Functions as a receptor. Medical search. Frequent questions

Moreover, many of these channels are receptors for ligands that elicit distinct psychophysical sensations, such as the heat associated with capsaicin and the cold felt with menthol. (nih.gov)
We studied binding of ligands from different wines to the peroxisome proliferator-activated receptor γ (PPARγ), a key factor in glucose and lipid metabolism. (rsc.org)
A corresponding class of transmembrane serine/threonine kinases has recently been discovered that act as cell surface receptors for ligands of the TGFβ superfamily. (biologists.com)
D-2 receptors are characterised by a high affinity for the buty-rophenones haloperidol 9 and spiperone 10 , but these ligands also apparently bind to D-1 receptors 11 . (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)
This review of the current literature highlights the versatility of the GR in forming homodimer interactions, as well as the ability to bind to alternate nuclear receptors, and investigates the potential implications such varying GR dimer conformations may have for the design of GR ligands with a safer side effect profile. (ed.ac.uk)
Cells synthesize and release signalling molecules (ligands), which produce a specific response only in those cells that have a receptor for that ligand. (lu.se)
The activity of about two-thirds of the 48 nuclear receptors is controlled by selective ligands (e.g. steroid hormones, retinoids, intracellular lipids), and is fine-tuned by transcriptional coregulators forming macromolecular complexes that activate (coactivators) or repress (corepressors) the expression of target genes by modulating the accessibility of the transcriptional machinery to DNA. (igbmc.fr)

abstract = 'Glucose-dependent insulinotropic polypeptide (GIP) and its receptor (GIPR) are involved in multiple physiological systems related to glucose metabolism, bone homeostasis and fat deposition. (ku.dk)

In mice lacking one copy of the BDNF gene ( BDNF +/− ), CB 1 R (GABA) responses were potentiated and were preserved from the action of haloperidol, a DA D 2 receptor (D 2 R) antagonist able to fully abolish CB 1 R (GABA) function in rewarded animals. (jneurosci.org)
Long-term treatment with a selective ET A-type receptor antagonist, markedly reduced hyperglycaemia and restored plasma glucose clearance rates towards normal. (portlandpress.com)
We report that ERα ligand oestradiol (E2) is significantly increased in human cervical cancer (CxCa) tissues and tumour-infiltrating Treg cells (CD4+CD25hiCD127low), whereas blocking ERα with the antagonist ICI 182,780 abolishes FOXP3 expression and impairs the function of CxCa infiltrating Treg cells. (ncbs.res.in)
The highly selective 5-HT2 receptor antagonist, MDL 100,907, was used to explore the role of serotonin in the stimulation of dopaminergic function produced by the amphetamine analogue 3,4-methylenedioxymethamphetamine (MDMA). (erowid.org)
The butyrophenone domperidone also binds to central dopamine receptors 12 , but it is a very weak antagonist of dopamine-sensitive adenylate cyclase 13 (Table 1), suggesting that it may bind only to D-2 receptors. (nature.com)
An inward current (Ix) was identified and this current was blocked by the P2 receptor antagonist, suramin, and inhibited by the ATP-degrading enzyme, apyrase. (ucl.ac.uk)

The androgen receptor (AR) is critical for the normal development of prostate and for its differentiated functions. (harvard.edu)
The AR gene provides instructions for making a protein called an androgen receptor. (medlineplus.gov)
The resulting androgen-receptor complex then binds to DNA and regulates the activity of androgen-responsive genes. (medlineplus.gov)
By turning the genes on or off as necessary, the androgen receptor helps direct the development of male sexual characteristics. (medlineplus.gov)
Some variants lead to an abnormally short version of the androgen receptor protein, while others result in the production of an abnormal receptor that cannot bind to androgens or to DNA. (medlineplus.gov)
Variants that eliminate the function of the androgen receptor cause complete androgen insensitivity syndrome. (medlineplus.gov)
Although the extended CAG region changes the structure of the androgen receptor, it is unclear how the altered protein damages nerve cells. (medlineplus.gov)
Researchers believe that a fragment of the androgen receptor protein containing the CAG repeats accumulates within these cells and interferes with normal cell functions. (medlineplus.gov)

Oestrogen Receptor-α binds the FOXP3 promoter and modulates regulatory T-cell function in human cervical cancer. (ncbs.res.in)
Receptor activation happens when collagen binds into preformed DDR dimers on cell membrane, when collagen is bound, a conformational change probably occurs, which causes cytosolic kinases to rotate to face each other, and their autophosphorylation. (wikipedia.org)

