Table 2 Summary of pharmacological parameters measured for apelin receptor variants

From: Structural and functional determination of peptide versus small molecule ligand binding at the apelin receptor

Variant

Expression

Fl. ligand binding

Radioligand binding

Function

Mem. eGFP (% WT)

Object count/ region

Mem. apelin647 (% WT)

Mem. ELA647 (% WT)

KD (nM)

Bmax (fmol/ mg)

Hill slope (nH)

pD2

Emax (ΔPWV)

WT

100.00 

± 23.52

17.00 

± 6.88

100.0 

± 27.09

100.00 

± 19.10

0.21 

± 0.05

236.80 

± 27.07

1.26 

± 0.22

8.32 

± 0.24

39.48 

± 3.93

V/L381.42

121.40 

± 31.87

16.58 

± 7.99

94.74 

± 17.52

92.53 

± 28.43

NBD

NBD

NBD

7.67 

± 0.48

42.55 

± 15.16

G/X451.49

32.18 

± 16.67

7.67 

± 3.68

12.18 

± 6.48

20.73 

± 12.55

NBD

NBD

NBD

T/M892.64

104.94 

± 34.40

19.83 

± 8.67

82.95 

± 24.46

31.75 

± 13.20

0.25 

± 0.04

440.47 

± 38.36

1.55 

± 0.22

7.72 

± 0.21

50.06 

± 8.32

R/H1684.64

119.93 

± 40.29

23.00 

± 10.04

2.53 

± 2.10

17.29 

± 9.42

NBD

NBD

NBD

n/a

5.49 

± 6.42

T/X2275.64

12.38 

± 3.90

5.08 

± 1.51

2.94 

± 2.78

14.83 

± 7.02

NBD

NBD

NBD

Untrans.

0.00

0.00

0.00

0.00

NBD

NBD

NBD

n/a

0.21 

± 7.07

  1. Colours indicate the missense (V/L381.42, blue; T/M892.64, red; R/H1684.64, magenta) or frameshift (G/X451.49, T/X2275.64, both yellow) variants.
  2. Mem. membrane, Fl. ligand fluorescent ligand, ΔPWV change in peak wavelength value, WT cells transfected with wild-type apelin receptor, Untrans. untransfected cells.