Mitogen-Activated Protein Kinase 10: A c-jun amino-terminal kinase that is found predominantly within NEURONS of the BRAIN, suggesting a role in stress-induced neuronal APOPTOSIS. Several isoforms of the protein with molecular sizes of 47 kDa and 52 kDa exist due to multiple ALTERNATIVE SPLICING.Arrestin: A 48-Kd protein of the outer segment of the retinal rods and a component of the phototransduction cascade. Arrestin quenches G-protein activation by binding to phosphorylated photolyzed rhodopsin. Arrestin causes experimental autoimmune uveitis when injected into laboratory animals.Arrestins: Regulatory proteins that down-regulate phosphorylated G-protein membrane receptors, including rod and cone photoreceptors and adrenergic receptors.Interleukin-1beta: An interleukin-1 subtype that is synthesized as an inactive membrane-bound pro-protein. Proteolytic processing of the precursor form by CASPASE 1 results in release of the active form of interleukin-1beta from the membrane.beta 2-Microglobulin: An 11-kDa protein associated with the outer membrane of many cells including lymphocytes. It is the small subunit of the MHC class I molecule. Association with beta 2-microglobulin is generally required for the transport of class I heavy chains from the endoplasmic reticulum to the cell surface. Beta 2-microglobulin is present in small amounts in serum, csf, and urine of normal people, and to a much greater degree in the urine and plasma of patients with tubular proteinemia, renal failure, or kidney transplants.Receptors, Adrenergic, beta: One of two major pharmacologically defined classes of adrenergic receptors. The beta adrenergic receptors play an important role in regulating CARDIAC MUSCLE contraction, SMOOTH MUSCLE relaxation, and GLYCOGENOLYSIS.Integrin beta3: An integrin beta subunit of approximately 85-kDa in size which has been found in INTEGRIN ALPHAIIB-containing and INTEGRIN ALPHAV-containing heterodimers. Integrin beta3 occurs as three alternatively spliced isoforms, designated beta3A-C.Receptors, Adrenergic, beta-2: A subclass of beta-adrenergic receptors (RECEPTORS, ADRENERGIC, BETA). The adrenergic beta-2 receptors are more sensitive to EPINEPHRINE than to NOREPINEPHRINE and have a high affinity for the agonist TERBUTALINE. They are widespread, with clinically important roles in SKELETAL MUSCLE; LIVER; and vascular, bronchial, gastrointestinal, and genitourinary SMOOTH MUSCLE.G-Protein-Coupled Receptor Kinase 1: A PROTEIN-SERINE-THREONINE KINASE that is found in PHOTORECEPTOR CELLS. It mediates light-dependent PHOSPHORYLATION of RHODOPSIN and plays an important role in PHOTOTRANSDUCTION.Eye ProteinsTransforming Growth Factor beta: A factor synthesized in a wide variety of tissues. It acts synergistically with TGF-alpha in inducing phenotypic transformation and can also act as a negative autocrine growth factor. TGF-beta has a potential role in embryonal development, cellular differentiation, hormone secretion, and immune function. TGF-beta is found mostly as homodimer forms of separate gene products TGF-beta1, TGF-beta2 or TGF-beta3. Heterodimers composed of TGF-beta1 and 2 (TGF-beta1.2) or of TGF-beta2 and 3 (TGF-beta2.3) have been isolated. The TGF-beta proteins are synthesized as precursor proteins.Transducin: A heterotrimeric GTP-binding protein that mediates the light activation signal from photolyzed rhodopsin to cyclic GMP phosphodiesterase and is pivotal in the visual excitation process. Activation of rhodopsin on the outer membrane of rod and cone cells causes GTP to bind to transducin followed by dissociation of the alpha subunit-GTP complex from the beta/gamma subunits of transducin. The alpha subunit-GTP complex activates the cyclic GMP phosphodiesterase which catalyzes the hydrolysis of cyclic GMP to 5'-GMP. This leads to closure of the sodium and calcium channels and therefore hyperpolarization of the rod cells. EC 3.6.1.-.Integrin alpha5beta1: An integrin found in FIBROBLASTS; PLATELETS; MONOCYTES, and LYMPHOCYTES. Integrin alpha5beta1 is the classical receptor for FIBRONECTIN, but it also functions as a receptor for LAMININ and several other EXTRACELLULAR MATRIX PROTEINS.Integrin beta4: Also known as CD104 antigen, this protein is distinguished from other beta integrins by its relatively long cytoplasmic domain (approximately 1000 amino acids vs. approximately 50). Five alternatively spliced isoforms have been described.Cattle: Domesticated bovine animals of the genus Bos, usually kept on a farm or ranch and used for the production of meat or dairy products or for heavy labor.Integrin alpha6beta4: This intrgrin is a key component of HEMIDESMOSOMES and is required for their formation and maintenance in epithelial cells. Integrin alpha6beta4 is also found on thymocytes, fibroblasts, and Schwann cells, where it functions as a laminin receptor (RECEPTORS, LAMININ) and is involved in wound healing, cell migration, and tumor invasiveness.Rod Cell Outer Segment: The portion of a retinal rod cell situated between the ROD INNER SEGMENT and the RETINAL PIGMENT EPITHELIUM. It contains a stack of photosensitive disk membranes laden with