Export receptors. Medical search. Frequent questions

The crucial role of androgen receptor (AR) in prostate cancer development is well documented, and its inhibition is a mainstay of prostate cancer treatment. (caltech.edu)
Structure-activity relationships of FXR-active compounds revealed by this screening were then compared against the androgen receptor, estrogen receptor α, peroxisome proliferator-activated receptors δ and γ and the vitamin D receptor. (nature.com)

Here, we report that the guanine nucleotide-binding protein (G protein)-coupled receptor-activated WD-repeat Gβ interacts with the glucocorticoid receptor (GR), comigrates with it into the nucleus and suppresses GR-induced transactivation of the glucocorticoid-responsive genes. (rupress.org)
Although many affected biological pathways are typically regulated by the glucocorticoid receptor (GR), during sepsis this is deficient and supplementation with exogenous glucocorticoids is often ineffective in reducing mortality. (suny.edu)
At the cellular level, the actions of glucocorticoids are mediated by a 94-kd protein, the glucocorticoid receptor (GR). The human (h) GR belongs to the steroid/thyroid/retinoic acid superfamily of nuclear receptors and functions as a ligand-dependent transcription factor that regulates the expression of glucocorticoid-responsive genes positively or negatively. (medscape.com)
A) Schematic representation of the structure of the human glucocorticoid receptor (hGR) gene. (medscape.com)

The disruption decreases Thr286 phosphorylation of alphaCaMKII, lowers phosphorylation of a key CaMKII substrate in the postsynaptic membrane (AMPA receptor subunit glutamate receptor 1), and produces deficits in hippocampal long-term potentiation and spatial learning. (caltech.edu)
What happens is you get presynaptic release of glutamate into the synaptic cleft, which causes postsynaptic depolarization mediated by the AMPA subtype of glutamate receptor. (hstalks.com)
AMPA receptors are tetrameric glutamate‐gated ion channels that mediate a majority of fast excitatory neurotransmission in the brain. (ucl.ac.uk)
We have employed two diazepam treatment regimes known to produce differing effects on withdrawal aversion in the rat and examined whether withdrawal-induced anxiety was accompanied by changes in AMPA receptor characteristics. (strath.ac.uk)
Taken together, these data are consistent with differential neuroadaptive processes in AMPA receptor plasticity being important in withdrawal from chronic benzodiazepines. (strath.ac.uk)

Marked accelerated evolution on this branch was also seen for some IGFBPs, but not the mannose 6-phosphate/IGF2 receptor or epidermal growth factor receptor. (figshare.com)

A growing body of literature implicates the peroxisome proliferators-activated receptors (PPARs) in the pathogenesis and treatment of NAFLD. (wjgnet.com)

Interactions between the NR2B receptor and CaMKII modulate synaptic plasticity and spatial learning. (caltech.edu)

Analysis of phosphorylation-dependent interactions downstream of VEGFR-1 in mammalian cells, which is generally hindered by the lack of ligand-induced receptor phosphorylation, was enabled by the development of chimeric receptors. (figshare.com)
The canonical TGFβ signalling pathway involves ligand-dependent assembly of a heteromeric receptor complex, receptor-kinase activation and subsequent phosphorylation and activation of SMAD proteins, which are transcriptional regulators that consequently accumulate in the nucleus. (nature.com)
SMAD phosphorylation by active receptors, and constitutive SMAD dephosphorylation by nuclear phosphatases, are coupled through nucleocytoplasmic shuttling of SMADs. (nature.com)
Phosphorylation of the receptor protein Pex5p modulates import of proteins into peroxisomes. (ruhr-uni-bochum.de)

To determine the function of these interactions, we derived transgenic mice expressing a ligand-activated carboxy-terminal NR2B fragment (cNR2B) by fusing this fragment to a tamoxifen (TAM)-dependent mutant of the estrogen receptor ligand-binding domain LBD(G521R). (caltech.edu)

Therefore, an inverse agonist of the S1P1 receptor is predicted to reduce signal transduction from PDGFβ receptor tyrosine kinase by blocking the constitutive activity of the G-protein coupled receptor. (strath.ac.uk)
Ligands of the transforming growth factor-β (TGFβ) superfamily of growth factors initiate signal transduction through a bewildering complexity of ligand-receptor interactions. (nature.com)

