6CJT
 
 | | Structure of the SthK cyclic nucleotide-gated potassium channel in complex with cGMP | | Descriptor: | (1R)-2-{[(S)-{[(2S)-2,3-dihydroxypropyl]oxy}(hydroxy)phosphoryl]oxy}-1-[(hexadecanoyloxy)methyl]ethyl (9Z)-octadec-9-enoate, CYCLIC GUANOSINE MONOPHOSPHATE, SthK cyclic nucleotide-gated potassium channel | | Authors: | Nimigean, C.M, Rheinberger, J. | | Deposit date: | 2018-02-26 | | Release date: | 2018-08-01 | | Last modified: | 2024-03-13 | | Method: | ELECTRON MICROSCOPY (3.46 Å) | | Cite: | Ligand discrimination and gating in cyclic nucleotide-gated ion channels from apo and partial agonist-bound cryo-EM structures.
Elife, 7, 2018
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6CJU
 | | Structure of the SthK cyclic nucleotide-gated potassium channel in complex with cAMP | | Descriptor: | (1R)-2-{[(S)-{[(2S)-2,3-dihydroxypropyl]oxy}(hydroxy)phosphoryl]oxy}-1-[(hexadecanoyloxy)methyl]ethyl (9Z)-octadec-9-enoate, ADENOSINE-3',5'-CYCLIC-MONOPHOSPHATE, SthK cyclic nucleotide-gated potassium channel | | Authors: | Nimigean, C.M, Rheinberger, J. | | Deposit date: | 2018-02-26 | | Release date: | 2018-08-01 | | Last modified: | 2024-03-13 | | Method: | ELECTRON MICROSCOPY (3.35 Å) | | Cite: | Ligand discrimination and gating in cyclic nucleotide-gated ion channels from apo and partial agonist-bound cryo-EM structures.
Elife, 7, 2018
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6CO7
 | | Structure of the nvTRPM2 channel in complex with Ca2+ | | Descriptor: | (2S)-3-(hexadecanoyloxy)-2-[(9Z)-octadec-9-enoyloxy]propyl 2-(trimethylammonio)ethyl phosphate, 2-acetamido-2-deoxy-beta-D-glucopyranose-(1-4)-2-acetamido-2-deoxy-beta-D-glucopyranose, CALCIUM ION, ... | | Authors: | Zhang, Z, Toth, B, Szollosi, A, Chen, J, Csanady, L. | | Deposit date: | 2018-03-12 | | Release date: | 2018-05-16 | | Last modified: | 2020-07-29 | | Method: | ELECTRON MICROSCOPY (3.07 Å) | | Cite: | Structure of a TRPM2 channel in complex with Ca2+explains unique gating regulation.
Elife, 7, 2018
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6CJQ
 | | Structure of the SthK cyclic nucleotide-gated potassium channel | | Descriptor: | (1R)-2-{[(S)-{[(2S)-2,3-dihydroxypropyl]oxy}(hydroxy)phosphoryl]oxy}-1-[(hexadecanoyloxy)methyl]ethyl (9Z)-octadec-9-enoate, SthK cyclic nucleotide-gated potassium channel | | Authors: | Nimigean, C.M, Rheinberger, J. | | Deposit date: | 2018-02-26 | | Release date: | 2018-08-01 | | Last modified: | 2024-03-13 | | Method: | ELECTRON MICROSCOPY (3.42 Å) | | Cite: | Ligand discrimination and gating in cyclic nucleotide-gated ion channels from apo and partial agonist-bound cryo-EM structures.
Elife, 7, 2018
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8JU6
 | | Structure of human TRPV4 with antagonist GSK279 | | Descriptor: | 1-({(5S,7S)-3-[5-(2-hydroxypropan-2-yl)pyrazin-2-yl]-7-methyl-2-oxo-1-oxa-3-azaspiro[4.5]decan-7-yl}methyl)-1H-benzimidazole-6-carbonitrile, Transient receptor potential cation channel subfamily V member 4,3C-GFP | | Authors: | Fan, J, Lei, X. | | Deposit date: | 2023-06-24 | | Release date: | 2024-05-08 | | Method: | ELECTRON MICROSCOPY (3.45 Å) | | Cite: | Structural Pharmacology of TRPV4 Antagonists.
