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Receptor active

Fig. 10. The receptor—G-protein sequence. An activated receptor interacts with the trimeric GDP-ligated receptor to cause an interchange of GDP by GTP and dissociation into the activated Ga—GTP (left) and G y (right) subunits. These then interact with a variety of effectors. The purpose of the activated... Fig. 10. The receptor—G-protein sequence. An activated receptor interacts with the trimeric GDP-ligated receptor to cause an interchange of GDP by GTP and dissociation into the activated Ga—GTP (left) and G y (right) subunits. These then interact with a variety of effectors. The purpose of the activated...
The ability of receptors to couple to G-proteins and initiate GTPase activity may also be independent of ligand. Thus, specific mutations in a- and P-adrenergic receptors have led to receptors that mediate agonist-independent activation of adenylyl cyclase (69,70). These mutations presumably mimic the conformational state of the ligand-activated receptor when they are activated conventionally by ligands. [Pg.279]

Biochemically, most quaternary ammonium compounds function as receptor-specific mediators. Because of their hydrophilic nature, small molecule quaternaries caimot penetrate the alkyl region of bdayer membranes and must activate receptors located at the cell surface. Quaternary ammonium compounds also function biochemically as messengers, which are generated at the inner surface of a plasma membrane or in a cytoplasm in response to a signal. They may also be transferred through the membrane by an active transport system. [Pg.378]

The extended ternary complex model can take into account the phenomenon of constitutive receptor activity. In genetically engineered systems where receptors can be expressed in high density, Costa and Herz [2] noted that high levels of receptor expression uncovered the existence of a population of spontaneously active receptors and that these receptors produce an elevated basal response in the system. The relevant factor is the ratio of receptors and G-proteins (i.e., elevated levels of receptor cannot yield constitutive activity in the absence of adequate amounts of G-protein, and vice versa). Constitutive activity (due to the [RaG] species) in the absence of ligand ([A] = 0) is expressed as... [Pg.49]

Active Receptor Species]11 AR [Total Receptor Species]11... [Pg.55]

It is assumed that the receptor species leading to G-protein activation (and therefore physiological response) are complexes between the activated receptor ([RJ) and the G-protein namely, [ARaG] + [RaG], The fraction of the response-producing species of the total receptor species (([ARaG] + [RaG])/Rtot) is denoted p and is given by... [Pg.56]

The first idea to consider is the effect of receptor density on sensitivity of a functional system to agonists. Clearly, if quanta of stimulus are delivered to the stimulus-response mechanism of a cell per activated receptor the amount of the total stimulus will be directly proportional to the number of receptors activated. Figure 5.8 shows Gi-protein-mediated responses of melanophores transiently transfected with cDNA for human neuropeptide Y-l receptors. As can be seen from this figure, increasing receptor expression (transfection with increasing concentrations of receptor cDNA) causes an increased potency and maximal response to the neuropeptide Y agonist PYY. [Pg.85]

Analyses for Inverse Agonists in Constitntively Active Receptor Systems... [Pg.108]

In constitutively active receptor systems (where the baseline is elevated due to spontaneous formation of receptor active states, see Chapter 3 for full discussion), unless the antagonist has identical affinities for the inactive receptor state, the spontaneously formed active state, and the spontaneously G-protein coupled state (three different receptor conformations, see discussion in Chapter 1 on receptor conformation) it will alter the relative concentrations of these species—and in so doing alter the baseline response. If the antagonist has higher affinity for the... [Pg.108]

FIGURE 6.12 Schild analysis for constitutively active receptor systems, (a) Competitive antagonism by the inverse agonist in a constitutively active receptor system with DR values calculated at the EC80. [Pg.110]

Used to estimate system independent potency of an inverse agonist in a constitutively active receptor system. [Pg.212]

X = transducer function for response to the full agonist and constitutive y active receptor state. [Pg.212]


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See also in sourсe #XX -- [ Pg.12 ]




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5-Receptor agonists pharmacological activity

