Activating receptors bind ligands. Medical search. Frequent questions

Hyperpolarization-activated cyclic nucleotide-modulated (HCN) channels are tetrameric membrane proteins that generate electrical rhythmicity in specialized neurons and cardiomyocytes. (nature.com)
ABA is a stress hormone perceived by the soluble receptor PYR1 (encoded by Pyrabactin resistance 1 ) and its related PYR1- like and R egulatory C omponent of ABA R ecepto r proteins ( PYL/RCAR , PYLs for simplicity) 18 . (nature.com)
GPRs are cell surface receptors that activate guanine-nucleotide binding proteins upon the binding of a ligand. (nih.gov)
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)
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)
In order for the Notch pathway to be activated, ligand-type proteins from neighbouring cells bind to the Notch receptor. (sciencedaily.com)
Activation may occur when these ligands, such as BMPs or a protein called activin A, attach (bind) to the receptor or to other proteins with which it forms a complex. (medlineplus.gov)
The formation of necrosome, a multiprotein complex that stimulates necroptosis, is tightly regulated by proteins downstream of the receptor and can be the deciding factor in inducing necroptosis. (news-medical.net)
γ-Secretase performs the subsequent cleavage at S3 releasing Notch intracellular domain (NICD) from the membrane and allowing for signal transduction through binding with the CBL-1, Su(H), Lag-1 family of DNA binding proteins. (mskcc.org)
EPCR protein is an N-glycosylated type I membrane protein that enhances the activation of protein C. [3] It belongs to the MHC class I / CD1 family of proteins, that is characterized by having a deep groove, that in other proteins in the family (but not in EPCR) is usually used for antigen binding. (wikidoc.org)
For instance, poxviruses including vaccinia virus encode 2 proteins that interfere with RNaseL and PKR pathways and 2 soluble IFN receptors that interfere with IFN-induced antiviral pathways. (cdc.gov)
Proteins that enhance gene expression when associated with ligand bound activated NUCLEAR RECEPTORS. (bvsalud.org)
Alternatively nuclear receptor coactivators can function as adaptor proteins that bring nuclear receptors into close proximity with transcriptional complexes. (bvsalud.org)
The TNF-alpha binds and results in altered regulation of pro-inflammatory and protective proteins. (medscape.com)

Soluble monomeric ligands bind the receptor but do not induce receptor autophosphorylation and activation (2). (rndsystems.com)

