Ligand and receptor. Medical search. Frequent questions

The mechanism by which the androgen receptor (AR) distinguishes between agonist and antagonist ligands is poorly understood. (rcsb.org)
With regard to opiate receptors, neither morphine, the prototypic mu agonist, nor kappa selective agonists (bremazocine,and U-50488) substituted for ibogaine. (erowid.org)
The concept of ligand bias at G protein-coupled receptors broadens the possibilities for agonist activities and provides the opportunity to develop safer, more selective therapeutics. (aspetjournals.org)
The design of the ligand is based upon 1-(3', 4'-dimethoxyphenethyl)-4-(3''-phenylpropyl) piperazine (1), a sigma1 agonist developed by Santen Pharmaceutical Co. Through a three-step synthesis, we have replaced one of the methyl groups with a diaminedithiol (DADT) chelating moiety attached through an alkyl chain (2). (umsystem.edu)
Interactions patterns between a reference agonist and the receptor, here exemplified on the β2 adrenergic receptor, were extracted from molecular dynamics simulations of the agonist/receptor complex and encoded in graphs used to train a one-class machine learning classifier. (biomedcentral.com)
The best models applied to post-process raw data from retrospective virtual screening obtained by docking of test libraries effectively filtered out irrelevant poses, discarding inactive and non-agonist ligands while identifying agonists. (biomedcentral.com)
While agonist ligands are known to have a higher binding affinity for the active state, and antagonists for the inactive state[ 12 ], the structures of the binding pocket in both states tend to be very similar [ 11 ]. (biomedcentral.com)

Follicle-stimulating hormone receptor (FSHR) is a G protein-coupled receptor (GPCR) with pivotal roles in reproduction. (frontiersin.org)
In turn, receptor signaling is known to drive or regulate GPCR trafficking. (frontiersin.org)
Here, we report that the recently sequenced genome from the red flour beetle Tribolium castaneum contains a gene coding for an oxytocin/vasopressin-like peptide, identical to the locust peptide, which we named inotocin (for insect oxytocin/vasopressin-like peptide) and a gene coding for an inotocin G protein-coupled receptor (GPCR). (lu.se)
This GPCR is strongly activated by low concentrations of inotocin (EC 50 , 5 × 10 -9 M), demonstrating that it is the inotocin receptor. (lu.se)
The computer-assisted discovery of GPCR ligands for therapeutic purposes therefore requires the development of predictive models of the pharmacological profile. (biomedcentral.com)

In contrast, the human AHR retains the ancestral sensitivity observed in primates to non-toxic endogenous AHR ligands (e.g. indole, indoxyl sulfate). (oregonstate.edu)
The actions of the endogenous ORL 1 -receptor ligand nociceptin on the membrane properties and synaptic currents in rat periaqueductal gray (PAG) neurons were examined by the use of whole-cell patch-clamp recording in brain slices. (jneurosci.org)
Endocannabinoid: endogenous cannabinoid receptor ligands with neuromodulatory action. (bvsalud.org)

The glucagon-like peptide-1 receptor (GLP-1R) is an important regulator of blood glucose homeostasis. (cam.ac.uk)

Although cellular and in vivo studies have provided considerable insight into the downstream consequences of Notch signalling, relatively little is known about the molecular basis of the receptor/ligand interaction and initial stages of activation. (nih.gov)
This orientation is further stabilized by an interaction between the ligand and the membrane. (nature.com)
However, the specific ligand of NTHi responsible for this interaction remains unknown. (lu.se)

