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チモロールは人炭酸脱水酵素I及びIIの酵素活性を活性化する。(発表論文抄録(2010))
https://fukuyama-u.repo.nii.ac.jp/records/8846
https://fukuyama-u.repo.nii.ac.jp/records/8846ce18fd1c-8fbd-4234-8b01-d05b0f7fabc9
| 名前 / ファイル | ライセンス | アクション |
|---|---|---|
杉本文子(発表論文抄録(2010)) (636.1 kB)
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| Item type | 紀要論文 / Departmental Bulletin Paper(1) | |||||
|---|---|---|---|---|---|---|
| 公開日 | 2018-01-15 | |||||
| タイトル | ||||||
| タイトル | チモロールは人炭酸脱水酵素I及びIIの酵素活性を活性化する。(発表論文抄録(2010)) | |||||
| タイトル | ||||||
| タイトル | Timolol activates the enzyme activities of human carbonic anhydrase I and II. | |||||
| 言語 | en | |||||
| 言語 | ||||||
| 言語 | eng | |||||
| キーワード | ||||||
| 言語 | en | |||||
| 主題Scheme | Other | |||||
| 主題 | Binding Sites | |||||
| キーワード | ||||||
| 言語 | en | |||||
| 主題Scheme | Other | |||||
| 主題 | Carbonic Anhydrase I | |||||
| キーワード | ||||||
| 言語 | en | |||||
| 主題Scheme | Other | |||||
| 主題 | Carbonic Anhydrase II | |||||
| キーワード | ||||||
| 言語 | en | |||||
| 主題Scheme | Other | |||||
| 主題 | Enzyme Activation | |||||
| キーワード | ||||||
| 言語 | en | |||||
| 主題Scheme | Other | |||||
| 主題 | Humans | |||||
| キーワード | ||||||
| 言語 | en | |||||
| 主題Scheme | Other | |||||
| 主題 | Timolol | |||||
| 資源タイプ | ||||||
| 資源タイプ識別子 | http://purl.org/coar/resource_type/c_6501 | |||||
| 資源タイプ | departmental bulletin paper | |||||
| 著者 |
Sugimoto, Ayako
× Sugimoto, Ayako× Ikeda, Hiroaki× Tsukamoto, Hidetoshi× Kihira, Kenji× Ishioka, Manabu× Hirose, Junzo× Hata, Toshiyuki× Fujioka, Haruto× Ono, Yukio |
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| 著者別名 | ||||||
| 識別子Scheme | WEKO | |||||
| 識別子 | 45230 | |||||
| 識別子Scheme | CiNii ID | |||||
| 識別子URI | http://ci.nii.ac.jp/nrid/9000001578120 | |||||
| 識別子 | 9000001578120 | |||||
| 姓名 | 杉本, 文子 | |||||
| 著者別名 | ||||||
| 識別子Scheme | WEKO | |||||
| 識別子 | 45231 | |||||
| 識別子Scheme | CiNii ID | |||||
| 識別子URI | http://ci.nii.ac.jp/nrid/9000017055616 | |||||
| 識別子 | 9000017055616 | |||||
| 姓名 | 池田, 博昭 | |||||
| 著者別名 | ||||||
| 識別子Scheme | WEKO | |||||
| 識別子 | 45232 | |||||
| 識別子Scheme | CiNii ID | |||||
| 識別子URI | http://ci.nii.ac.jp/nrid/9000017493268 | |||||
| 識別子 | 9000017493268 | |||||
| 姓名 | 塚本, 秀利 | |||||
| 著者別名 | ||||||
| 識別子Scheme | WEKO | |||||
| 識別子 | 45233 | |||||
| 識別子Scheme | CiNii ID | |||||
| 識別子URI | http://ci.nii.ac.jp/nrid/9000017055617 | |||||
| 識別子 | 9000017055617 | |||||
| 姓名 | 木平, 健治 | |||||
| 著者別名 | ||||||
| 識別子Scheme | WEKO | |||||
| 識別子 | 46323 | |||||
| 姓名 | 石岡, 学 | |||||
| 著者別名 | ||||||
| 識別子Scheme | WEKO | |||||
| 識別子 | 45879 | |||||
| 識別子Scheme | CiNii ID | |||||
| 識別子URI | http://ci.nii.ac.jp/nrid/1000070080215 | |||||
| 識別子 | 1000070080215 | |||||
| 姓名 | 廣瀬, 順造 | |||||
| 著者別名 | ||||||
| 識別子Scheme | WEKO | |||||
| 識別子 | 45236 | |||||
| 識別子Scheme | CiNii ID | |||||
| 識別子URI | http://ci.nii.ac.jp/nrid/9000014625803 | |||||
| 識別子 | 9000014625803 | |||||
| 姓名 | 秦, 季之 | |||||
| 著者別名 | ||||||
| 識別子Scheme | WEKO | |||||
| 識別子 | 45305 | |||||
| 識別子Scheme | CiNii ID | |||||
| 識別子URI | http://ci.nii.ac.jp/nrid/9000005179805 | |||||
| 識別子 | 9000005179805 | |||||
| 姓名 | 藤岡, 晴人 | |||||
| 著者別名 | ||||||
| 識別子Scheme | WEKO | |||||
| 識別子 | 45238 | |||||
| 識別子Scheme | CiNii ID | |||||
| 識別子URI | http://ci.nii.ac.jp/nrid/9000002578762 | |||||
| 識別子 | 9000002578762 | |||||
| 姓名 | 小野, 行雄 | |||||
| 抄録 | ||||||
| 内容記述タイプ | Abstract | |||||