Scholars@Duke publication: Characterizing the peroxisome proliferator-activated receptor (PPARγ) ligand binding potential of several major flame retardants, their metabolites, and chemical mixtures in house dust. (duke.edu)
Many of these contaminants act via the activation of the peroxisome proliferator-activated receptor γ (PPARγ) nuclear receptor.Our goal was to determine the PPARγ ligand binding potency of several major flame retardants, including polybrominated diphenyl ethers (PBDEs), halogenated phenols and bisphenols, and their metabolites. (duke.edu)
Ligand binding activity of indoor dust and its bioactivated extracts were also investigated.We used a commercially available fluorescence polarization ligand binding assay to investigate the binding potency of flame retardants and dust extracts to human PPARγ ligand-binding domain. (duke.edu)
Rosiglitazone was used as a positive control.Most of the tested compounds exhibited dose-dependent binding to PPARγ. (duke.edu)
Mono(2-ethylhexyl) tetrabromophthalate, halogenated bisphenols and phenols, and hydroxylated PBDEs were found to be potent PPARγ ligands. (duke.edu)
A 3-16% increase in PPARγ binding potency was observed following bioactivation of the dust using rat hepatic S9 fractions.Our results suggest that several flame retardants are potential PPARγ ligands and that metabolism may lead to increased binding affinity. (duke.edu)
The PPARγ binding activity of house dust extracts at levels comparable to human exposure warrants further studies into agonistic or antagonistic activities and their potential health effects. (duke.edu)
Peroxisome proliferator-activated receptor alpha (PPAR-α), also known as NR1C1 (nuclear receptor subfamily 1, group C, member 1), is a nuclear receptor protein functioning as a transcription factor that in humans is encoded by the PPARA gene. (wikipedia.org)
Together with peroxisome proliferator-activated receptor delta and peroxisome proliferator-activated receptor gamma, PPAR-alpha is part of the subfamily of peroxisome proliferator-activated receptors. (wikipedia.org)
It was the first member of the PPAR family to be cloned in 1990 by Stephen Green and has been identified as the nuclear receptor for a diverse class of rodent hepatocarcinogens that causes proliferation of peroxisomes. (wikipedia.org)
PPAR-α is primarily activated through ligand binding. (wikipedia.org)
PPAR-alpha is activated under conditions of energy deprivation and is necessary for the process of ketogenesis, a key adaptive response to prolonged fasting. (wikipedia.org)
Activation of PPAR-alpha promotes uptake, utilization, and catabolism of fatty acids by upregulation of genes involved in fatty acid transport, fatty acid binding and activation, and peroxisomal and mitochondrial fatty acid β-oxidation. (wikipedia.org)
which is a Docosanoid derivative of the omega-3 fatty acid DHA was isolated as an endogenous high affinity ligand for PPAR-alpha in the rat and mouse brain. (wikipedia.org)
The 7(S) enantiomer bound with micromolar affity to PPAR alpha with 10 fold higher affinity compared to the (R) enantiomer and could trigger dendritic activation. (wikipedia.org)
We show that the human CYP27 gene is under coupled regulation by retinoids and ligands of PPARs via a PPAR-retinoic acid receptor response element in its promoter. (nih.gov)
Peroxisome proliferator-activated receptor γ (PPARγ) is a major therapeutic target for the treatment of type 2 diabetes. (rcsb.org)
SB1495 occupies the Arm3 region near the Ω loop of the PPARγ ligand-binding domain, whereas its enantiomeric analogue SB1494 binds to the Arm2 region. (rcsb.org)
Peroxisome proliferator-activated receptor-γ (PPARγ) controls adipogenesis and glucose metabolism. (jci.org)
It was reported recently that PPARγ activation by its agonistic ligands modifies lymphocyte function. (jci.org)
In contrast to T cells, which did not exhibit a significant difference, B cells from PPARγ +/- showed an enhanced proliferative response to stimulation by either lipopolysaccharide or cross-linking of antigen receptors. (jci.org)
Peroxisome proliferator-activated receptor-γ (PPARγ) is one of the isotypes of peroxisome proliferator-activated receptors, which are a group of closely related nuclear receptors. (jci.org)
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)
X-ray crystallography of human PPAR isoforms has revealed important residues responsible for ligand binding, heterodimerisation and co-factor interactions. (sigmaaldrich.com)
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)

They found that a molecule that binds toll-like receptors (TLR) doubles the early antibody response to an antigen, and shifts it to a more effective, IgG form. (nationaljewish.org)
dsRNA, ssRNA, and CpG oligonucleotides are ligands for toll-like receptors (TLRs) and modulate antiviral immunity through TLR signaling pathways and IFN induction ( 2 ). (cdc.gov)
Rationale: Pattern recognition receptors such as membrane bound Toll-Like Receptors (TLRs) and cytoplasmic Nod-like receptors (NLRs) of surface epithelial cells and antigen presenting cells detect airborne pathogens and activate innate immune response providing the first line of defense against these inflammatory agents. (cdc.gov)

Peroxisome proliferator-activated receptor gamma (PPARgamma) and liver X receptor alpha (LXRalpha) have been linked to the regulation of these processes. (nih.gov)

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 channels are primarily activated by voltage but are receptors as well, binding the intracellular ligand cyclic AMP. (nature.com)
We report here that SMN deficiency, induced in the astroglioma cell line U87MG after lentiviral transduction with a shSMN construct, was associated with an increase in the expression of the main components of Notch signaling pathway, namely its ligands, Jagged1 and Delta1, the Notch receptor and its active intracellular form (NICD). (mdpi.com)
When the ligand and receptor come into contact, the Notch receptor is processed and the intracellular part moves to the nucleus to activate gene expression. (sciencedaily.com)
We sought to extend the receptor-desensitization paradigm for use with a cultured cell system, in which an intracellular calcium signal rather than a contractile response might be used as an index of receptor activation. (aspetjournals.org)
The membrane-bound Notch segment that results from this cleavage, known as Notch Intracellular Truncation domain (NEXT), is a γ-secretase substrate. (mskcc.org)
Intracellular events, such as blocking of microbial attachment factors such as fimbriae (hairlike structures) and other adhesins (putative receptors), have been observed (Naidu and Bidlack, 1998). (ift.org)
Physiologic functions (eg, contraction, secretion) are usually regulated by multiple receptor-mediated mechanisms, and several steps (eg, receptor-coupling, multiple intracellular 2nd messenger substances) may be interposed between the initial molecular drug-receptor interaction and ultimate tissue or organ response. (msdmanuals.com)
Ability to bind to a receptor is influenced by external factors as well as by intracellular regulatory mechanisms. (msdmanuals.com)
Transient transfection of intracellular Notch1 (Notch1-IC) into a pre-B cell line resulted in the down-regulation of EBF-regulated promoters and diminished the capacity of EBF to activate these promoters in an epithelial cell line. (lu.se)

