Thermodynamics-based mechanism for the regulation of substrate binding affinity of proton coupled drug transporters
| Project/Area Number |
23790060
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| Research Category |
Grant-in-Aid for Young Scientists (B)
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| Allocation Type | Multi-year Fund |
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| Research Field |
Physical pharmacy
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| Research Institution | Toho University (2012-2013)
Matsuyama University (2011) |
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Principal Investigator |
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| Project Period (FY) |
2011 – 2013
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| Project Status |
Completed (Fiscal Year 2013)
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| Budget Amount *help |
¥4,290,000 (Direct Cost: ¥3,300,000、Indirect Cost: ¥990,000)
Fiscal Year 2013: ¥1,300,000 (Direct Cost: ¥1,000,000、Indirect Cost: ¥300,000)
Fiscal Year 2012: ¥1,300,000 (Direct Cost: ¥1,000,000、Indirect Cost: ¥300,000)
Fiscal Year 2011: ¥1,690,000 (Direct Cost: ¥1,300,000、Indirect Cost: ¥390,000)
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| Keywords | 等温滴定型熱量計 / 薬物輸送 / 分子認識 / 相互作用エネルギー / 多剤排出輸送担体 / プロトン/オリゴペプチド輸送担体 / 熱力学量 / 薬物輸送担体 / 無細胞タンパク質合成系 / alternative access model / EmrE / YdgR |
|---|
| Research Abstract |
Regulation of the binding affinity of the substrate into transporter is one of crucial factors to transport the substrate through the membrane. In this study, we had investigated the interaction between proton coupled drug transporters and these substrates by isothermal titration calorimetry (ITC) is a technique that can analyze the interaction energy with the substrate, and discussed the thermodynamics based mechanism of proton coupled substrate transport. (1) In the study of EmrE as antiporter, the interaction between EmrE and TPP+ depends on pH. At higher pH, the affinity increases, and the driving force becomes from enthalpy-driven to entropy-driven, and it is indicated that Glu25 might be one of determinant residues to drive the substrate binding. (2) In the study of YdgR as synporter, it was found that the driving force of interaction between YdgR and Val-Ala is entropy change, and it was not depend on pH.
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Report
(4 results)
Research Products
(31 results)
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[Journal Article] A common variant of leucine-rich repeat-containing 16A (LRRC16A) gene is associated with gout susceptibility2014
Author(s)
Sakiyama, M. Matsuo, H. Shimizu, S. Chiba, T. Nakayama, A. Takada, Y. Nakamura, T. Takada, T. Morita, E. Naito, M. Wakai, K. Inoue, H. Tatsukawa, S. Sato, J. Shimono, K. Makino, T. Satoh, T. Suzuki, H. Kanai, Y. Hamajima, N. Sakurai, Y. Ichida, K. Shimizu, T. Shinomiya, N.
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Journal Title
Hum Cell
Volume: 27(1)
Issue: 1
Pages: 1-4
DOI
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Peer Reviewed
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[Book] Photo-induced proton transfers of microbial rhodopsins. Molecular Photochemistry - Various Aspects2012
Author(s)
Kikukawa, T., Tamogami, J., Shimono, K., Demura, M., Nara, T., Kamo, N
Total Pages
282
Publisher
Book edited by Dr. Satyen Saha(DOI; 10.5772/34105)
Related Report
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[Book] Molecular Photochemistry - Various Aspects (Book edited by Dr. Satyen Saha) Chapter 5 "Photo-induced proton transfers of microbial rhodopsins."2012
Author(s)
Kikukawa, T., Tamogami, J., Shimono, K., Demura, M., Nara, T., Kamo, N.
Publisher
Intech
Related Report
