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題 名 | Thermodynamic Analysis of Human Retinal Acetylcholinesterase Inhibition Using an Anti-Alzheimer's Drug, Tacrine, through the Development of a Dual Substrate and Temperature Model=阿茲海默藥物塔克林(Tacrine)抑制人類視網膜乙醯膽鹼酯酶的熱力學分析及雙受質雙溫度模式的推導 |
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作 者 | Kamal,Mohammad A.; Alhomida,Abdullah S.; Al-rajhi,Ali A.; Al-jafari,Abdulaziz A.; | 書刊名 | Proceedings of the National Science Council : Part B, Life Science |
卷 期 | 24:3 2000.07[民89.07] |
頁 次 | 頁108-115 |
分類號 | 361.1925 |
關鍵詞 | 阿茲海默藥物; 塔克林; 視網膜乙醯膽鹼酯酶; 雙受質雙溫度模式; Acetylcholinesterase; Alzheimer's disease; Energetic; Inhibition; Retina; Tacrine; Thermodynamics; |
語 文 | 英文(English) |
英文摘要 | The present study determines the energy parameters, such as the Gibb's free energy change (.DELTA. G), enthalpy change (.DELTA. H), heat of activation (.DELTA. H*), entropy change (.DELTA. S), temperature coefficient (Q10) and activation energy (Ea), of human retinal acetylcholinesterase (AChE, EC 3.1.1.7) inhibition by tacrine. The stereo-frequency collisions factor (PZ, the number of sterically and energetically favorable collisions occurring between tacrine and AChE) was also studied in this investigation. Tacrine significantly increased the value of .DELTA. G, .DELTA. H, .DELTA. H*, Q10, Ea and PZ factor, and decreased the value of .DELTA. S for AChE. Since there is no known report on the inhibition of human retinal AChE by tacrine, these results were compared with the reported values for the energy parameters of camel retinal and chicken brain AChE inhibition by an anti-cancer drug, cyclophosphamide. The uniqueness of this approach lies in the development of the 'dual substrate and dual temperature' model, which may open up a new, more efficient avenue for the study of various enzyme catalyzed reactions. |
本系統中英文摘要資訊取自各篇刊載內容。