Results: Serum-free conditions greatly enhanced sensitivity without reducing specificity in ligand binding assays. (nist.gov)
Likewise, antigen/antibody complexes are bound by the FcR of APCs and processed in a unique fashion dependent on the epitope specificity of the bound antibody. (hindawi.com)
Furthermore, we used this assay to develop a PAR 1 receptor-activating probe [Ala-parafluoroPhe-Arg-Cha-Cit-Tyr-NH 2 (Cit-NH 2 )], which displays a high degree of specificity for PAR 1 over PAR 2 , and we used the assay to quantitate the ability of trypsin to disarm the activation of PAR 1 by thrombin. (aspetjournals.org)
Although these receptors are structurally similar, they determine specificity for four ligands-GDNF, Neurturin (NRTN), Artemin (ARTN) and Persephin (PSPN). (medsci.org)
Our findings also demonstrate that MmoR functions as a trigger for sMMO expression due to the high specificity and selectivity for enhancer-binding sequences. (bvsalud.org)

nuclear receptor. (duke.edu)
Our findings suggest that nuclear receptor-regulated CYP27 expression is likely to be a key integrator of retinoic acid receptor-PPARgamma-LXR signaling, relying on natural ligands and contributing to lipid metabolism in macrophages. (nih.gov)
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)
The effect of pyrroloquinoline quinine (PQQ) on receptor activator of nuclear factor-κB ligand (RANKL)-induced osteoclast formation was examined using RAW 264.7 macrophage-like cells. (nih.gov)
PQQ inhibited the activation of nuclear factor of activated T cells (NFATc1), a key transcription factor of osteoclastogenesis, in RANKL-stimulated cells. (nih.gov)
The estrogen receptor is a nuclear receptor that is activated upon ligand binding and subsequently translocates to the nuclear. (wikipathways.org)
Pathways for ligand activated nuclear receptors to unravel the genomic responses induced by hepatotoxicants. (wikipathways.org)

When GFLs bind with GFRα, they form complexes and associate with the RET receptor, subsequently activating downstream signaling. (medsci.org)
IFN-α and IFN-γ work by binding their receptors and activating downstream antiviral pathways involving the dsRNA-dependent protein kinase (PKR), the 2´, 5´ oligoadenylate synthetase/RNase L, or the MxA protein. (cdc.gov)
Pathogen-associated molecular patterns, such as lipopolysaccharide (LPS) in bacterial cell walls and bacterial flagella, acts as ligands to trigger for downstream pathways that release inflammatory mediators such as TNF-alpha and interleukins (IL1B, IL2, IL6 and IL18). (cdc.gov)

For the binding affinity of the second, third and fourth ligand, our results suggest pronounced cooperativity in the sequence positive, negative and positive, respectively. (nature.com)
Its ability to bind two Fe +3 ions with high affinity, in cooperation with two HCO 3 - ions, contributes to its major structure-functional properties, including antimicrobial activity. (ift.org)
Scatchard analysis revealed loss of receptor number without changes in receptor affinity. (diabetesjournals.org)
A drug's ability to affect a given receptor is related to the drug's affinity (probability of the drug occupying a receptor at any given instant) and intrinsic efficacy (intrinsic activity-degree to which a ligand activates receptors and leads to cellular response). (msdmanuals.com)
Drugs, aging, genetic mutations, and disorders can increase (upregulate) or decrease (downregulate) the number and binding affinity of receptors. (msdmanuals.com)
The binding affinity and selectivity are lower (Kd = 184.6 ± 6.2 nM) than those of MmoR. (bvsalud.org)
MmoR interacts with the upstream activator sequence (UAS) with a strong binding affinity (Kd = 12.5 ± 0.5 nM). (bvsalud.org)
however, its binding affinity to UAS decreases in a low-copper-containing medium. (bvsalud.org)