| 内容記述 | Timolol, a beta-blocker, has been shown to be an effective ocular hypotensive agent when used alone or with carbonic anhydrase inhibitor on ocular hypertensive or open angle glaucoma patients. The effect of timolol hemihydrate on the CO(2) hydration activities of human carbonic anhydrase (HCA) I and II and their reaction mechanisms were investigated. Timolol activates the enzyme activities of HCA I and HCA II. In HCA I and II, the enzyme kinetic results clearly showed that timolol increases the value of V(max) but does not influence the value of K(m). The enzyme kinetic method showed that timolol noncompetitively activates HCA I and II activities through the formation of a ternary complex consisting of the enzyme, the substrate, and timolol. These results indicate that timolol binds apart from the narrow cavity of the active site. AutoDocking results showed that timolol binds at the entrance of the active site cavity in a region where the proton shuttle residue, His 64, of HCA I or II, is placed. The enzyme kinetic and AutoDocking results showed that timolol might weakly bind near the proton shuttle residue, His 64, to accelerate the proton transfer rate from His 64 to the buffer components. It is known that efficient activators of carbonic anhydrase possess a bulky aromatic/heterocyclic moiety and a primary/secondary amino group in their molecular structure. Timolol has a heterocyclic moiety and a secondary amino group, which are typical structures in efficient activators of carbonic anhydrase. | |||||
| 内容記述 | ||||||
| 内容記述タイプ | Other | |||||
| 内容記述 | Timolol, a beta-blocker, has been shown to be an effective ocular hypotensive agent when used alone or with carbonic anhydrase inhibitor on ocular hypertensive or open angle glaucoma patients. The effect of timolol hemihydrate on the CO(2) hydration activities of human carbonic anhydrase (HCA) I and II and their reaction mechanisms were investigated. Timolol activates the enzyme activities of HCA I and HCA II. In HCA I and II, the enzyme kinetic results clearly showed that timolol increases the value of V(max) but does not influence the value of K(m). The enzyme kinetic method showed that timolol noncompetitively activates HCA I and II activities through the formation of a ternary complex consisting of the enzyme, the substrate, and timolol. These results indicate that timolol binds apart from the narrow cavity of the active site. AutoDocking results showed that timolol binds at the entrance of the active site cavity in a region where the proton shuttle residue, His 64, of HCA I or II, is placed. The enzyme kinetic and AutoDocking results showed that timolol might weakly bind near the proton shuttle residue, His 64, to accelerate the proton transfer rate from His 64 to the buffer components. It is known that efficient activators of carbonic anhydrase possess a bulky aromatic/heterocyclic moiety and a primary/secondary amino group in their molecular structure. Timolol has a heterocyclic moiety and a secondary amino group, which are typical structures in efficient activators of carbonic anhydrase. | |||||
| 書誌情報 |
福山大学薬学部研究年報 en : Annual report of the Faculty of Pharmacy & Pharmaceutical Sciences, Fukuyama University 号 29, p. 57-58, 発行日 2011-12-25 |
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| 出版者 | ||||||
| 出版者 | 福山大学薬学部 | |||||
| ISSN | ||||||
| 収録物識別子タイプ | ISSN | |||||
| 収録物識別子 | 0288-724X | |||||
| 書誌レコードID | ||||||
| 収録物識別子タイプ | NCID | |||||
| 収録物識別子 | AN10064550 | |||||