RHODOPSIN.Integrin beta Chains: Integrin beta chains combine with integrin alpha chains to form heterodimeric cell surface receptors. Integrins have traditionally been classified into functional groups based on the identity of one of three beta chains present in the heterodimer. The beta chain is necessary and sufficient for integrin-dependent signaling. Its short cytoplasmic tail contains sequences critical for inside-out signaling.beta 2-Glycoprotein I: A 44-kDa highly glycosylated plasma protein that binds phospholipids including CARDIOLIPIN; APOLIPOPROTEIN E RECEPTOR; membrane phospholipids, and other anionic phospholipid-containing moieties. It plays a role in coagulation and apoptotic processes. Formerly known as apolipoprotein H, it is an autoantigen in patients with ANTIPHOSPHOLIPID ANTIBODIES.Phosphorylation: The introduction of a phosphoryl group into a compound through the formation of an ester bond between the compound and a phosphorus moiety.Integrin alpha4beta1: Integrin alpha4beta1 is a FIBRONECTIN and VCAM-1 receptor present on LYMPHOCYTES; MONOCYTES; EOSINOPHILS; NK CELLS and thymocytes. It is involved in both cell-cell and cell- EXTRACELLULAR MATRIX adhesion and plays a role in INFLAMMATION, hematopoietic cell homing and immune function, and has been implicated in skeletal MYOGENESIS; NEURAL CREST migration and proliferation, lymphocyte maturation and morphogenesis of the PLACENTA and HEART.Cell Line: Established cell cultures that have the potential to propagate indefinitely.Integrin alpha2beta1: An integrin found on fibroblasts, platelets, endothelial and epithelial cells, and lymphocytes where it functions as a receptor for COLLAGEN and LAMININ. Although originally referred to as the collagen receptor, it is one of several receptors for collagen. Ligand binding to integrin alpha2beta1 triggers a cascade of intracellular signaling, including activation of p38 MAP kinase.Signal Transduction: The intracellular transfer of information (biological activation/inhibition) through a signal pathway. In each signal transduction system, an activation/inhibition signal from a biologically active molecule (hormone, neurotransmitter) is mediated via the coupling of a receptor/enzyme to a second messenger system or to an ion channel. Signal transduction plays an important role in activating cellular functions, cell differentiation, and cell proliferation. Examples of signal transduction systems are the GAMMA-AMINOBUTYRIC ACID-postsynaptic receptor-calcium ion channel system, the receptor-mediated T-cell activation pathway, and the receptor-mediated activation of phospholipases. Those coupled to membrane depolarization or intracellular release of calcium include the receptor-mediated activation of cytotoxic functions in granulocytes and the synaptic potentiation of protein kinase activation. Some signal transduction pathways may be part of larger signal transduction pathways; for example, protein kinase activation is part of the platelet activation signal pathway.Antigens: Substances that are recognized by the immune system and induce an immune reaction.Molecular Sequence Data: Descriptions of specific amino acid, carbohydrate, or nucleotide sequences which have appeared in the published literature and/or are deposited in and maintained by databanks such as GENBANK, European Molecular Biology Laboratory (EMBL), National Biomedical Research Foundation (NBRF), or other sequence repositories.Light: That portion of the electromagnetic spectrum in the visible, ultraviolet, and infrared range.Cells, Cultured: Cells propagated in vitro in special media conducive to their growth. Cultured cells are used to study developmental, morphologic, metabolic, physiologic, and genetic processes, among others.Integrins: A family of transmembrane glycoproteins (MEMBRANE GLYCOPROTEINS) consisting of noncovalent heterodimers. They interact with a wide variety of ligands including EXTRACELLULAR MATRIX PROTEINS; COMPLEMENT, and other cells, while their intracellular domains interact with the CYTOSKELETON. The integrins consist of at least three identified families: the cytoadhesin receptors(RECEPTORS, CYTOADHESIN), the leukocyte adhesion receptors (RECEPTORS, LEUKOCYTE ADHESION), and the VERY LATE ANTIGEN RECEPTORS. Each family contains a common beta-subunit (INTEGRIN BETA CHAINS) combined with one or more distinct alpha-subunits (INTEGRIN ALPHA CHAINS). These receptors participate in cell-matrix and cell-cell adhesion in many physiologically important processes, including embryological development; HEMOSTASIS; THROMBOSIS; WOUND HEALING; immune and nonimmune defense mechanisms; and oncogenic transformation.Interleukin-1: A soluble factor produced by MONOCYTES; MACROPHAGES, and other cells which activates T-lymphocytes and potentiates their response to mitogens or antigens. Interleukin-1 is a general term refers to either of the two distinct proteins, INTERLEUKIN-1ALPHA and INTERLEUKIN-1BETA. The biological effects of IL-1 include the ability to replace macrophage requirements for T-cell activation.Antigens, CD29: Integrin beta-1 chains which are expressed as heterodimers that