Autoantibodies can bind to basic structural molecules and interfere with the synthesis of structural elements and facilitate the uptake of antigen. (hindawi.com)
Left panel: antigen bound by antibody is taken up via FcR on APCs such as dendritic cells or macrophages. (hindawi.com)
Right panel: antigen binds to the BCR of antigen-specific B cells and is internalized. (hindawi.com)
So the researchers decided to inject mice with the synthetic antigen plus a molecule that binds an innate receptor, known as TLR ligand. (nationaljewish.org)

However, evidence is now accumulating for rapid corticosteroid actions 25 , 26 , and the existence of membrane-bound steroid receptors that may mediate these rapid actions 27 , 28 . (ersjournals.com)
Only membrane-bound or Fc‑clustered ligands are capable of activating the receptor in vitro . (rndsystems.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)

Our data illustrate the usefulness of the HEK cell assay for evaluating the PAR 1 /PAR 2 selectivity of PAR-activating agonists. (aspetjournals.org)

GPR75 is a member of the G protein-coupled receptor family. (nih.gov)
G Protein-Coupled Receptor 75 (GPR75) As a Novel Molecule for Targeted Therapy of Cancer and Metabolic Syndrome. (nih.gov)
20-HETE Signals Through G-Protein-Coupled Receptor GPR75 (G(q)) to Affect Vascular Function and Trigger Hypertension. (nih.gov)
Cloning and characterization of a novel orphan G-protein-coupled receptor localized to human chromosome 2p16. (nih.gov)
Dr. Marchese has had a long-standing interest in understanding the molecular mechanisms governing G protein-coupled receptor signaling. (mcw.edu)
Research in the Marchese lab is directed towards understanding the molecular mechanisms governing G protein-coupled receptor (GPCR) signaling. (mcw.edu)
Follicle-stimulating hormone receptor (FSHR) is a G protein-coupled receptor (GPCR) with pivotal roles in reproduction. (frontiersin.org)

Endogenous ligands include fatty acids such as arachidonic acid as well as other polyunsaturated fatty acids and various fatty acid-derived compounds such as certain members of the 15-hydroxyeicosatetraenoic acid family of arachidonic acid metabolites, e.g. 15(S)-HETE, 15(R)-HETE, and 15(S)-HpETE and 13-hydroxyoctadecadienoic acid, a linoleic acid metabolite. (wikipedia.org)
It remains to be identified how activation of these receptors is connected and regulated by endogenous lipid molecules. (nih.gov)
Each receptor shows a differential pattern of tissue expression and is activated by structurally diverse compounds including endogenous long-chain fatty acids. (sigmaaldrich.com)
Ligand-induced stimulation of endogenous Notch receptors with Delta4 mimicked the activity of Notch1-IC toward EBF. (lu.se)

Deposited immune complexes can activate complement and effector cells. (hindawi.com)
The Fc portion of antibodies in immune complexes can be bound by C1q of the classical complement pathway, which eventually leads to the release of C5a and C3a. (hindawi.com)
This thesis work aims to replace Ru polipyridyl complexes by Fe carbene complexes, that by clever ligand design have approached suitable photosensitiser properties. (lu.se)
For the Fe(II) carbene complexes investigated, small changes in the ligand structure influenced both what excited state (charge-transfer or metal-centred) that was mainly populated and the lifetime of the state. (lu.se)
For the Fe(III) carbene complexes investigated, there was instead one dominating charge-transfer excited state that was rather unaffected by changes to the ligand. (lu.se)
In one study of a large set of protein-ligand complexes, we tried to improve the free energies of binding by using MD simulations with QM-derived charges, which sometimes led to improved results, but not always. (lu.se)

