花屋 賢悟 (ハナヤ ケンゴ)

Hanaya, Kengo

写真a

所属(所属キャンパス)

薬学部 薬科学科 有機薬化学講座 (芝共立)

職名

専任講師

学位 【 表示 / 非表示

  • 博士(薬学), 東京理科大学, 課程, 2012年03月

    Design and Synthesis of Biomedical Tools and Metalloprotease Inhibitors Based on Chemical Properties of 8-Quinolinol and Their Sulfonates

 

論文 【 表示 / 非表示

  • Copper-mediated peptide arylation selective for the N-terminus

    Mary K. Miller, Haopei Wang, Kengo Hanaya, Olivia Zhang, Alex Berlaga and Zachary T. Ball

    Chemical Science (ROYAL SOCIETY OF CHEMISTRY)  2020年09月

    研究論文(学術雑誌), 共著, 査読有り

  • Improved preparation of vitexin from hot water extract of Basella alba, the commercially available vegetable Malabar spinach (“Tsurumurasaki” in Japanese) and the application to semisynthesis of chafuroside B

    Kurahayashi K., Hanaya K., Higashibayashi S., Sugai T.

    Bioscience, Biotechnology and Biochemistry (Bioscience, Biotechnology and Biochemistry)  84 ( 8 ) 1554 - 1559 2020年08月

    ISSN  09168451

     概要を見る

    © 2020, © 2020 Japan Society for Bioscience, Biotechnology, and Agrochemistry. Hot water extraction of D-arabinofuranosylvitexin from the raw leaves of commercially available Basella alba “Tsurumurasaki” and subsequent acidic hydrolysis was improved to be a procedure using a high-pressure steam sterilizer to afford vitexin. The amount was estimated to be 14.1 mg from 1 g of dry weight of the raw leaves, whose recovery was calculated to be 95% based on the estimated content of D-arabinofuranosylvitexin in B. alba raw leaves. The product was dehydratively cyclized between hydroxy groups on the carbohydrate and flavone skeletons under modified Mitsunobu reaction conditions in N,N-dimethylformamide to give chafuroside B, which is known to be a bioactive Oolong tea polyphenol. Through these transformations, 10.2 mg of chafuroside B could be semisynthesized from 1 g of dry weight of the raw leaves, and the efficiency was improved compared to that from the extraction from Oolong tea (3.4 μg from 1 g of dry weight).

  • Comprehensive semisyntheses of catathelasmols C, D, and E from D-glutamic acid, utilizing lipase-catalyzed site-selective reactions on intermediates

    Hashiba R., Hashimoto R., Nishiguchi M., Kobayashi T., Hanaya K., Higashibayashi S., Sugai T.

    Bioscience, Biotechnology and Biochemistry (Bioscience, Biotechnology and Biochemistry)  84 ( 7 ) 1339 - 1344 2020年07月

    ISSN  09168451

     概要を見る

    © 2020, © 2020 Japan Society for Bioscience, Biotechnology, and Agrochemistry. Catathelasmols C, D, and E, which had been isolated from Catathelasma imperiale as inhibitors for 11-hydroxysteroid dehydrogenases, were comprehensively semisynthesized from commercially available D-glutamic acid. The key synthetic intermediate, (R)-pentane-1,2,5-triol, was site-selectively acetylated by treatment with vinyl acetate and Candida antarctica lipase B (Novozym 435) in tetrahydrofuran (THF) at 25°C to furnish 1,5-diacetate (catathelasmol E, quantitative). The acetylation occurred site-selectively on the primary alcohols at the C-1 and C-5 positions over the secondary alcohol at the C-2 position. Dichromic acid oxidation provided 2-oxopentane-1,5-diyl diacetate (catathelasmol C, 78%). Burkholderia cepacia lipase-catalyzed transesterification with methanol in THF at–5°C proceeded preferentially on the acetate at C-1 located adjacent to the C-2 carbonyl group over the other terminal acetate at the C-5 position. 5-Hydroxy-4-oxopentyl acetate (catathelasmol D) was obtained in 53% yield.

  • Accumulation of major linezolid metabolites in patients with renal impairment

    Souza E., Crass R.L., Felton J., Hanaya K., Pai M.P.