Adv Sci, 2024
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8JU5
 | | Structure of human TRPV4 with antagonist A1 | | Descriptor: | 4-[(3~{S},4~{S})-4-(aminomethyl)-1-(5-chloranylpyridin-2-yl)sulfonyl-4-oxidanyl-pyrrolidin-3-yl]oxy-2-fluoranyl-benzenecarbonitrile, Transient receptor potential cation channel subfamily V member 4,3C-GFP | | Authors: | Fan, J, Lei, X. | | Deposit date: | 2023-06-24 | | Release date: | 2024-05-08 | | Method: | ELECTRON MICROSCOPY (3.74 Å) | | Cite: | Structural Pharmacology of TRPV4 Antagonists.
Adv Sci, 2024
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8JVJ
 | | Structure of human TRPV4 with antagonist A2 and RhoA | | Descriptor: | Transforming protein RhoA, Transient receptor potential cation channel subfamily V member 4,3C-GFP, [6-[[4-(2,4-dimethyl-1,3-thiazol-5-yl)-1,3-thiazol-2-yl]amino]pyridin-3-yl]-[(1~{S},5~{R})-3-[5-(trifluoromethyl)pyrimidin-2-yl]-3,8-diazabicyclo[3.2.1]octan-8-yl]methanone | | Authors: | Fan, J, Lei, X. | | Deposit date: | 2023-06-28 | | Release date: | 2024-05-08 | | Method: | ELECTRON MICROSCOPY (3.44 Å) | | Cite: | Structural Pharmacology of TRPV4 Antagonists.
Adv Sci, 2024
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8JVI
 | | Structure of human TRPV4 with antagonist A2 | | Descriptor: | Transient receptor potential cation channel subfamily V member 4,3C-GFP, [6-[[4-(2,4-dimethyl-1,3-thiazol-5-yl)-1,3-thiazol-2-yl]amino]pyridin-3-yl]-[(1~{S},5~{R})-3-[5-(trifluoromethyl)pyrimidin-2-yl]-3,8-diazabicyclo[3.2.1]octan-8-yl]methanone | | Authors: | Fan, J, Lei, X. | | Deposit date: | 2023-06-28 | | Release date: | 2024-05-08 | | Method: | ELECTRON MICROSCOPY (3.21 Å) | | Cite: | Structural Pharmacology of TRPV4 Antagonists.
Adv Sci, 2024
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7JUP
 | | Structure of human TRPA1 in complex with antagonist compound 21 | | Descriptor: | 1-({3-[(3R,5R)-5-(4-fluorophenyl)oxolan-3-yl]-1,2,4-oxadiazol-5-yl}methyl)-7-methyl-1,7-dihydro-6H-purin-6-one, Transient receptor potential cation channel subfamily A member 1 | | Authors: | Rohou, A, Rouge, L. | | Deposit date: | 2020-08-20 | | Release date: | 2021-03-31 | | Last modified: | 2024-03-06 | | Method: | ELECTRON MICROSCOPY (3.05 Å) | | Cite: | Tetrahydrofuran-Based Transient Receptor Potential Ankyrin 1 (TRPA1) Antagonists: Ligand-Based Discovery, Activity in a Rodent Asthma Model, and Mechanism-of-Action via Cryogenic Electron Microscopy.