Activation of kinase activity occurs after ligand recognition and binding. (rndsystems.com)
CD140b is a cell surface tyrosine kinase receptor for members of the platelet-derived growth factor family. (biolegend.com)
Ligand binding activates the receptor kinase through a process of oligomerization and transphosphorylation. (thermofisher.com)
CSF1R is a tyrosine kinase transmembrane receptor and member of the CSF1/PDGF receptor family of tyrosine-protein kinases. (thermofisher.com)
Mutations in the gene encoding CSF1R have been associated with a predisposition to myeloid malignancy.Tyrosine-protein kinase that acts as cell-surface receptor for CSF1 and IL34 and plays an essential role in the regulation of survival, proliferation and differentiation of hematopoietic precursor cells, especially mononuclear phagocytes, such as macrophages and monocytes. (thermofisher.com)
It is a receptor tyrosine kinase involved in the development and the maturation of the central and the peripheral nervous systems through regulation of neuron survival, proliferation, migration, differentiation, and synapse formation and plasticity. (tcdb.org)
PQQ augmented the expression of type I interferon receptor (IFNAR) and enhanced the IFN-β-mediated janus kinase (JAK1) and signal transducer and activator of transcription (STAT1) expression. (nih.gov)
Artemin, a neuronal survival factor in the glial cell line-derived neurotrophic factor family, binds the glycosylphosphatidylinositol-anchored protein GFRα3 and the receptor tyrosine kinase Ret. (jneurosci.org)
GDNF family ligands (GFLs) activate the Ret receptor tyrosine kinase through binding of glycosylphosphatidylinositol-anchored GDNF family receptor α coreceptors (GFRα1-4) ( Sariola and Saarma, 2003 ). (jneurosci.org)
The GDNF family ligands (GFLs) function through a glycosyl-phosphatidylinositol-(GPI) anchored coreceptor, GDNF family receptor alpha (GFRα), and rearranged during transfection (RET), a well-known receptor tyrosine kinase involved in kidney development, spermatogonial stem cell maintenance, and the development and maintenance of the sympathetic, parasympathetic, and enteric nervous systems [ 1 , 2 ]. (medsci.org)
We also ran QM/MM simulations on casein-kinase 2 (CK2), where the ligand and a few surrounding residues were treated at the QM level, and the rest of the system at the MM level. (lu.se)

The PDGFRβ is heavily phosphorylated on numerous tyrosine residues through both autophosphorylation and ligand-dependent processes. (biolegend.com)

This is the basic and "extremely simple activation system" of the Notch signalling pathway, which is based on short distance contact between cells through a ligand and a receptor. (sciencedaily.com)
In a developing wing and through a technique called Clonal Analysis, the researchers manipulated groups of cells, among groups of normal cells, to remove Notch receptor expression. (sciencedaily.com)
As expected, the cells lacking Notch did not activate the pathway, but what was surprising was the observation that neighbouring cells did. (sciencedaily.com)
Indeed, the analyses demonstrated that the Notch receptor sequesters the ligands and prevents these from connecting to the Notch receptors of adjoining cells. (sciencedaily.com)
The experiments showed that the absence of the receptor in the mutated cells leaves many ligands free, ready to enter into contact with Notch receptors of the non-manipulated cells. (sciencedaily.com)
It is strange, but in the cell emitting the signal, Notch receptor captures the ligands by acting as a silencer while in the cell receiving the signal the binding of ligands with Notch allows activation of the pathway. (sciencedaily.com)
In other words, Notch is a kind of double agent and exerts opposing functions: repressing or activating the pathway depending on whether it is located in cells emitting or receiving the signal. (sciencedaily.com)
They speculate that it does because the ligand-receptor system of Notch activation has been conserved in all organisms. (sciencedaily.com)
The cells destined to become lymphocytes receive the appropriate signalling through Notch receptors. (sciencedaily.com)
In more than half T-ALL patients the Notch receptor is permanently activated in the T-cell precursors. (sciencedaily.com)
Mature Notch receptors are activated by binding to ligands (Jagged-1, -2 and Delta-like -1, -3, and -4) located on adjacent signal-presenting cells. (mskcc.org)

Secreted autoantibodies specific to receptors or receptor ligands can activate or inhibit receptor functions. (hindawi.com)
Another protein called FKBP12 can turn off (inhibit) ACVR1 by binding to the receptor and preventing inappropriate (leaky) activation in the absence of ligands. (medlineplus.gov)
On the other hand, PQQ did not inhibit the signaling pathway from RANK/RANKL binding to NFATc1 activation, including NF-κB and mitogen-activated protein kinases (MAPKs). (nih.gov)

Synthetic ligands include the fibrate drugs, which are used to treat hyperlipidemia, and a diverse set of insecticides, herbicides, plasticizers, and organic solvents collectively referred to as peroxisome proliferators. (wikipedia.org)
Our new modules enable ligand-programmable multi-channel CID systems for plant and eukaryotic synthetic biology that can empower new plant-based and microbe-based sensing modalities. (nature.com)
Starting with the Escherichia coli lac operon in the 1970s, many synthetic ligand-regulated circuits have been built by rewiring natural systems for new functions 1 . (nature.com)