Although the mechanism of action of ibogaine, a hallucinogen that may be useful in the treatment of addiction, remains unknown, receptor binding studies suggest that ibogaine produces its effects via interactions with multiple receptor types. (erowid.org)
In an attempt to determine which of these receptor interactions are involved in the in vivo effects of ibogaine, ligands for sigma, PCP, and opiate receptors were assessed for their ability to substitute for or to antagonize the ibogaine-induced discriminative stimulus (10 mg/kg I.P., 60 min presession) in Fischer-344 rats. (erowid.org)
In contrast to sigma2 and opiate receptors, ibogaine's reported interactions with NMDA receptors do not appear to be involved in its discriminative stimulus, as neither PCP nor MK-801 produced a significant level of ibogaine-appropriate responding. (erowid.org)
Identifying ligand-dependent AHR interactions and signaling pathways is essential for understanding toxicity of this class of environmentally relevant compounds. (oregonstate.edu)
The present study used in vitro expression systems to investigate interactions of members of the KDN series with δ-κ heterodimers through competition binding using selective ligands and the mitogen-activated protein kinase (MAPK) assay. (aspetjournals.org)
A network data frame (tibble) with ligand-receptor interactions suitable for use with NicheNet. (omnipathdb.org)
Data from the study of N-methylbicuculline suggest that it is promiscuous due to the flexibility of the orthosteric binding site of pLGIC members as well as the number of interactions the ligand can form, therefore a favourable orientation can always be adopted. (dundee.ac.uk)
Investigation of these ligands could further understanding of protein-ligand interactions with GBP and AcAChBP, as well as the physiological receptors GlyR and nAChR. (dundee.ac.uk)
Signaling is regulated by the interactions between receptors and their ligands, it can be stimulated by agonists, or inhibited by antagonists or inverse agonists. (biomedcentral.com)
The performance of the method depends on the relevance of the structural data, in particular the conformation of the targeted site, the binding mode of the reference ligand, and the approach used to compare the interactions formed by the docked ligand with those formed by the reference ligand in the crystallographic structure. (biomedcentral.com)

Membrane trafficking of G protein-coupled receptors (GPCRs) tightly orchestrates the signaling from this superfamily of signaling receptors. (frontiersin.org)
G-protein-coupled receptors (GPCRs) are typically considered to function as monomers. (aspetjournals.org)
Opioid receptors belong to rhodopsin receptor family of GPCRs. (aspetjournals.org)
G protein-coupled receptors (GPCRs) constitute the largest family of membrane proteins in humans. (biomedcentral.com)

The score can be interpreted in terms of ligand binding, but not ligand function. (biomedcentral.com)
deletion (20-22), no cases of HIV infection had while others are selective in terms of ligand been reported in studies of more than 60 persons binding. (cdc.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)

We performed in silico molecular docking and dynamic studies and demonstrated that type and size of substitution at the C17 position of the cortisol backbone confer a unique stable conformation to GR on ligand binding that is critical for inhibitory activity. (oregonstate.edu)
Lymphocyte activation gene 3 (LAG3) is an inhibitory immune checkpoint receptor that restrains autoimmune and antitumor responses, but its evolutionarily conserved cytoplasmic tail lacks classical inhibitory motifs. (bvsalud.org)

ancestral variant) in the ligand-binding domain of the aryl hydrocarbon receptor (AHR) gene. (oregonstate.edu)
Ligand-Specific Transcriptional Mechanisms Underlie Aryl Hydrocarbon Receptor-Mediated Developmental Toxicity of Oxygenated PAHs. (oregonstate.edu)
Like parent PAHs, OPAHs exert structure-dependent mutagenic activities and activation of the aryl hydrocarbon receptor (AHR) and cytochrome p450 metabolic pathway. (oregonstate.edu)

JAK2 is a member of the class I type tyrosine kinase family of enzymes and is involved in signal transduction for erythropoietin , thrombopoietin, and granulocyte colony-stimulating factor (G-CSF) receptors among other entities. (msdmanuals.com)

These receptors, a subset of the Class A/1 (Rhodopsin-like) family, all bind peptide ligands which include the chemokines, opioids and somatostatins. (reactome.org)
We assessed the efficacy and potency of structurally distinct KOR small molecule and peptide ligands. (ku.edu)

On the other hand, due to the scarcity of sigma2 selective ligands, less is understood about this subtype. (umsystem.edu)
Scholars@Duke publication: Multidimensional de novo design reveals 5-HT2B receptor-selective ligands. (duke.edu)

Selective androgen receptor modulators (SARMs) are essentially prostate sparing androgens, which provide therapeutic potential in osteoporosis, male hormone replacement, and muscle wasting. (rcsb.org)
Herein we report crystal structures of the androgen receptor (AR) ligand-binding domain (LBD) complexed to a series of potent synthetic nonsteroidal SARMs with a substituted pendant arene referred to as the B-ring. (rcsb.org)
Recently, our laboratory discovered selective androgen receptor modulators, which structurally resemble the nonsteroidal AR antagonists bicalutamide and hydroxyflutamide but act as agonists for the androgen receptor in a tissue-selective manner. (rcsb.org)

In search of new dual-acting histamine H/sigma-1 receptor ligands, we designed a series of compounds structurally based on highly active ligands previously studied and described by our team. (iasp-pain.org)

