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  Molecular basis for human aquaporin inhibition

Huang, P., Abacka, H., Wilson, C. J., Wind, M. L., Rutzler, M., Hagstroem-Andersson, A., et al. (2024). Molecular basis for human aquaporin inhibition. PNAS, 121(7): e2319682121. doi:10.1073/pnas.2319682121.

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Item Permalink: https://hdl.handle.net/21.11116/0000-000F-0E55-3 Version Permalink: https://hdl.handle.net/21.11116/0000-000F-0E56-2
Genre: Journal Article

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huang-et-al-2024-molecular-basis-for-human-aquaporin-inhibition.pdf (Publisher version), 3MB
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 Creators:
Huang, Peng, Author
Abacka, Hannah, Author
Wilson, Carter J.1, 2, Author           
Wind, Malene Lykke, Author
Rutzler, Michael, Author
Hagstroem-Andersson, Anna, Author
Gourdon, Pontus, Author
de Groot, Bert L.1, 2, Author           
Venskutonyte, Raminta, Author
Lindkvist-Petersson, Karin, Author
Affiliations:
1Research Group of Computational Biomolecular Dynamics, Max Planck Institute for Multidisciplinary Sciences, Max Planck Society, ou_3350134              
2Department of Theoretical and Computational Biophysics, Max Planck Institute for Multidisciplinary Sciences, Max Planck Society, ou_3350132              

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 Abstract: Cancer invasion and metastasis are known to be potentiated by the expression of aquaporins (AQPs). Likewise, the expression levels of AQPs have been shown to be prognostic for survival in patients and have a role in tumor growth, edema, angiogenesis, and tumor cell migration. Thus, AQPs are key players in cancer biology and potential targets for drug development. Here, we present the single-particle cryo-EM structure of human AQP7 at 3.2-Å resolution in complex with the specific inhibitor compound Z433927330. The structure in combination with MD simulations shows that the inhibitor binds to the endofacial side of AQP7. In addition, cancer cells treated with Z433927330 show reduced proliferation. The data presented here serve as a framework for the development of AQP inhibitors.

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Language(s): eng - English
 Dates: 2024-02-062024-02-13
 Publication Status: Issued
 Pages: -
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 Table of Contents: -
 Rev. Type: Peer
 Identifiers: DOI: 10.1073/pnas.2319682121
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Title: PNAS
  Other : Proceedings of the National Academy of Sciences of the United States of America
  Other : Proceedings of the National Academy of Sciences of the USA
  Abbreviation : Proc. Natl. Acad. Sci. U. S. A.
Source Genre: Journal
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Publ. Info: Washington, D.C. : National Academy of Sciences
Pages: - Volume / Issue: 121 (7) Sequence Number: e2319682121 Start / End Page: - Identifier: ISSN: 0027-8424
CoNE: https://pure.mpg.de/cone/journals/resource/954925427230