Assay ligand receptor. Medical search. Frequent questions

The FMP assay reliably detected both partial agonists and stereoselectivity. (ku.edu)
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)
d) EMA401 and PD123319, which are commonly regarded as AT(2)R antagonists, are partial agonists at the AT(2)R. Collectively, we have developed and tested an assay based on the measurement and quantification of NO release in HAEC or in AT(2)R-CHO cells that is suitable for the characterisation of novel and established AT(2)R ligands. (mdc-berlin.de)
A fluorescence resonance energy transfer-based assay was used to screen a 10,000-compound chemical library for ER agonists. (rcsb.org)
From the screen, we identified a family of ERbeta-selective agonists whose members contain bulky oxabicyclic scaffolds in place of the planar scaffolds common to most ER ligands. (rcsb.org)
These agonists are 10-50-fold selective for ERbeta in competitive binding assays and up to 60-fold selective in transactivation assays. (rcsb.org)
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)
GTPγS binding assays for GPCR agonists screen. (diwou.com)
Second, different agonists vary in efficacy and can stimulate receptor activity to a different extent 5 . (nature.com)
The current studies provide novel insights into the pharmacology of GPR40 and indicate that G protein-coupled receptors which respond to fatty acids, and potentially to other lipid ligands, can be occupied by endogenous agonists before assay and that this may mask the pharmacology of the receptor and may be mistaken for high levels of constitutive activity. (aspetjournals.org)
The homogeneous assay kit format allows you to detect agonists, antagonists, and allosteric modulators. (discoverx.com)

Ligand binding assays provide a measure of the interactions that occur between two molecules, such as protein-bindings, as well as the degree of affinity (weak, strong, or no connection) for which the reactants bind together. (wikipedia.org)
A biosensor assay for studying ligand-membrane receptor interactions: Binding of antibodies and HIV-1 Env to chemokine receptors. (integralmolecular.com)
Binding of the 2-carbon-modified analogues does not change the positions of the amino acids in the ligand binding site and has no effect on the interactions in the coactivator binding pocket. (rcsb.org)
Electrostatic and hydrophobic interactions between the peptide and the LBD stabilize the active receptor conformation. (rcsb.org)
A comparison of these structures with existing ER structures suggests that the ERbeta selectivity of OBCP ligands can be attributed to a combination of their interactions with Met-336 in ERbeta and Met-421 in ERalpha. (rcsb.org)
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)
BMPR family of proteins is a valuable tool for studying ligand-receptor interactions, downstream signaling events, and determining therapeutic targets. (news-medical.net)
Therefore, smFRET has been limited to studies of inter-receptor interactions in cellular membranes and receptors in detergent environments. (nature.com)
In this study we have examined the interactions of CB1 and D2 receptors on adenylate cyclase. (jneurosci.org)
signaling interactions between these receptors have not been investigated extensively. (jneurosci.org)
X-ray crystallography of human PPAR isoforms has revealed important residues responsible for ligand binding, heterodimerisation and co-factor interactions. (sigmaaldrich.com)
However, these receptors exhibit a high degree of sequence variability at their NH(2)-terminal domain, which suggests the possibility of receptor-specific interactions with co-regulator proteins. (nih.gov)
The complexity of interactions between orthosteric and allosteric ligands is revealed by a number of adequate biochemical and electrophysiological assay systems. (aspetjournals.org)

Coactivator proteins such as SRC1 and CBP/p300 are recruited by agonist bound receptors and promote initiation of transcription by remodelling the chromatin structure while coactivators such as the PPAR binding protein (PBP) and TRAP220 interact directly with the transcriptional machinery. (sigmaaldrich.com)
Here we have identified Ran-binding protein in the microtubule-organizing center (RanBPM) to be a novel AR-interacting protein by yeast two-hybrid assay and have confirmed this interaction by glutathione S-transferase- and His-tagged pull-down assays. (nih.gov)

