Homologous desensitization is distinguished from heterologous desensitization, a process in which repeated stimulation of a receptor by an agonist results in desensitization of the stimulated receptor as well as other, usually inactive, receptors on the same cell. (wikipedia.org)
The process of homologous desensitization has been extensively studied utilizing G protein-coupled receptors (GPCRs). (wikipedia.org)
While the different mechanisms for desensitization are still being characterized, there are currently four known mechanisms: uncoupling of receptors from associated G proteins, endocytosis, degradation, and downregulation. (wikipedia.org)
GRKs selectively modify activated receptors such that no heterogeneous desensitization will occur. (wikipedia.org)
Additionally, ß-arrestins are better at inactivating ßARK-phosphorylated receptors rather than protein kinase A-phosphorylated receptors, which suggests that the arrestins preferentially mediate homologous desensitization. (wikipedia.org)
We developed a calcium signaling-based assay, using cultured human embryonic kidney cells (HEK), that evaluates simultaneously, the activation/desensitization or blockade of the proteinase-activated receptors, PAR 1 and PAR 2 . (aspetjournals.org)
Furthermore, we reasoned that, provided receptor cross-desensitization did not occur, it would be advantageous to assess PAR-targeted ligands in a cell that expressed both receptors. (aspetjournals.org)
Receptor activation1
We sought to extend the receptor-desensitization paradigm for use with a cultured cell system, in which an intracellular calcium signal rather than a contractile response might be used as an index of receptor activation. (aspetjournals.org)
Blockade1
If intracranial recurrence occurs during the treatment with PD-1 blockade therapies, aggressive local therapies could be worthwhile. (bvsalud.org)
Rapid1
Receptor uncoupling/phosphorylation is the most rapid form of desensitization that happens within a cell, as its effects are seen within seconds to minutes of agonist application. (wikipedia.org)
Process1
This compensatory process occurs over a time scale of 2-3 days, ensuring that discrete synaptic events are not lost, but rather the system "set point" is readjusted. (frontiersin.org)
Factors3
The survival of a graft in a host, the factors responsible for the survival and the changes occurring within the graft during growth in the host. (lookformedical.com)
This can either occur by cell surface receptor interactions, as in the case with peptide growth factors, or by interactions with intracellular molecules, as in the case with steroid hormones. (beauty104.com.tw)
However, FGFs 11-14, also known as FGF homologous factors 1-4 (FHF1-FHF4), have been shown to have distinct functional differences compared to the FGFs. (beauty104.com.tw)
Response4
Homologous desensitization occurs when a receptor decreases its response to an agonist at high concentration. (wikipedia.org)
While heterologous desensitization occurs rapidly at low agonist concentrations, homologous desensitization shows a dose dependent response and usually begins at significantly higher concentrations. (wikipedia.org)
Thus, our data suggest that NO-induced desensitization of the cGMP response is caused by the phosphorylation and subsequent activity increase of phosphodiesterase type 5. (rupress.org)
Specific2
The mechanism of desensitization involves the action of a specific GRK, denoted ßARK, and also ß-arrestins. (wikipedia.org)
It may be nonspecific as in the administration of immunosuppressive agents (drugs or radiation) or by lymphocyte depletion or may be specific as in desensitization or the simultaneous administration of antigen and immunosuppressive drugs. (lookformedical.com)
Heterologous desensitization5
Homologous desensitization is distinguished from heterologous desensitization, a process in which repeated stimulation of a receptor by an agonist results in desensitization of the stimulated receptor as well as other, usually inactive, receptors on the same cell. (wikipedia.org)
While heterologous desensitization occurs rapidly at low agonist concentrations, homologous desensitization shows a dose dependent response and usually begins at significantly higher concentrations. (wikipedia.org)
Scholars@Duke publication: Unidirectional, heterologous desensitization of the pertussis toxin receptor by the CD3/TCR complex. (duke.edu)
When this occurs after stimulation by the primary agonist for a given receptor it is termed homologous desensitization, and heterologous desensitization when to an agonist binding to a different type of receptor. (duke.edu)
These observations suggest a model in which T cells can regulate amplification of a non-AgR stimulatory pathway by heterologous desensitization. (duke.edu)
Receptor15
Homologous desensitization occurs when a receptor decreases its response to an agonist at high concentration. (wikipedia.org)
For GPCRs generally, each mechanism of homologous desensitization begins with receptor phosphorylation by an associated G protein-coupled receptor kinase (GRK). (wikipedia.org)
Receptor uncoupling/phosphorylation is the most rapid form of desensitization that happens within a cell, as its effects are seen within seconds to minutes of agonist application. (wikipedia.org)
The ß2 adrenergic receptor was the first to have its desensitization studied and characterized. (wikipedia.org)
The mechanism of homologous desensitization for the β2 receptor is as follows: Agonist binds and activates the receptor, which changes to an active conformational state. (wikipedia.org)
This phosphorylation increases the affinity of β-arrestin for the receptor, resulting in uncoupling of the α subunit of the heterotrimeric G-protein from the receptor, producing desensitization. (wikipedia.org)
citation needed] In contrast to receptor uncoupling, endocytosis can occur through multiple pathways. (wikipedia.org)
ß3-Adrenergic receptor downregulation also occurs after high-fat diet feeding, concurrent with catecholamine resistance and elevated inflammation. (bvsalud.org)
Functions in regulating agonist-mediated G-protein coupled receptor (GPCR) signaling by mediating both receptor desensitization and resensitization processes. (nih.gov)
