Synergistic FRET assays for drug discovery targeting RyR2 channels
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Graphical abstract
Keywords
Calcium channel
RyR
Sarco/endoplasmic reticulum
Fluorescence lifetime
Calcium leak
Abbreviations
7,8-DHF
7,8-Dihydroxyflavone hydrate
A-CaM
acceptor labeled calmodulin
A-DPc10
acceptor labeled DPc10
AET
2-(2-Aminoethyl)isothiourea dihydrobromide
APDC
Ammonium pyrrolidinedithiocarbamate
BSA
bovine serum albumin
CaMKII
Calcium/calmodulin-dependent protein kinase II
CaT
calcium transient
cDPCP
cis-diammine(pyridine)chloroplatinum(II) chloride
CPVT
catecholaminergic polymorphic ventricular tachycardia
Ctrl
control
D-FKBP
donor-labeled FK506 binding protein 12.6
DMPP
1,1-dimethyl-4-phenylpiperazinium iodide
E
FRET efficiency
E
east
EGTA
(ethylene glycol-bis(β-aminoethyl ether)-N,N,N′,N′-tetra-acetic acid)
FLT
fluorescence lifetime
HEPES
(4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid)
HTS
high-throughput screening
LOPAC
library of pharmacologically active compounds
N
North
NOBP
6-nitroso-1,2-benzopyrone
Pice
piceatannol
PIPES
piperazine-N,N′-bis(2-ethanesulfonic acid)
PKA
protein kinase A
R(−)-2-OH-Npa HBr
R(−)-2,10,11-trihydroxy-N-propylnoraporphine hydrobromide
R(−)-NPA
N-propylnorapomorphine
Ro90
Ro 90–7501
RyR
ryanodine receptor
S
south
SR
sarcoplasmic reticulum
SERCA
sarco/endoplasmic reticulum Ca-ATPase
W
west
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