Given the critical nature of receptor internalization and endosomal signaling for FSHR activity, we assessed whether these compounds exhibit differential abilities to alter receptor endosomal trafficking and signaling within the VEE. (frontiersin.org)
All compounds exhibited a similar requirement for receptor internalization to increase cAMP and proportion of FSHR endosomes with active Gαs, suggesting regulation of cAMP signaling induced by T1 may be altered. (frontiersin.org)
The growth hormone (GH) receptor (GHR) is a mammalian plasma membrane protein whose internalization is mediated by the ubiquitin-proteasome pathway. (portlandpress.com)
In cell-based assays, TRV130 elicits robust G protein signaling, with potency and efficacy similar to morphine, but with far less β -arrestin recruitment and receptor internalization. (aspetjournals.org)
therefore, we have analyzed domains and individual amino acids in the cytoplasmic region of the rat GHR required for ligand-mediated receptor internalization, receptor down-regulation, and transcriptional signaling. (ku.dk)
These results demonstrate that phenylalanine 346 is essential for GHR internalization and down-regulation but not for transcriptional signaling, suggesting that ligand-mediated endocytosis is not a prerequisite for GH-induced gene transcription. (ku.dk)

Bond probabilities between each ligand investigated and Qi receptor residues in the ranges F10 to I44 and I190 to F235. (figshare.com)
A subfamily of ligand-gated ion channel receptors that share a characteristic loop which is formed by a disulfide bond between two CYSTEINE residues. (bvsalud.org)

ATRA and related retinoids inhibit ROR beta but not ROR alpha transcriptional activity suggesting that high-affinity, subtype-specific ligands could be designed for the identification of ROR beta target genes. (nih.gov)
Intermediate levels of generalization were observed with the subtype nonselective sigma ligands 3-(3-hydroxyphenyl)-N-(1-propyl)-piperidine [(+)-3-PPP] (69.0%) and 1,3-di(2-tolyl)guanidine (DTG) (73.5%) but not with the sigma1-selective agents (+)-N-allylnormetazocine [(+)-SKF 10,047] and (+)-pentazocine. (erowid.org)
This research project is focused on the preparation of a Tc-99m labeled complex designed to retain high affinity to the sigma1 receptor subtype. (umsystem.edu)

Morphine pharmacology in β -arrestin-2 knockout mice suggested that a ligand that promotes coupling of the μ -opioid receptor (MOR) to G proteins, but not β -arrestins, would result in higher analgesic efficacy, less gastrointestinal dysfunction, and less respiratory suppression than morphine. (aspetjournals.org)
The screens were conducted to discover new ligands of the proteins. (dundee.ac.uk)
This positioning allows the receptor to attach (bind) to other proteins, called ligands, outside the cell and to receive signals that help the cell respond to its environment. (medlineplus.gov)

As a whole, these studies provide critical new insight for receptor-based drug design of nonsteroidal AR agonists and antagonists. (rcsb.org)
This lack of standard assays has hampered the development of new drugs targeting the AT(2)R. Therefore, we aimed at developing a reliable, technically easy assay for the determination of intrinsic activity of AT(2)R ligands, primarily for distinguishing between AT(2)R agonists and antagonists. (mdc-berlin.de)
Regarding the selectivity of KDN21 for phenotypic δ and κ opioid receptors, we investigated the effect of KDN21 on the activation of MAPKs [extracellular signal-regulated kinases 1 and 2 (ERK1/2)] by δ- or κ-selective agonists. (aspetjournals.org)
The results of studies with selective agonists and antagonists in vivo are consistent with cooperativity between δ and κ receptors, and it has been proposed that the putative δ 1 and κ 2 opioid receptor subtypes are actually phenotypes ( Portoghese and Lunzer, 2003 ). (aspetjournals.org)

In contrast, no ligands for the retinoic acid receptor-related orphan receptors beta and gamma (ROR beta and gamma) have been identified, yet structural data and structure-function analyses indicate that ROR beta is a ligand-regulated nuclear receptor. (nih.gov)
The discovery of the gene sequences and predicted protein structures, role of CCR5 alleles has prompted studies of but their ligands have not been identified the possible role of many other host genes in (orphan receptors). (cdc.gov)

Divergent Ah receptor ligand selectivity during hominin evolution. (oregonstate.edu)

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)

