• Title/Summary/Keyword: and receptors

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G Protein-Coupled Receptors: Molecular Organization and Regulatory Mechanisms

  • Caron, Marc G.
    • Proceedings of the Korean Society of Applied Pharmacology
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    • 1994.04a
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    • pp.82-87
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    • 1994
  • Signal transduction through G protein-coupled receptors comprises three functional components, a receptor, a G protcin and a effector protein. Work over the last sevcral ycars has led to the characterization or virtually all of the components or these systems. what has come out or those studies is that these mechanisms of signal transduction are pervasive in nature being found in mammalian and avian species, as well as lower organisms such as yeast and slime mold. It is known that G protein-coupled receptors mediate the action of such diverse molecules such as small hormones and neurotransmitters, small peptide molecules as well as glycoprotein hormones and various sensory perceptions such as light, olfaction and most likely taste.

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Enantioselective Recognition of Amino Alcohols and Amino Acids by Chiral Binol-Based Aldehydes with Conjugated Rings at the Hydrogen Bonding Donor Sites

  • Kim, Ji-Young;Nandhakumar, Raju;Kim, Kwan-Mook
    • Bulletin of the Korean Chemical Society
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    • v.32 no.4
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    • pp.1263-1267
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    • 2011
  • Novel binol-based uryl and guanidinium receptors having higher ring conjugation at the periphery of the hydrogen bonding donor sites have been synthesized and utilized to study the enantioselective recognition of 1,2-aminoalcohols and chirality conversion of natural amino acids via imine bond formation. There is a remarkable decrease in the stereoselectivites as the conjugation increases at the periphery of hydrogen bonding donor sites. The guanidinium-based receptors show more selectivity towards the amino alcohol than that of the uryl based ones due to its charge reinforced hydrogen bonds. The conversion efficiency of L-amino acids to Damino acids by the uryl-based receptors is higher than that of the guanidinium-based ones.

Autophagy as an Innate Immune Modulator

  • Oh, Ji Eun;Lee, Heung Kyu
    • IMMUNE NETWORK
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    • v.13 no.1
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    • pp.1-9
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    • 2013
  • Autophagy is a fundamental cellular process in eukaryotic cells for maintaining homeostasis by degrading cellular proteins and organelles. Recently, the roles of autophagy have been expanded to immune systems, which in turn modulate innate immune responses. More specifically, autophagy acts as a direct effector for protection against pathogens, as well as a modulator of pathogen recognition and downstream signaling in innate immune responses. In addition, autophagy controls autoimmunity and inflammatory disorders by negative regulation of immune signaling. In this review, we focus on recent advances in the role of autophagy in innate immune systems.

A Naked Eye Detection of Fluoride with Urea Receptors Which have both an Azo Group and a Nitrophenyl Group as a Signaling Group

  • Dang, Nhat Tuan;Park, Jin-Joo;Jang, Soon-Min;Kang, Jong-Min
    • Bulletin of the Korean Chemical Society
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    • v.31 no.5
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    • pp.1204-1208
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    • 2010
  • Anion recognition via hydrogen-bonding interactions could be monitored with changes in UV-vis absorption spectra and in some cases easily monitored with naked eye. Urea receptors 1 and 2 connected with both an azo group and a nitrophenyl group as a signaling group for color change proved to be an efficient naked eye receptor for the fluoride ion. The anion recognition phenomena of the receptors 1 and 2 via hydrogen-bonding interactions were investigated through UV-vis absorption and $^1H$ NMR spectra.

Evolutionary and Comparative Genomics to Drive Rational Drug Design, with Particular Focus on Neuropeptide Seven-Transmembrane Receptors

  • Furlong, Michael;Seong, Jae Young
    • Biomolecules & Therapeutics
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    • v.25 no.1
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    • pp.57-68
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    • 2017
  • Seven transmembrane receptors (7TMRs), also known as G protein-coupled receptors, are popular targets of drug development, particularly 7TMR systems that are activated by peptide ligands. Although many pharmaceutical drugs have been discovered via conventional bulk analysis techniques the increasing availability of structural and evolutionary data are facilitating change to rational, targeted drug design. This article discusses the appeal of neuropeptide-7TMR systems as drug targets and provides an overview of concepts in the evolution of vertebrate genomes and gene families. Subsequently, methods that use evolutionary concepts and comparative analysis techniques to aid in gene discovery, gene function identification, and novel drug design are provided along with case study examples.

