Biomedical Engineering Reference
In-Depth Information
Table 3.1
(continued)
Receptor
Class/
a
subclass
Year
PDB code
Resolution (Å)
Ligand
Type
b
Conformational state
Reference
Human chemokine
CXCR4
R/γ
2010
3ODU
2.5
IT1t
Antagonist
Inactive
Wu et al. [
90
]
2010
2OE0
2.9
CVX15
Antagonist
Inactive
Wu et al. [
90
]
Human dopamine D3
R/α
2010
3PBL
2.9
Eticlopride
Antagonist
Inactive
Chien et al. [
91
]
Human histamine H1
R/α
2011
3RZE
3.1
Doxepin
Inverse agonist
Inactive
Shimamura et al. [
92
]
Human sphingosine
1-phosphate
R/α
2012
3V2Y
2.8
ML056
Antagonist
Inactive
Hanson et al. [
93
]
Human M2 muscarinic
acetylcholine
R/α
2012
3UON
3.0
QNB
Antagonist
Inactive
Haga et al. [
94
]
Rat M3 muscarinic
acetylcholine
R/α
2012
4DAJ
3.4
Tiotropium
Inverse agonist
Inactive
Kruse et al. [
95
]
Mouse μ-opioid
R/γ
2012
4DKL
2.8
β-FNA
Irreversible
antagonist
Inactive
Manglik et al. [
96
]
Human κ-opioid
R/γ
2012
4DJH
2.9
JDTic
Selective
antagonist
Inactive
Wu et al. [
77
]
Mouse δ-opioid
R/γ
2012
4EJ4
3.4
Naltrindole
Selective
antagonist
Inactive
Granier et al. [
97
]
Human nociceptin/
orphanin FQ
R/γ
2012
4EA3
3.0
C-24
Antagonist
Inactive
Thompson et al. [
98
]
Rat neurotensin
R/β
2012
4GRV
2.8
Neurotensin
Agonist
Intermediate
White et al. [
99
]
Human protease acti-
vated receptor
1
R/δ
2012
3VW7
2.2
Vorapaxar
Antagonist
Inactive
Zhang C. et al. [
100
]
Human chemokine
CXCR1
R/γ
2012
2LNL
NMR
-
-
inactive
Park et al. [
28
]
a
GRAFS classification [
6
]
b
see Fig.
3.1
Ternary complex with:
c
11 amino acid C terminal fragment of Gt α-subunit,
d
camelid nanobody,
e
Gs protein
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