These findings, along with observations that ibogaine has appreciable affinity for sigma2 receptors, suggest that these receptors may be involved in the ibogaine discriminative stimulus. (erowid.org)
The latter observations taken together with the finding that both nalorphine (>100 microM) and diprenorphine (30 microM) have extremely low affinity for sigma2 receptors, suggest that the ibogaine-appropriate responding produced by these agents is not mediated by sigma2 receptors. (erowid.org)
When DES-induced transcription factors were analyzed, estrogen receptor element (ERE), nuclear factor κB (NF-κB), nuclear factor of activated T cells (NF-AT), and activator protein-1 motifs on the Fas promoter, as well as ERE, NF-κB, and NF-AT motifs on the FasL promoter, showed binding affinity with the transcription factors. (aspetjournals.org)
However, we kept in mind that within the previous series, a pair of closely related compounds, and , differing only in the piperazine/piperidine moiety in the structural core showed a significantly different affinity at sigma-1 receptors (σRs). (iasp-pain.org)
We have shown previously that when using [ 3 H]diprenorphine as radioligand, KDN21 displayed greatly enhanced affinity in this series for coexpressed δ and κ opioid receptors (CDK). (aspetjournals.org)
In this regard, the use of the selective radioligands [ 3 H]naltrindole and [ 3 H]norbinaltorphimine (nor-BNI) in competition binding studies revealed that KDN21 has much higher affinity than other KDN members for CDK and bound to CDK more selectively relative to mixed δ and κ opioid receptors or singly expressed δ and κ opioid receptors. (aspetjournals.org)
A polytryptophan peptide that contains a single arginine residue (WRWWWW) serves as a receptor in affinity capillary electrophoresis to assess the degree of carboxylation. (cdc.gov)

Since the discovery of the two main cannabinoid receptors CB1 and CB2 in the early '90, intensive research reviled a substantial influence of this system on many physiological and pathophysiological processes. (logos-verlag.de)
The aim of the present study was to examine the effect of the synthetic endocannabinoid (eCB) analogue, arachidonyl-2′-chloroethylamide (ACEA), on calcitonin gene-related peptide (CGRP) release in the dura and trigeminal ganglion (TG), as cannabinoids are known to activate G i/o -coupled cannabinoid receptors type 1 (CB1), resulting in neuronal inhibition. (ku.dk)

As we previously reported, receptor activator of nuclear factor kappa-B (RANK) ligand (RANKL)/RANK signaling on M2 macrophages promotes the production of chemokines and proinflammatory cytokines to maintain the immunosuppressive tumor environment of extramammary Paget's disease (EMPD). (iiarjournals.org)
For example, Paget's cells release soluble receptor activator of nuclear factor kappa-B ligand (sRANKL) into the tumor microenvironment, stimulating RANK + TAMs to produce CCL17, which recruits Tregs into the lesional skin of patients with extramammary Paget's disease (EMPD) ( 11 , 17 ). (iiarjournals.org)
Description: The receptor activator of NF-kappaB ligand (RANK-L) is a recently discovered member of the TNF-ligand family involved in the regulation of the T cell-dependent immune response, lymph node organogenesis and bone formation. (glucagon-receptor.com)
Prolia works by blocking a protein called RANK (receptor activator of nuclear factor kappa beta) and helps prevent bone cells called osteoclasts from breaking down bone in the body. (medlineplus.gov)

GBP is based on Aplysia californica acetylcholine binding protein (AcAChBP), a surrogate for the nicotinic acetylcholine receptor (nAChR). (dundee.ac.uk)
[ 1 , 2 ] Although the chief target of the autoimmune attack in most cases is the skeletal muscle nicotinic acetylcholine receptor (nAChR), other antigenic targets that are components of the neuromuscular junction (NMJ) have also been implicated. (medscape.com)

In a combinatorial synthetic approach, several new libraries of new ligands were synthesised and subsequently pharmacological tested. (logos-verlag.de)
The phenylpiperazine and phenylpiperidine chemical classes of ligands have been identified to bind at sigma1 receptor sites and a pharmacological model has been proposed. (umsystem.edu)
An important step toward this goal would be the development of pharmacological tools that selectively target opioid receptor heterodimers. (aspetjournals.org)
The development of a new drug targeting a member of this family requires to take into account the pharmacological profile of the designed ligands in order to elicit the desired response. (biomedcentral.com)
Here, we propose a new method based on the conformational dynamics of a single protein-ligand reference complex to improve the biased selection of ligands with specific pharmacological properties in a structure-based virtual screening exercise. (biomedcentral.com)