J.Med.Chem., 64, 2021
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7JPX
 | | Rabbit Cav1.1 in the presence of 100 micromolar amlodipine in nanodiscs at 2.9 Angstrom resolution | | Descriptor: | (2S)-3-(hexadecanoyloxy)-2-[(9Z)-octadec-9-enoyloxy]propyl 2-(trimethylammonio)ethyl phosphate, 1,2-DIACYL-SN-GLYCERO-3-PHOSPHOCHOLINE, 1,2-DIACYL-SN-GLYCERO-3-PHOSPHOETHANOLAMINE, ... | | Authors: | Yan, N, Gao, S. | | Deposit date: | 2020-08-10 | | Release date: | 2020-11-18 | | Last modified: | 2021-03-10 | | Method: | ELECTRON MICROSCOPY (2.9 Å) | | Cite: | Structural Basis of the Modulation of the Voltage-Gated Calcium Ion Channel Ca v 1.1 by Dihydropyridine Compounds*.
Angew.Chem.Int.Ed.Engl., 60, 2021
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7JPL
 | | Rabbit Cav1.1 in the presence of 10 micromolar (S)-(-)-Bay K8644 in nanodiscs at 3.4 Angstrom resolution | | Descriptor: | 1,2-DIACYL-SN-GLYCERO-3-PHOSPHOCHOLINE, 1,2-DIACYL-SN-GLYCERO-3-PHOSPHOETHANOLAMINE, CALCIUM ION, ... | | Authors: | Yan, N, Gao, S. | | Deposit date: | 2020-08-09 | | Release date: | 2020-11-18 | | Last modified: | 2021-03-10 | | Method: | ELECTRON MICROSCOPY (3.4 Å) | | Cite: | Structural Basis of the Modulation of the Voltage-Gated Calcium Ion Channel Ca v 1.1 by Dihydropyridine Compounds*.
Angew.Chem.Int.Ed.Engl., 60, 2021
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7JPW
 | | Rabbit Cav1.1 in the presence of 100 micromolar (R)-(+)-Bay K8644 in nanodiscs at 3.2 Angstrom resolution | | Descriptor: | 1,2-DIACYL-SN-GLYCERO-3-PHOSPHOCHOLINE, 1,2-DIACYL-SN-GLYCERO-3-PHOSPHOETHANOLAMINE, CALCIUM ION, ... | | Authors: | Yan, N, Gao, S. | | Deposit date: | 2020-08-10 | | Release date: | 2020-11-18 | | Last modified: | 2021-03-10 | | Method: | ELECTRON MICROSCOPY (3.2 Å) | | Cite: | Structural Basis of the Modulation of the Voltage-Gated Calcium Ion Channel Ca v 1.1 by Dihydropyridine Compounds*.
Angew.Chem.Int.Ed.Engl., 60, 2021
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7K4F
 | | Cryo-EM structure of human TRPV6 in complex with (4- phenylcyclohexyl)piperazine inhibitor 31 | | Descriptor: | 5-[(4-{cis-4-[3-(trifluoromethyl)phenyl]cyclohexyl}piperazin-1-yl)methyl]pyridin-2(1H)-one, CALCIUM ION, Transient receptor potential cation channel subfamily V member 6 | | Authors: | Neuberger, A, Nadezhdin, K.D, Singh, A.K, Sobolevsky, A.I. | | Deposit date: | 2020-09-15 | | Release date: | 2020-12-09 | | Last modified: | 2024-03-06 | | Method: | ELECTRON MICROSCOPY (3.75 Å) | | Cite: | Inactivation-mimicking block of the epithelial calcium channel TRPV6.
Sci Adv, 6, 2020
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7K4D
 | | Cryo-EM structure of human TRPV6 in complex with (4- phenylcyclohexyl)piperazine inhibitor 3OG | | Descriptor: | 5-[(4-{trans-4-hydroxy-4-[3-(trifluoromethyl)phenyl]cyclohexyl}piperazin-1-yl)methyl]pyridin-2(1H)-one, CALCIUM ION, Transient receptor potential cation channel subfamily V member 6 | | Authors: | Neuberger, A, Nadezhdin, K.D, Singh, A.K, Sobolevsky, A.I. | | Deposit date: | 2020-09-15 | | Release date: | 2020-12-09 | | Last modified: | 2024-03-06 | | Method: | ELECTRON MICROSCOPY (3.66 Å) | | Cite: | Inactivation-mimicking block of the epithelial calcium channel TRPV6.