Here, we explored the mechanistic role of RIP140 in breast cancer and its involvement in estrogen receptor α (ERα) transcriptional regulation of gene expression. (aacrjournals.org)
Acyl-CoA synthetase-4, a new regulator of mTOR and a potential therapeutic target for enhanced estrogen receptor function in receptor-positive and -negative. (oncotarget.com)
In addition, we demonstrate a synergistic effect on cell growth inhibition by the combination of rosiglitazone and tamoxifen, an estrogen receptor α (ERα) inhibitor. (oncotarget.com)
Pharmacologic therapy for osteoporosis includes most commonly the use of antiresorptive agents to decrease bone resorption, such as bisphosphonates, denosumab, and the selective estrogen-receptor modulator (SERM) raloxifene. (medscape.com)
Synergistic activation of estrogen receptor with combinations of environmental chemicals. (cdc.gov)

Pharmacological agents that promote expression or activation of the ADGRG1 receptor may represent a novel approach for the treatment of T2D. (lu.se)
To understand the receptor signaling related with weight loss, we examined the pharmacological properties of two rare missense GIPR variants, R190Q (rs139215588) and E288G (rs143430880) linked to lower body mass index (BMI) in carriers. (ku.dk)
Using a combination of MO-based knockdowns, pharmacological inhibitors and rescue assays we demonstrate that Npr3 cooperate with guanylate cyclase natriuretic peptide receptor 1 (Npr1) and natriuretic peptides (Nppa/Nppc) to regulate NC and CP formation, pointing at a broad requirement of this signaling pathway in early embryogenesis. (gene-tools.com)
This family has several receptor subtypes with different pharmacological selectivity, which overlaps in some cases, for various adenosine and uridine nucleotides. (nih.gov)
The pharmacological profile of P2X2 and P2X4 receptors expressed in oocytes were examined under normal and extreme ionic conditions. (ucl.ac.uk)

125I-IGF-I binding was increased in both 950Tyr (WT) (14-fold) and truncated human IGF-I receptor (952STOP) stable transfectants (50-fold), when compared to untransfected cells that contained endogenous rat IGF-I receptors. (jci.org)
The expected suppression of GH by endogenous rat IGF-I receptors was completely abrogated in 952STOP transfectants (P (jci.org)
Mutant 952STOP cells were therefore completely devoid of biological signaling to GH despite the presence of endogenous rat IGF-I receptors. (jci.org)
Thus mutant IGF-I receptors block ligand-mediated endogenous rat IGF-I signaling by functioning as a dominant negative forming nonfunctional human/rat hybrid receptors. (jci.org)
Next, I showed that the expression of P2X4R was sufficient to enhance the cytosolic Ca2+ response to the activation of endogenous histamine H1 receptors and to promote lysosome fusion. (cam.ac.uk)
It was confirmed that oocytes lack endogenous P2X receptors, and were unaffected by P2X receptor antagonists and allosteric modulators. (ucl.ac.uk)

The role of ESRRa in cellular metabolism is largely dependent on its transcriptional regulation of mitochondrial function and biogenesis through collaboration with the peroxisome proliferator-activated receptor γ coactivator-1 alpha (PGC1a) 6 . (nature.com)

The effect of BDNF was restricted to CB 1 Rs controlling GABA-mediated IPSCs (CB 1 R (GABA) ), whereas CB 1 Rs modulating glutamate transmission and GABA B receptors were not affected. (jneurosci.org)
Dose-response curves constructed with sustained agonist application suggest that the 50% effective concentration (EC 50 ) for peak glutamate-evoked current at NMDARs is 1 to 10 μM, whereas that of α-amino-3-hydroxy-5-methyl-4-isoxazole propionate (AMPA) receptors is ∼500 μM. (aspetjournals.org)
The type-5 metabotropic glutamate receptor (mGluR5) has been shown to modulate brain plasticity and function, and is a therapeutic target in neurological diseases outside of stroke. (lu.se)
Glutamate receptors function in learning and memory. (bvsalud.org)

The product of this gene belongs to the family of G-protein coupled receptors. (nih.gov)
The protein encoded by P2RY8 gene is composed of 359-amino acids and belongs to the P2Y family of G-protein coupled receptors that are preferentially activated by adenosine and uridine nucleotides. (atlasgeneticsoncology.org)

