Purinergic P2X(2) receptor desensitization depends on coupling between ectodomain and C-terminal domain

Mu-Lan He¹, Taka-Aki Koshimizu, Melanija Tomić

¹Endocrinology and Reproduction Research Branch, National Institute of Child Health and Human Development, National Institutes of Health, Bethesda, Maryland 20892-4510, USA.

|October 23, 2002

Abstract:

The wild-type P2X(2) purinergic receptor (P2X(2a)R) and its splice form lacking the intracellular Val(370)-Gln(438) C-terminal sequence (P2X(2b)R) respond to ATP stimulation with comparable EC(50) values and peak current/calcium responses but desensitize in a receptor-specific manner. P2X(2a)R desensitizes slowly and P2X(2b)R desensitizes rapidly. We studied the effects of different agonists, and of substituting the ectodomain, on the pattern of calcium signaling by P2X(2a)R and P2X(2b)R. Both receptors showed similar EC(50) values (estimated from the peak calcium response) and IC(50) values (estimated from the rate of calcium signal desensitization) for agonists, in the order 2-MeS-ATP

Related Experiment Videos

Purinergic P2X(2) receptor desensitization depends on coupling between ectodomain and C-terminal domain

Related Concept Videos

MRS2339, a cardiac P2X4 receptor nucleotide activator, improves systolic function in heart failure.

PI4-kinase A is essential for survival of the GnRH neurons.

Knockout of PI4-Kinase A in GnRH Neurons Causes their Prepubertal Death.

Heterogeneity between VIP and GRP neurons underlies AVP receptor signaling in the mouse suprachiasmatic nucleus.

Heterogeneity of Sox2-expressing cells in mouse pituitary and their roles in postnatal gonadotroph differentiation.

Heterogeneity of Sox2-expressing cells in mouse pituitary and their roles in postnatal gonadotroph differentiation.

An integrated structural and functional profiling approach uncovers the mechanisms of pregnane X receptor binding and activation by pharmaceutical and environmental compounds.

Anchored kinase and phosphatase signaling networks in amyloid β-induced synaptic dysfunction.

Where are peptide ligands of potassium channels sourced from?

Regulation of organic anion transporting polypeptide 1B1 transport function by lysine deacetylase 6.

Neuroprotective in vitro effects of histone deacetylase 6-selective inhibitor SW-100 toward oxaliplatin-derived toxicity.

Emerging roles of platelet DNA in cancer detection and noninvasive prenatal testing.

Thermal Inactivation of Penicillin Acylase from Escherichia coli: Rate-Limiting Step and Role of Protein Aggregation.

Deuterated Aprotic Electrolytes Enable Rechargeable Lithium Batteries With High (Electro)Chemical and Thermal Stability.

Using 19F NMR to quantify enthalpy-entropy compensation in protein-protein interactions.

The Effect of Solvation Sphere Composition on the Nucleophilic Substitution Mechanism: The Hunt for the Elusive Carbocation Intermediate.

Exploring the Boundaries of Aromaticity in Complex Structures and Excited States Through Computational Analysis.

Determination of coverage-dependent surface reaction rates using λ-dynamics: Application to molecular desorption.

Related Experiment Videos

Purinergic P2X(2) receptor desensitization depends on coupling between ectodomain and C-terminal domain

Abstract:

Related Concept Videos

Related Articles