Sci Adv, 6, 2020
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7JPK
 | | Rabbit Cav1.1 in the presence of 100 micromolar (S)-(-)-Bay K8644 in nanodiscs at 3.0 Angstrom resolution | | Descriptor: | 1,2-DIACYL-SN-GLYCERO-3-PHOSPHOCHOLINE, 1,2-DIACYL-SN-GLYCERO-3-PHOSPHOETHANOLAMINE, CALCIUM ION, ... | | Authors: | Yan, N, Gao, S. | | Deposit date: | 2020-08-09 | | Release date: | 2020-11-18 | | Last modified: | 2021-03-10 | | Method: | ELECTRON MICROSCOPY (3 Å) | | Cite: | Structural Basis of the Modulation of the Voltage-Gated Calcium Ion Channel Ca v 1.1 by Dihydropyridine Compounds*.
Angew.Chem.Int.Ed.Engl., 60, 2021
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7K4B
 | | Cryo-EM structure of human TRPV6 in complex with (4- phenylcyclohexyl)piperazine inhibitor cis-22a | | Descriptor: | 1,2-DIOLEOYL-SN-GLYCERO-3-PHOSPHOCHOLINE, 1-[cis-4-(3-methylphenyl)cyclohexyl]-4-(pyridin-3-yl)piperazine, CALCIUM ION, ... | | Authors: | Neuberger, A, Nadezhdin, K.D, Singh, A.K, Sobolevsky, A.I. | | Deposit date: | 2020-09-15 | | Release date: | 2020-12-09 | | Last modified: | 2024-03-06 | | Method: | ELECTRON MICROSCOPY (3.1 Å) | | Cite: | Inactivation-mimicking block of the epithelial calcium channel TRPV6.
Sci Adv, 6, 2020
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7JPV
 | | Rabbit Cav1.1 in the presence of 1 micromolar (S)-(-)-Bay K8644 in nanodiscs at 3.4 Angstrom resolution | | Descriptor: | 1,2-DIACYL-SN-GLYCERO-3-PHOSPHOCHOLINE, 1,2-DIACYL-SN-GLYCERO-3-PHOSPHOETHANOLAMINE, CALCIUM ION, ... | | Authors: | Yan, N, Gao, S. | | Deposit date: | 2020-08-10 | | Release date: | 2020-11-18 | | Last modified: | 2021-03-10 | | Method: | ELECTRON MICROSCOPY (3.4 Å) | | Cite: | Structural Basis of the Modulation of the Voltage-Gated Calcium Ion Channel Ca v 1.1 by Dihydropyridine Compounds*.
Angew.Chem.Int.Ed.Engl., 60, 2021
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7K4C
 | | Cryo-EM structure of human TRPV6 in complex with (4- phenylcyclohexyl)piperazine inhibitor Br-cis-22a | | Descriptor: | 1-(5-bromopyridin-3-yl)-4-[cis-4-(3-methylphenyl)cyclohexyl]piperazine, CALCIUM ION, Transient receptor potential cation channel subfamily V member 6 | | Authors: | Neuberger, A, Nadezhdin, K.D, Singh, A.K, Sobolevsky, A.I. | | Deposit date: | 2020-09-15 | | Release date: | 2020-12-09 | | Last modified: | 2024-03-06 | | Method: | ELECTRON MICROSCOPY (3.78 Å) | | Cite: | Inactivation-mimicking block of the epithelial calcium channel TRPV6.
Sci Adv, 6, 2020
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7K4E
 | | Cryo-EM structure of human TRPV6 in complex with (4- phenylcyclohexyl)piperazine inhibitor 30 | | Descriptor: | 5-({4-[(1R,4S)-3'-methyl[1,2,3,4-tetrahydro[1,1'-biphenyl]]-4-yl]piperazin-1-yl}methyl)pyridin-2(1H)-one, Transient receptor potential cation channel subfamily V member 6 | | Authors: | Neuberger, A, Nadezhdin, K.D, Singh, A.K, Sobolevsky, A.I. | | Deposit date: | 2020-09-15 | | Release date: | 2020-12-09 | | Last modified: | 2024-03-06 | | Method: | ELECTRON MICROSCOPY (4.34 Å) | | Cite: | Inactivation-mimicking block of the epithelial calcium channel TRPV6.
