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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