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Cannabinoid non-can...
Cannabinoid non-cannabidiol site modulation of TRPV2 structure and function
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- Zhang, Liying (author)
- Lund University,Lunds universitet,Neurofarmakologi och smärta,Forskargrupper vid Lunds universitet,Neuropharmacology and pain,Lund University Research Groups,University of Copenhagen,Lund Univ, Sweden; Lund Univ, Sweden; Univ Copenhagen, Denmark
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- Simonsen, Charlotte (author)
- Lund University,Lunds universitet,Avdelningen för klinisk kemi och farmakologi,Institutionen för laboratoriemedicin,Medicinska fakulteten,Division of Clinical Chemistry and Pharmacology,Department of Laboratory Medicine,Faculty of Medicine,Lund Univ, Sweden
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- Zimova, Lucie (author)
- Institute of Physiology of the Academy of Sciences of the Czech Republic,Czech Acad Sci, Czech Republic
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- Wang, Kaituo (author)
- University of Copenhagen,Univ Copenhagen, Denmark
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- Moparthi, Lavanya (author)
- Linköpings universitet,Linköping University,Avdelningen för molekylär medicin och virologi,Medicinska fakulteten,Wallenberg Centre for Molecular Medicine
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- Gaudet, Rachelle (author)
- Harvard University,Harvard Univ, MA USA
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- Ekoff, Maria (author)
- Karolinska Institute,Karolinska University Hospital,Karolinska Univ Hosp, Sweden; Karolinska Univ Hosp, Sweden
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- Nilsson, Gunnar (author)
- Karolinska Institutet,Karolinska Institute,Karolinska University Hospital,Karolinska Univ Hosp, Sweden; Karolinska Univ Hosp, Sweden
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- Hellmich, Ute A. (author)
- Friedrich Schiller University Jena,Goethe University,Friedrich Schiller Univ Jena, Germany; Goethe Univ, Germany
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- Vlachova, Viktorie (author)
- Institute of Physiology of the Academy of Sciences of the Czech Republic,Czech Acad Sci, Czech Republic
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- Gourdon, Pontus (author)
- Lund University,Lunds universitet,Membranproteinstrukturbiologi,Forskargrupper vid Lunds universitet,Membrane Protein Structural Biology,Lund University Research Groups,University of Copenhagen,Lund Univ, Sweden; Univ Copenhagen, Denmark
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- Zygmunt, Peter M. (author)
- Lund University,Lunds universitet,Neurofarmakologi och smärta,Forskargrupper vid Lunds universitet,Neuropharmacology and pain,Lund University Research Groups,Lund Univ, Sweden
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(creator_code:org_t)
- 2022-12-05
- 2022
- English.
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In: Nature Communications. - : Springer Science and Business Media LLC. - 2041-1723. ; 13
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Abstract
Subject headings
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- TRPV2 is a ligand-operated temperature sensor with poorly defined pharmacology. Here, we combine calcium imaging and patch-clamp electrophysiology with cryo-electron microscopy (cryo-EM) to explore how TRPV2 activity is modulated by the phytocannabinoid Δ9-tetrahydrocannabiorcol (C16) and by probenecid. C16 and probenecid act in concert to stimulate TRPV2 responses including histamine release from rat and human mast cells. Each ligand causes distinct conformational changes in TRPV2 as revealed by cryo-EM. Although the binding for probenecid remains elusive, C16 associates within the vanilloid pocket. As such, the C16 binding location is distinct from that of cannabidiol, partially overlapping with the binding site of the TRPV2 inhibitor piperlongumine. Taken together, we discover a new cannabinoid binding site in TRPV2 that is under the influence of allosteric control by probenecid. This molecular insight into ligand modulation enhances our understanding of TRPV2 in normal and pathophysiology.
Subject headings
- MEDICIN OCH HÄLSOVETENSKAP -- Medicinska och farmaceutiska grundvetenskaper -- Cell- och molekylärbiologi (hsv//swe)
- MEDICAL AND HEALTH SCIENCES -- Basic Medicine -- Cell and Molecular Biology (hsv//eng)
- MEDICIN OCH HÄLSOVETENSKAP -- Medicinsk bioteknologi -- Medicinsk bioteknologi (hsv//swe)
- MEDICAL AND HEALTH SCIENCES -- Medical Biotechnology -- Medical Biotechnology (hsv//eng)
- MEDICIN OCH HÄLSOVETENSKAP -- Medicinska och farmaceutiska grundvetenskaper -- Läkemedelskemi (hsv//swe)
- MEDICAL AND HEALTH SCIENCES -- Basic Medicine -- Medicinal Chemistry (hsv//eng)
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- By the author/editor
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Zhang, Liying
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Simonsen, Charlo ...
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Zimova, Lucie
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Wang, Kaituo
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Moparthi, Lavany ...
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Gaudet, Rachelle
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Ekoff, Maria
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Nilsson, Gunnar
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Hellmich, Ute A.
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Vlachova, Viktor ...
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Gourdon, Pontus
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Zygmunt, Peter M ...
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- MEDICAL AND HEALTH SCIENCES
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MEDICAL AND HEAL ...
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and Basic Medicine
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and Cell and Molecul ...
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- MEDICAL AND HEALTH SCIENCES
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MEDICAL AND HEAL ...
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and Medical Biotechn ...
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and Medical Biotechn ...
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- MEDICAL AND HEALTH SCIENCES
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MEDICAL AND HEAL ...
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and Basic Medicine
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and Medicinal Chemis ...
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Nature Communica ...
- By the university
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Lund University
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Linköping University
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Karolinska Institutet