Andrews, Allison-Lynn , Holloway, John W. , Puddicombe, Sarah M. , Holgate, Stephen T. and Davies, Donna E. (2002) Kinetic analysis of the interleukin-13 receptor complex. (soton.ac.uk)

The NR2B subunit of the NMDA receptor interacts with several prominent proteins in the postsynaptic density, including calcium/calmodulin-dependent protein kinase II (CaMKII). (caltech.edu)
NMDA receptors: neuroprotective or excitotoxic? (hstalks.com)
And one particular focus in the lab is on an important source of calcium influx, the NMDA subtype of ionotrophic glutamate receptors. (hstalks.com)
So a typical glutamatergic synapse, such as the one shown in the cartoon here, the NMDA receptor is a very important source of activity-dependent calcium influx. (hstalks.com)
This postsynaptic depolarization alleviates the voltage-dependent magnesium block on the NMDA receptor. (hstalks.com)
And it's this calcium that is a major mediator of the neuroprotective, as well as the toxic effects of NMDA receptor activity. (hstalks.com)
And the origins of the field, the research into the control of survival and death by NMDA receptors can be traced back to a paper published in 1957 by Lucas and Newhouse. (hstalks.com)
And that this calcium influx was mediated by the NMDA receptor, the NMDA subtype of ionotrophic glutamate receptors. (hstalks.com)
And extremely soon afterwards, it became clear that NMDA receptor-mediated excitotoxity was physiologically relevant because it was implicated in contributing to neuronal loss and dysfunction in acute disorders, particularly stroke and traumatic brain injury. (hstalks.com)
The activation of Ca2+-permeable N-methyl-D-aspartic acid (NMDA) receptor channels (NMDARs) is crucial for the development and survival of neurons, but many cancers use NMDAR-mediated signaling as well, enhancing the growth and invasiveness of tumors. (tu-darmstadt.de)

In addition, the observed dependence of some of these effects on a specific tyrosine residue within VEGFR-2 suggested that the chimeric receptors couple to downstream effectors in a manner analogous to that of the full-length receptors. (figshare.com)
These findings are the first to report that a GPCR inverse-agonist reduces growth factor-induced receptor tyrosine kinase signaling, fundamentally broadening their mechanism of action. (strath.ac.uk)
protein tyrosine phosphatase, non-receptor. (wikigenes.org)

Beta-2 Adrenergic Receptor s (B2ARs) are a type of G Protein-Coupled Receptor (GPCR) . (proteopedia.org)

Potent selective H4 receptor agonists and antagonists have been synthesized and in vivo studies have indicated their action on H4 receptor. (eurekaselect.com)

To study the structural basis of pathological remodelling and altered calcium channel functional states in the heart, we sought to re-purpose high-affinity ligands of the cardiac calcium channel, the ryanodine receptor (RyR2), into super-resolution imaging probes. (whiterose.ac.uk)
Figure 1: Ligands, receptors and SMADs. (nature.com)
Drug discovery efforts aimed at developing selective ligands for this receptor, both as therapeutics and as experimental tools, have largely failed as they focused on targeting the acetylcholine (ACh) binding site, which is identical in all five mAChR subtypes. (monash.edu)

Three of the five classes of Bn receptor antagonists that interacted with higher affinity with the fBB 4 -R functioned as fBB 4 -R antagonists and two as partial agonists. (acs.org)
In addition, anti-inflammatory effects of H4 receptor antagonists, with special emphasis to JNJ7777120, a selective H4 receptor antagonist have been focused exhaustively. (eurekaselect.com)

Nucleocytoplasmic transport of large molecules, including proteins and RNAs, require transport receptors. (nii.ac.jp)
The import of proteins containing a classical nuclear localization signal (NLS) requires the NLS import receptor, a heterodimer of importin alpha and beta subunits. (wikipedia.org)
First, the protein cleaves several other proteins called cytokine receptors on the surface of cells. (medlineplus.gov)
These peptides are exported to the cell surface, where they attach to major histocompatibility complex (MHC) class I proteins. (medlineplus.gov)
Here the possibility that this is accompanied by a corresponding episode of accelerated evolution of IGF1 receptor (IGF1R), insulin receptor (IR) and/or IGF binding proteins (IGFBPs) was investigated. (figshare.com)
The AF-1 plays an important role in the interaction of the receptor with molecules necessary for the initiation of transcription, such as coactivators, chromatin modulators, and basal transcription factors, including RNA polymerase II, TATA-binding protein (TBP), and a host of TBP-associated proteins (TAFIIs). (medscape.com)