Dual Piperidine-Based Histamine H and Sigma-1 Receptor Ligands in the Treatment of Nociceptive and Neuropathic Pain. (iasp-pain.org)

Ligand binding induces conformational changes that allow ions to flow through a pore generated by the TMD. (dundee.ac.uk)
The time interval that one can simulate (typically a microsecond) is too short for directly watching biologically interesting processes, such as conformational changes, ligand binding, and enzymatic reactions. (lu.se)

Click on one of the subfamilies of IgSF or TNFRSF co-signaling receptors shown in the Explore Pathways box below to see how the different members of each family affect T cell activation. (rndsystems.com)
TRV130 successfully translates evidence that analgesic and adverse MOR signaling pathways are distinct into a biased ligand with differentiated pharmacology. (aspetjournals.org)

Using nondenaturing mass spectrometry and scintillation proximity assays we found that all-trans retinoic acid (ATRA) and several retinoids bind to the ROR beta ligand-binding domain (LBD). (nih.gov)
Thus, standard commercially-available assays cannot be applied to test for agonistic or antagonistic properties of AT(2)R ligands. (mdc-berlin.de)
5'OH dsRNA has been shown to activate RIG-I, indicating an overlap in ligands between LGP2 and RIG-I. Competition assays show 5'OH dsRNA preferentially interacts with LGP2, suggesting a mechanism in which LGP2 sequesters non-PAMP ligand of RIG-I to diminish misactivations. (rutgers.edu)

Lysosomal inhibitors prolong the half-life of both receptor and ligand. (portlandpress.com)
The development of targeted therapies, including prostacyclin analogs, endothelin receptor antagonists, and tyrosine kinase inhibitors, has revolutionized the treatment of PAH. (reportsnreports.com)

Immunohistochemical staining of MMP1 and MMP25 as well as chemokine (C-C motif) ligand (CCL) 5 in the lesional skin from five patients with PCAC showed a substantial number of MMP1-bearing cells and MMP25-bearing cells, as well as CCL5-producing cells, that were distributed in the lesional skin. (iiarjournals.org)
One major discovery was that members of the chemokine receptor family serve as cofactors for HIV entry into cells. (cdc.gov)
We describe the role of allelic polymorphism in the gene coding for the CCR5 chemokine receptor with regard to susceptibility to and disease course of HIV infection. (cdc.gov)
Several human chemokine receptors have been sons than for those homozygous for the wild classified as such on the basis of similarity of type CCR5 (12,17-19,23). (cdc.gov)
What Are Chemokine Receptors? (cdc.gov)

But what makes the sigma receptors so great is the fact that they bind a variety of ligands. (umsystem.edu)
Differentiation into Th1 depends on the presence of IFN-γ and IL-12, which bind to receptors on the surface of CD4 T cells 5 . (bvsalud.org)

Hallberg, B. & Palmer, R. H. Mechanistic insight into ALK receptor tyrosine kinase in human cancer biology. (nature.com)

Other experiments revealed that the binding of naltrindole to δ opioid receptors could increase the binding of nor-BNI to κ opioid receptors and vice versa, suggesting reciprocal allosteric modulation of receptors in the heterodimer. (aspetjournals.org)

Also, the homologous histamine receptor (HisR) from Apis mellifera was investigated to understand how histamine binds and relate this binding to potentially mislabelled receptors in mammals. (dundee.ac.uk)
Evidence suggests that C1q binds a receptor present on phagocytic cells, termed C1qRP. (medscape.com)
The C3a receptor binds C3a and C4a. (medscape.com)
Epidermal growth factor receptor binds to at least seven different ligands. (medlineplus.gov)

The ligand-dependent suppression of TCR signaling by the immune checkpoint receptor LAG3 depends on the cytoplasmic RRFSALE motif. (bvsalud.org)

To our knowledge, this is the first report on the molecular cloning of an oxytocin/vasopressin-like receptor and its ligand from arthropods. (lu.se)
In vivo assessment of these corticosteroid analogs is essential to understand the difference in molecular signaling of the ligands that share the corticosteroid backbone. (oregonstate.edu)

The ameliorating effects of red wine on metabolic diseases may be partially explained by the presence of PPARγ ligands . (rsc.org)