Agonist responses to Ang II were absent for AT 1 -G45R and significantly reduced in potency for AT 1 -C289W (11-fold) and AT 1 -F204S (57-fold) compared with the wild-type (WT) receptor. (aspetjournals.org)
Evidence suggests that N -methyl- d -aspartate receptors (NMDARs) have a relatively high affinity for agonist compared with non-NMDA receptors. (aspetjournals.org)
Neither receptor alone was sufficient to promote lysosome fusion in response to the agonist BzATP. (cam.ac.uk)
[ 17 ] and a short course of a sedative-hypnotic or melatonin receptor agonist. (medscape.com)
In this study, we evaluated the functionality of A1 adenosine receptor through development of zebrafish (6-7-day-, 3-, 8-, and 24-month-old), assessing (I) the effects of the agonist N6-cyclopenthyladenosine (CPA) over locomotor parameters , (II) the anticonvulsant properties of CPA and adenosine per se in the pentylenetetrazol -induced seizure, and (III) the gene expression of adora1b through development. (bvsalud.org)

Although these data indicate that stimulation of CB 1 Rs promotes BDNF release and activity, the effects of BDNF activity on CB 1 R function are poorly characterized. (jneurosci.org)
Stimulation of postsynaptic GABA B receptors generally triggers inhibition of adenylate cyclase and activation of G protein-gated inwardly rectifying K + (GIRK/Kir3) channels, leading to cell hyperpolarisation (Kaupmann et al. (springer.com)
This receptor is coupled to the stimulation of the phosphoinositide and adenylyl cyclase pathways and behaves as a selective purinoceptor. (nih.gov)
Both Orexin receptors have been shown to couple strongly with Ca2+ ion elevations and phospholipase C. Low concentrations of Orexin causes OX1R stimulation, activating a Ca2+ influx [3] . (proteopedia.org)
Unlike other tyrosine-kinase receptors, maximal activation of receptors occurs 18 hours after collagen stimulation. (wikipedia.org)

Functional analysis using the cell-based assay receptor selection and amplification technology (R-SAT) revealed that three variants (AT 1 -G45R, AT 1 -F204S, and AT 1 -C289W) displayed altered responses to Ang II and other AT 1 receptor agonists and antagonists. (aspetjournals.org)
Recent research has surprisingly indicated that both agonists and antagonists of GIPR may be useful in the treatment of obesity and type 2 diabetes, as both result in weight loss when combined with GLP-1 receptor activation. (ku.dk)

Primary astrocytes were stimulated with LPS following TRAF6 siRNA or control transfection, and NF-κB, MAPKs, chemokine, and chemokine receptor expression levels evaluated by western blotting and ELISA. (researchsquare.com)
Among certain better-characterized co-receptors, the HIV-1 co-receptor function of CMKLR1/ChemR23 resembles that of the chemokine receptor, CCR3. (lu.se)

Although these platelet activation processes are relatively well-studied as a function of the platelet environment, only since recently it is becoming clear that a multitude of proteases present in plasma or produced by platelets themselves are important for the distinct properties of platelet populations, often by cleaving specific receptors. (frontiersin.org)
The generation of receptors specific for antigens is a unique and complex process that generates 10 12 specific receptors for each cell type of the adaptive immune system, including T and B cells. (medscape.com)

The purinergic receptor P2Y11 choreographs the polarization, mitochondrial metabolism, and migration of T lymphocytes. (nih.gov)

These data demonstrate that polymorphic variation in the human AT 1 receptor induces loss of functional phenotypes, which may constitute the molecular basis of variability of AT 1 receptor-mediated physiological responses. (aspetjournals.org)
The molecular mechanism by which vascular endothelial receptors (VEGFRs) control vessel growth and function in physiological and pathological settings is under intensive study, but questions remain. (helsinki.fi)