Histamine and its receptors are classical inflammatory mediators in peripheral tissues and also function in the brain. (eurekaselect.com)
The results of physiological and pharmacological studies revealed that brain histamine and its receptors are involved in the regulation of obesity and diabetes mellitus. (eurekaselect.com)
Leptin has been shown to regulate obesity and diabetes partially via brain histamine and its receptors. (eurekaselect.com)
In this review, we focused on the roles of brain histamine and its receptors in regulating obesity and diabetes mellitus. (eurekaselect.com)
Until recently histamine was thought to act on three receptors - H1, H2 and H3. (eurekaselect.com)
Merely a decade back, sequencing of human genome has revealed a new histamine receptor - H4 receptor. (eurekaselect.com)
the pharmacological profile of the protein is quite different from other histamine receptors. (eurekaselect.com)

We identified truncating mutations in distinct X-linked gamma-aminobutyric acid A (GABAA) receptor subunit-encoding genes, GABRQ and GABRA3, in two different families. (nih.gov)

Although the signalling pathways induced by VEGF have been well-studied, the precise molecular mechanisms remain to be determined, particularly with respect to the relative contribution of the individual receptors. (figshare.com)
Maintaining bile acid (BA) homeostasis is important and regulated by BA activated receptors and signaling pathways. (aspetjournals.org)

It signals via its cognate receptor, a complex of IL-13 receptor ?1 chain (IL-13R?1) with IL-4R? (soton.ac.uk)
To identify their cognate receptors, the grapevine family of LysM receptor kinases (LysM‐RKs) was annotated and their gene expression profiles were characterized. (uzh.ch)

In this study the role of adenosine A(1) receptors for the control of respiration was investigated in vivo. (uni-regensburg.de)
To this end, respiration of unrestrained adult and neonatal adenosine A1 receptor knockout mice (A(1)R(-/-)) was measured in a plethysmographic device. (uni-regensburg.de)
In conclusion, these data indicate that the adenosine A(1) receptor is an important molecular component mediating hypoxic depression in adult mice and it appears to stabilize respiration of neonatal mice. (uni-regensburg.de)
Controls of cAMP production and BRET assays in cells expressing minigenes and in cells expressing the ghrelin GHS1a receptor instead of one of the adenosine receptors. (figshare.com)

A number of these diseases arise from defects in the tumour necrosis factor (TNF) receptor signalling pathway leading to elevated levels of inflammatory cytokines. (whiterose.ac.uk)

A receptor family, retinoic-acid-inducible gene I (RIG-I)-like receptors (RLRs) consist of three members, RIG-I, MDA5 and LGP2. (rutgers.edu)
A separate line of investigation suggests an association between a functional polymorphism in the promoter region for the human dopamine 4 receptor gene (DRD4) and sensitivity to novelty. (upm.es)
Alternative splicing of the hGR gene in exon 9 generates 2 highly homologous receptor isoforms, termed α and β. (medscape.com)

The binding properties are also reported illustrating the modulation of the binding properties of these species by the modification of the hydrogen-bonding patterns of the receptor molecule, namely 1,3- N , N' -bis[4-(dibenzylamino)-6-(butylamino)-1,3,5-triazin-2-yl]xylylenediamine ( 1 ). (open.ac.uk)
The transport receptors recognize cargo molecule and the receptor-cargo complexes are translocated through the nuclear pore complex. (nii.ac.jp)

Extracellular stimuli that activate cell surface receptors modulate glucocorticoid actions via as yet unclear mechanisms. (rupress.org)

In chapter 2 we exploit the unique "two-state" pharmacology of BQCA to investigate allosteric modulation at a chemogenetically modified M1 mAChR, developed as an alternative means to achieve selective receptor targeting in vivo. (monash.edu)
As a consequence, caution must be exercised when interpreting studies of allosteric modulation using chemogenetically modified receptors in vivo. (monash.edu)

Neuroadaptive changes in neural activity occur in limbo-cortical structures although changes at the level of the GABAA receptor do not provide an adequate explanation for these functional changes. (strath.ac.uk)