The foundations for which ligand binding assay have been built are a result of Karl Landsteiner, in 1945, and his work on immunization of animals through the production of antibodies for certain proteins. (wikipedia.org)
The compound is a weak ligand for the retinoic acid receptor proteins (RARs) and related cellular retinoic acid binding proteins (CRABPI/II) and can, therefore, be used as a replacement for ATRA in cellular assays involving retinoid signaling processes. (sigmaaldrich.com)
Both D1 and D2 dopamine receptors also couple to adenylate cyclase via G-proteins. (jneurosci.org)
whereas dopamine D2 receptors inhibit adenylate cyclase via G i -proteins ( Sibley and Monsma, 1992 ). (jneurosci.org)
A greater understanding of the mechanism of transcriptional regulation by nuclear receptors has lead to the identification of multiple accessory proteins that bind to the nuclear receptors in a ligand-dependent manner. (sigmaaldrich.com)
The nuclear receptor corepressor (N-CoR) or silencing mediator of retinoid and thyroid receptors (SMRT) proteins bind and mediate repression of transcription by the unliganded receptors. (sigmaaldrich.com)
Among the range of proteins shown to co-localize to WPB is angiopoietin-2 (Angpt-2), a ligand of the receptor tyrosine kinase Tie-2. (imperial.ac.uk)
We combined data from six prospective epidemiological studies of 30-77-year-old individuals with type 2 diabetes in whom 80 circulating proteins were measured by proximity extension assay. (springer.com)
5% false discovery rate) between risk of MACE and eight proteins: matrix metalloproteinase (MMP)-12, IL-27 subunit α (IL-27a), kidney injury molecule (KIM)-1, fibroblast growth factor (FGF)-23, protein S100-A12, TNF receptor (TNFR)-1, TNFR-2 and TNF-related apoptosis-inducing ligand receptor (TRAIL-R)2. (springer.com)
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)
When he was based at the University of Rochester, he and his research team pioneered methods for purifying steroid hormone receptor proteins to study their relationships in human breast cancer. (aacc.org)
His team helped establish tamoxifen as adjuvant therapy for breast cancer and the use of receptor proteins as tissue biomarkers of a patient's prognosis and therapy response. (aacc.org)
He was one of the first investigators to identify a correlation between the presence of estrogen receptor proteins in a breast cancer biopsy and response to either additive or surgical ablative hormone therapy. (aacc.org)
DRIPs are a distinct set of ligand-dependent proteins that interact with the vitamin D receptor (VDR). (novusbio.com)
Our research focuses on proteins involved in inflammation, specifically the involvement of cysteinyl leukotriene receptors. (lu.se)

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)
BioDuro-Sundia's radioisotope laboratory in Jiangsu, China is part of the in vitro biology department of our drug discovery business unit, which mainly provides in vitro pharmacological assays and metabolic assays based on cellular or biochemical reactions. (diwou.com)
Peptide profiling, a novel ER ligand screening assay, is a method that can potentially identify SERMS by correlating in vitro ER conformation with in vivo biological response. (umsystem.edu)
All three are potent and selective GR ligands in vitro. (dtic.mil)
The material from each step isscreened using acellular and in vitro assays for evaluating general toxicity, mechanisms of toxicity, and macrophage function. (cdc.gov)

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)
The complex pharmacology of G-protein-coupled receptors (GPCRs) is defined by their multi-state conformational dynamics. (nature.com)
GPCRs recognize a large variety of endogenous extracellular signaling molecules transmitting their corresponding signals inside the cell, and this process can be modulated by synthetic ligands or drug molecules. (nature.com)

