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. 2023 Jul 10;9:70. doi: 10.1038/s41421-023-00579-3

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© The Author(s) 2023

Open Access This article is licensed under a Creative Commons Attribution 4.0 International License, which permits use, sharing, adaptation, distribution and reproduction in any medium or format, as long as you give appropriate credit to the original author(s) and the source, provide a link to the Creative Commons license, and indicate if changes were made. The images or other third party material in this article are included in the article’s Creative Commons license, unless indicated otherwise in a credit line to the material. If material is not included in the article’s Creative Commons license and your intended use is not permitted by statutory regulation or exceeds the permitted use, you will need to obtain permission directly from the copyright holder. To view a copy of this license, visit http://creativecommons.org/licenses/by/4.0/.

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Fig. 1 — a 3D reconstruction of mTRPV4_apo with each subunit individually colored. The gray bars define the position of the cell membrane. b Cartoon representation of mTRPV4_apo with each subunit individually colored. c Cartoon representation of one subunit of mTRPV4_apo with domains colored in a rainbow. d Profile of pore radii in mTRPV4_apo. The region in red is too narrow to allow a water molecule to pass. e Cylinder representation of mTRPV4 compared to xTRPV4 in the apo state. f 3D reconstruction of mTRPV4_GSK101.The electron density of a GSK101 molecule is highlighted in red. g Ensemble plot of the GSK101 molecule in the cavity formed between S1 to S4 of mTRPV4 in all-atom MD simulations. h GSK101 inside mTRPV4, with the labeling of key residues in the binding sites. i Concentration-response curves of GSK101 activation in WT mTRPV4 and mutants (n = 3–8 cells). Data were presented as mean ± s.e.m. j Profile of pore radii in mTRPV4_GSK101 compared with mTRPV4_apo. k Side view of conformational changes of mTRPV4_GSK101 compared with mTRPV4_apo. Only one subunit was shown for clarity. l Bottom view from the intracellular side of conformational changes of mTRPV4_GSK101 compared with mTRPV4_apo. m Top view from the extracellular side of conformational changes of mTRPV4_GSK101 compared with mTRPV4_apo. n 3D reconstruction of mTRPV4_{GSK101_RR}. The electron density of a Ruthenium Red molecule is highlighted in red. o Cartoon representation of Ruthenium Red in mTRPV4. Key residues close to Ruthenium Red are shown. p Profile of pore radii in mTRPV4_{GSK101_RR}. q Concentration-response curves of Ruthenium Red inhibition in WT TRPV4 and mutants (n = 3–4 cells). Data were presented as mean ± s.e.m. r The electron density of an Agonist-1 molecule is highlighted in red. s Ensemble plot of the Agonist-1 molecule in the binding pocket formed between S1 to S4 of mTRPV4 in all-atom MD simulations. t Cartoon representation of Agonist-1 in mTRPV4. Key residues close to Ruthenium Red are shown. u Concentration-response curves of Agonist-1 activation in WT TRPV4 and mutants (n = 3–4 cells). Data were presented as mean ± s.e.m. v Profile of pore radii in mTRPV4_{Agonist1_RR}. w Side view of the conformational changes of mTRPV4_{Agonist1_RR} compared with mTRPV4_apo. Only one subunit was shown for clarity. x Bottom view from the intracellular side of mTRPV4_{Agonist1_RR} compared with mTRPV4_apo. y Top view from the extracellular side of the conformational changes of mTRPV4_{Agonist1_RR} compared with mTRPV4_apo.