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Molecular basis for...
Molecular basis for human aquaporin inhibition
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- Huang, Peng (author)
- Lund University,Lunds universitet,Institutionen för experimentell medicinsk vetenskap,Medicinska fakulteten,Medicinsk strukturbiologi,Forskargrupper vid Lunds universitet,Department of Experimental Medical Science,Faculty of Medicine,Medical Structural Biology,Lund University Research Groups
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- Åbacka, Hannah (author)
- Lund University,Lunds universitet,Institutionen för experimentell medicinsk vetenskap,Medicinska fakulteten,Medicinsk strukturbiologi,Forskargrupper vid Lunds universitet,LUCC: Lunds universitets cancercentrum,Övriga starka forskningsmiljöer,Department of Experimental Medical Science,Faculty of Medicine,Medical Structural Biology,Lund University Research Groups,LUCC: Lund University Cancer Centre,Other Strong Research Environments
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- Wilson, Carter J (author)
- Max Planck Institute for Multidisciplinary Sciences
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- Wind, Malene Lykke (author)
- University of Copenhagen
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- Rűtzler, Michael (author)
- Apoglyx AB
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- Hagström-Andersson, Anna (author)
- Lund University,Lunds universitet,Avdelningen för klinisk genetik,Institutionen för laboratoriemedicin,Medicinska fakulteten,LUCC: Lunds universitets cancercentrum,Övriga starka forskningsmiljöer,Division of Clinical Genetics,Department of Laboratory Medicine,Faculty of Medicine,LUCC: Lund University Cancer Centre,Other Strong Research Environments
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- Gourdon, Pontus (author)
- Lund University,Lunds universitet,Institutionen för experimentell medicinsk vetenskap,Medicinska fakulteten,Medicinsk strukturbiologi,Forskargrupper vid Lunds universitet,Department of Experimental Medical Science,Faculty of Medicine,Medical Structural Biology,Lund University Research Groups,University of Copenhagen
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- de Groot, Bert L (author)
- Max Planck Institute for Multidisciplinary Sciences
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- Venskutonytė, Raminta (author)
- Lund University,Lunds universitet,Institutionen för experimentell medicinsk vetenskap,Medicinska fakulteten,Medicinsk strukturbiologi,Forskargrupper vid Lunds universitet,LINXS - Institute of advanced Neutron and X-ray Science,Kemiska institutionen,Institutioner vid LTH,Lunds Tekniska Högskola,Department of Experimental Medical Science,Faculty of Medicine,Medical Structural Biology,Lund University Research Groups,Department of Chemistry,Departments at LTH,Faculty of Engineering, LTH
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- Lindkvist-Petersson, Karin (author)
- Lund University,Lunds universitet,Institutionen för experimentell medicinsk vetenskap,Medicinska fakulteten,Medicinsk strukturbiologi,Forskargrupper vid Lunds universitet,LINXS - Institute of advanced Neutron and X-ray Science,Kemiska institutionen,Institutioner vid LTH,Lunds Tekniska Högskola,LUCC: Lunds universitets cancercentrum,Övriga starka forskningsmiljöer,Department of Experimental Medical Science,Faculty of Medicine,Medical Structural Biology,Lund University Research Groups,Department of Chemistry,Departments at LTH,Faculty of Engineering, LTH,LUCC: Lund University Cancer Centre,Other Strong Research Environments
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(creator_code:org_t)
- 2024
- 2024
- English 8 s.
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In: Proceedings of the National Academy of Sciences of the United States of America. - 1091-6490. ; 121:7
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http://dx.doi.org/10... (free)
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Abstract
Subject headings
Close
- 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.
Subject headings
- MEDICIN OCH HÄLSOVETENSKAP -- Klinisk medicin -- Cancer och onkologi (hsv//swe)
- MEDICAL AND HEALTH SCIENCES -- Clinical Medicine -- Cancer and Oncology (hsv//eng)
- MEDICIN OCH HÄLSOVETENSKAP -- Medicinska och farmaceutiska grundvetenskaper -- Cell- och molekylärbiologi (hsv//swe)
- MEDICAL AND HEALTH SCIENCES -- Basic Medicine -- Cell and Molecular Biology (hsv//eng)
Keyword
- Humans
- Aquaporins/metabolism
- Neoplasms
- Aquaporin 1/metabolism
Publication and Content Type
- art (subject category)
- ref (subject category)
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