神经生物学

Nerve fibers innervate every organ of the body and are involved in monitoring changes of the external and internal environment. Innervation directly controls a variety of physiological responses in an adaptive manner. Today, many lines of research indicate that also the immunological ...

In this chapter, methods for the analysis of allosterism in equilibrium binding and functional assays are described. The functional response to activation of a G protein-coupled receptor is usually measured at a point downstream from receptor activation in the signaling pathway, and the ...

Phosphorylation of G protein-coupled receptors (GPCRs) occurs within seconds of agonist stimulation and is one of the most prevalent mechanisms through which signalling of this super receptor family is regulated. Although traditionally associated with receptor desensitis ...

The development of new therapeutic drugs acting at G protein-coupled receptors (GPCRs) whose ligand specificity is known is of great importance to the pharmaceutical industry and to the population at large. It is also vital that surrogate ligands can be identified for GPCRs at which the endog ...

A remarkable potential exists for current and future development of therapeutic drugs acting at GPCRs. As one of the initial steps in GPCR drug development, in vitro assays are required to characterize the pharmacology of new ligands acting at distinct GPCRs. This is routinely accomplished ...

G protein-coupled receptor (GPCR) responsiveness is dynamically regulated by various mechanisms, allowing fine-tuning of cell signaling. Modulation of GPCR plasma membrane density, via their release from intracellular compartments, constitutes a recently identified i ...

Similar to many other plasma membrane proteins, G protein-coupled receptors (GPCRs) are synthesized in the endoplasmic reticulum (ER). After proper assembly and folding, the receptors are transported from the ER through the Golgi to the cell surface. As the first step in the anterograde tra ...

The G protein-coupled receptors (GPCRs) are a superfamily of transmembrane receptors that �structurally possess an extracellular amino terminus, seven transmembrane domains linked by extracellular and intracellular loops, and a cytoplasmic carboxyl terminus. They are sy ...

G protein-coupled receptors (GPCRs) represent the largest family of membrane receptors. These proteins respond to a broad diversity of environmental stimuli and ligands, modulate most physiological processes, and represent prime therapeutic targets. Detecting GPCRs in vivo, ...

In pharmacology, a central tenet of receptor theory has been that different agonists acting at a particular G protein-coupled receptor subtype produce the same profile of cellular responses. In recent years, advances in molecular pharmacology and the availability of diverse cell sign ...

With the rise of interest in receptor–receptor interaction research, optimization of experimental designs to study the nature of interactions has become increasingly important. In this chapter, traditional experimental designs and their associated statistics are reviewe ...

G protein-coupled receptors (GPCRs) are ancestrally related membrane proteins on cells that mediate the pharmacological effect of most drugs and neurotransmitters. GPCRs are the largest group of membrane receptor proteins encoded in the human genome. Using the case study of vertebr ...

G protein-coupled receptors (GPCRs) participate in a variety of physiological functions and are major targets of pharmaceutical drugs. More than 600 GPCRs have been identified in the human genome. Although GPCRs are expressed in multiple tissues and individual tissues express multi ...

The genes for G protein-coupled receptors (GPCRs) including those encoding the classical mu, delta, and kappa opioid receptors (MOR, DOR, and KOR); cannabinoid receptors (CB1); ACTH receptor (melanocortin receptor type 2, MC2R); and serotonin receptors (5HT1B) have been a focus of the studi ...

Alternative pre-mRNA splicing involves editing of a gene to generate a number of different mRNAs and proteins. It provides a mechanism for only 20,000 genes to generate hundreds of thousands of proteins. Like other proteins, it is estimated that 50% of G protein-coupled receptors undergo alte ...

The G protein-coupled receptors (GPCRs) form the largest and most multi-functional protein �superfamilies known. From a drug discovery and pharmaceutical industry perspective, the GPCRs are among the most commercially and economically important groups of proteins yet identi ...

A new approach for characterizing the plasma membrane delivery of G protein-coupled receptors is described in this chapter. This approach uses an existing technology, the regulated secretion/aggregation technology (RPD™), to cause the accumulation of G protein-coupled recepto ...

Drugs targeting the opioid neurotransmission system have been used for centuries recreationally and for medical purposes. In spite of this vast experience and competence in opioid pharmacotherapy, fine details about the cellular and molecular mechanisms underlying opioid rec ...

G protein-coupled receptors (GPCRs) are the major sites of actions for the body’s endogenous hormones and neurotransmitters which make them ideal targets for pharmaceutical development with the goal of either mimicking the normal transmitter response or tempering it. In recent year ...

Technologies developed to interfere with gene transcripts were developed back in the 1980. However, it was not before the last decade that light was shed on the underlying mechanisms of what is now known as RNA interference. From then, RNAi was propelled to the forefront as a revolutionizing appro ...