Table 1 Binding and biological activity parameters of secretin probes on CHO cell lines expressing human WT and mutant SecR

From: Impact of secretin receptor homo-dimerization on natural ligand binding

 

pKi

P values vs Sec

Bmax × 103 sites/cells

P values vs Sec

pEC50

P values vs Sec

SecR WT

 Sec

8.5 ± 0.1

 

68 ± 5

 

11.3 ± 0.1

 

 Alexa488-Sec

7.6 ± 0.1**

0.001

66 ± 7

0.762

10.2 ± 0.2**

0.001

 (Lys13-Alexa488)Sec

8.3 ± 0.1

0.30

67 ± 6

0.993

10.6 ± 0.2*

0.027

 (Lys22-Alexa488)Sec

8.2 ± 0.1

0.098

68 ± 7

0.998

10.8 ± 0.1

0.10

 Sec-Gly28-(Cys29-Alexa488)

8.1 ± 0.1

0.07

66 ± 8

0.654

11.1 ± 0.1

0.93

SecR(G264A,I268A)

 Sec

8.6 ± 0.1

 

60 ± 6

 

10.6 ± 0.1#

0.029

 Alexa488-Sec

7.6 ± 0.2**

0.004

62 ± 4

0.926

9.4 ± 0.3**

0.002

 (Lys13-Alexa488)Sec

8.3 ± 0.2

0.47

61 ± 5

0.981

9.9 ± 0.3

0.10

 (Lys22-Alexa488)Sec

8.1 ± 0.1

0.14

61 ± 9

0.996

9.9 ± 0.1

0.069

 Sec-Gly28-(Cys29-Alexa488)

8.6 ± 0.1

>0.99

61 ± 8

0.972

10.5 ± 0.2

0.98

  1. Values are expressed in means ± S.E.M. of four independent experiments performed in duplicate, and significant differences were tested using one-way ANOVA with Dunnett’s post-test.
  2. *P < 0.05, **P < 0.01, significantly different from natural secretin peptide at the same receptor construct; #P < 0.05, significantly different from the same condition at the SecR WT construct.
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