However, CD56 dim NK cells can produce cytokines, specifically IFN-γ, after cell triggering via NKp46 of NKp30 activating receptors or after stimulation with combinations of IL-2, IL-12, and IL-15 ( 7 ). (frontiersin.org)
The transferred B1-receptors induced calcium influx after B1-receptor agonist stimulation: a response abrogated by a specific B1-receptor antagonist. (lu.se)
Microvesicles derived from neutrophils also transferred B1-receptors to wild-type human embryonic kidney cells and induced calcium influx after stimulation. (lu.se)

Chromosomal translocations involving chromosome bands 5q31-33 that contain the gene encoding the platelet-derived growth factor beta receptor (PDGFRB) are associated with a significant minority of patients with BCR/ABL1-negative chronic myeloid neoplasms. (atlasgeneticsoncology.org)
The 18A2 monclonal antibody recognizes human CD140b also known as the platelet-derived growth factor receptor, beta polypeptide, PDGFR1, and PDGFRß. (biolegend.com)

Electrostatic and hydrophobic interactions between the peptide and the LBD stabilize the active receptor conformation. (rcsb.org)

They function as transcription factors activated by ligands, regulating gene expression in deoxyribonucleic acid (DNA) specific response elements. (researchandmarkets.com)

The researchers found that the TLR ligand spurred other cells to release type I interferon. (nationaljewish.org)

A water molecule is observed between His 301 and His 393 in this structure, and it preserves the orientation of the histidines in the binding site. (rcsb.org)
Description: The AFS98 monoclonal antibody reacts with the mouse CD115 molecule, a receptor for macrophage colony stimulating factor (M-CSF) or colony stimulating factor-1 (CSF-1). (thermofisher.com)

The lifetime of the drug-receptor complex is affected by dynamic processes (conformation changes) that control the rate of drug association and dissociation from the target. (msdmanuals.com)

The inflammatory process in asthma involves the increased expression of various pro-inflammatory chemokines, cytokines, growth factors, lipid mediators, adhesion molecules, enzymes, and receptors for the same inflammatory mediators 21 . (ersjournals.com)
The ACVR1 protein is normally turned on (activated) at appropriate times by molecules called ligands. (medlineplus.gov)
Binding of B-chain containing PDGF molecules can stimulate cell proliferation. (biolegend.com)
an intact cell wall would almost always also contain other molecules that activate the innate immune response as well. (nationaljewish.org)
Ligands for CD11a/CD18 are intercellular adhesion molecules (ICAMs), ligands for CD11b/CD18 are complement C3bi and ICAMs, and ligands for CD11c/CD18 are C3bi and ICAMs. (medscape.com)

Membrane trafficking of G protein-coupled receptors (GPCRs) tightly orchestrates the signaling from this superfamily of signaling receptors. (frontiersin.org)

These compounds act on target cells by binding to estrogen receptors, ERα and/or ERβ. (researchandmarkets.com)
Estrogen receptors: therapies targeted to receptor subtypes. (wikipathways.org)

Endothelial protein C receptor (EPCR) also known as activated protein C receptor (APC receptor) is a protein that in humans is encoded by the PROCR gene . (wikidoc.org)

There are two classes of receptors, designated A and B. Both the A and B class receptors have an extracellular region consisting of a globular domain, a cysteine-rich domain, and two fibronectin type III domains. (rndsystems.com)
Robust activation of wound-induced transcription from ple and Ddc requires Toll pathway components ranging from the extracellular ligand Spatzle to the Dif transcription factor. (sdbonline.org)

The PAR 1 -selective agonist that we developed using the assay should prove useful for studying the effects of selectively activating PAR 1 in vivo. (aspetjournals.org)
In vivo , the ligands and receptors display reciprocal expression (3). (rndsystems.com)