Radioligands are used to measure the ligand binding to receptors and should ideally have high affinity, low non-specific binding, high specific activity to detect low receptor densities, and receptor specificity. (wikipedia.org)
Saturation binding analysis can determine receptor affinity and density. (wikipedia.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)
Especially, it has unsurpassed specificity and sensitivity in the detection of membrane receptors such as GPCR receptor-ligand binding affinity test and extracellular substance uptake assays. (diwou.com)
Radioligand-binding assay, including GPCR receptor-ligand binding affinity test. (diwou.com)
The HAESA co-receptor SERK1, a positive regulator of the floral abscission pathway, allows for high-affinity sensing of the peptide hormone by binding to an Arg-His-Asn motif in IDA. (elifesciences.org)
RESULTS: Static-binding assays revealed that Angpt-2 bound to VWF with high affinity (KD,app ∼3 nM) in a pH and calcium-dependent manner. (imperial.ac.uk)
The αβ T-cell coreceptor CD4 enhances immune responses more than 1 million-fold in some assays, and yet the affinity of CD4 for its ligand, peptide-major histocompatibility class II (pMHC II) on antigen-presenting cells, is so weak that it was previously unquantifiable. (lu.se)
Here, we report that a soluble form of CD4 failed to bind detectably to pMHC II in surface plasmon resonance-based assays, establishing a new upper limit for the solution affinity at 2.5 mM. (lu.se)
Calculations indicated, however, that CD4/pMHC II binding would increase rates of T-cell receptor (TCR) complex phosphorylation by threefold via the recruitment of Lck, with only a small, 2-20% increase in the effective affinity of the TCR for pMHC II. (lu.se)
The affinity of CD4/pMHC II therefore seems to be set at a value that increases T-cell sensitivity by enhancing phosphorylation, without compromising ligand discrimination. (lu.se)

Ligand binding assays are used primarily in pharmacology for various demands. (wikipedia.org)
TRV130 successfully translates evidence that analgesic and adverse MOR signaling pathways are distinct into a biased ligand with differentiated pharmacology. (aspetjournals.org)

We explored the utility of the real-time FLIPR Membrane Potential (FMP) assay as a method to assess kappa opioid receptor (KOR)-induced hyperpolarization. (ku.edu)
A membrane receptor reagent and assay is disclosed in which liposomes are bound to an evanescent wave emitting surface. (google.com)

Such probes may be useful to investigate the biological role of CB2 receptors in cellular assays. (nih.gov)

Methods: Peroxisome Proliferator-Activated Receptor gamma (PPARγ) ligand binding assays were used to identify obesogens. (nist.gov)
DOSS was found to be a significant obesogen by ligand binding assays, PPAR-driven luciferase induction in vivo and fat cell induction. (nist.gov)
PPAR-RXR heterodimers can also be activated by ligand binding to either receptor partner independently. (sigmaaldrich.com)
With the involvement of PPARs in many diverse metabolic pathways there is great clinical interest in the potential utility of PPAR ligands for the treatment of cancer, inflammation, psoriasis, atherosclerosis, dyslipidaemia, neurological disorders, obesity and diabetes. (sigmaaldrich.com)

Results: Serum-free conditions greatly enhanced sensitivity without reducing specificity in ligand binding assays. (nist.gov)
Compared with conventional biological sample detection techniques, Radioisotope assay has distinct advantages such as high specificity, high sensitivity at the nanomolar level, short detection time, accurate positioning, and quantification, etc. (diwou.com)

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)
One cryoEM and over 50 high-resolution X-ray crystallographic structures are available for antagonist- or agonist-bound A 2A AR and for its ternary complex with an agonist and an engineered G protein, making this receptor an excellent model system for investigating GPCR structural dynamics. (nature.com)
For example, the ligand tamoxifen, a commonly used breast cancer pharmaceutical, exhibits an ER antagonist response in the breast and an ER agonist response in the bone. (umsystem.edu)
This augmentation was blocked by the CB1 receptor antagonist SR141716A or the D2 antagonist sulpride. (jneurosci.org)
e) Antagonist but partial agonist in transactivation assays but inhibitor of adipocyte differentiation. (sigmaaldrich.com)

Tumor size, grade, axillary lymph node status, steroid hormone receptor status, and human epidermal growth factor receptor 2 (HER2)/neu overexpression are the factors that most commonly influence treatment decisions and are discussed in detail below. (medscape.com)

Type I receptors consist of BMPR1B (ALK6) and BMPR1A (also called ALK3), while type II receptors comprise BMPR2 and ActRII (Activin receptor type II) subtypes. (news-medical.net)
Two subtypes of cannabinoid receptors have been identified. (jneurosci.org)
The C-terminal ligand-binding domain (regions E/F) is the site of ligand docking and has the most diversity between the pharmacologically distinct subtypes. (sigmaaldrich.com)