are noncovalently associated with specific alpha-chains of the CD49 family (CD49a-f). CD29 is expressed on resting and activated leukocytes and is a marker for all of the very late activation antigens on cells. (from: Barclay et al., The Leukocyte Antigen FactsBook, 1993, p164)Integrin alpha6beta1: A cell surface receptor mediating cell adhesion to the EXTRACELLULAR MATRIX and to other cells via binding to LAMININ. It is involved in cell migration, embryonic development, leukocyte activation and tumor cell invasiveness. Integrin alpha6beta1 is the major laminin receptor on PLATELETS; LEUKOCYTES; and many EPITHELIAL CELLS, and ligand binding may activate a number of signal transduction pathways. Alternative splicing of the cytoplasmic domain of the alpha6 subunit (INTEGRIN ALPHA6) results in the formation of A and B isoforms of the heterodimer, which are expressed in a tissue-specific manner.Vision, Ocular: The process in which light signals are transformed by the PHOTORECEPTOR CELLS into electrical signals which can then be transmitted to the brain.RNA, Messenger: RNA sequences that serve as templates for protein synthesis. Bacterial mRNAs are generally primary transcripts in that they do not require post-transcriptional processing. Eukaryotic mRNA is synthesized in the nucleus and must be exported to the cytoplasm for translation. Most eukaryotic mRNAs have a sequence of polyadenylic acid at the 3' end, referred to as the poly(A) tail. The function of this tail is not known for certain, but it may play a role in the export of mature mRNA from the nucleus as well as in helping stabilize some mRNA molecules by retarding their degradation in the cytoplasm.Receptors, Adrenergic, beta-1: A subclass of beta-adrenergic receptors (RECEPTORS, ADRENERGIC, BETA). The adrenergic beta-1 receptors are equally sensitive to EPINEPHRINE and NOREPINEPHRINE and bind the agonist DOBUTAMINE and the antagonist METOPROLOL with high affinity. They are found in the HEART, juxtaglomerular cells, and in the central and peripheral nervous systems.Adrenergic beta-2 Receptor Agonists: Compounds bind to and activate ADRENERGIC BETA-2 RECEPTORS.Binding Sites: The parts of a macromolecule that directly participate in its specific combination with another molecule.Photoreceptor Cells, Invertebrate: Specialized cells in the invertebrates that detect and transduce light. They are predominantly rhabdomeric with an array of photosensitive microvilli. Illumination depolarizes invertebrate photoreceptors by stimulating Na+ influx across the plasma membrane.Recombinant Proteins: Proteins prepared by recombinant DNA technology.Base Sequence: The sequence of PURINES and PYRIMIDINES in nucleic acids and polynucleotides. It is also called nucleotide sequence.Integrin alpha1beta1: Integrin alpha1beta1 functions as a receptor for LAMININ and COLLAGEN. It is widely expressed during development, but in the adult is the predominant laminin receptor (RECEPTORS, LAMININ) in mature SMOOTH MUSCLE CELLS, where it is important for maintenance of the differentiated phenotype of these cells. Integrin alpha1beta1 is also found in LYMPHOCYTES and microvascular endothelial cells, and may play a role in angiogenesis. In SCHWANN CELLS and neural crest cells, it is involved in cell migration. Integrin alpha1beta1 is also known as VLA-1 and CD49a-CD29.Transfection: The uptake of naked or purified DNA by CELLS, usually meaning the process as it occurs in eukaryotic cells. It is analogous to bacterial transformation (TRANSFORMATION, BACTERIAL) and both are routinely employed in GENE TRANSFER TECHNIQUES.Protein Conformation: The characteristic 3-dimensional shape of a protein, including the secondary, supersecondary (motifs), tertiary (domains) and quaternary structure of the peptide chain. PROTEIN STRUCTURE, QUATERNARY describes the conformation assumed by multimeric proteins (aggregates of more than one polypeptide chain).Glycogen Synthase Kinase 3: A glycogen synthase kinase that was originally described as a key enzyme involved in glycogen metabolism. It regulates a diverse array of functions such as CELL DIVISION, microtubule function and APOPTOSIS.Retinal Rod Photoreceptor Cells: Photosensitive afferent neurons located in the peripheral retina, with their density increases radially away from the FOVEA CENTRALIS. Being much more sensitive to light than the RETINAL CONE CELLS, the rod cells are responsible for twilight vision (at scotopic intensities) as well as peripheral vision, but provide no color discrimination.Kinetics: The rate dynamics in chemical or physical systems.Estrogen Receptor beta: One of the ESTROGEN RECEPTORS that has greater affinity for ISOFLAVONES than ESTROGEN RECEPTOR ALPHA does. There is great sequence homology with ER alpha in the DNA-binding domain but not in the ligand binding and hinge domains.Amino Acid Sequence: The order of amino acids as they occur in a polypeptide chain. This is referred to as the primary structure of proteins. It is of fundamental importance in determining PROTEIN CONFORMATION.G-Protein-Coupled Receptor Kinase 3: A ubiquitously expressed G-protein-coupled receptor