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丁香实验推荐阅读
Functional Properties of Virus-Encoded and Virus-Regulated G Protein-Coupled Receptors

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. ...

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Discovery and Function of the Very Large G Protein-Coupled Receptor

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 ...

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Functional Evolution of Opioid Family G Protein-Coupled Receptors

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 ...

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Investigation of G Protein-Coupled Receptor Function and Regulation Using Antisense

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 ...

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Signalosome Profiling Reveals Allosteric Interactions Between G Protein-Coupled Receptors

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 ...

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Using In Vitro Mutagenesis to Characterize Structure-Function Relationships in G Protein-Coupled Receptors

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 ...

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The CRE Luc Mouse Model for Bioimaging Ligand Activation of G Protein-Coupled Receptors

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 ...

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Inducing Conformational Changes in G Protein-Coupled Receptors by Domain Coupling

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 ...

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Rescue of Defective G Protein-Coupled Receptor Function by Intermolecular Cooperation

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 ...

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Design of Super-arrestins for Gene Therapy of Diseases Associated with Excessive Signaling of G Protein-Coupled Receptors

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 ...

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Use of Optogenetic Approaches to Control Intracellular Signaling of G Protein-Coupled Receptors

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 ...

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Viral Infection for G Protein-Coupled Receptor Expression in Eukaryotic Cells

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 ...

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Importance of G Protein-Coupled Receptor Genetics in Clinical Medicine

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 ...

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Pharmacogenomics of G Protein-Coupled Receptor Signaling and Other Pathways in Essential Hypertension

Essential hypertension represents a cluster of genetically determined physiological abnormalities that is influenced by environmental factors and the individual’s lifestyle. Essential hypertension is a major public health challenge because it affects one in every three a ...

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Exon Sequencing of G Protein-Coupled Receptor Genes and Perspectives for Disease Treatment

G protein-coupled receptors (GPCRs) comprise the largest family of membrane-spanning proteins in humans with approximately 800 members. GPCRs carry out an extensive array of biological functions and are privileged drug targets. Exon sequencing identified several disease-ca ...

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Gene Therapy Using G Protein-Coupled Receptors for the Treatment of Cardiovascular Disease

Cardiovascular diseases are the most common cause of death worldwide, and despite advances in treatments, mortality rates still remain elevated. Heart failure prevalence is increasing and accounts for half a million deaths per year in the USA. Thus, there is an urgent need to develop new thera ...

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Novel Mechanisms of G Protein-Coupled Receptor Oligomer and Ion Channel Interactions in Nociception

G protein-coupled receptors (GPCRs) represent the largest family of cell surface receptors that are involved in regulating several physiological and behavioral responses in organisms. Indeed, over half of all the approved drugs on the market target GPCRs. Over the past 20 years, several l ...

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Discovery and Characterization of Leucine-Rich Repeat-Containing G Protein-Coupled Receptors

Leucine-rich repeat-containing G protein-coupled receptors (LGRs) are type A rhodopsin-like GPCRs that include the glycoprotein pituitary hormone receptors for the thyroid-stimulating, follicle-stimulating, and luteinizing hormones (TSH, FSH, and LH); a pair of receptors ...

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The Role of G-Protein-Coupled Receptors in Adult Neurogenesis

Adult neurogenesis is the process of creating new brain cells during adulthood. This involves several stages including proliferation, migration, differentiation, integration, and survival. G-protein-coupled receptors (GPCRs) regulate this process in both neurogenic re ...

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Utilizing RNA-Seq to Define Phytochemical-Induced Alterations in Insulin and IGF-Regulated Transcriptomes

Cancer at its root is a genetic disease brought on by genomic alterations that lead to uncontrolled cell division, metastasis, and enhanced cell survival. The study of genomics can address many of the genetic abnormalities associated with cancer and represents a rapidly progressing field. ...

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