The deubiquitination of the PTS1-import receptor Pex5p is required for peroxisomal matrix protein import. (ruhr-uni-bochum.de)
Cysteine-specific ubiquitination protects the peroxisomal import receptor Pex5p against proteasomal degradation. (ruhr-uni-bochum.de)

These nuclear hormone receptors impact on hepatic triglyceride accumulation and insulin resistance. (wjgnet.com)

Interferon-alpha (IFN-alpha) potentiates immune responses against viral pathogens that induce toll-like receptor-3 (TLR3) activation but evokes severe major depressive disorder in humans by mechanisms that remain insufficiently described. (uni-koeln.de)
Many receptors and factors play important roles in the innate immune response. (rutgers.edu)
This histidine is critical for RNA discrimination by RIG-I. Unlike RIG-I, the role of the innate immune receptor LGP2 is not well understood. (rutgers.edu)
Phylogenetic analysis clearly distinguished three V. vinifera LysM‐RKs (VvLYKs) located in the same clade as the Arabidopsis CHITIN ELICITOR RECEPTOR KINASE1 (AtCERK1), which mediates chitin‐induced immune responses. (uzh.ch)

For the most part, the residues that change on this branch could not be associated with specific functional aspects (ligand binding, receptor dimerization, glycosylation) and the physiological significance of this coevolution remains to be established. (figshare.com)
The A to T mutation at position 458 that could produce a dimerization defective receptor is shown. (medscape.com)

Analysis of receptor sequences from a range of primates and some non-primate mammals showed that accelerated evolution did indeed occur on this branch in the case of IGF1R and IR, but not for the similar insulin receptor-related receptor (IRRR) which does not bind insulin or IGF1. (figshare.com)
Overall the results suggest that adaptive coevolution of IGF1, insulin and their receptors and some IGFBPs occurred during the evolution of NWM. (figshare.com)

The levels of presynaptic protein vesicular glutamate transporter (VGLUT)-1 and postsynaptic protein postsynaptic density-95 (PSD95) were specifically decreased, whereas the expression of both synaptic and extrasynaptic alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid receptor 1 (AMPAR1) was increased by IFN-alpha and poly(I:C) delivery. (uni-koeln.de)

We have shown previously that brain relaxin-3 mRNA levels positively correlate with sucrose and alcohol intake, and that central antagonism of relaxin-3 receptors (RXFP3) attenuates alcohol self-administration and alcohol-seeking in rats, but food-seeking behaviour and palatable food consumption in mice. (edu.au)

We examined a newly characterized class of compounds that target nucleo-cytoplasmic shuttling by binding to the catalytic groove of the nuclear export protein XPO1 (also known as CRM1, chromosome region maintenance protein 1). (nih.gov)

Detailed kinetic analyses of the binding properties of the heteromeric complexes suggested a sequential mechanism for the binding of IL-13 to its signaling receptor, in which IL-13 first binds to IL-13R?1 and this then recruits IL-4? (soton.ac.uk)
The impact of exposures on bile acid (BA) signaling and Farnesoid X receptor-mediated gut-liver crosstalk is emerging. (aspetjournals.org)

These fatty acids are transported to the liver, where they are used for triglyceride synthesis and are exported as very-low-density lipoprotein (VLDL), which is elevated in these patients. (medscape.com)

We hypothesized that bradykinin receptor inhibition alleviates the vascular dysfunction in a transgenic arcAβ mouse model of cerebral amyloidosis and that fMRI techniques can be used to monitor the treatment response. (uzh.ch)

We now report that inverse agonism of the S1P1 receptor with SB649146 reduced the endocytosis of the PDGFβ receptor-S1P1 receptor complex and the stimulation of p42/p44 MAPK and cell migration in response to PDGF. (strath.ac.uk)

The complex permits the utilization of active G-protein subunits (made available by constitutively active S1P1 receptor) by the PDGFβ receptor kinase to transmit signals to p42/p44 MAPK in response to PDGF. (strath.ac.uk)

The synthesis of bis(triazine) molecules capable of acting as synthetic receptors for barbiturate guest molecules is described. (open.ac.uk)
A proteomic screen for target molecules revealed that CRM1 inhibitors in neurons prevented nuclear export of molecules associated with axonal damage while retaining transcription factors modulating neuroprotection. (nih.gov)