Changes in the Central Dopaminergic Systems in the Streptozotocin-induced Diabetic Rats

  • Lim, D.K.;Lee, K.M.;Ho, I.K.
    • Archives of Pharmacal Research
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    • v.17 no.6
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    • pp.398-404
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    • 1994
  • The behavioral response, depamine metabolism, and characteristics of dopamine subtypes after developing the hyperlycemia were studied in the striata of rats. In animals developed hyperglycemia, the on-set duration of cataleptic behavior responded to SCH 23390 injection was delayed abd shortened, respectively. However, the cataleptic response to spiperone occurred significantly earlier in on-set and prolonged in duration. Dopamine metabolites, dihydroxyphenylacetic acid (DDPAC) and homovanillic acid (HVA), were significantly reduced in teh striata of hyeprglycemic rats. However, level of DA was significantly increased. It is noted that the ratios of DOPAC and HVA to DA were decreased, suggesting decreased tumover of DA. The affinity of striatal D-1 receptors was significantly increased without changes in the number of binding sites, while the maximum binding number of D-2 recptors was significantly increased without affecting its affinity in the diabetic rats. These results indicate that the dopaminergic activity in striatia was altered in hyperglycemic rats. Furthermore, it suggests that the upregulation of dopamine receptors might be due to the decreased dopamine matabolism.

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Computational evaluation of interactions between olfactory receptor OR2W1 and its ligands

  • Oh, S. June
    • Genomics & Informatics
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    • v.19 no.1
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    • pp.9.1-9.5
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    • 2021
  • Mammalian olfactory receptors are a family of G protein-coupled receptors (GPCRs) that occupy a large part of the genome. In human genes, olfactory receptors account for more than 40% of all GPCRs. Several types of GPCR structures have been identified, but there is no single olfactory receptor whose structure has been determined experimentally to date. The aim of this study was to model the interactions between an olfactory receptor and its ligands at the molecular level to provide hints on the binding modes between the OR2W1 olfactory receptor and its agonists and inverse agonists. The results demonstrated the modes of ligand binding in a three-dimensional model of OR2W1 and showed a statistically significant difference in binding affinity to the olfactory receptor between agonists and inverse agonists.

Inhaled Volatile Molecules-Responsive TRP Channels as Non-Olfactory Receptors

  • Hyungsup Kim;Minwoo Kim;Yongwoo Jang
    • Biomolecules & Therapeutics
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    • v.32 no.2
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    • pp.192-204
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    • 2024
  • Generally, odorant molecules are detected by olfactory receptors, which are specialized chemoreceptors expressed in olfactory neurons. Besides odorant molecules, certain volatile molecules can be inhaled through the respiratory tract, often leading to pathophysiological changes in the body. These inhaled molecules mediate cellular signaling through the activation of the Ca2+-permeable transient receptor potential (TRP) channels in peripheral tissues. This review provides a comprehensive overview of TRP channels that are involved in the detection and response to volatile molecules, including hazardous substances, anesthetics, plant-derived compounds, and pheromones. The review aims to shed light on the biological mechanisms underlying the sensing of inhaled volatile molecules. Therefore, this review will contribute to a better understanding of the roles of TRP channels in the response to inhaled molecules, providing insights into their implications for human health and disease.

System-Wide Expression and Function of Olfactory Receptors in Mammals

  • Oh, S. June
    • Genomics & Informatics
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    • v.16 no.1
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    • pp.2-9
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    • 2018
  • Olfactory receptors (ORs) in mammals are generally considered to function as chemosensors in the olfactory organs of animals. They are membrane proteins that traverse the cytoplasmic membrane seven times and work generally by coupling to heterotrimeric G protein. The OR is a G protein-coupled receptor that binds the guanine nucleotide-binding $G{\alpha}_{olf}$ subunit and the $G{\beta}{\gamma}$ dimer to recognize a wide spectrum of organic compounds in accordance with its cognate ligand. Mammalian ORs were originally identified from the olfactory epithelium of rat. However, it has been recently reported that the expression of ORs is not limited to the olfactory organ. In recent decades, they have been found to be expressed in diverse organs or tissues and even tumors in mammals. In this review, the expression and expected function of olfactory receptors that exist throughout an organism's system are discussed.

Ethanol Extract of Polygalae Radix Augments Pentobarbital-Induced Sleeping Behaviors through $GABA_Aergic$ Systems

  • Lee, Chung-Il;Lee, Mi Kyeong;Oh, Ki-Wan
    • Natural Product Sciences
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    • v.19 no.2
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    • pp.179-185
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    • 2013
  • Polygalae radix (PR) has traditionally been used as a sedative and anti-stress agent in oriental countries for a long time. PR which contains many ingredients is especially rich in saponins. This study was performed to investigate whether ethanol extract of PR enhances pentobarbital-induced sleep behaviors. In addition, possible mechanisms also were investigated. PR inhibited locomotor activity in mice. PR increased sleep rate and sleep time by concomitant administration with sub-hypnotic dose of pentobarbital (28 mg/kg). PR prolonged total sleeping time, and shortened sleep latency induced by pentobarbital (42 mg/kg). In addition, PR increased intracellular chloride concentration in primary cultured neuronal cells. The expression level of glutamic acid decarboxylase (GAD) were increased, and ${\gamma}$-aminobutyric acid $(GABA)_A$ receptors subunits were modulated by PR, especially increasing ${\gamma}$-subunit expression. In conclusion, PR augments penobarbital-induced sleep behaviors through activation of $GABA_A$ receptors and chloride channel complex.