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Autoradiographic detection of ligand binding to tissue sections has been used to localize, quantify, and characterize a diverse range of sites. Enzymes have been studied using selective inhibitors, ion channels using naturally occurring toxins, and second messenger systems using ...

A receptor is an allosteric macromolecule (usually associated with a particular cell type) that binds a specific chemical substance (usually secreted by another cell) and in the process undergoes a defined conformational change that triggers a series of biochemical and physiologic ...

Most of the autoradiography performed in human brain involves cutting sections from blocks of tissue or single hemispheres containing relevant areas. The resultant images are restricted to the particular region being studied and do not allow an overview of the plane in which the region is si ...

This chapter describes a functional assay which measures the increase in guanine nucleotide exchange at G-proteins in cell membranes, resulting from agonist binding to G-protein-coupled receptors (GPCRs), by monitoring the binding of GTPγS, a radiolabeled, hydrolysis-resist ...

In situ hybridization histochemistry (ISHH), first described in 1969 by Gall and Pardue and John et al. (1,2) and northern hybridization, first described by Alwine et al. (3), have become very powerful and now quite well established techniques in many research areas, including that of receptor re ...

G protein-coupled receptors (GPCRs) are the number one class of receptor targets for the pharmacotherapy of many pathological and disease states. This chapter presents an overview of the chapter topics presented in this new volume on the genetics of GPCRs.

The valuable source of large-scale genomic information initiated attempts to identify the origin(s) of G protein-coupled receptors (GPCR), count and categorize those genes, and follow their evolutionary history. Being present in fungi, plants, and unicellular eukaryotes, GPCR mu ...

During coevolution with their hosts, viruses have developed several survival strategies that involve exploitation of 7 transmembrane spanning (7TM) G protein-coupled receptors (GPCRs). These include virus-encoded GPCRs and ligands and viral regulation of endogenous GPCRs. ...

The very large G protein-coupled receptor 1 (VLGR1), also known as MASS1 or GPR98, is most notable among the family of adhesion GPCR for its size. Encoded by an 18.9 kb open reading frame, the ~700 kDa primary translation product is by far the largest GPCR and, additionally, the largest cell surface protein k ...

Opioid receptors are a family of receptors that belong to the type A GPCR group. Opioid receptors mediate a large myriad of physiological responses in different vertebrate species. There is evidence for the existence of opioid receptors from very early in evolution, and here we discuss a possib ...

Delineation of GPCR function and regulation has relied heavily on the available pharmacological tools to manipulate GPCR activity, inhibit GPCR interacting proteins, or modulate downstream signaling molecules. Where appropriate agents are unobtainable, alternative mol ...

G protein-coupled receptors (GPCRs) comprise the largest group of cell surface receptors, translating environmental signals into cellular responses via cognate G protein partners. Contrary to our initial understanding, most GPCRs do not function in living cells as monomers, but mo ...

The use of in vitro mutagenesis to characterize structure-function relationships in G protein-coupled receptors has led to the identification of specific amino acid residues that contribute to ligand binding, G protein coupling, and receptor folding. Mutagenesis is commonly used ...

Numerous assays have been developed to investigate the interactions between GPCRs and their ligands since GPCRs are key therapeutic targets. Reporter-based assays using the cAMP response element (CRE) coupled with bioluminescence from a luciferase reporter have been used exten ...

Our understanding of GPCR function has advanced considerably in the past few years primarily because advances were made in elucidating structures of several GPCRs and a new era of conformational dynamic studies of GPCRs is in fast progress. Traditional pharmacological studies in tiss ...

G protein-coupled receptors (GPCRs) transduce signals from a wide variety of extracellular stimuli such as ions, photons, odors, tastants, hormones, and neurotransmitters and hence are central players in communication between the cells of multicellular organisms and their envi ...

Numerous congenital disorders, ranging from night blindness to cancer, are associated with signaling by overactive GPCR mutants. Excessive GPCR signaling also underlies certain acquired pathological conditions. The coupling of most GPCRs to their cognate G proteins is stopped by ...

The tractability of light-activated receptors makes them attractive tools by which to study the brain. They allow for the noninvasive and specific control of neuronal signaling and could allow for the study of receptor pathways that occur faster than the rate of diffusion. Furthermore, with ...

This chapter describes the protocol for the preparation of recombinant adenoviruses and infection of target cells to transiently express G protein-coupled receptors (GPCRs) or other proteins of interest. Adenoviruses are non-enveloped viruses containing a linear double-st ...

Progress in areas of research from the field of G protein-coupled receptor (GPCR) signaling now shows that GPCRs are involved in a broad range of cellular regulatory activities. By virtue of widespread distribution and important roles in cell physiology and biochemistry, GPCRs play multi ...