kinase subtype that has specificity for the agonist-occupied form of BETA-ADRENERGIC RECEPTORS and a variety of other G-PROTEIN-COUPLED RECEPTORS. Although it is highly homologous to G-PROTEIN-COUPLED RECEPTOR KINASE 2, it is not considered to play an essential role in regulating myocardial contractile response.Adrenergic beta-Agonists: Drugs that selectively bind to and activate beta-adrenergic receptors.Transforming Growth Factor beta1: A subtype of transforming growth factor beta that is synthesized by a wide variety of cells. It is synthesized as a precursor molecule that is cleaved to form mature TGF-beta 1 and TGF-beta1 latency-associated peptide. The association of the cleavage products results in the formation a latent protein which must be activated to bind its receptor. Defects in the gene that encodes TGF-beta1 are the cause of CAMURATI-ENGELMANN SYNDROME.Dark Adaptation: Adjustment of the eyes under conditions of low light. The sensitivity of the eye to light is increased during dark adaptation.Protein Transport: The process of moving proteins from one cellular compartment (including extracellular) to another by various sorting and transport mechanisms such as gated transport, protein translocation, and vesicular transport.Receptors, Adrenergic, beta-3: A subclass of beta-adrenergic receptors (RECEPTORS, ADRENERGIC, BETA). The beta-3 adrenergic receptors are the predominant beta-adrenergic receptor type expressed in white and brown ADIPOCYTES and are involved in modulating ENERGY METABOLISM and THERMOGENESIS.Mutation: Any detectable and heritable change in the genetic material that causes a change in the GENOTYPE and which is transmitted to daughter cells and to succeeding generations.Mice, Knockout: Strains of mice in which certain GENES of their GENOMES have been disrupted, or "knocked-out". To produce knockouts, using RECOMBINANT DNA technology, the normal DNA sequence of the gene being studied is altered to prevent synthesis of a normal gene product. Cloned cells in which this DNA alteration is successful are then injected into mouse EMBRYOS to produce chimeric mice. The chimeric mice are then bred to yield a strain in which all the cells of the mouse contain the disrupted gene. Knockout mice are used as EXPERIMENTAL ANIMAL MODELS for diseases (DISEASE MODELS, ANIMAL) and to clarify the functions of the genes.Cell Adhesion: Adherence of cells to surfaces or to other cells.Beta Rhythm: Brain waves with frequency between 15-30 Hz seen on EEG during wakefulness and mental activity.GTP-Binding Proteins: Regulatory proteins that act as molecular switches. They control a wide range of biological processes including: receptor signaling, intracellular signal transduction pathways, and protein synthesis. Their activity is regulated by factors that control their ability to bind to and hydrolyze GTP to GDP. EC 3.6.1.-.Models, Molecular: Models used experimentally or theoretically to study molecular shape, electronic properties, or interactions; includes analogous molecules, computer-generated graphics, and mechanical structures.Opsins: Photosensitive proteins in the membranes of PHOTORECEPTOR CELLS such as the rods and the cones. Opsins have varied light absorption properties and are members of the G-PROTEIN-COUPLED RECEPTORS family. Their ligands are VITAMIN A-based chromophores.
ARF6
SMART: Pfam domain Arrestin N
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AgonistKinasesSeven-transmembrane receptorsMediateSignal transductionAbstractGRK2Alpha-2 adrenergic recARRB2GeneLigandsRegulateInteractionScaffoldChemokineRecruitmentDopamineDistinctPharmacologyGenesOpioid receptorsBeta1-adrenergic receptorOlfactoryAdaptor proteinPhosphorylatesInhibitResiduesInteractionsUbiquitinationERK1TransmembraneCellular2001Angiotensin II type 1A receptorsShenoyAntibodyEpidermal growth f
Agonist21
- Members of arrestin/beta-arrestin protein family are thought to participate in agonist-mediated desensitization of G protein-coupled receptors and cause specific dampening of cellular responses to stimuli such as hormones, neurotransmitters, or sensory signals, as well as having signalling roles in their own right. (wikipedia.org)
- The protein may interact with the agonist DOI in 5-HT2A receptor signaling. (wikipedia.org)
- The adrenergic beta-2 receptors are more sensitive to EPINEPHRINE than to NOREPINEPHRINE and have a high affinity for the agonist TERBUTALINE. (harvard.edu)
- The human beta-2 adrenergic receptor in complex with the partial inverse agonist carazolol . (wikipedia.org)
- Implicit in the traditional scheme of receptor function is the concept of linear efficacy, which is the notion that a given ligand is equally effective at stimulating or inhibiting all cellular responses regulated by a given receptor (traditional agonist or antagonist). (aspetjournals.org)
- However, the receptor conformation induced by this ligand may simultaneously permit signaling through another mechanism, unrelated to G protein activity, thus making it an agonist for this second pathway ( Fig. 1 ). (aspetjournals.org)
