Journal of Biological Chemistry
Volume 296, January–June 2021, 100345
Research ArticleA lipid-anchored neurokinin 1 receptor antagonist prolongs pain relief by a three-pronged mechanism of action targeting the receptor at the plasma membrane and in endosomes
Under a Creative Commons license
open access
Keywords
drug delivery
endosome
G-protein-coupled receptor
cell signaling
pain
lipid conjugation
tachykinin
Abbreviations
AC
adenylyl cyclase
BACE-1
β-site amyloid precursor protein cleaving enzyme 1
BRET
bioluminescence resonance energy transfer
cAMP
cyclic adenosine monophosphate
Chol
biotin conjugated to cholestanol via a PEG linker
CFP
cyan fluorescent protein
Cy5
cyanine 5
Cy5-Chol
cyanine 5 with cholestanol linked via PEG
Cy5-OEt
cyanine 5 with an ethyl ester linked via PEG
cytoCKAR
cytosolic C kinase activity reporter FRET biosensor
cytoEpac2
cytosolic Epac2-camps FRET biosensor
DAG
diacylglycerol
DMEM
Dulbecco’s modified Eagle’s medium
EGFR
epidermal growth factor receptor
ERK
extracellular signal regulated kinase (mitogen activated protein kinase)
FBS
fetal bovine serum
FCS
fluorescence correlation spectroscopy
GPCR
G protein-coupled receptor
InsP3
inositol trisphosphate
NK1R
neurokinin 1 receptor
OEt
ethyl ester
PKA
protein kinase A
PKC
protein kinase C
pmEpac2
plasma membrane localized Epac2-camps FRET biosensor
RLuc8
Renilla luciferase
SP
substance P
Span
Spantide I
Span-Chol
Spantide I conjugated to cholestanol via PEG linker
TAMRA
tetramethylrhodamine
YFP
yellow fluorescent protein
Cited by (0)
Present address for Quynh N. Mai: Cardiovascular Research Institute, Department of Biochemistry and Biophysics, University of California, San Francisco, CA 94158.
This article contains supporting information.
© 2021 The Authors. Published by Elsevier Inc on behalf of American Society for Biochemistry and Molecular Biology.