Table 1 Average percentage deuterium uptake of small NNC2648 antagonist and des-His1-[Nle9-Ala11-Ala16]-glucagon-NH2 peptide antagonist-bound GCGR at 10 s.

From: Conformational states of the full-length glucagon receptor

Region

Peptide

HDX at 10 s (%)

% Accessible amide protons*

  

NNC2648 bound

des-His 1 -[Nle 9 -Ala 11 -Ala 16 ]-glucagon-NH 2 bound

apo

Glucagon bound

ECD

FLFEKWKL (31–38)

13.3±5.9

3.8±5.4

20.7±9.5

0.3±1.9

Stalk

IEVQKEVAKM (128–137)

59.6±14.6

6.5±6.2

12.7±6.0

0.9±3.3

ECL1

LRTRYSQKIGDDL (198–210)

45.8±3.3

27.2±2.2

42.6±12.7

28.4±13.7

ICL2

ATLPERSF (256–263)

67.9±8.9

56.3±3.3

51.6±16.9

52.2±10.2

TM6

AKSTLTL (348–354)

2.7±0.3

3.2±2.9

0±0

0±0

ECL3

FVTDEHAQGTLRSAKL (367–382)

44.6±4.2

36.3±2.5

42.3±9.8

35.4±8.1

  1. ECD, extracellular domain; ECL1, first extracellular loop; ECL3, third extracellular loop; GCGR, glucagon receptor; HDX, hydrogen/deuterium exchange; ICL2, intracellular loop 2; MD, molecular dynamics; TM6, transmembrane helix 6.
  2. Predicted average amide proton accessibilities of apo-GCGR and glucagon-GCGR derived from MD simulations.
  3. *Values are presented as mean±s.d. of 5,000 snapshots in the last 500-ns simulations of the apo and complex systems, respectively.
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