BDNF potently inhibited CB 1 R function in the striatum, through a mechanism mediated by altered cholesterol metabolism and membrane lipid raft function. (jneurosci.org)
Oestrogen controls Foxp3 expression in regulatory T cells (Treg cells) via a mechanism thought to involve oestrogen receptor alpha (ERα), but the molecular basis and functional impact of ERα signalling in Treg cells remain unclear. (ncbs.res.in)
Salt and water reclamation in the kidney may depend on flow rate, since a common mechanosensory mechanism can release enough ATP to activate those P2X receptors regulating ENaC and AQP2 channel function in the distal nephron. (ucl.ac.uk)
We have described the genomic organization of cmklr1 in mouse and analysed the regulatory mechanism behind the corresponding receptor expression. (lu.se)
We conclude that neuronal circuitry subserving sensorimotor function after stroke is depressed by a mGluR5-dependent maladaptive plasticity mechanism that can be restored by mGluR5 inhibition. (lu.se)

Context: Adhesion G protein-coupled receptor (GPCR)-G1 (ADGRG1) is the most abundant GPCR in human pancreatic islets, but its role in islet function is unclear. (lu.se)

GABA B receptors are the G protein-coupled receptors for GABA, the main inhibitory neurotransmitter in the brain, and through coupling to different intracellular signal transduction mechanisms they mediate slow inhibitory postsynaptic potentials (IPSPs) (Bettler et al. (springer.com)
Orexin receptors produce neuroexcitation through postsynaptic depolarization by activating non-selective cation channels, inhibiting K+ channels, and activating Na+/Ca2+ exchange. (proteopedia.org)

However, how Kap114p associates with yTBP to exert its multifaceted functions has remained elusive. (sinica.edu.tw)

The action of BDNF on CB 1 R (GABA) function was tyrosine kinase dependent and was complete even after receptor sensitization with cocaine or environmental manipulations activating the dopamine (DA)-dependent reward system. (jneurosci.org)
In vivo microdialysis confirmed that 5-HT2 receptor blockade with MDL 100,907 attenuated MDMA-induced increases in extracellular concentrations of striatal dopamine. (erowid.org)
The results suggest a permissive role for 5-HT2 receptors in the activation of the dopamine system which occurs during states of high serotonergic activity or during conditions of elevated dopamine efflux with high D2 receptor occupancy. (erowid.org)
In other dopamine-rich areas of the central nervous system, there is evidence for multiple dopamine receptor types 4-7 , and two sub-types have been suggested 8 . (nature.com)
In the retina of many species, a dopamine-sensitive adenylate cyclase has been demonstrated 14,15 , indicating the presence of D-1 receptors. (nature.com)

In the current study, melatonin receptor expression by human islets was examined by reverse transcription-polymerase chain reaction (RT-PCR) and the effects of exogenous melatonin on intracellular calcium ([Ca2+](i)) levels and islet hormone secretion were determined by single cell microfluorimetry and radioimmunoassay, respectively. (lincoln.ac.uk)

Functioning and Gene Expression of Adenosine A 1 Receptor During Zebrafish ( Danio rerio ) Development. (bvsalud.org)
The A1 adenosine receptor is the most widely expressed P1 receptor in vertebrates , performing inhibitory tone of the nervous system . (bvsalud.org)
To avoid confounding factors, such as locomotor effects, during any brain function investigation using A1 adenosine receptor as a target, the concentration below 75 µM or below the dose of 20 mg.kg-1 of CPA is ideal for zebrafish at larval and adult stages, respectively. (bvsalud.org)

The activity of these hormones is mediated by proteins belonging to the nuclear receptor superfamily. (igbmc.fr)

Since a metabolic switch has been reported for left heart failure, we sought to describe any potential changes in cardiac fuel metabolism and mitochondrial function in RVF. (ersjournals.com)
Moreover, due to their effects on metabolism, proliferation and inflammation, their receptors are therapeutic targets for pathologies refractory to current treatments such as various autoimmune and rare diseases, as well as cancers. (igbmc.fr)

P2X4 receptors (P2X4R) are ligand-gated ion channels activated by ATP and with a high permeability to Ca2+. (cam.ac.uk)

Shisa7 is a type-I transmembrane protein interacting with AMPA-type receptors. (elifesciences.org)

D-1 receptors are associated with an adenylate cyclase system whereas D-2 receptors are not. (nature.com)

Estrogen-related receptor alpha (ESRRa) regulates a number of cellular processes including development of bone and muscles. (nature.com)
Altogether the results of my project improve our understanding of how the P2X4R Ca2+ channel regulates lysosome function. (cam.ac.uk)

ATP activates P2X receptors in the apical surface of kidney epithelial cells. (ucl.ac.uk)
While abnormal keratin filament structure and function can explain hypohidrosis and epithelial differentiation abnormalities, the absence of dermatoglyphics is not well understood. (medscape.com)