5-Receptor antagonists pharmacological activity

Acetylcholine receptor activation cycle

Acetylcholine receptor-inducing activity

Acetylcholine receptor-inducing activity ARIA)

Acetylcholine receptors active site

Activation of receptors

Activation of the Cytoplasmic Apo-Receptor Complexes

Active conformation metabotropic glutamate receptors

Activity receptor profiling

Adenosine A3 receptor activation

Agonist receptor activation

Agonist receptor activity

Antiestrogens estrogen receptor activation mechanisms

Anxiolytics serotonin receptor-active

Apoptosis death receptor activation

Calcitonin receptors, osteoclast activity

Calcium NMDA receptor activation

Calcium channels receptor-mediated activation

Cannabinoid receptor constitutive activity

Cell surface receptors activation

Chemokine receptor activation

Chemokine receptor activation, molecular

Cholinergic receptors activation process

Cholinergic receptors activators

Cholinergic receptors structure-activity relationships

Constitutive activated receptor

Constitutive active receptor

Constitutive active/androstane receptor

Constitutive activity of receptors

Constitutive androstane receptor activation

Constitutive androstane receptor activators

Constitutively Active Receptors and Inverse Agonists

Constitutively Active Viral Chemokine Receptors Tools for Immune Subversion and Pathogenesis

Constitutively activating receptor

Constitutively active receptor CAR

Delta receptors activation

Electrochemical recognition of anionic guest species by redox-active receptor molecules

Electrochemical recognition of charged and neutral guest species by redox-active receptor

Electrochemical recognition of charged and neutral guest species by redox-active receptor molecules

ErbB receptors activating

Erythropoietin-receptor activators

Estrogen receptor binding activity

Estrogen receptors activity assessment

Estrogen-receptors activation mechanisms

Estrogen-receptors antiestrogen activity

Estrogenic receptor activity

Fenfluramine receptor activation

Formyl peptide receptor activation

Functional assays receptor activation

G-protein coupled receptors activation

G-protein receptors, activation

G-protein-coupled receptors active

GABAa receptors, activation

GABAa receptors, activation barbiturate binding site

GABAa receptors, activation benzodiazepine binding site

GABAa receptors, activation binding affinities

GABAa receptors, activation modulatory sites

GABAa receptors, activation structure

GABAa receptors, activation subtypes

Glutamate-activated receptors

H2-receptor activity

Herpesviruses Encode Constitutively Active Viral Chemokine Receptors

Hi-receptor activity

Histamine H3 receptor, activation

Histamine receptor antagonists) structure-activity relationship

Hormone independent gene activation by truncated receptors

Hormone-activated receptor tyrosine

Hormone-activated receptor tyrosine kinase

Insulin receptor activated

Insulin receptor tyrosyl kinase activity

Insulin receptor, activation

K-Receptor agonists pharmacological activity

K-Receptor antagonists pharmacological activity

Kappa receptors activation

Kappa-opioid receptor activation

Ligand-activated nuclear receptor

Ligands peroxisome proliferator-activated receptor

Lumophore-spacer-receptor systems with redox active guests

MSP Receptor Regulation or Activation

Mechanism of Thrombin Receptor Activation

Mitogen-activated protein kinase cell-surface receptors

Mitogen-activated protein kinase growth factor receptor signaling

Mouse vas deferens activity in receptor binding assa

Mu receptors activation

Muscarinic cholinergic receptors activation process

Muscarinic receptors activation

NMDA receptors activation

NMDA receptors physiological activity

Neuronal nicotinic acetylcholine receptors activation

Neuronal receptors activation

Nicotinic acetylcholine receptors activation mechanism

Nicotinic cholinergic receptors activation process

Nicotinic receptors activation

Novel Receptor Active Substances

Nuclear hormone receptor activator

Nuclear peroxisome proliferator activated receptor

Nuclear receptors, retinoid-induced gene activation

Opioid receptors activation

P-Opioid receptor activity in guinea-pig ileum

P-Receptor agonists pharmacological activity

P-Receptor antagonists pharmacological activity

PEROXISOME PROLIFERATED -ACTIVATED RECEPTORS (PPARS)