We directly compared the potency of U50,488 and Dyn (1−13)NH2 in the FMP and [35S]GTPγS binding assays, and found that both were approximately 10 times more potent in the cellular fluorescence assay. (ku.edu)
We found that measurement of NO release by DAF-FM fluorescence in primary human aortic endothelial cells (HAEC) or in AT(2)R-transfected CHO cells is a reliable assay for the characterization of AT(2)R ligands. (mdc-berlin.de)
A detection method is used to determine the presence and extent of the ligand-receptor complexes formed, and this is usually determined electrochemically or through a fluorescence detection method. (wikipedia.org)
Fluorescence microscopy, fluorescent retinoid binding assay, fluorescence spectroscopy. (sigmaaldrich.com)
LightOx23 can be utilised to study retinoid behaviour using fluorescence microscopy, employed in a competitive fluorometric ligand-binding assay for direct determination of the strength of binding of non-fluorescent retinoids to a protein target, and as a fluorophore in fluorescence spectroscopy. (sigmaaldrich.com)

Using KOR-selective peptides with varying efficacies, we found that the FMP assay allowed high throughput quantification of peptide efficacy. (ku.edu)
Specifically, despite the human body's endogenous receptors, hormones, and other neurotransmitters, pharmacologists utilize assays in order to create drugs that are selective, or mimic, the endogenously found cellular components. (wikipedia.org)
These differences have stimulated the search for subtype-selective ligands. (rcsb.org)
The weak uterotrophic activity of these ligands in immature rats and their ability to stimulate expression of an ERbeta regulated gene in human U2OS osteosarcoma cells provides more physiological evidence of their ERbeta-selective nature. (rcsb.org)
In this work we synthesized 18 biphenylic carboxamides as new CB2-selective ligands and evaluated their pharmacological profiles. (nih.gov)
This dual ligand quality characterizes what is now known as a selective estrogen receptor modulator (SERM). (umsystem.edu)
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)

Follicle-stimulating hormone receptor (FSHR) is a G protein-coupled receptor (GPCR) with pivotal roles in reproduction. (frontiersin.org)
Cannabinoids exert many of their effects through activation of G i -protein-coupled receptors. (jneurosci.org)
This article reviews the current status of allosteric modulation at family C G-protein coupled receptors in the light of their specific structural features on the one hand and current concepts in receptor theory on the other hand. (aspetjournals.org)
Family C G-protein-coupled receptors are characterized by a large extracellular domain containing the orthosteric agonist binding site known as the "venus flytrap module" because of its bilobal structure and the dynamics of its activation mechanism. (aspetjournals.org)
She is investigating two different ligands and their receptive G-protein coupled receptors WNT5A/Frizzle and cysteinyl leukotriene C4/CysLTR2 signaling pathways which both upregulates 15-PGDH and induce re-differentiation of colon cancer cells. (lu.se)

Peroxisome proliferator activated receptors (PPARs) are members of the nuclear hormone receptor superfamily of ligand-activated transcription factors that are related to retinoid, steroid and thyroid hormone receptors. (sigmaaldrich.com)

Each ligand is screened using a two-hybrid fusion protein reporter gene assay. (umsystem.edu)

Such advances provide researchers with the ability not only to quantify hormones and hormone receptors, but also to contribute important pharmacological information in drug development and treatment plans. (wikipedia.org)
Low molecular weight (LMW) allosteric FSHR ligands were developed for use in assisted reproductive technology yet could also provide novel pharmacological tools to study FSHR. (frontiersin.org)
An important step toward this goal would be the development of pharmacological tools that selectively target opioid receptor heterodimers. (aspetjournals.org)

Allosteric receptor modulation is an attractive concept in drug targeting because it offers important potential advantages over conventional orthosteric agonism or antagonism. (aspetjournals.org)

Hence, it is desirable to start with a biochemical assay followed by a cell-based assay to corroborate results in a physiological context (that is, to provide orthogonal validation). (genengnews.com)
eXpress Assay kits developed by Eurofins DiscoverX ® are ready-to-use (RTU) cell-based assay kits for functional mechanism of action (MOA) or binding assay for drug discovery target validation, screening and hit ID, and lead optimization applications. (discoverx.com)

a) This data is compiled from multiple literature and from different human assays - binding assays and transactivation assays. (sigmaaldrich.com)

