-molecule inhibitors of indoleamine-2,3-dioxygenase. Bioorg Med Chem Lett. 20, 5126-5129, 2010
・S-trityl-L-cysteine derivative induces caspase-independent cell death in K562 human chronic myeloid leukemia cell line. Cancer Lett. 298, 99-106, 2010
・Kinesin spindle protein (KSP) inhibitors with 2,3-fused indole scaffolds. J Med Chem. 53, 5054-5058, 2010
・Identification of a small-molecule inhibitor of the interaction between Survivin and Smac/DIABLO. Biochem Biophys Res Commun. 393, 253-258, 2010
・Biochemical analysis of cellular target of S-trityl-L-cysteine derivatives using affinity matrix. Bioorg Med Chem Lett. 20, 1578-1580, 2010
・Dynasore, a dynamin inhibitor, suppresses lamellipodia formation and cancer cell invasion by destabilizing actin filaments. Biochem Biophys Res Commun. 390, 1142-1148, 2009
・Bis(hetero)aryl derivatives as unique kinesin spindle protein inhibitor. Bioorg Med Chem Lett. 19, 3405–3409, 2009
・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
・Synthesis and biological evaluation of boron peptide analogues of Belactosin C as proteasome inhibitors. Bioorg Med Chem Lett. 19, 3220-3224, 2009
・Novel high-throughput screening system for identifying STAT3-SH2 antagonists. Biochem Biophys Res Commun. 80, 627-631, 2009
・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. Organic Lett. 10, 3571-3574, 2008
・ 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
・Therapeutic potential of mitotic kinesin inhibitors in cancer. Expert Opin Ther Patents 18, 253-274, 2008
・Synthesis and biological evaluation of l-cysteine derivatives as mitotic kinesin Eg5 inhibitors. Bioorg Med Chem Lett. 17, 3921-3924, 2007
・Telomerase inhibitors identified by a forward chemical genetics approach using a yeast strain with shortened telomere length. Chem & Biol. 13, 1-8, 2006
・ゲノム創薬とテーラーメード医療, 新しい遺伝子工学, 175-188, 2006
・産学連携による新たな創薬研究を目指して, 化学, 60, 34, 2005
・ファルマバレー構想, ファルマシア, 41, 161-165, 2005
・hnRNP L enhances sensitivity of the cells to KW-2189. Int J Cancer, 108, 679-685, 2004
・A new structural class of proteasome inhibitors identified microbial screening using yeast-based assay. Biochem Pharmacol. 67, 227-234, 2004
・A novel telomerase template antagonist (GRN163) as a potential anticancer agent. Cancer Res. 63, 3931-3939, 2003


教育・研究に対する考え方

教育:実践的な創薬研究を通して、将来の創薬を担う研究者を育成
研究:分子レベルでのがんの理解と新しい治療戦略、治療薬の提唱


研究シーズ集に関するキーワード

低分子医薬シード、分子標抗がん剤、探索研究、スクリーニング、化合物デザインと合成、構造活性相関、構造最適化、作用機序解析


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