PPARy modulator proliferator-activated receptor

PPARy, Peroxisome proliferator activated receptor gamma

Partial agonism and the two-state model of receptor activation

Peroxisomal proliferator-activated receptors

Peroxisomal proliferator-activated receptors Subject

Peroxisome Proliferator-Activated Receptor y Coactivator-la

Peroxisome Proliferator-Activated Receptor y Ligands

Peroxisome Proliferator-Activated Receptor y-Agonists and Stroke

Peroxisome proliferation-activated receptor

Peroxisome proliferation-activated receptor PPAR)

Peroxisome proliferator activated receptor -a agonists

Peroxisome proliferator activated receptor binding protein

Peroxisome proliferator activated receptor interaction with genes

Peroxisome proliferator activated receptor species difference

Peroxisome proliferator activated receptor-y

Peroxisome proliferator activator receptor- (PPAR

Peroxisome proliferator activator receptor-a

Peroxisome proliferator-activated receptor 7 agonists

Peroxisome proliferator-activated receptor PPAR agonists)

Peroxisome proliferator-activated receptor PPAR)

Peroxisome proliferator-activated receptor PPAR) pathway

Peroxisome proliferator-activated receptor PPARa activation

Peroxisome proliferator-activated receptor PPARa)

Peroxisome proliferator-activated receptor PPARy)

Peroxisome proliferator-activated receptor PPARy) agonists

Peroxisome proliferator-activated receptor action mechanisms

Peroxisome proliferator-activated receptor activation

Peroxisome proliferator-activated receptor agonists thiazolidinediones

Peroxisome proliferator-activated receptor alpha

Peroxisome proliferator-activated receptor alpha activator

Peroxisome proliferator-activated receptor alpha gene

Peroxisome proliferator-activated receptor alpha protein

Peroxisome proliferator-activated receptor atherosclerosis

Peroxisome proliferator-activated receptor balance

Peroxisome proliferator-activated receptor beta

Peroxisome proliferator-activated receptor chemistry

Peroxisome proliferator-activated receptor effects

Peroxisome proliferator-activated receptor gamma

Peroxisome proliferator-activated receptor gene expression alterations

Peroxisome proliferator-activated receptor human response

Peroxisome proliferator-activated receptor inflammation

Peroxisome proliferator-activated receptor inhibition studies

Peroxisome proliferator-activated receptor insulin sensitivity improvement

Peroxisome proliferator-activated receptor insulin sensitization

Peroxisome proliferator-activated receptor isoforms

Peroxisome proliferator-activated receptor lipid oxidation products

Peroxisome proliferator-activated receptor mechanisms

Peroxisome proliferator-activated receptor modulator

Peroxisome proliferator-activated receptor oxidative stress

Peroxisome proliferator-activated receptor pioglitazone

Peroxisome proliferator-activated receptor polyunsaturated fatty acids

Peroxisome proliferator-activated receptor rosiglitazone

Peroxisome proliferator-activated receptor signaling

Peroxisome proliferator-activated receptor target gene identification

Peroxisome proliferator-activated receptor thiazolidinedione insulin sensitizers

Peroxisome proliferator-activated receptor tissue expression

Peroxisome proliferator-activated receptor transcriptional regulation

Peroxisome proliferator-activated receptor troglitazone

Peroxisome proliferator-activated receptor-alpha (PPAR

Peroxisome proliferator-activated receptor-y (PPAR

Peroxisome proliferator-activated receptor-y agonists

Peroxisome proliferator-activated receptors

Peroxisome proliferator-activated receptors PPARs), fatty acid ligands

Peroxisome proliferator-activated receptors dual agonists

Peroxisome proliferator-activated receptors functions

Peroxisome proliferator-activated receptors structure

Peroxisome proliferators activated receptor PPAR)

