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RyR2

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Target not currently curated in GtoImmuPdb

Target id: 748

Nomenclature: RyR2

Family: Ryanodine receptors (RyR)

Contents:

Gene and Protein Information Click here for help
Species TM P Loops AA Chromosomal Location Gene Symbol Gene Name Reference
Human 6 0 4967 1q43 RYR2 ryanodine receptor 2
Mouse 7 0 4966 13 4.38 cM Ryr2 ryanodine receptor 2, cardiac
Rat 7 0 4953 17q12.1 Ryr2 ryanodine receptor 2
Previous and Unofficial Names Click here for help
ARVD2 | cardiac muscle ryanodine receptor | cardiac muscle ryanodine receptor-calcium release channel | ryanodine receptor 2 | ryanodine receptor 2, cardiac | RYR-2 | arrhythmogenic right ventricular dysplasia 2 | VTSIP | ryanodine receptor 2 (cardiac)
Database Links Click here for help
Alphafold Q92736 (Hs), Q9ERN6 (Mm), B0LPN4 (Rn)
CATH/Gene3D 1.25.10.10
ChEMBL Target CHEMBL4403 (Hs), CHEMBL3388 (Rn)
Ensembl Gene ENSG00000198626 (Hs), ENSMUSG00000021313 (Mm), ENSRNOG00000017060 (Rn)
Entrez Gene 6262 (Hs), 20191 (Mm)
Human Protein Atlas ENSG00000198626 (Hs)
KEGG Gene hsa:6262 (Hs), mmu:20191 (Mm)
OMIM 180902 (Hs)
Pharos Q92736 (Hs)
UniProtKB Q92736 (Hs), Q9ERN6 (Mm), B0LPN4 (Rn)
Wikipedia RYR2 (Hs)
Functional Characteristics Click here for help
Ca2+: (P Ca/P K6) single-channel conductance: 90 pS (50 mM Ca2+), 720 pS (210 mM K+)

Download all structure-activity data for this target as a CSV file go icon to follow link

Activators
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Concentration range (M) Holding voltage (mV) Reference
caffeine Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs - - - - -
⤷ pharmacological; mM range
cytosolic Ca2+ Click here for species-specific activity table Ligand is endogenous in the given species Hs - - - - -
⤷ endogenous; μM range
luminal Ca2+ Click here for species-specific activity table Ligand is endogenous in the given species Hs - - - - -
⤷ endogenous
cytosolic ATP Small molecule or natural product Click here for species-specific activity table Ligand is endogenous in the given species Ligand has a PDB structure Hs - - - - -
⤷ endogenous; mM range
suramin Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs - - - - -
⤷ pharmacological; μM range
ryanodine Small molecule or natural product Click here for species-specific activity table Hs - - - - -
⤷ pharmacological; nM - μM range
Inhibitors
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Concentration range (M) Holding voltage (mV) Reference
carvedilol Small molecule or natural product Approved drug Click here for species-specific activity table Hs Inhibition 4.8 pIC50 - - 1
⤷ pIC50 4.8 (IC50 1.59x10-5 M) [1]
Description: Inhibition of R4496C mutant RyR2 (expressed in HEK293 cells)-mediated store-overload induced calcium release after 8 to 10 mins using a fura-2/AM dye-based fluorescence assay.
VK-II-86 Small molecule or natural product Hs Inhibition 4.8 pIC50 - - 1
⤷ pIC50 4.8 (IC50 1.68x10-5 M) [1]
Description: Inhibition of R4496C mutant RyR2 (expressed in HEK293 cells)-mediated store-overload induced calcium release after 8 to 10 mins using a fura-2/AM dye-based fluorescence assay.
Antagonists
Key to terms and symbols Click column headers to sort
Ligand Sp. Action Value Parameter Reference
cytosolic Ca2+ Click here for species-specific activity table Ligand is endogenous in the given species Hs Antagonist - -
⤷ Conc range: > 1x10-3 M
cytosolic Mg2+ Click here for species-specific activity table Ligand is endogenous in the given species Hs Antagonist - -
⤷ mM range
Channel Blockers
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Concentration range (M) Holding voltage (mV) Reference
ryanodine Small molecule or natural product Click here for species-specific activity table Hs - - - > 1x10-4 -
⤷ Conc range: > 1x10-4 M
ruthenium red Click here for species-specific activity table Hs - - - - -
⤷
procaine Small molecule or natural product Approved drug Click here for species-specific activity table Hs - - - - -
⤷

References

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1. Smith CD, Wang A, Vembaiyan K, Zhang J, Xie C, Zhou Q, Wu G, Chen SR, Back TG. (2013) Novel carvedilol analogues that suppress store-overload-induced Ca2+ release. J Med Chem, 56 (21): 8626-55. [PMID:24124794]

How to cite this page

Ryanodine receptors (RyR): RyR2. Last modified on 18/12/2018. Accessed on 08/12/2024. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=748.