To investigate why subtle structural changes to both the ligand and the receptor (i.e. mutations) result in drastic changes in activity, we studied structure-activity relationships for nonsteroidal AR ligands through crystallography and site-directed mutagenesis, comparing bound conformations of R-bicalutamide, hydroxyflutamide, and two previously reported nonsteroidal androgens, S-1 and R-3. (rcsb.org)
Somatic and germline activating mutations of the ALK kinase receptor in neuroblastoma. (nature.com)
Lung cancers with EGFR gene mutations tend to respond to treatments that specifically target the overactive epidermal growth factor receptor protein that allows cancer cells to constantly grow and divide. (medlineplus.gov)
Mutations of the thrombopoietin receptor gene ( MPL ) or the calreticulin ( CALR ) gene also may be the cause of primary myelofibrosis. (msdmanuals.com)

A receptor is made up of five subunits. (dundee.ac.uk)
These receptors typically contain five subunits with the cysteine-loop occurring near an N-terminal extracellular domain. (bvsalud.org)

KDN21 is a bivalent ligand that contains δ and κ opioid antagonist pharmacophores linked through a 21-atom spacer. (aspetjournals.org)
KDN21 contains δ and κ opioid receptor antagonist pharmacophores that are connected through a 21-atom spacer ( Fig. 1 ). (aspetjournals.org)

A converse goal of receptor-ligand kinetics is to estimate the rate constants and/or dissociation constants of the receptors and ligands from experimental kinetic or equilibrium data. (wikipedia.org)
ligands, based on the measured ligand binding dissociation constant (Kd). (duke.edu)

Alternate glucocorticoid receptor ligand binding structures influence outcomes in an in vivo tissue regeneration model. (oregonstate.edu)
Non-invasive imaging of the sigma receptor in vivo would lead to a better understanding of the role that sigma receptors play in health and disease. (umsystem.edu)
Although the in vitro binding data were consistent with the in vivo study, it did not identify the binding characteristics of each of the bridged receptors. (aspetjournals.org)

Experiments with antibodies against different receptor tail sections show that degradation of the GHR cytosolic domain precedes degradation of the extracellular GH-binding domain. (portlandpress.com)

With the discovery of the protective arm of the renin-angiotensin system (RAS), interest has grown in protective RAS-related receptors such as the angiotensin AT(2)-receptor [AT(2)R] as potential new drug targets. (mdc-berlin.de)

The ICD is the site of cell- receptor communication. (dundee.ac.uk)
We found that LAG3 reduced the response to T cell receptor stimulation in the presence of MHC class II molecules to a lesser extent compared with the receptor programmed cell death protein 1 . (bvsalud.org)
This signal together with the T Cell Receptor (TCR) induces the expression of GATA-3. (bvsalud.org)

Thus, the present study offers evidence that unlike NMDA receptors, both sigma2 and opiate receptors may be involved in the ibogaine discriminative stimulus. (erowid.org)

The Notch receptor is part of a core signalling pathway which is highly conserved in all metazoan species. (nih.gov)

The analysis of CGRP release data was combined with immunohistochemistry in order to study the cellular localization of CB1, cannabinoid receptor type 2 (CB2), CGRP and receptor activity modifying protein 1 (RAMP1), a subunit of the functional CGRP receptor, in the TG. (ku.dk)
Aim: To evaluate the involvement of Th2 cells in different periods of the active phase of experimental periodontal disease and expression of the R1 subunit of the receptor for IFN-γ during the early and advanced progression of the disease. (bvsalud.org)

RÉSUMÉ L'objectif de l'étude était d'évaler l'importance clinique du ligand de CD40 soluble (sCD40L) chez des patients atteints d'un carcinome hépatocellulaire (CHC) associé au virus de l'hépatite C (VHC). (who.int)

The estrogen receptor (ER) is a transcription factor whose activity is normally activated by the hormone estradiol and inhibited by antiestrogen. (eurekamag.com)
It has been found that certain mutational changes in the activation function-2 region in the hormone-binding domain of the human ER result in ligand activity inversion mutants, i.e. receptors that are now activated by antiestrogen and inhibited by estrogen. (eurekamag.com)
These findings highlight the means by which the carboxyl-terminal region in domain E functions to interpret the activity of a ligand, and they demonstrate that rather minimal changes in the ER can result in receptors with inverted response to antiestrogen and estrogen. (eurekamag.com)
The MSDS of Estrogen for receptor is available from Karlan upon request. (phantome.org)