Targeted mutagenesis in the mouse has indicated that there are specific individual functions for the TR genes in vivo. (nih.gov)
The deletion of combinations of TRalpha and TRbeta variants has revealed that additional functions are convergently regulated by both TR genes and indicates that control of an extended range of functions is facilitated by a network of specific and common TR pathways. (nih.gov)
Loss of function analysis shows that knockdown of esrra impairs expression of genes including sox9, col2a1, sox5, sox6, runx2 and col10a1 thus induces abnormally formed cartilage in pharyngeal arches. (nature.com)
This review addressed AR regulated genes that may be critical for PCa, and how AR may acquire new functions during PCa development and progression. (harvard.edu)
Results: ADGRG1 is the most abundant GPCR mRNA in both human and mouse islets, and its expression inhumanislets strongly correlates with genes important for β-cell function and T2 Drisk. (lu.se)
The tkv receptor is therefore involved in delimiting the expression domains of homeotic genes in the visceral mesoderm. (biologists.com)
The hormone-receptor pair functions as a highly selective lock-and-key system that modulates the expression of many genes and the activities of target cells. (igbmc.fr)
Studies sug- terized by flow cytometry using anti between the immune response and the gest that HCV inhibits receptor genes in CD3, CD56 and CD16 monoclonal virus replication rate [5] and play a cru- the activation of NK cells [20], and the antibodies. (who.int)

The TRs are nuclear receptors that act as ligand-regulated transcription factors. (nih.gov)
Despite their markedly increased ligand binding and prolonged receptor half-life, 952STOP transfectants failed to transduce the IGF-I signal to suppress growth hormone (GH). (jci.org)
Objective: Investigate how ADGRG1 expression and activation by its ligand, collagen III, impacts β-cell function in normal and type 2 diabetic (T2D) islets. (lu.se)

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)
Despite the unique pharmacology of BQCA, the molecular mechanisms of its binding and function and the structural basis of its M₁ mAChR selectivity remain poorly defined. (monash.edu)

ASM-024 induced no serious adverse events, but caused cough in 22% and 48% of the subjects with 50 mg and 200 mg, respectively, compared with 10% who were on placebo.CONCLUSIONS: ASM-024 did not inhibit allergen-induced asthmatic response and related airway inflammation, but reduced methacholine airway responsiveness and slightly improved lung function. (hindawi.com)
These receptors trigger inflammation through the NFkB-dependent and interferon regulatory factor-dependent signaling pathway. (medscape.com)
The receptor displays a high homology to chemoattractant-like receptors involved in inflammation processes. (lu.se)

Also, oocytes lacked muscarinic receptors. (ucl.ac.uk)
The M₁ muscarinic acetylcholine receptor (mAChR) is predominantly expressed in the brain where it plays a major role in mediating cognitive processes such as learning and memory. (monash.edu)

G-protein coupled receptors (GPCRs), located on the cell surface, play an important role in this communication. (lu.se)

The receptors are present in many of the body's tissues, where they attach (bind) to androgens. (medlineplus.gov)
Collagen receptors are membrane proteins that bind the extracellular matrix protein collagen, the most abundant protein in mammals. (wikipedia.org)

Here, we addressed the functional interplay between BDNF and cannabinoid CB 1 receptors (CB 1 Rs) in the striatum, a brain area in which both BDNF and CB 1 s play a role in the emotional consequences of stress and of rewarding experiences. (jneurosci.org)
We also investigated whether the neuromodulatory effects of THC are related to the local expression of its key molecular target, cannabinoid-type-1 (CB1R) but not type-2 (CB2R) receptor. (kcl.ac.uk)
We also investigated whether the neuromodulatory effects of THC are related to the local expression of its key molecular target, cannabinoid-type-1 (CB1R) but not type-2 (CB2R) receptor.MethodsA systematic search was conducted of acute THC-challenge studies using fMRI, PET, and arterial spin labelling in accordance with established guidelines. (kcl.ac.uk)