Found in the cell membrane, this protein activates a signalling pathway that regulates the expression of genes that make the cell divide, grow, migrate, specialise or die. (sciencedaily.com)
We found that most of the previously described PAR 1 -targeted agents can also activate/desensitize PAR 2 , and most of these peptides can also activate a calcium signaling pathway in a target cell that possesses PAR 2 along with PAR 1 . (aspetjournals.org)
After binding its hormone FSH, FSHR undergoes internalization to very early endosomes (VEEs) for its acute signaling and sorting to a rapid recycling pathway. (frontiersin.org)
A recent study has identified the molecular pathway that, when activated, prompts hair growth from dormant hair follicles and, when blocked, prevents the growth of unwanted hair. (medicaldaily.com)
Genetic epistasis and biochemical analyses revealed that Senju regulates the Toll signaling pathway at a step that converts Toll ligand Spatzle to its active form. (sdbonline.org)
Furthermore, the Spätzle (Spz) family ligands for the Toll receptor are transcriptionally upregulated by activated JNK signalling in a non-cell-autonomous manner, providing a molecular mechanism for JNK-induced Toll pathway activation. (sdbonline.org)
Protein C is an anti-coagulant serine protease activated by the blood coagulation pathway. (wikidoc.org)

Here we analyze the complex activation mechanism of homotetrameric HCN2 channels by confocal patch-clamp fluorometry and kinetically quantify all ligand binding steps and closed-open isomerizations of the intermediate states. (nature.com)
Banks, M.I., Pearce, R.A. & Smith, P.H. Hyperpolarization-activated cation current ( I h) in neurons of the medical nucleus of the trapezoid body: voltage-clamp analysis and enhancement by norepinephrine and cAMP suggest a modulatory mechanism in the auditory brain system. (nature.com)
Thus, we found a novel mechanism by which microvesicles transfer functional receptors and promote kinin-associated inflammation. (lu.se)
Previous studies have proposed transcriptional regulation of MMOs, including sMMO and pMMO, while we provide further evidence to elucidate its mechanism using a purified enhancer-binding protein (MmoR) and transcription factor (σ54). (bvsalud.org)

In contrast, thrombin receptor-activating peptides derived from the human PAR 1 receptor sequence (e.g. (aspetjournals.org)
1. Is electrophilic or can be metabolical y activated to electrophiles does not alter the linear sequence of nucleotides (or bases) in the DNA, 2. (who.int)

However, insulin-induced downregulation of insulin receptors was: (1) demonstrable in receptor-positive cells, (2) dependent on insulin concentration, (3) temporally unrelated to insulin internalization, and (4) prevented by culture at 4°C but not by cycloheximide at 37°C. Recovery of insulin receptors required further culture of cells in media depleted of insulin for 24 h. (diabetesjournals.org)

a) This data is compiled from multiple literature and from different human assays - binding assays and transactivation assays. (sigmaaldrich.com)
Binding assays indicated that these interactions are blocked by the copper ion. (bvsalud.org)

There, it activates transcription of target genes involved in essential cellular processes. (wikipathways.org)

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)
Here, we review tumor-NK cell interactions, discuss the mechanisms by which NK cells generate an antitumor immune response, and discuss NK cell-based therapeutic strategies targeting activating, inhibitory, and co-stimulatory receptors. (frontiersin.org)
We mostly used molecular mechanics (MM) in order to model the protein-ligand interactions, which is more approximate than quantum-mechanical (QM) methods, but necessary to reduce the computational cost when doing calculations on protein-ligand systems, which often contain tens of thousand of atoms. (lu.se)

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)
The protein is also involved in Plasmodium falciparum malaria as subtypes of the Plasmodium falciparum erythrocyte membrane protein 1 (PfEMP1) family use EPCR of the host as a receptor. (wikidoc.org)
Each ligand may interact with multiple receptor subtypes. (msdmanuals.com)

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)
binding and activation in extracts from environmentally relevant dust samples was also investigated. (duke.edu)
This complex interaction of the subunits leads to a preferential stabilization of states with zero, two or four ligands and suggests a dimeric organization of the activation process: within the dimers the cooperativity is positive, whereas it is negative between the dimers. (nature.com)
Figure 3: Fit of ligand binding and activation by a Markovian state model. (nature.com)
Binding of the Fc portion of the antibodies to FcR leads to activation of effector cells and further release of proinflammatory cytokines and proteolytic enzymes, mediators of antibody-dependent cell-mediated cytotoxicity (ADCC). (hindawi.com)
Upon activation and cleavage of C3, C3b is formed as a major fragment that covalently binds to its target (see Table 1). (medscape.com)
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)
We developed a calcium signaling-based assay, using cultured human embryonic kidney cells (HEK), that evaluates simultaneously, the activation/desensitization or blockade of the proteinase-activated receptors, PAR 1 and PAR 2 . (aspetjournals.org)
NK cell activation and the triggering of effector functions is governed by a complex set of activating and inhibitory receptors. (frontiersin.org)
The protein encoded by this gene is a receptor for protein C that enhances its activation. (wikidoc.org)
During vasculitis, activation of the kinin system induces inflammation, whereby the kinin B1-receptor is expressed and activated after ligand binding. (lu.se)
After activation C3b can bind covalently, via its reactive thiolester, to cell surface carbohydrates or immune aggregates. (lu.se)