These studies provide the first crystallographic evidence of the mechanism by which nonsteroidal ligands interact with the wild type AR. (rcsb.org)
Our data reveal a mechanism of RTK activation that allows dimerization by either dimeric (ALKAL2) or monomeric (ALKAL1) ligands. (nature.com)
This mechanism is underpinned by an unusual architecture of the receptor-ligand complex. (nature.com)

Antigen: KLH-conjugated synthetic peptide encompassing a sequence within human sRANK Ligand. (glucagon-receptor.com)
Comparisons of structural sequence and binding data for both ligands suggested that GBP may be a good surrogate of the GlyR heteromer. (dundee.ac.uk)

nuclear receptor. (duke.edu)

A main goal of receptor-ligand kinetics is to determine the concentrations of the various kinetic species (i.e., the states of the receptor and ligand) at all times, from a given set of initial concentrations and a given set of rate constants. (wikipedia.org)
The total concentrations of receptor and ligands are sometimes varied systematically to estimate these constants. (wikipedia.org)
Les concentrations sériques de sCD40L circulant et d'interleukine 10 circulante ont été analysées à l'aide de la méthode immuno-enzymatique chez 30 patients positifs pour le VHC avec un CHC, chez 30 patients patients positifs pour le VHC avec une cirrhose du foie, et chez 30 volontaires d'âge correspondant en bonne santé avec des anticorps anti-VHC négatifs servant de groupe témoin. (who.int)

However, it is still not clear how such dimeric opioid receptors are organized and what role they play in signaling. (aspetjournals.org)

Retinoids regulate gene expression through binding to the nuclear retinoic acid receptors (RARs) and retinoid X receptors (RXRs). (nih.gov)
A receptor family, retinoic-acid-inducible gene I (RIG-I)-like receptors (RLRs) consist of three members, RIG-I, MDA5 and LGP2. (rutgers.edu)
Earlier HIV infec- receptor gene polymorphism in HIV infection, tion diagnosis, inhibition of ongoing HIV replica- only genes of the HLA system were thought to tion with antiretroviral therapy (in industrialized protect against HIV infection. (cdc.gov)
The EGFR gene provides instructions for making a receptor protein called the epidermal growth factor receptor, which spans the cell membrane so that one end of the protein remains inside the cell and the other end projects from the outer surface of the cell. (medlineplus.gov)
These gene changes result in a receptor protein that is constantly turned on (constitutively activated), even when it is not bound to a ligand. (medlineplus.gov)

LAG3- blocking antibodies attenuated LAG3-mediated inhibition in our reporter cells and enhanced reporter cell activation even in the absence of LAG3 ligands , indicating that they could potentially enhance T cell responses independently of their blocking effect. (bvsalud.org)

Of the 8 plasma membrane receptors for complement, only deficiencies of CR3 and CR4 due to CD18 deficiency have been described, known as leukocyte adhesion deficiency (LAD) type 1 . (medscape.com)

Anatomy20

Organisms11

Diseases1

Chemicals and Drugs128

Analytical, Diagnostic and Therapeutic Techniques and Equipment35

Phenomena and Processes61

Disciplines and Occupations2

Technology, Industry, Agriculture1

Information Science6

Health Care1

Agonist7

GPCR5

Endogenous3

Glucagon-like pep1

Interaction3

Interactions10

GPCRs4

Terms of ligand2

Peroxisome prolifer1

Inhibitory2

Aryl hydrocar3

Signal Transduction1

Peptide ligands2

Selective ligands2

Androgen receptor3

Structurally1

Internalization6

Residues2

Subtype3

Proteins3

Agonists4

Orphan receptors2

Selectivity1

High-affinity1

Affinity7

Cannabinoid receptors2

Activator4

Nicotinic acetylch2

Pharmacological5

Sigma-1 recept1

Conformational2

Pathways2

Assays3

Inhibitors2

Chemokine5

Bind2

Tyrosine kinase1

Allosteric1

Binds4

Cytoplasmic1

Molecular2

PPAR1

Mutations4

Five subunits2

Antagonist2

Dissociation2

Vivo3

Experiments1

Angiotensin1

Cell receptor3

Sigma21

Signalling pathway1

Subunit2

Soluble1

Estrogen4

Mechanism3

Sequence2

Nuclear receptor1

Concentrations3

Dimeric1

Gene5

Antibodies1

Plasma membrane1