The activities of adhesion and signaling receptors in platelets are controlled by several mechanisms. (frontiersin.org)
The flow-dependent adhesion of platelets to those and other extracellular matrix components is stabilized by a panel of integrins, including integrin α 2 β 1 , α IIb β 3 , and α 6 β 1 (adhesive platelet population), while the initial activation of platelets is achieved by signaling via the collagen/laminin receptor, glycoprotein VI (GPVI). (frontiersin.org)
Platelet membrane glycoproteins, mainly GPIa/IIa, GPVI and probably GPIV as well, function as receptors engaged in platelet adhesion to collagen. (wikipedia.org)

Thus, GABA B receptors are associated with GIRK and Ca V 2.1 channels in different subcellular compartments. (springer.com)
Reeve, J. E. , Kohl, M. M. , Rodríguez-Moreno, A. , Paulsen, O. and Anderson, H. L. (2012) Caged intracellular NMDA receptor blockers for the study of subcellular ion channel function. (gla.ac.uk)
We have previously synthesized a caged form of the use-dependent N-methyl-D-aspartate (NMDA) receptor ion channel blocker MK801 and used intracellular photolysis of this compound to demonstrate the subcellular location of NMDA receptor ion channels involved in synaptic plasticity. (gla.ac.uk)

Our preliminary study found that CCL2 was mainly co-localized with the astroglial marker glial fibrillary acidic protein (GFAP), while the CCL2 receptor chemokine C-C motif receptor 2 (CCR2) was mainly co-localized with the neuronal nuclear marker NeuN in TBI model rats, suggesting that CCL2‒CCR2 signaling is a major driver of neuroinflammation, neurodegeneration, and concomitant motor and cognitive dysfunction following TBI [9]. (researchsquare.com)

We describe how these are activated, which are their target proteins, and how their proteolytic activity modulates platelet functions. (frontiersin.org)
In particular, ESRR alpha (ESRRa) and ESRR gamma (ESRRg) are key metabolic regulators of energy homeostasis and abnormal functions of these proteins are linked to metabolic syndromes including diabetes and fatty liver disease 5 . (nature.com)

Defective IGF-I receptors may function therefore as dominant negative phenotypes which suppress normal receptor responses in pituitary cells. (jci.org)
However, studies of synaptic NMDAR responses indicate that these receptors may not be saturated during single release events at many synapses. (aspetjournals.org)
The P2Y(11) receptor of human M2 macrophages activates canonical and IL-1 receptor signaling to translate the extracellular danger signal ATP into anti-inflammatory and pro-angiogenic responses. (nih.gov)

Hybrid receptors were studied in GC rat pituitary cells overexpressing either wild-type 950Tyr (WT) human insulin-like growth factor I (IGF-I) receptors or mutant human IGF-I receptors truncated at position 952 in the beta subunit transmembrane region (952STOP). (jci.org)
These receptors comprise an α and β transmembrane subunit, which are noncovalently bound. (wikipedia.org)
Another part of the receptor consists of transmembrane helix with a short cytosolic domain. (wikipedia.org)

Using a "humanized" hybrid rat CMKLR1/ChemR23 receptor as model, it was shown that the major determinants for HIV-1 and HIV-2 interaction with the receptor reside to a varying degree in the N-terminus and second extracellular loop, whereas the viral interaction in the case of SIV primarily involves the second extracellular loop. (lu.se)
Integrins function as the major cell receptor for extracellular matrix protein. (wikipedia.org)

Metabolic cell labeling followed by immunoprecipitation with monoclonal alpha and beta subunit-specific antibodies revealed the presence of hybrid rat/truncated human receptors, truncated transfected human receptors, and WT human IGF-I holotetramers. (jci.org)

Thyroid hormone receptors (TRs) play a central role in mediating the actions of thyroid hormone in development and homeostasis in vertebrate species. (nih.gov)
The angiotensin II type 1 (AT 1 ) receptor is the primary effector for angiotensin II (Ang II), a key peptide regulator of blood pressure and fluid homeostasis. (aspetjournals.org)

Glycoprotein VI Receptor GPVI belongs to immunoglobulin family of glycoproteins. (wikipedia.org)
When damage occurs, endothelial collagen is uncovered and is bound by GPVI receptor on platelets. (wikipedia.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)
This study demonstrates that such an approach may not be valid, as chemogenetic modification of the M₁ mAChR leads to changes in the allosteric behaviour of BQCA that are not reminiscent of its behaviour at the native receptor. (monash.edu)
As a consequence, caution must be exercised when interpreting studies of allosteric modulation using chemogenetically modified receptors in vivo. (monash.edu)
Using multiple behavioral tests we observed that treatment with negative allosteric modulators (NAMs) of mGluR5 (MTEP, fenobam, and AFQ056) for 12 days, starting 2 or 10 days after stroke, restored lost sensorimotor functions, without diminishing infarct size. (lu.se)