- In the mouse bleomycin model of right ventricular failure, the alpha1A -adrenergic receptor subtype agonist A61603 prevents right ventricular failure. (antikoerper-online.de)
- We stimulated HEK293 cells stably expressing Flag-tagged β2AR-eGFP with 10 μM beta-adrenergic agonist (isoproterenol) and made use of proteomics and targeted mass spectrometry (MS) to quantify the molar ration of phosphorylation on S355 and S356 versus non-phosphorylated receptor in agonist-treated cells. (jmolecularsignaling.com)
- It contains a beta-3 adrenergic receptor agonist combined with hyaluronic acid, a substance naturally found in the human body and commonly used in products like skin moisturisers. (freethesaurus.com)
- We have previously shown that the antinociception dose-response curve for peripherally restricted doses of the KOR agonist (-)-( trans )-3,4-dichloro- N -methyl- N -[2-(1-pyrrolidinyl)cyclohexyl]benzeneacetamide (U50488) has an inverted U shape. (aspetjournals.org)
- In contrast, R126N-CCR5 not only retained agonist-promoted phosphorylation and -arrestin-dependent endocytosis but also displayed a higher basal phosphorylation than wild-type CCR5. (39kf.com)
- The rate of transcription of the beta 2-adrenergic receptor gene is increased in response to beta-adrenergic agonist stimulation of the receptor at the cell surface. (duke.edu)
- The GRKs constitute a family of serine / threonine kinases that specifically bind to and phosphorylate agonist-activated serpentine receptors. (eurekaselect.com)
- It also predicts that ligands can have many different efficacies for the many behaviors that the receptor can exhibit (referred to as "pluridimensional efficacy"), leading to a breakdown in the common classifications of agonist and antagonist. (aspetjournals.org)
- A single efficacy allows the use of equiactive potency ratios for receptor and drug classification, because these cancel cellular effects and yield a measure of related agonist activity that depends only on affinity and efficacy. (aspetjournals.org)
- Because these are unique properties of the agonist and receptor (irrespective of cell type), they could be used to characterize relative agonism in one system for prediction of effect in any other system (including the therapeutic one). (aspetjournals.org)
- This provided a powerful tool to pharmacology, because the effects of cellular coupling and receptor density could be cancelled through the use of the null method, i.e., it is assumed that the cell will process equal levels of response to any agonist in the same manner. (aspetjournals.org)
- Dynamic properties of the somatostatin type 2A receptor were therefore examined in resting conditions and after agonist activation in living hippocampal neurons. (jneurosci.org)
- We then observed by live-cell imaging that, after agonist activation, membrane-associated receptors induce the recruitment of β-arrestin 1-enhanced green fluorescent protein (EGFP) and β-arrestin 2-EGFP to the plasma membrane. (jneurosci.org)
- Live-cell confocal imaging was then used to visualize early and late trafficking events of this receptor after agonist activation. (jneurosci.org)
- These data suggest that neural- and endothelial- inhibitory effects in autoantibodies from older adult diabetes with nephropathy and obesity/inflammation-associated complications are mediated by agonist autoantibodies directed against the 5-hydroxytryptamine 2 receptor positively coupled to the phospholipase C/inositol triphosphate/ cytosolic Ca2+ release pathway. (symbiosisonlinepublishing.com)
Kinases11
- Receptor tyrosine kinases (RTKs) usually function as dimeric or tetrameric cell surface receptors and mediate signals through tyrosine phosphorylation events ( 10 , 22 , 52 ). (asm.org)
- This inactivation is achieved, in part, by the binding of a soluble protein, arrestin, which uncouples the receptor from the downstream G protein after the receptors are phosphorylated by G protein-coupled receptor kinases. (ebi.ac.uk)
- Abnormality of G-protein-coupled receptor kinases at prodromal and early stages of Alzheimer's disease: an association with early beta-amyloid accumulation. (semanticscholar.org)
- These data suggest the existence of a family of receptor kinases which may serve broadly to regulate receptor function. (genecards.org)
- The closely related G protein-coupled receptor kinases GRK2 and GRK3 are both expressed in cardiac myocytes. (semanticscholar.org)
- Effect of different G protein-coupled receptor kinases on phosphorylation and desensitization of the alpha1B-adrenergic receptor. (semanticscholar.org)
- Src‐family tyrosine kinases are another major group of cellular signal transducers and have been demonstrated to directly relay signals from membrane receptors ( Thomas and Brugge, 1997 ). (embopress.org)
- Most important are special enzymes called G protein-coupled receptor kinases which phosphorylate the receptors and lead to their desensitization which occurs when they bind a second protein called barrestin. (duke.edu)
- This pathway mediates the ligand-triggered uptake of several G-protein-coupled receptors such as α 2a - and β 1 -adrenergic, dopaminergic D3 and D4 receptors and muscarinic acetylcholine receptor 4, the receptor tyrosine kinases EGFR, HGFR, VEGFR, PDGFR, NGFR and IGF1R, as well as interleukin-2 receptor. (nature.com)
