Sandbox Reserved 1652: Difference between revisions

Line 58:

'''Phosphorylation''' of the TRPV1 receptor leads to its sensitization.Phosphorylations occurs on multiple phosphorylation sites at both N-terminal and C-terminal sites of TRPV1 by [https://en.wikipedia.org/wiki/Kinase kinases]. Phosphorylations are either caused by '''PKC''' (IP3 signalling), by '''PKA''' (AMPc signalling) or by '''CamKII'''.<ref>K. W. Ho, N. J. Ward, et D. J. Calkins, « TRPV1: a stress response protein in the central nervous system », Am. J. Neurodegener. Dis., vol. 1, no 1, p. 1‑14, avr. 2012.</ref><ref>G. Smutzer et R. K. Devassy, « Integrating TRPV1 Receptor Function with Capsaicin Psychophysics », Advances in Pharmacological Sciences, janv. 14, 2016.</ref>

PKC phosphorlyates TRPV1 at S800,S502, PKA phosphorylates TRPV1 at S116. The phosphorylation of TRPV1 lead to an increase in the expression of TRPV1 at the membrane surface.<ref>K. W. Ho, N. J. Ward, et D. J. Calkins, « TRPV1: a stress response protein in the central nervous system », Am. J. Neurodegener. Dis., vol. 1, no 1, p. 1‑14, avr. 2012.</ref>. Moreover, phosphorylated TRPV1 would have a reduced channel opening threshold.<ref>G. Bhave et al., « Protein kinase C phosphorylation sensitizes but does not activate the capsaicin receptor transient receptor potential vanilloid 1 (TRPV1) », Proc. Natl. Acad. Sci., vol. 100, no 21, p. 12480‑12485, oct. 2003, doi: 10.1073/pnas.2032100100.</ref>. As a result phosphorylated TRPV1 are more responsive to agonist because they are '''overexpressed''' and the same quantity of agonist leads to a better openings of ion channels.

PKC phosphorlyates TRPV1 at S800,S502, PKA phosphorylates TRPV1 at S116. The phosphorylation of TRPV1 lead to an increase in the expression of TRPV1 at the membrane surface.<ref>K. W. Ho, N. J. Ward, et D. J. Calkins, « TRPV1: a stress response protein in the central nervous system », Am. J. Neurodegener. Dis., vol. 1, no 1, p. 1‑14, avr. 2012.</ref>. Moreover, phosphorylated TRPV1 would have a reduced channel opening threshold.<ref>G. Bhave et al., « Protein kinase C phosphorylation sensitizes but does not activate the capsaicin receptor transient receptor potential vanilloid 1 (TRPV1) », Proc. Natl. Acad. Sci., vol. 100, no 21, p. 12480‑12485, oct. 2003, doi: 10.1073/pnas.2032100100.</ref>. As a result phosphorylated TRPV1 are more responsive to agonist because they are '''overexpressed''' and because the same quantity of agonist leads to a better openings of ion channels.

====Desensitization====

Sandbox Reserved 1652: Difference between revisions

Navigation menu

Page actions

Page actions

Personal tools

Navigation

Search

Tools

@@ Line 58: / Line 58: @@
 '''Phosphorylation''' of the TRPV1 receptor leads to its sensitization.Phosphorylations occurs on multiple phosphorylation sites at both N-terminal and C-terminal sites of TRPV1 by [https://en.wikipedia.org/wiki/Kinase kinases]. Phosphorylations are either caused by '''PKC''' (IP3 signalling), by '''PKA''' (AMPc signalling) or by '''CamKII'''.<ref>K. W. Ho, N. J. Ward, et D. J. Calkins, « TRPV1: a stress response protein in the central nervous system », Am. J. Neurodegener. Dis., vol. 1, no 1, p. 1‑14, avr. 2012.</ref><ref>G. Smutzer et R. K. Devassy, « Integrating TRPV1 Receptor Function with Capsaicin Psychophysics », Advances in Pharmacological Sciences, janv. 14, 2016.</ref>
-PKC phosphorlyates TRPV1 at S800,S502, PKA phosphorylates TRPV1 at S116. The phosphorylation of TRPV1 lead to an increase in the expression of TRPV1 at the membrane surface.<ref>K. W. Ho, N. J. Ward, et D. J. Calkins, « TRPV1: a stress response protein in the central nervous system », Am. J. Neurodegener. Dis., vol. 1, no 1, p. 1‑14, avr. 2012.</ref>. Moreover, phosphorylated TRPV1 would have a reduced channel opening threshold.<ref>G. Bhave et al., « Protein kinase C phosphorylation sensitizes but does not activate the capsaicin receptor transient receptor potential vanilloid 1 (TRPV1) », Proc. Natl. Acad. Sci., vol. 100, no 21, p. 12480‑12485, oct. 2003, doi: 10.1073/pnas.2032100100.</ref>. As a result phosphorylated TRPV1 are more responsive to agonist because they are '''overexpressed''' and the same quantity of agonist leads to a better openings of ion channels.
+PKC phosphorlyates TRPV1 at S800,S502, PKA phosphorylates TRPV1 at S116. The phosphorylation of TRPV1 lead to an increase in the expression of TRPV1 at the membrane surface.<ref>K. W. Ho, N. J. Ward, et D. J. Calkins, « TRPV1: a stress response protein in the central nervous system », Am. J. Neurodegener. Dis., vol. 1, no 1, p. 1‑14, avr. 2012.</ref>. Moreover, phosphorylated TRPV1 would have a reduced channel opening threshold.<ref>G. Bhave et al., « Protein kinase C phosphorylation sensitizes but does not activate the capsaicin receptor transient receptor potential vanilloid 1 (TRPV1) », Proc. Natl. Acad. Sci., vol. 100, no 21, p. 12480‑12485, oct. 2003, doi: 10.1073/pnas.2032100100.</ref>. As a result phosphorylated TRPV1 are more responsive to agonist because they are '''overexpressed''' and because the same quantity of agonist leads to a better openings of ion channels.
 ====Desensitization====