This sequence pattern is conserved among diverse plant peptides, suggesting that plant peptide hormone receptors may share a common ligand binding mode and activation mechanism. (elifesciences.org)
Expanded natural killer cells killed both allogeneic and autologous primary myeloma cells avidly via a perforin-mediated mechanism in which the activating receptor NKG2D, natural cytotoxicity receptors, and DNAX-accessory molecule-1 played a central role. (haematologica.org)
Therefore, the anorexigenic effect exerted by the CBD could be the result of a multitarget mechanism, involving the whole endocannabinoid receptor system, particularly in the hypothalamus. (researchgate.net)
TCDD for every step of the mechanism described for 2,3,7,8-TCDD carcinogenesis in humans including receptor binding, gene expression, protein activity changes, cellular replication, oxidative stress, promotion in initiation-promotion studies and complete carcinogenesis in laboratory animals. (who.int)

We assessed the efficacy and potency of structurally distinct KOR small molecule and peptide ligands. (ku.edu)
To provide insight into the molecular mechanisms of their activity and selectivity, we determined the crystal structures of the ERalpha ligand-binding domain (LBD) and a peptide from the glucocorticoid receptor-interacting protein 1 (GRIP1) coactivator complexed with the ligands OBCP-3M, OBCP-2M, and OBCP-1M. (rcsb.org)
After screening a ligand against a library of fifteen different peptides, a unique peptide profile will figuratively illustrate the induced ER conformation. (umsystem.edu)
Each ligand was found to have a unique peptide profile and, implicitly, a distinct ER conformation. (umsystem.edu)
Floral abscission is controlled by the leucine-rich repeat receptor kinase (LRR-RK) HAESA and the peptide hormone IDA. (elifesciences.org)

To better understand the molecular changes associated with AD, genome-wide association studies (GWAS) have identified hundreds of candidate genes linked to the disease, like the receptor tyrosine kinase EphA1. (sdbonline.org)
Roles for Eph receptor tyrosine kinase signaling in the formation of topographic patterns of axonal connectivity have been well established in vertebrate visual systems. (sdbonline.org)
A role for a Drosophila Eph receptor tyrosine kinase (Eph) in the control of photoreceptor axon and cortical axon topography in the developing visual system is described. (sdbonline.org)

Radioactive kinase assay for kinase inhibitor screen. (diwou.com)
2014 ). The available genetic and biochemical evidence suggests that IDA and HAESA together control floral abscission, but it is poorly understood if IDA is directly sensed by the receptor kinase HAESA and how IDA binding at the cell surface would activate the receptor. (elifesciences.org)

Phenotypic cellular assay models more accurately reflect the complex biology of disease, allows for multiparametric measurement of ex vivo or in vivo events, and enables the characterization of intractable target(s). (genengnews.com)

Many targets, such as estrogen and androgen receptors, related to the endocrine disrupting, have been studied. (mdpi.com)

There are numerous types of ligand binding assays, both radioactive and non-radioactive. (wikipedia.org)
Essential aspects of binding assays include, but are not limited to, the concentration level of reactants or products (see radioactive section), maintaining the equilibrium constant of reactants throughout the assay, and the reliability and validity of linked reactions. (wikipedia.org)

Such receptors exhibit unique ligand-binding specificities and mediate distinct signaling cascades, even though they could cross-interact with other TGF-β family ligands. (news-medical.net)
DRIPs bind to several nuclear receptors to mediate ligand-dependent enhancement of transcription by VDR and the thyroid hormone receptor in cell-free transcription assays. (novusbio.com)

Estrogen receptors alpha (ERalpha) and beta (ERbeta) have distinct functions and differential expression in certain tissues. (rcsb.org)
Allosteric ligands modulate receptor function by binding to a site distinct from the recognition site for the endogenous agonist. (aspetjournals.org)

