Table 1 Binding of GLP-2 and teduglutide with GLP-2R mutantsa.

From: A unique hormonal recognition feature of the human glucagon-like peptide-2 receptor

 

Human GLP-2 (1–33)

Teduglutide

Receptor mutant

pIC50

% Binding of WTb

pIC50

% Binding of WT

WT (1–553)

8.5 ± 0.07

99.2 ± 2.3

8.8 ± 0.05

99.7 ± 1.9

Y1821.43A

9.1 ± 1.2

3.4 ± 1.0***

9.2 ± 0.8

3.2 ± 1.3***

Y1861.47A

N.B.c

N.B.

N.B.

N.B.

K2312.67A

N.B.

N.B.

N.B.

N.B.

R242ECL1E

N.B.

N.B.

N.B.

N.B.

R242ECL1A

8.0 ± 0.5

4.2 ± 0.6***

8.7 ± 0.8

5.1 ± 1.5***

D244ECL1A

8.6 ± 0.2

69.1 ± 4.9***

9.0 ± 0.2

77.5 ± 5.7***

N247ECL1A

8.2 ± 0.1

130.7 ± 4.5***

8.6 ± 0.1

135.2 ± 4.4***

W249ECL1A

9.0 ± 1.2

2.2 ± 1.2***

8.8 ± 1.7

2.9 ± 2.0***

Y252ECL1A

8.4 ± 0.8

8.3 ± 1.8***

9.0 ± 0.6

6.3 ± 1.7***

H2683.37A

8.0 ± 1.4

2.1 ± 0.8***

9.7 ± 3.2

0.7 ± 1.8***

N334ECL2 A

9.5 ± 1.8

2.4 ± 1.3***

9.7 ± 2.7

2.0 ± 2.1***

W3405.36A

7.1 ± 0.4

7.3 ± 0.6***

8.8 ± 0.7

8.6 ± 1.8***

R3445.40A

8.6 ± 0.5

5.0 ± 0.8***

9.3 ± 0.6

3.5 ± 0.8***

K4147.35 A

8.5 ± 0.2

15.2 ± 1.0***

8.7 ± 0.2

13.9 ± 0.8***

ECL1 (GLP-1R)d

8.9 ± 1.7

3.4 ± 1.3***

7.8 ± 0.7

1.2 ± 0.5***

ECL1 (poly-alanine)d

8.2 ± 1.3

3.0 ± 1.1***

N.B.

N.B.

  1. ***P  < 0.001.
  2. aAll data were fitted with a three-parameter logistic curve to obtain pIC50 values. Data represent means ± SEM of at least three independent experiments performed in duplicate. One-way ANOVA and Dunnett’s post hoc tests were used to determine statistical differences.
  3. bWT wild-type.
  4. cN.B. no binding of the radioligand.
  5. dGLP-2R mutants with ECL1 (residues 236–257) substituted by the corresponding segment of GLP-1R or poly-alanine are labeled as ECL1 (GLP-1R) and ECL1 (poly-alanine), respectively.
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