Internalisation of the protease-activated receptor 1: Role of the third intracellular loop and of the cytoplasmic tail

  • Authors:
    • Xin Chen
    • Jeannig Berrou
    • Cecile Vigneau
    • Francoise Delarue
    • Eric Rondeau
  • View Affiliations

  • Published online on: June 1, 2001     https://doi.org/10.3892/ijmm.7.6.653
  • Pages: 653-658
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Abstract

To analyse the mechanisms of PAR-1 internalisation, we constructed several PAR-1 mutants and stably expressed them in CHO cells. Our study shows that the Ser306↷Ala mutation (S306A), which eliminates a potential site of phosphorylation by PKC in the third intracellular loop of PAR-1, did not change the rate of phosphorylation but reduced the rate of thrombin-induced internalisation of the PAR-1 mutant (58 versus 78% of membrane PAR-1 in 15 min, p<0.005). Deletion of the last 43 amino acid residues of the PAR-1 cytoplasmic tail completely suppressed the thrombin phosphorylation of the mutated receptor and significantly reduced its internalisation upon activation. This deletion also inhibited the PMA-induced and the agonist-independent internalisation of the receptor. The Tyr371↷Ala mutation (Y371A), in a NPXXY motif of the seventh transmembrane domain of the receptor had no effect on the receptor behaviour. Our results indicate that both the C-tail and the third intracellular loop are involved in PAR-1 internalisation induced by thrombin while only the C-tail plays a role in the PMA-induced and in the agonist-independent PAR-1 internalisation.

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June 2001
Volume 7 Issue 6

Print ISSN: 1107-3756
Online ISSN:1791-244X

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Spandidos Publications style
Chen X, Berrou J, Vigneau C, Delarue F and Rondeau E: Internalisation of the protease-activated receptor 1: Role of the third intracellular loop and of the cytoplasmic tail. Int J Mol Med 7: 653-658, 2001
APA
Chen, X., Berrou, J., Vigneau, C., Delarue, F., & Rondeau, E. (2001). Internalisation of the protease-activated receptor 1: Role of the third intracellular loop and of the cytoplasmic tail. International Journal of Molecular Medicine, 7, 653-658. https://doi.org/10.3892/ijmm.7.6.653
MLA
Chen, X., Berrou, J., Vigneau, C., Delarue, F., Rondeau, E."Internalisation of the protease-activated receptor 1: Role of the third intracellular loop and of the cytoplasmic tail". International Journal of Molecular Medicine 7.6 (2001): 653-658.
Chicago
Chen, X., Berrou, J., Vigneau, C., Delarue, F., Rondeau, E."Internalisation of the protease-activated receptor 1: Role of the third intracellular loop and of the cytoplasmic tail". International Journal of Molecular Medicine 7, no. 6 (2001): 653-658. https://doi.org/10.3892/ijmm.7.6.653