There are two common strategies that are adopted for this type of experiment: Increasing the amount of radioligand added while maintaining both the constant specific activity and constant concentration of radioligand, or decreasing the specific activity of the radioligand due to the addition of an unlabeled ligand. (wikipedia.org)
To date, we have completed radioligand receptor binding assays and MOA assays for a number of domestic and international clients and received consistent praise from our clients for delivering data with high accuracy. (diwou.com)

The results were confirmed using caspase specific inhibitors and caspase activity assays. (cdc.gov)

These data demonstrate that the FMP assay is a sensitive method for assessing κ-opioid receptor induced hyperpolarization, and represents a useful approach for quantification of potency, efficacy and desensitization of KOR ligands. (ku.edu)
ligand binding potency and activation of several groups of major semi-volatile organic compounds (SVOCs) that are ubiquitously detected in indoor environments, including flame retardants such as polybrominated diphenyl ethers (PBDEs) and Firemaster 550 (FM550), and other SVOCs such as phthalates, organotins, halogenated phenols and bisphenols. (duke.edu)
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)

When the ER is bound, the ligand induces a unique ER shape and in turn causes an array of tissue-specific biological responses. (umsystem.edu)
Preclinical studies have shown that resveratrol induces immunomodulatory effects, including the upregulation of NKG2D receptors on natural killer cells (NK) that it promotes the NKG2D-dependent killing of tumor cells [ 13 , 14 ] and the induction of regulatory T cells (Treg) in the colonic tissues of mice exposed to colonic inflammatory stress [ 15 ]. (hindawi.com)

Both estradiol and xenoestrogens can bind two estrogen receptors (ERs), ER alpha and ER beta, to elicit biological responses. (umsystem.edu)
Dr. Wittliff was among the first investigators to discover that estrogen receptors serve as a biomarker predicting a patient's risk of recurrence and response to hormone therapy. (aacc.org)

Glucocorticoid receptor activity was also enhanced when RanBPM was overexpressed, whereas estrogen receptor activity remained unchanged. (nih.gov)
The purpose of this project is to develop radioligands to measure glucocorticoid receptor GR expression in enzalutamide resistant prostate cancer. (dtic.mil)

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)
These bicyclic ligands show promise as lead compounds that can target ERbeta. (rcsb.org)
Each receptor shows a differential pattern of tissue expression and is activated by structurally diverse compounds including endogenous long-chain fatty acids. (sigmaaldrich.com)
Dr. Wittliff and IA, Inc., patented receptor-based fiber-optic biosensors that detect endocrine-disrupting compounds in the environment. (aacc.org)
The screening pipeline started by assessing Lipinski's rule of five (RO5), drug-likeness, and pan-assay interference compounds (PAINS) which were used to generate a pharmacophore model using D-captopril as a standard inhibitor. (bvsalud.org)

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)
However, it is still not clear how such dimeric opioid receptors are organized and what role they play in signaling. (aspetjournals.org)
Three representative terations in the opioid system have been re- opioid ligands were measured in plasma ported in patients with liver disease. (who.int)

Mutational analysis and chimeric constructs have revealed that allosteric modulators of the calcium-sensing, metabotropic glutamate and GABA B receptors bind to the seven transmembrane domain, through which they modify signal transduction after receptor activation. (aspetjournals.org)

The receptors are ligand inducible transcription factors that exhibit unique biological actions. (umsystem.edu)

Within the striatum, CB1 receptors have been shown to be localized on the same neurons as G i -coupled dopamine D2 receptors. (jneurosci.org)
The two populations also contain different populations of dopamine receptors. (jneurosci.org)
The effects on dopamine (DA) release and dopamine transporter (DAT) gene expression were assayed in hypothalamic HypoE22 cells. (researchgate.net)
Linkage and comparative mapping studies indicate that the transferred chromosome segment contains a number of candidate genes for hypertension, including genes encoding a brain dopamine receptor and a renal epithelial potassium channel. (jci.org)

nuclear receptor. (duke.edu)
The role of nuclear-receptor ligands may, in part, be to recruit such a cofactor complex to the receptor and, in doing so, to enhance transcription of target genes. (novusbio.com)