However, our lab has uncovered a new non-transcriptional role of HIF-1α interacting with and activating γ-secretase. (mskcc.org)

Importantly, renal biopsies from two patients with vasculitis showed leukocyte-derived microvesicles bearing B1-receptors docking on glomerular endothelial cells. (lu.se)
Microvesicles derived from B1-receptor-transfected human embryonic kidney cells transferred B1-receptors to wild-type human embryonic kidney cells, lacking the receptor, and to glomerular endothelial cells. (lu.se)

Expression of the GFRα3 receptor is primarily restricted to the peripheral nervous system and is found in a subpopulation of nociceptive sensory neurons of the dorsal root ganglia (DRGs) that coexpress the Ret and TrkA receptor tyrosine kinases and the thermosensitive channel TRPV1. (jneurosci.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)

Li Q, Cao Z, Zhao S. The Emerging Portrait of Glial Cell Line-derived Neurotrophic Factor Family Receptor Alpha (GFRα) in Cancers. (medsci.org)
Glial cell line-derived neurotrophic factor family receptor alpha (GFRα) members have been widely connected to the mechanisms contributing to cell growth, differentiation, cell migration and tissue maturation. (medsci.org)

This system is unique because of the relative ease with which ligand recognition can be reprogrammed. (nature.com)
In the auxin and jasmonic acid systems, ligand recognition is shared between protein-binding partners. (nature.com)

Moreover they induce the upregulation of activating FcR on effector cells. (hindawi.com)

BMP receptors span 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)

Gauss, R., Seifert, R. & Kaupp, U.B. Molecular identification of a hyperpolarization-activated channel in sea urchin sperm. (nature.com)
Molecular and functional heterogeneity of hyperpolarization-activated pacemaker channels in the mouse CNS. (nature.com)
Overview of Pharmacodynamics Pharmacodynamics (sometimes described as what a drug does to the body) is the study of the biochemical, physiologic, and molecular effects of drugs on the body and involves receptor binding. (msdmanuals.com)

In combination with other cellular changes, abnormal ACVR1 receptor activity can make cells grow and divide uncontrollably, leading to cancer. (medlineplus.gov)
This receptor is found in moderate levels on some normal cells and as the gene's name implies, it is involved in cellular responses to growth factors. (cancerquest.org)
Activated receptors directly or indirectly regulate cellular biochemical processes (eg, ion conductance, protein phosphorylation, DNA transcription, enzymatic activity). (msdmanuals.com)
selectivity relates largely to physicochemical binding of the drug to cellular receptors. (msdmanuals.com)

Early antibody levels doubled when the TLR ligand was added. (nationaljewish.org)

Anatomy22

Organisms12

Chemicals and Drugs111

Analytical, Diagnostic and Therapeutic Techniques and Equipment38

Phenomena and Processes71

Disciplines and Occupations2

Information Science6

Health Care1

Proteins15

Monomeric ligands bind the receptor1

PPAR27

Toll-like rece3

Peroxisome Proli1

Soluble1

Intracellular9

Specificity5

Nuclear7

Downstream3

Affinity8

Antigen4

Membrane-bound2

Retinoid X Recepto1

Agonists1

Protein-Coupled Receptor7

Endogenous4

Complexes6

Kinase11

Autophosphorylation1

Notch11

Inhibit3

Synthetic3

Stimulation3

Platelet-derive2

Peptide1

Gene expression1

Type I interferon1

Molecule2

Conformation1

Molecules5

Superfamily1

Estrogen2

Humans1

Extracellular2

Vivo2

Pathway7

Mechanism4

Sequence2

Downregulation1

Assays2

Transcription of target genes1

Interactions3

Subtypes3

Activation12

Transcriptional1

Endothelial cells2

Primarily1

Allosteric1

Family receptor2

Recognition2

Upregulation1

Cell membrane1

Molecular3

Cellular4

Antibody1