- We suggest that these receptors can be pharmacologically targeted by modification of their unique internal inhibitors the G protein coupled receptor kinases (GRKs). (eurekaselect.com)
- Lymperopoulos A, Bathgate A. Pharmacogenomics of the heptahelical receptor regulators G-protein-coupled receptor kinases and arrestins: the known and the unknown. (springer.com)
Seven-transmembrane receptors2
- β-adrenergic receptors (β1AR and β2AR) and angiotensin II type 1A receptors (AT1aR) are seven transmembrane receptors that are common therapeutic targets for the treatment of hypertension, renal disease, and heart failure. (aspetjournals.org)
- Beta-arrestin-biased ligands at seven-transmembrane receptors. (duke.edu)
Mediate4
- Recently, ARRDC3 and not β‐arrestin2 was reported to mediate Nedd4 recruitment to the β 2 adrenergic receptor (β 2 AR) to regulate receptor ubiquitination and degradation [ 17 ]. (embopress.org)
- Adrenergic alpha2a receptor belongs to the group of nine adrenoceptors that mediate the biological actions of adrenaline and noradrenaline. (creative-biogene.com)
- Jane-Wit et al (2007) β 1-adrenergic receptor autoantibodies mediate dilated cardiomyopathy by agonistically inducing cardiomyocyte apoptosis. (tocris.com)
- To identify the G-protein coupled receptor(s) on neuroblastoma and endothelial cells which mediate neural- and endothelial cellinhibitory effects in plasma autoantibodies from a subset of older type 2 diabetes with neurologic and vascular co-morbidity. (symbiosisonlinepublishing.com)
Signal transduction1
- To address this, Evolutionary Trace was used to produce D 2 R mutants with strongly biased signal transduction for either the G-protein or β-arrestin interactions. (pnas.org)
Abstract1
- Abstract -β-Adrenergic modulation of the L-type Ca 2+ current ( I CaL ) was characterized for different developmental stages in murine embryonic stem cell-derived cardiomyocytes using the whole-cell patch-clamp technique at 37°C. Cardiomyocytes first appeared in embryonic stem cell-derived embryoid bodies grown for 7 days (7d). (ahajournals.org)
GRK22
- GRK2 levels are increased by ∼2-fold in muscle and adipose tissue in the animal models tested, as well as in lymphocytes from metabolic syndrome patients. (diabetesjournals.org)
- We also demonstrate that GRK2 and the uncoupling protein beta-arrestin associate with the receptor, forming a macromolecular complex shortly after MCP-1 binding. (scienceopen.com)
Alpha-2 adrenergic rec3
- Cloning and expression of a human kidney cDNA for an alpha 2-adrenergic receptor subtype. (duke.edu)
- An alpha 2-adrenergic receptor subtype has been cloned from a human kidney cDNA library using the gene for the human platelet alpha 2-adrenergic receptor as a probe. (duke.edu)
- Philipp M, Brede M, Hein L. Physiological significance of alpha(2)-adrenergic receptor subtype diversity: one receptor is not enough. (springer.com)
ARRB22
- Beta-arrestin-2, also known as arrestin beta-2, is an intracellular protein that in humans is encoded by the ARRB2 gene. (wikipedia.org)
- On www.antibodies-online.com are 98 Arrestin, beta 2 (ARRB2) Antibodies from 23 different suppliers available. (antibodies-online.com)
Gene10
- Arrestin, beta 1, also known as ARRB1, is a protein which in humans is encoded by the ARRB1 gene. (wikipedia.org)
- Beta-arrestin2, a novel member of the arrestin/beta-arrestin gene family. (ebi.ac.uk)
- Functional regions of beta ARK are described with respect to their location within the exon-intron organization of the gene. (wikidoc.org)
- One of the most extensively studied asthma susceptible gene is adrenergic receptor b2 (ADRB2).5 ADRB2 is a small intron-less gene located on 5q31, a region that is genetically linked to asthma and related phenotypes. (freethesaurus.com)
- Association of arg16gly and gln27glu, [beta]2-adrenergic receptor gene polymorphism with asthma. (freethesaurus.com)
- Among around 80 identified polymorphisms in the beta-2 adrenergic receptor gene, ADRB2 Arg16Gly polymorphism is one of the most common nonsynonymous SNPs [1, (freethesaurus.com)
- The beta-1 adrenergic receptor (β 1 adrenoreceptor), also known as ADRB1 , is a beta-adrenergic receptor , and also denotes the human gene encoding it. (worldheritage.org)
- A cAMP response element in the beta 2-adrenergic receptor gene confers transcriptional autoregulation by cAMP. (duke.edu)
- 8 Whereas G protein-dependent ERK translocates to the nucleus for gene transcription, arrestin-dependent ERK remains within the cytoplasm. (ahajournals.org)
- Mouse double minute 2 homolog ( MDM2 ) also known as E3 ubiquitin-protein ligase Mdm2 is a protein that in humans is encoded by the MDM2 gene . (wikipedia.org)
Ligands2
- More specifically, the possibility of selecting or designing novel ligands that differentially activate only a subset of functions via a single receptor holds great promise for the treatment of diseases such as heart failure and hypertension. (aspetjournals.org)