Her research involves methods as tissue microarray (TMA) of colon cancer patients for immunohistochemistry (IHC) and Western blot, qPCR, transfection, luciferase assay, immunofluorescens on colon cancer cell lines. (lu.se)

The factors that need to be considered include: selection of the most appropriate assay technologies, reading modalities, and experimental models (biochemical, cellular, or animal). (genengnews.com)
Biochemical assays are simpler to execute than their cellular counterparts and offer better consistency. (genengnews.com)
Our discovery biology team in Jiangsu R&D center has accumulated extensive experience in method development and compound screening using biochemical and cell-based phenotypic-functional assays to conduct research services for targets of different classes. (diwou.com)

On the other hand, such techniques are also available to create receptor antagonists in order to prevent further cascades. (wikipedia.org)

Some newer types are called "mix-and-measure" assays because they do not require separation of bound from unbound ligand. (wikipedia.org)
For the agonist-bound A 2A AR, we detected faster (390 ± 80 µs) ligand efficacy-dependent dynamics. (nature.com)

Targeting type-2 cannabinoid receptor (CB2) is considered a feasible strategy to develop new drugs for the treatment of diseases like neuropathic pain, chronic inflammation, neurodegenerative disorders and cancer. (nih.gov)
Pertussis toxin treatment of striatal neurons prevented the inhibition of cAMP accumulation by D2 receptors but unmasked a cannabinoid receptor-mediated stimulatory effect on cAMP accumulation. (jneurosci.org)
The cannabinoid receptor-stimulated accumulation of cAMP was blocked in a concentration-dependent manner by SR141716A, suggesting that the response was regulated through the CB1 receptor. (jneurosci.org)

They often have no effect on their own and therefore act only in conjunction with physiological receptor activation. (aspetjournals.org)

PPARs have a highly conserved DNA binding domain (region C) and a diverse ligand-independent activation domain (region A/B) which can confer constitutive activity on the receptor. (sigmaaldrich.com)

PPARs regulate gene expression by heterodimeric partnering with retinoid X receptors (RXR) and subsequent binding to specific response elements (PPREs) in the promoter regions of target genes. (sigmaaldrich.com)
HER2 overexpression or HER2 gene amplification as determined by an accurate and validated assay (see sections 4.4 and 5.1). (who.int)

A major contribution to laboratory medicine was made when Dr. Wittliff, working with NEN/DuPont, developed the first FDA-approved kits for assessing steroid receptor concentrations in tumor biopsies. (aacc.org)
As compared to passage-matched control cells, SWCNT-transformed BEAS-2B cells exhibited resistance to apoptosis induced by death ligands, e.g., tumor necrosis factor-a and Fas ligand, but not by inducers of mitochondria-mediated apoptosis, e.g., antimycin A and cisplatin, suggesting death receptor pathway as the primary pathway of defective apoptosis in SWCNT-transformed cells. (cdc.gov)
The tumor microenvironment in the context of colon cancer and with a focus on the inflammatory mediators leukotriene D 4 (LTD 4 ) and prostaglandins (PGE 2 ) and their respective receptors. (lu.se)
These mediators and their receptors are enriched in colon cancer cells and colon cancer tissues, which demonstrate there, contribute to tumor development and progression. (lu.se)

Sensitivity of an assay dictates the detection of the target within the dynamic range of the assay with the caveat that the lower limit of detection could vary marginally from batch to batch. (genengnews.com)
Both assay format and detection technology play major roles in sensitivity. (genengnews.com)
The dynamic range of an assay defines both the lower and upper limits of detection. (genengnews.com)

However, an interaction between D2 and CB1 receptors has not been established. (jneurosci.org)
METHODS: Static-binding assays were used to probe the interaction between Angpt-2 and VWF. (imperial.ac.uk)