Sequence is implicated in osseous and cartilage development, and the receptor is also suggested to have a pathophysiological role as one of the co-receptors involved in human and simian immunodeficiency virus (HIV-1 and SIV)-infection of CD4+ immune cells. (lu.se)

Orexin-A can be described as a non-subtype-selective neuropeptide that is capable of binding to either OX1R and OX2R, the two possible Orexin receptors, with roughly equal affinities. (proteopedia.org)

The team led by Dr. Kuo-Chiang Hsia (Institute of Molecular Biology, Academia Sinica) and Dr. Wei-Yi Chen (Institute of Biochemistry and Molecular Biology, College of Life Sciences, National Yang Ming Chiao Tung University) presents a cryo-EM structure of Kap114p, one of the Kap-βs, in complex with TATA box binding protein and reveals a non-canonical function beyond nuclear transport that modulates TBP-dependent transcription. (sinica.edu.tw)
The mouse chemerin receptor gene, mcmklr1, utilizes alternative promoters for transcription and is regulated by all-trans retinoic acid. (lu.se)
Nuclear receptors are transcription factors that transduce hormone signaling into a transcriptional response. (igbmc.fr)

Discoidin domain receptors form a subgroup of receptor tyrosine kinases. (wikipedia.org)

To pursue this notion, we have pharmacologically characterized seven known and putative nonsynonymous AT 1 receptor variants. (aspetjournals.org)
Variants that only slightly reduce the activity of the receptor cause mild androgen insensitivity syndrome. (medlineplus.gov)

Metabotropic GABA B receptors mediate slow inhibitory effects presynaptically and postsynaptically through the modulation of different effector signalling pathways. (springer.com)
To understand the spatial relationship of GABA B receptors with two key effector ion channels, the G protein-gated inwardly rectifying K + (GIRK/Kir3) channel and the voltage-dependent Ca 2+ channel, biochemical and immunohistochemical approaches were performed. (springer.com)
These data provide a better framework for understanding the different roles played by GABA B receptors and their effector ion channels in the cerebellar network. (springer.com)

1991. Effects of polychlorinated biphenyls with Ah receptor affinity on lymphoid development in the thymus and the bursa of Fabricius on chick embryos in ovo and in mouse thymus anlagen in vitro . (cdc.gov)
The functional high affinity IL-12 receptor is composed of at least IL12rb1 and IL12rb2. (lu.se)

Functional GABA B receptors are obligate heterodimers composed of GABA B1 and GABA B2 subunits, and they are implicated in a number of disorders, including cognitive impairments, nociception, anxiety, depression and epilepsy (Bettler et al. (springer.com)
also known as the thymic stromal lymphopoietin receptor), which together with IL7 receptor alpha forms a heterodimeric complex that acts at the functional receptor for thymic stromal lymphopoietin (reviewed in Roll and Reuther, 2010). (atlasgeneticsoncology.org)

The results indicate that beneficial effects of ETA receptor blockade on gastrointestinal function may result from an improvement in insulin sensitivity with concomitant reduction of the severity of hyperglycaemia. (portlandpress.com)
ETA receptor blockade may represent a new therapeutic principle for improving glucose tolerance in Type II diabetes and could be beneficial in alleviating or preventing hyperglycaemia-related secondary complications in this condition. (portlandpress.com)

The requirements for tkv in dorsal closure, visceral mesoderm and trachea development assign novel functions to dpp or a closely related member of the TGFβ superfamily. (biologists.com)

Loss-of-Function Mutation in Toll-Like Receptor 4 Prevents Diet-Induced Obesity and Insulin Resistance. (diabetesjournals.org)

This study investigated the pathogenic functions of TRAF6 signaling following TBI in vivo and in vitro. (researchsquare.com)

There are eight mammalian P2Y receptors known to date ( P2Y1 , P2Y2 , P2Y4 , P2Y6 , P2Y11 , P2Y12 , P2Y13 and P2Y14 ) and they are found in most human tissues. (atlasgeneticsoncology.org)

