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Constitutive activity of G-protein-coupled receptors: cause of disease and common property of wild-type receptors
A systematic overview on constitutively active G-protein-coupled receptors (GPCRs), a rapidly evolving area in signal transduction research, and inverse agonists and Na+ that stabilize the R state, and pertussis toxin that uncouples GPCRs from Gi/Go-proteins are provided. Expand
A liquid chromatography-coupled tandem mass spectrometry method for quantitation of cyclic di-guanosine monophosphate.
This work has established a robust and highly sensitive high performance liquid chromatography-coupled tandem mass spectrometry (HPLC-MS/MS) based method for the quantitation of c-di-GMP and investigated various method performance parameters such as limit of detection (LOD), lower limit of quantitation (LLOQ), linearity, accuracy, recovery and analyte stability. Expand
Inhibitors of membranous adenylyl cyclases.
The current literature on mAC inhibitors is reviewed, and structuralurally diverse inhibitors targeting the catalytic site and allosteric sites (e.g. the diterpene site) have been identified. Expand
Structural Instability of a Constitutively Active G Protein-coupled Receptor
It is proposed that the mutation that confers constitutive activity to the β2 adrenergic receptor removes some stabilizing conformational constraints, allowing CAM to more readily undergo transitions between the inactive and the active states and making the receptor more susceptible to denaturation. Expand
High Constitutive Activity of the Human Formyl Peptide Receptor*
The data show that the human FPR possesses high constitutive activity, and identifies an inverse FPR agonist, i.e. a compound that suppresses constitutive FPR activity. Expand
G-protein-coupled receptors in HL-60 human leukemia cells.
HL-60 human leukemia cells are a widely employed model system for the analysis of signal transduction processes mediated via regulatory heterotrimeric guanine nucleotide-binding proteins (G-proteins) and there are substantial differences in the agonist/antagonist profiles of H2-receptor-mediated cAMP formation and rises in cytosolic Ca2+ concentration. Expand
Molecular and cellular analysis of human histamine receptor subtypes.
Current knowledge of hH(x)Rs endogenously expressed in human cells and recombinantly expressed in mammalian and insect cells is summarized and multiple systems and parameters have to be studied to increase drug safety and efficacy. Expand
Hrs-2 is an ATPase implicated in calcium-regulated secretion
The results suggest a role for Hrs-2 in regulating secretory processes through calcium- and nucleotide-dependent modulation of vesicle-trafficking protein complexes through calcium's role in neurotransmitter-containing vesicles and on the presynaptic membrane. Expand
The effect of pH on beta(2) adrenoceptor function. Evidence for protonation-dependent activation.
Evidence is provided that protonation increases basal activity by destabilizing the inactive state of the receptor and the pH sensitivity of beta(2)AR activation is not abrogated by mutation of Asp(130). Expand
High constitutive activity and a G-protein-independent high-affinity state of the human histamine H(4)-receptor.
The human histamine H(4)-receptor (hH(4)R) is expressed in mast cells and eosinophils and mediates histamine (HA)-induced chemotaxis via G(i)-proteins. For a detailed investigation ofExpand