Our results indicate that PSA potentiates synaptic AMPA receptor properties and that cyclothiazide, a known inhibitor of AMPA receptor desensitization does not occlude PSA effects on AMPA receptor activity. (auburn.edu)
We hypothesized that the attenuation of the GIRK current would lead to a recovery of neuronal excitability whereby desensitization of the receptor would lead to a new steady state of POMC neuron activity reflecting the sustained GIRK current observed after the initial decline from peak with continued agonist exposure. (jneurosci.org)
Altogether, the data show that somatodendritic MORs in POMC neurons inhibit neuronal activity through at least two effectors with distinct levels of receptor reserve and that differentially reflect receptor desensitization. (jneurosci.org)
SIGNIFICANCE STATEMENT Desensitization of the μ-opioid receptor (MOR) is thought to underlie the development of cellular tolerance to opiate therapy. (jneurosci.org)
The data show that somatic MORs in POMC neurons couple to multiple effectors that have differential sensitivity to desensitization of the receptor. (jneurosci.org)
Here, through a combination of RNA-Seq and electrophysiological studies on induced pluripotent stem cell (iPSC)-derived motor neurons (MNs), we show that increased expression of GluA1 AMPA receptor (AMPAR) subunit occurs in MNs with C9ORF72 mutations that leads to increased Ca 2+ -permeable AMPAR expression and results in enhanced selective MN vulnerability to excitotoxicity. (nature.com)
Mediate2
Additionally, ß-arrestins are better at inactivating ßARK-phosphorylated receptors rather than protein kinase A-phosphorylated receptors, which suggests that the arrestins preferentially mediate homologous desensitization. (wikipedia.org)
The cytosolic arrestin proteins mediate desensitization of activated G protein-coupled receptors (GPCRs) via competition with G proteins for the active phosphorylated receptors. (biomedcentral.com)
Agonist3
They are sometimes denoted as agonist-dependent and agonist-independent desensitization respectively. (wikipedia.org)
The nAChR channel opens in response to the binding of agonist (activation) but also becomes refractory to activation in the course of prolonged exposure to nicotinic agonists (desensitization). (jneurosci.org)
Activation of somatic μ-opioid receptors (MORs) in hypothalamic proopiomelanocortin (POMC) neurons leads to the activation of G-protein-coupled inward rectifier potassium (GIRK) channels and hyperpolarization, but in response to continued signaling MORs undergo acute desensitization resulting in robust reduction in the peak GIRK current after minutes of agonist exposure. (jneurosci.org)
Protein-coupled receptors1
The process of homologous desensitization has been extensively studied utilizing G protein-coupled receptors (GPCRs). (wikipedia.org)
Organisms1
Homologous desensitization serves as a mechanism for tachyphylaxis and helps organisms to maintain homeostasis. (wikipedia.org)
Mechanism2
The mechanism of desensitization involves the action of a specific GRK, denoted ßARK, and also ß-arrestins. (wikipedia.org)
This indicates that PSA, in addition to decreasing the desensitization of AMPA receptors may also act through another mechanism. (auburn.edu)
Exposure1
While resistant to classical desensitization pathways, its mRNA (Adrb3) and protein expression are dramatically downregulated after ligand exposure (homologous desensitization). (bvsalud.org)
Intracellular2
The third and final wave occurs at intracellular compartments and could be elicited by G proteins or β -arrestins. (aspetjournals.org)
We also identified several key residues at the interface between the two pores that are functionally important, particularly Asp509, which confers intracellular pH-dependent desensitization to OTOP channels. (elifesciences.org)
Stimulation2
To examine potential interactions of CEACAMs in neutrophil signaling, the effects on neutrophil adhesion to human umbilical vein endothelial cells of a set of CD66 mAbs was tested following desensitization to stimulation by various combinations of these mAbs. (biomedcentral.com)
Addition of a CD66 mAb in the absence of calcium results in desensitization of neutrophils to stimulation by that CD66 mAb. (biomedcentral.com)
Proteins1
While the different mechanisms for desensitization are still being characterized, there are currently four known mechanisms: uncoupling of receptors from associated G proteins, endocytosis, degradation, and downregulation. (wikipedia.org)
Contrast1
In contrast, desensitization of cells to CEACAM1 and any two of the other CEACAMs left the cells unresponsive to all CD66 mAbs. (biomedcentral.com)
Absence1
In the absence of a repair template the double-strand breaks were religated by non-homologous end joining resulting in deletion of G 4 C 2 repeats (Fig. 1a ). (nature.com)
Action2
However, both glucosides possess the capacity of specifically inhibiting the precipitating action of homologous antisugar-protein serum. (nih.gov)
Prolonged activation of somatic MORs in POMC neurons robustly inhibited action potential firing and Ca 2+ activity despite desensitization of the MOR and reduced activation of a potassium current over the same time course. (jneurosci.org)
Results1
The current data show that desensitization of neutrophils to any two CEACAMs results in selective desensitization to those two CEACAMs, while the cells remain responsive to the other two neutrophil CEACAMs. (biomedcentral.com)
Cells1
Similar interactions may occur in other cells expressing CEACAMs. (biomedcentral.com)
Final1
[ 75 ] Altogether, when looking at the overview of clinical studies on immunotherapy with Rhus extracts (collated in Table 2 ), it is hard to escape the impression that the poorer was the design of a trial (e.g., lack of placebo control and no objective outcome measures), the more the final conclusions were in favor of Rhus desensitization. (medscape.com)
Similar1
Allergenic reactions similar to those caused by crustaceans may occur following the ingestion of certain edible insects (Belluco et al. (researchgate.net)