    Antimicrobial Agents and Chemotherapy (Antimicrobial Agents and Chemotherapy)  64 ( 5 )  2020年05月

    ISSN  00664804

     概要を見る

    © 2020 American Society for Microbiology. All Rights Reserved. In patients with renal impairment (n=22 of 39), the median serum concentrations of linezolid, PNU-142300, and PNU-142586 were 1.6-, 3.3-, 2.8-fold higher, respectively, than in patients without renal impairment. Metabolite concentrations in paired samples were poorly correlated with linezolid concentrations (r2 = 0.26 for PNU-142300 and 0.06 for PNU-142586). Linezolid and its metabolites share potential toxicophores that deserve characterization to mitigate higher myelosuppression risk in patients with renal impairment.

  • Stepwise approach for sterically hindered C<inf>sp<sup>3</sup></inf>-C<inf>sp<sup>3</sup></inf> bond formation by dehydrogenative: O -alkylation and Lewis acid-catalyzed [1,3]-rearrangement towards the arylalkylcyclopentane skeleton of sesquiterpenes

    Fujitani B., Hanaya K., Sugai T., Higashibayashi S.

    Chemical Communications (Chemical Communications)  56 ( 25 ) 3621 - 3624 2020年03月

    ISSN  13597345

     概要を見る

    This journal is © The Royal Society of Chemistry. A stepwise dehydrogenative cross-coupling method was developed for the formation of sterically hindered Csp3-Csp3 bonds. Intramolecular dehydrogenative O-alkylation of a β-ketoester by 2,3-dichloro-5,6-dicyano-p-benzoquinone to form an oxolane followed by Lewis acid-catalyzed [1,3]-rearrangement furnished the sesquiterpene arylmethylcyclopentane skeleton. The formal syntheses of herbertane-type β-herbertenol, cuparane-type enokipodins A and B were also achieved.

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KOARA(リポジトリ)収録論文等 【 表示 / 非表示

研究発表 【 表示 / 非表示

  • ボロン酸を活用した生体高分子の化学修飾

    花屋賢悟

    2019年度若手研究者のためのセミナー, 2019年08月, 公開講演,セミナー,チュートリアル,講習,講義等

  • Nickel(II)-mediated arylation of biopolymers with arylboronic acid

    Kengo Hanaya, Mary K. Miller, Jun Ohata, Alicia E. Mangubat-Medina, Zachary T. Ball

    ISABC 2019 — 15th International Symposium on Applied Bioinorganic Chemistry, 2019年06月, 口頭(一般)

  • ニッケル触媒を用いたシステイン選択的アリール化反応

    花屋 賢悟, 大畠 潤, Mary K. MILLER, Alicia E. MANGUBAT-MEDINA, Zachary T. BALL

    日本薬学会 第139年会, 2019年03月, 口頭(一般)

  • Selective chemical protein modification with nickel(II) and arylboronic acid

    Kengo Hanaya, Jun Ohata, Mary K. Miller, Alicia E. Mangubat-Medina, Zachary T. Ball

    日本化学会 第99春季年会, 2019年03月, 口頭(一般)

  • Development of enzyme-activatable sulfonate-based prodrugs for active targeting therapy

    SASAKI Akio, SHOJI Mitsuru, SUGAI Takeshi, HANAYA Kengo

    ICC05-AEM2016, 2016年09月, ポスター(一般)

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競争的資金等の研究課題 【 表示 / 非表示

  • ボロン酸を用いるクロスカップリング反応を基盤としたタンパク質化学修飾法の開発

    2019年04月
    -
    2021年03月

    文部科学省・日本学術振興会, 科学研究費助成事業, 花屋 賢悟, 若手研究, 補助金,  代表

  • スルホン酸エステルを母核とした刺激応答性リンカーの開発とプロドラッグへの応用

    2016年04月
    -
    2019年03月

    文部科学省・日本学術振興会, 科学研究費補助金(文部科学省・日本学術振興会), 花屋 賢悟, 補助金, 

  • 刺激応答性リンカーの創製に向けたアミノスルホン酸エステルの分子内環化反応の開発

    2016年04月
    -
    2017年03月

    公益財団法人 日本科学協会, 笹川科学研究助成, 花屋 賢悟, 補助金,  代表

  • 酵素触媒を活用した不斉誘導体化試薬の創製 (超高感度化と効率的供給法の開発)

    2015年04月
    -
    2016年03月

    日本私立学校振興・共済事業団, 学術研究振興資金(若手研究者奨励金), 花屋 賢悟, 補助金,  代表

 

担当授業科目 【 表示 / 非表示

  • 課題研究(有機薬化学)

    2020年度

  • 演習(有機薬化学)

    2020年度

  • 卒業研究1(薬学科)

    2020年度

  • 高度研究機器特別演習

    2020年度

  • 英語演習(薬学科)

    2020年度

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