In this review we also address other TNFR signalling disorders such as (TNF) receptor-associated periodic syndrome (TRAPS), RELA haploinsufficiency, RIPK1-associated immunodeficiency and autoinflammation, X-linked ectodermal dysplasia and immunodeficiency (X-EDA-ID) and we review the most recent advances surrounding these diseases and therapeutic approaches currently used to target these diseases. (whiterose.ac.uk)
The chimeric receptors were significantly activated in response to ligand, thereby enabling studies of this signalling with the putative effectors PKB/Akt, PLC and ERK1.2. (figshare.com)
In addition, nuclear accumulation of active nuclear SMAD complexes is dynamically maintained in strict accordance with the degree of receptor activation at any time of signalling. (nature.com)

To select a subset of the search results, click "Selective Export" button and make a selection of the items you want to export. (suny.edu)
The discovery of benzyl quinolone carboxylic acid (BQCA), the first positive allosteric modulator (PAM) with high selectivity for the M₁ mAChR, has lead to a renaissance in selective targeting of this receptor family. (monash.edu)

Cleaving these receptors reduces their ability to transmit chemical signals into the cell, which affects the process of inflammation. (medlineplus.gov)

fBB 4 -R expression in cells widely used for other Bn receptor subtypes was unsuccessful as was expression in two frog cell lines. (acs.org)
However, stable fBB 4 -R cell lines were obtained in CHO-K1 cells which were shown to faithfully demonstrate the correct pharmacology of the related Bn receptor, the GRP receptor, when expressed in these cells. (acs.org)
Here, we solved crystal structures of a transport receptor and transport receptor complex with the high accuracy measurement using a improved synchrotron beamline for the cell structural biological research. (nii.ac.jp)
The data obtained with SB649146 also suggest that the constitutively active endogenous S1P1 receptor enhances PDGFinduced cell migration. (strath.ac.uk)
We applied a genomic DNA-based approach to concurrently study the immunoglobulin-heavy (IGH) and T cell receptor (TCR) β and δ chain loci of 95 individuals. (ucl.ac.uk)

of B2AR, reducing the basal activity of the receptor. (proteopedia.org)

Farnesoid X receptor (FXR) and its regulated target networks in both the liver and the intestines are critical in suppressing BA synthesis and promoting BA transport and enterohepatic circulation. (aspetjournals.org)

Recently, a fourth member of the bombesin (Bn) receptor family (fBB 4 -R) was isolated from a cDNA library from the brain of the frog, Bombina orientalis . (acs.org)

Application of the branch-sites method showed dN/dS ratios significantly greater than 1.0 for both receptor ectodomains and for IGFBP1, and allowed identification of residues likely to have been subject to selection. (figshare.com)
These residues were concentrated in the N-terminal half of the IGF1R ectodomain but the C-terminal half of the IR ectodomain, which could have implications for the formation of hybrid receptors. (figshare.com)

While genes from the GABAergic pathway have previously been thought to be involved in the pathophysiology of ASD, this is the first report of ASD patients with truncating mutations in GABA receptors genes. (nih.gov)

In summary, bradykinin receptors blockade recovered cerebral vascular dysfunction in a mouse model of cerebral amyloidosis. (uzh.ch)

Which when, coincident with glutamate binding to the receptor, opens the channel and in flows sodium, and importantly calcium. (hstalks.com)

Anatomy18

Organisms4

Chemicals and Drugs47

Analytical, Diagnostic and Therapeutic Techniques and Equipment5

Phenomena and Processes24

Information Science3

Androgen receptor2

Glucocorticoid receptor4

AMPA5

Epidermal growth f1

Peroxisome1

Synaptic plasticity1

Phosphorylation4

Estrogen receptor1

Signal transduction2

Interleukin-13 recep1

NMDA10

Tyrosine3

GPCR1

Agonists and antagonists1

Ligands3

Antagonists2

Proteins6

Histamine7

Subunit1

Pathways2

Cognate2

Adenosine4

Inflammatory1

Gene3

Molecule2

Modulate1

Vivo2

GABAA1

Import receptor2

Hepatic1

Immune4

Dimerization2

Insulin2

Postsynaptic1

RATS1

Cytoplasmic1

Signaling2

Triglyceride1

Alleviates1

Endocytosis1

Subunits1

Molecules2

Signalling3

Selective2

Reduces1

Cell5

Basal1

Synthesis1

CDNA1

Residues2

Genes1

Cerebral1

Calcium1