Sci Adv, 6, 2020
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7L2O
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7L2K
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7L2U
 | | cryo-EM structure of DkTx-bound minimal TRPV1 in open state | | Descriptor: | (11R,14S)-17-amino-14-hydroxy-8,14-dioxo-9,13,15-trioxa-14lambda~5~-phosphaheptadecan-11-yl decanoate, (2S)-1-(butanoyloxy)-3-{[(R)-hydroxy{[(1r,2R,3S,4S,5R,6S)-2,3,4,5,6-pentahydroxycyclohexyl]oxy}phosphoryl]oxy}propan-2-yl tridecanoate, SODIUM ION, ... | | Authors: | Zhang, K, Julius, D, Cheng, Y. | | Deposit date: | 2020-12-17 | | Release date: | 2021-09-22 | | Last modified: | 2021-10-13 | | Method: | ELECTRON MICROSCOPY (3.47 Å) | | Cite: | Structural snapshots of TRPV1 reveal mechanism of polymodal functionality.
Cell, 184, 2021
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7L2R
 | | Cryo-EM structure of DkTx-bound minimal TRPV1 at the pre-open state | | Descriptor: | (2S)-1-(butanoyloxy)-3-{[(R)-hydroxy{[(1r,2R,3S,4S,5R,6S)-2,3,4,5,6-pentahydroxycyclohexyl]oxy}phosphoryl]oxy}propan-2-yl tridecanoate, (9R,12R)-15-amino-12-hydroxy-6,12-dioxo-7,11,13-trioxa-12lambda~5~-phosphapentadecan-9-yl undecanoate, SODIUM ION, ... | | Authors: | Zhang, K, Julius, D, Cheng, Y. | | Deposit date: | 2020-12-17 | | Release date: | 2021-09-22 | | Last modified: | 2021-10-13 | | Method: | ELECTRON MICROSCOPY (3.3 Å) | | Cite: | Structural snapshots of TRPV1 reveal mechanism of polymodal functionality.
Cell, 184, 2021
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7L2M
 | | Cryo-EM structure of DkTx/RTX-bound full-length TRPV1 | | Descriptor: | SODIUM ION, Tau-theraphotoxin-Hs1a, Transient receptor potential cation channel subfamily V member 1, ... | | Authors: | Zhang, K, Julius, D, Cheng, Y. | | Deposit date: | 2020-12-17 | | Release date: | 2021-09-22 | | Last modified: | 2021-10-13 | | Method: | ELECTRON MICROSCOPY (3.84 Å) | | Cite: | Structural snapshots of TRPV1 reveal mechanism of polymodal functionality.
Cell, 184, 2021
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7L2H
 | | Cryo-EM structure of unliganded full-length TRPV1 at neutral pH | | Descriptor: | (10R,13S)-16-amino-13-hydroxy-7,13-dioxo-8,12,14-trioxa-13lambda~5~-phosphahexadecan-10-yl tridecanoate, (2S)-1-(butanoyloxy)-3-{[(R)-hydroxy{[(1r,2R,3S,4S,5R,6S)-2,3,4,5,6-pentahydroxycyclohexyl]oxy}phosphoryl]oxy}propan-2-yl tridecanoate, SODIUM ION, ... | | Authors: | Zhang, K, Julius, D, Cheng, Y. | | Deposit date: | 2020-12-17 | | Release date: | 2021-09-22 | | Last modified: | 2021-10-13 | | Method: | ELECTRON MICROSCOPY (2.63 Å) | | Cite: | Structural snapshots of TRPV1 reveal mechanism of polymodal functionality.
Cell, 184, 2021
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