Peroxisome proliferators activator receptor

Peroxisome proliferators activator receptor PPAR) agonists

Peroxisome proliferators-activated receptor

Peroxisome-activator receptor-alpha

Peroxisome-activator receptor-alpha expression

Peroxisome-proliferator activated receptors PPARs)

Platelet activating factor receptor-mediated activities

Platelet activation receptors

Platelet-activating factor receptor

Platelet-activating factor receptor antagonists

Pregnane-activated receptor

Prolactin receptor activation

Proliferator-activated receptor

Proliferator-activated receptor PPAR)-gamma

Prostanoid receptors selective ligands and structure-activity relationships

Protease-activated receptor

Protease-activated receptor signaling

Protease-activated receptors reaction

Protein tyrosine phosphorylation receptor activation

Proteinase-activated receptors

Quantitative structure-activity relationship estrogen receptor binding affinity

Receptor Activation, Tyrosine Kinase Activity, and in Cultured Vascular Smooth Muscle Cells

Receptor activation

Receptor activation

Receptor activation mechanism

Receptor activation, molecular processes

Receptor activator of NF-kB

Receptor activator of NF-kB ligand

Receptor activator of nuclear factor

Receptor activator of nuclear factor-kB ligand

Receptor activities, regulation

Receptor activity

Receptor activity

Receptor activity dopamine

Receptor activity modifying proteins

Receptor activity modulating proteins

Receptor activity muscarinic

Receptor activity, conjugates

Receptor agonists/activators

Receptor binding assay activity

Receptor blocking activity

Receptor constitutively active

Receptor destroying activity

Receptor molecules, redox-active

Receptor molecules, redox-active electrochemical recognition

Receptor molecules, redox-active, electrochemical recognition of charged and

Receptor molecules, redox-active, electrochemical recognition of charged and neutral

Receptor molecules, redox-active, electrochemical recognition of charged and neutral guest

Receptor molecules, redox-active, electrochemical recognition of charged and neutral guest species

Receptor natural killer cells, activation

Receptor signaling complexes activated

Receptor tyrosine kinase Activation

Receptor tyrosine kinase activity, insulin

Receptor-independent activation

Receptors activated solely by synthetic

Receptors activated solely by synthetic ligands

Receptors antitumor activity

Receptors constitutive activity

Receptors intrinsic enzyme activity

Receptors membrane-bound, activation

Receptors redox-active

Receptors redox-active center

Receptors with Associated Tyrosine Kinase Activity

Receptors with Kinase Activity

Receptors with enzymatic activity

Receptors with guanylate cyclase activity

Receptors with intrinsic enzymatic activity

Receptors with protein kinase activity

Receptors with serine/threonine kinase activity

Receptors with tyrosine kinase activity

Receptors without enzymatic activity

Regulation of Receptor Activity

Selective drugs, activity toward receptors

Serotonin receptor activity

Serotonin receptor-active agents

Signal Transmission via Transmembrane Receptors with Tyrosine-specific Protein Kinase Activity

Smad anchor for receptor activation

Structural Determinants of Ligand Binding and Receptor Activation by CC Chemokines

Structure-activity relationships drug-receptor interactions

Structure-activity relationships of dopamine receptor agonists

Structure-activity relationships receptor mapping

T cell receptor activation

Test Systems Addressing 5-HT4 Receptor Agonist Activity

The Distinction between Agonist Binding and Receptor Activation

The Estrogen Receptors and Their Multiple Gene Activation Mechanisms

The Law of Mass Action, binding sites and receptors—understanding why specific, potent biological activity is a rare property for any one chemical to possess

The Peroxisome Proliferator Activated Receptor

The del Castillo-Katz Mechanism 1. Relationship between Agonist Concentration and Fraction of Receptors in an Active Form

Thrombin receptor activation

Thrombin receptor-activating peptide TRAP)

Thrombin receptor-activating peptides

Thromboxane receptor activation

Towards electrochemical recognition of neutral guest species by redox-active receptor molecules

Urokinase plasminogen activator receptor

Urokinase-type plasminogen activator receptor

Urokinase-type plasminogen activator receptor uPAR)

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