By eliminating lengthy, time-consuming, and expensive cell culture steps, eXpress assay kits enable you to screen your small molecule or biologic therapeutics and generate accurate, precise, and reproducible functional data in just a few hours. (discoverx.com)

utilized a cell-free immunoprecipitation assay to analyze the neutralizing potential of the mouse monoclonal antibody 3F6 to hinder the BMPR2-ECD ligand-binding activity. (news-medical.net)
Antibody 3F6 reduces BMPR2-ECD ligand-binding activity in a modified immunoprecipitation assay. (news-medical.net)
Neutralizing the ligand-binding activity of BMPR2-ECD using various amounts of 3F6. (news-medical.net)
Results are quantified by ELISA and expressed as mean ± SEM relative to the ligand-binding activity of BMPR2-ECD in the absence of 3F6. (news-medical.net)
A variety of assays have been developed for measure endocrine related activity. (mdpi.com)
End-point analyses, like ELISA, are less informative and rely upon labeling the reactants and adsorbing one of them, which can spoil their native activity, give high non-specific background signals, and limit the scope of an assay. (intechopen.com)
Cannabinoids act at the CB1 receptor to inhibit adenylate cyclase activity via a pertussis toxin-sensitive G-protein. (jneurosci.org)
EphA1 mis-expression did not cause neurodegeneration, shorten lifespan or affect memory but flies mis-expressing the wild-type or mutant receptor were hyper-aroused, had reduced sleep , a stronger circadian rhythm and increased clock neuron activity and excitability. (sdbonline.org)
In addition, transient overexpression of RanBPM in prostate cancer cell lines resulted in enhanced AR activity in a ligand-dependent fashion. (nih.gov)
These data demonstrate that RanBPM interacts with steroid receptors to selectively modify their activity. (nih.gov)

A ligand binding assay (LBA) is an assay, or an analytic procedure, which relies on the binding of ligand molecules to receptors, antibodies or other macromolecules. (wikipedia.org)
This type of analytic test can be used to test for the presence of target molecules in a sample that are known to bind to the receptor. (wikipedia.org)
Wash-based assays can be used to circumvent interference caused by highly complex sample types, as molecules within the matrix that contribute to interference are washed away. (genengnews.com)
Here, we performed smFRET experiments on functionally active human A 2A adenosine receptor (A 2A AR) molecules embedded in freely diffusing lipid nanodiscs to study their intramolecular conformational dynamics. (nature.com)
These three phenomena indicate that receptors are highly dynamic molecules and sample several active and inactive states stochastically (for review, see refs. (nature.com)
This is in contrast to taste-enhancing molecules, which bind to different parts of sweet and umami receptors. (aspetjournals.org)

In turn, receptor signaling is known to drive or regulate GPCR trafficking. (frontiersin.org)

Steroid receptor family members share significant homology at their DNA and ligand-binding domains. (nih.gov)

2MbisP binds to the receptor despite the absence of the 25-hydroxyl group. (rcsb.org)
While estradiol binds both receptors equally, some xenoestrogens have been shown to bind ER beta preferentially. (umsystem.edu)

IDA binding to HAESA allows another receptor protein called SERK1 to bind to HAESA, which results in the release of signals inside the cell that trigger the shedding of organs. (elifesciences.org)

Anatomy17

Organisms9

Chemicals and Drugs99

Analytical, Diagnostic and Therapeutic Techniques and Equipment29

Phenomena and Processes49

Disciplines and Occupations2

Information Science6

Agonists12

Interactions13

Binding protein2

Proteins15

Vitro5

GPCRs5

Affinity12

Pharmacology2

Membrane2

Cellular assays1

PPAR4

Specificity2

Antagonist6

Human epidermal growth f1

Subtypes3

Fluorescence5

Selective7

Protein-coupled5

Superfamily1

Reporter gene1

Pharmacological3

Agonism1

Cell-based assay2

Transactivation1

Mechanism4

Peptide5

Tyrosine kinase3

Kinase2

Characterization1

Androgen receptors1

Radioactive2

Mediate2

Distinct2

Radioligand2

Inhibitors1

Potency3

Induces2

Estrogen receptors2

Glucocorticoid receptor2

Compounds6

Opioid3

Signal transduction1

Biological1

Dopamine4

Nuclear2

Luciferase1

Biochemical3

Antagonists1

Bound2

Cannabinoid3

Physiological1

Constitutive Activity1

Gene2

Tumor4

Detection3

Interaction2

Small molecule1

Activity10

Molecules6

GPCR1

Homology1

Binds2

Bind1