PAH was induced in S-D rats by a combination of a VEGF-receptor blocker followed by 4 weeks of 10% hypoxia (SuHx).Gene expression was evaluated by RT-PCR and confirmed by western blot. (ersjournals.com)

These peripheral cold receptors, both Aδ- and C-fibers, have thermal thresholds (i.e., the temperature at which nerve impulses are generated) for cold activation between 30-20°C, temperatures considered to be innocuously cool [ 4 , 6 ]. (nih.gov)
In seminal studies conducted by Hensel and Zotterman in the 1950s, menthol elicited its "cool" sensation by increasing the threshold temperature for activation of cold receptors [ 13 ]. (nih.gov)
Beneficial effects of collagen type III on β-cell function via activation of the cAMP/protein kinase A pathway, suppression of RhoA and caspase-3 activity, increased β-cell viability, and proliferation were abolished when ADGRG1 was downregulated in β-cells. (lu.se)
We propose that Npr3 acts as a clearance receptor to regulate local concentrations of natriuretic peptides for optimal cGMP production through Npr1 activation, and as a signaling receptor to control cAMP levels through inhibition of adenylyl cyclase. (gene-tools.com)
The results indicate that the peptide domains necessary for receptor activation differ for human and mouse TIG2/chemerin or that the maximal response of the mouse receptor is lower than in human. (lu.se)
The exact way of receptor activation is unknown so far. (wikipedia.org)
Together with integrin receptor α2β1 they provide coagulation cascade activation when a blood-vessel is damaged. (wikipedia.org)

The proteases involved are of different origins and types: (i) present as precursor in plasma, (ii) secreted into the plasma by activated platelets or other blood cells, or (iii) intracellularly activated and cleaving cytosolic receptor domains. (frontiersin.org)

This study investigated how P2X receptors operate in extreme ionic environments. (ucl.ac.uk)

Together, these data suggest that E2-mediated ERα signalling is critical for the sustenance of FOXP3 expression and Treg cell function in human CxCa via direct interaction of ERα with FOXP3 promoter. (ncbs.res.in)
Conclusions:Wedemonstrate a mechanistic link between ADGRG1 expression andβ-cell function. (lu.se)
AT 1 -C289W and AT 1 -F204S displayed reduced binding affinities of 3- and 5-fold and reduced cell surface expression of 43 and 60% of that observed for the WT receptor, respectively. (aspetjournals.org)
Here we describe the complex expression pattern of thick veins ( tkv ), which encodes a receptor for dpp . (biologists.com)
RT-PCR amplifications indicated that human islets express mRNAs coding for MT1 and MT2 melatonin receptors, although MT2 mRNA expression was very low. (lincoln.ac.uk)
Analysis of MT, receptor mRNA expression at the single cell level indicated that it was expressed by human islet alpha-cells, but not by beta-cells. (lincoln.ac.uk)
1994. Ah receptor in embryonic mouse palate and effects of TCDD on receptor expression. (cdc.gov)
At 7 days postinfection, lymphocytes from Listeria-infected rats showed significant increases in CD4+ and CD8+ cell counts and the CD8+/CD4+ ratio and exhibited increased production of IFN-gamma and IL-2 receptor expression compared with the noninfected control. (cdc.gov)

Ligands8

Abstract1

Antagonist6

Androgen receptor8

Binds2

Estrogen receptor5

Pharmacological5

Endogenous6

Peroxisome prolifer1

Glutamate4

Family of G-protein c2

Agonist5

Stimulation5

Antagonists2

Chemokine receptor2

Specific receptors2

Purinergic receptor1

Physiological2

Mechanism5

Human pancreatic islets1

Postsynaptic2

Exert1

Dopamine5

Melatonin receptor1

Adenosine3

Nuclear receptor1

Metabolism2

P2X41

AMPA1

Adenylate cyclase1

Regulates2

Epithelial2

Genes8

Ligand3

Selectivity2

Inflammation3

Muscarinic2

Protein-coupled1

Bind2

Cannabinoid3

Adhesion3

Subcellular3

Neuronal1

Proteins2

Responses3

Transmembrane3

Extracellular2

Metabolic1

Homeostasis2

GPVI2

Allosteric4

Sequence1

Subtype1

Transcription3

Tyrosine1

Variants2

Effector3

Affinity2

Functional2

Blockade2

Superfamily1

Mutation1

Vivo1

Mammalian1

Gene expression1

Activation7

Cytosolic1

Study investigated1

Expression8