- Several allosteric ligands to these receptors have been identified and these appear to bind within the seven transmembrane region. (europeanpharmaceuticalreview.com)
Regulate1
- Two functionally distinct alpha2-adrenergic receptors regulate sympathetic neurotransmission. (springer.com)
Interaction7
- 1997). "Arrestin/clathrin interaction. (wikipedia.org)
- non‐visual arrestin 2 and 3) contain a characteristic α‐helix in the N‐terminal domain and a polar core that keeps the molecule constrained in a basal conformation, which is disrupted on arrestin-receptor interaction [ 8 , 9 ]. (embopress.org)
- Therefore, multiple functions may be seen via a single receptor-ligand interaction and a subsequent unique receptor conformation change. (aspetjournals.org)
- A 38-mer peptide, whose sequence reflected residues 12 through 49 of PDE4D5, encompasses the entire N-terminal RACK1 Interaction Domain (RAID1) together with a portion of the beta-arrestin binding site. (mdc-berlin.de)
- We suggest that the binding of PDE4D5 to the WD-repeat protein, RACK1, may occur in a manner akin to the helix-helix interaction shown for G(gamma) binding to the WD-repeat protein, G(beta). (mdc-berlin.de)
- The interaction with beta-arrestin exploits a greater circumference on the RAID1 helix, and involves two residues (Glu27, Asp28) that do not contribute to RACK1 binding. (mdc-berlin.de)
- In contrast, the interaction of RACK1 with RAID1 is extended over a greater length of the helix and includes Leu37/Leu38, which do not contribute to beta-arrestin binding. (mdc-berlin.de)
Scaffold1
- Downstream of PAR 2 , β-arrestins scaffold and activate ERK1/2, while inhibiting PI3K. (biomedcentral.com)
Chemokine4
- CC chemokine receptor 5 (CCR5) is a G protein-coupled receptor that governs migration of leukocytes and serves as a coreceptor for the R5 tropic strains of human immunodeficiency virus (HIV). (39kf.com)
- Monocyte chemoattractant protein 1 (MCP-1) is a member of the chemokine cytokine family, whose physiological function is mediated by binding to the CCR2 and CCR4 receptors, which are members of the G protein-coupled receptor family. (scienceopen.com)
- Several herpes- and poxviruses have captured chemokine receptors from their hosts and modified these to their own benefit. (pubmedcentralcanada.ca)
- The human and viral chemokine receptors belong to class A 7 transmembrane (TM) receptors which are characterized by several structural motifs like the DRY-motif in TM3 and the C-terminal tail. (pubmedcentralcanada.ca)
Recruitment6
- As the carboxyl terminal region is important for beta-arrestin binding, these results demonstrate that recruitment of beta-arrestin2 to carboxyl terminal region of beta2AR is important for ERK localization to the nucleus. (nih.gov)
- Moreover, genetic models of G protein-biased opioid receptors and replication of previous knockout experiments suggest that reduced or abolished arrestin recruitment does not improve therapeutic window for MOR-induced analgesia versus respiratory depression. (aspetjournals.org)
- Baillie GS, Sood A, McPhee I, Gall I, Perry SJ, Lefkowitz RJ, Houslay MD (2003) Beta-Arrestin-mediated PDE4 cAMP phosphodiesterase recruitment regulates beta-adrenoceptor switching from Gs to Gi. (springer.com)
- Visualization of arrestin recruitment by a G-protein-coupled receptor. (duke.edu)
- Further studies revealed that recruitment of arrestin3 to the β 2 -adrenergic receptor orchestrates the sequestration of Gq-coupled receptor-induced ERK to the cytosol through direct binding of ERK to arrestin. (ahajournals.org)
- To investigate whether odorant receptor activation leads to the recruitment of β-arrestin2 to the receptor protein, we tagged β-arrestin2 with GFP and visualized its redistribution upon activation of hOR17-4 with bourgeonal in HEK293 cells. (biologists.org)
Dopamine1
Distinct4
- However, recent evidence indicates that these two structural classes of receptors are not as functionally distinct as previously thought ( 5 , 6 , 13 , 20 , 27 , 35 ). (asm.org)
- These results have implications for how distinct biological responses of CCR5 might rely on a different set of receptor conformations. (39kf.com)
- 5-HT1A and histamine H1 receptors in HeLa cells stimulate phosphoinositide hydrolysis and phosphate uptake via distinct G protein pools. (duke.edu)
- Philipp M, Hein L. Adrenergic receptor knockout mice: distinct functions of 9 receptor subtypes. (springer.com)
Pharmacology1
- Although a number of tissue systems have been used over the years, the bulk of pharmacology aimed at receptor and new chemical entity classification was done with a limited number of reliable and serviceable tissues (i.e., guinea pig ileum, rat atria, rabbit aortae, etc. (aspetjournals.org)
Genes4
- Bonner TI, Buckley NJ, Young AC, Brann MR: Identification of a family of muscarinic acetylcholine receptor genes. (t3db.ca)
- title=Chromosomal organization of adrenergic receptor genes. (enacademic.com)
- title=Genetic mapping of adrenergic receptor genes in humans. (enacademic.com)
- Most of the MDM2-controlled genes also responded to the inactivation of the Polycomb Repressor Complex 2 ( PRC2 ) and its catalytic component EZH2 . (wikipedia.org)
Opioid receptors6
- Kappa Opioid Receptors Drive a Tonic Aversive Component of Chronic Pain. (nih.gov)
- Mu-opioid receptors in nociceptive afferents produce a sustained suppression of hyperalgesia in chronic pain. (nih.gov)
- Morphine activation of mu opioid receptors causes disinhibition of neurons in the ventral tegmental area mediated by β-arrestin2 and c-Src. (nih.gov)
- Dr. Evans is also director of a NIH-funded center - The Center for Opioid Receptors and Drugs of Abuse or CSORDA. (ucla.edu)
- Activation of kappa opioid receptors (KORs) expressed by peripheral sensory neurons that respond to noxious stimuli (nociceptors) can reduce neurotransmission of pain stimuli from the periphery to the central nervous system. (aspetjournals.org)
- Opioid receptors are key targets for drugs used for the treatment of pain. (aspetjournals.org)
Beta1-adrenergic receptor1
- Beta-arrestin-mediated beta1-adrenergic receptor transactivation of the EGFR confers cardioprotection. (duke.edu)
Olfactory3
- The sensory neurons that initiate olfaction and vision are olfactory sensory neurons (OSN), also referred to as olfactory receptor neurons (ORN), and photoreceptors (PR). (frontiersin.org)
- (A) OSN are defined by the expression of a unique odorant receptor, OSN expressing the same receptor (red, green, blue, or orange) are dispersed throughout the olfactory epithelium (OE) but the axons of these OSN converge to synapse in the same glomeruli of the olfactory bulb (OB). (frontiersin.org)
- Previously, we demonstrated that inefficient olfactory receptor (OR) expression at the plasma membrane is attributable, in part, to degradation of endoplasmic reticulum (ER)-retained ORs by the ubiquitin-proteasome system and sequestration of ORs in ER aggregates that are degraded by autophagy. (biomedcentral.com)
Adaptor protein1
- Growth factor receptor-bound protein 10 (GRB10 adaptor protein)(Insulin receptor-binding protein GRB-IR). (nctu.edu.tw)
Phosphorylates2
- c-Src phosphorylates SHC transforming protein 1 ( Shc ) and Growth factor receptor-bound protein 2 ( GRB2 ), activating Son of sevenless homolog ( SOS )/ H-Ras / c-Raf-1 and subsequent MEK and Erk activation [ 12 ], [ 13 ]. (bio-rad.com)
- Phosphorylates microtubule-associated protein 2 (MAP2). (nctu.edu.tw)
Inhibit1
- Arrestin beta 2, like arrestin beta 1, was shown to inhibit beta-adrenergic receptor function in vitro. (wikipedia.org)
Residues1
- These extracellular loops also contain two highly-conserved cysteine residues that form disulfide bonds to stabilize the receptor structure. (wikidoc.org)
Interactions1
- Functional specialization of beta-arrestin interactions revealed by proteomic analysis. (duke.edu)
Ubiquitination2
- Here, we report that treatment of cells for 12 h with insulin (100 ng/ml) induces an ∼50% decrease in cellular β-arrestin-1 content due to ubiquitination of β-arrestin-1 and proteosome-mediated degradation. (asm.org)
- beta-arrestin-1 competitively inhibits insulin-induced ubiquitination and degradation of insulin receptor substrate 1. (duke.edu)
ERK11
- Phosphospecific-ERK1/2 was from Cell Signal. (ahajournals.org)
Transmembrane2
- The seven transmembrane α-helix structure of a G-protein-coupled receptor. (wikidoc.org)
- Receptors of this family are characterized by seven highly hydrophobic transmembrane helix structures. (ijbs.com)
Cellular3
- Cellular trafficking of G protein-coupled receptor/beta-arrestin endocytic complexes. (nih.gov)
- To explore what adaptors serve what functions in β 2 AR trafficking, we performed a series of biochemical and cellular assays to compare β‐arrestin2 with ARRDC3. (embopress.org)
- Deubiquitinating enzyme involved in various processes such as cellular migration and beta-2 adrenergic receptor/ADRB2 recycling. (abcam.co.jp)
Angiotensin II type 1A receptors3
- Receptor/beta-arrestin complex formation and the differential trafficking and resensitization of beta2-adrenergic and angiotensin II type 1A receptors. (nih.gov)
- β-Adrenergic and angiotensin II type 1A receptors are therapeutic targets for the treatment of a number of common human diseases. (aspetjournals.org)
- This review examines the functional selectivity of β-adrenergic and angiotensin II type 1A receptors with respect to their ability to signal via both G protein-dependent and G protein-independent mechanisms, with a focus on the multifunctional protein β-arrestin. (aspetjournals.org)
Shenoy1
- Lefkowitz, Shenoy: Transduction of receptor signals by beta-arrestins. (antibodies-online.com)
Antibody2
- The following product was used in this experiment: beta Arrestin 1 Polyclonal Antibody from Thermo Fisher Scientific, catalog # PA5-35089, RRID AB_2552399. (thermofisher.com)
- This peptide was used for the production of goat polyclonal anti-beta 1 Adrenergic Receptor antibody (GTX89376). (genetex.com)
Epidermal growth f2
- Interestingly, the UIM-containing endocytic adaptors epidermal growth factor receptor protein substrate 15 and Epsin exhibited preferential binding to PLIC-2 over PLIC-1. (cmu.edu)
- Epidermal growth factor receptor. (springer.com)
