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Journal articles on the topic 'Receptors'

Author: Grafiati

Published: 4 June 2021

Last updated: 25 July 2025

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1

Tibrewal, Richa, Reynoldly Kharsyntiew, Farida Dawood, and Archana Sharma. "A REVIEW ON G-PROTEIN COUPLED RECEPTOR." International Journal of Current Pharmaceutical Review and Research 13, no. 04 (2021): 01–09. https://doi.org/10.5281/zenodo.12664417.

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AbstractG protein–coupled receptors (GPCRs), also known as seven-(pass)-transmembrane domainreceptors, 7TM receptors, heptahelical receptors, serpentine receptor, and G protein–linkedreceptors (GPLR), constitute a large protein family of receptors that detect molecules outsidethe cell and activate internal signal transduction pathways and, ultimately, cellular responses.Coupling with G proteins, they are called seven-transmembrane receptors because they passthrough the cell membrane seven times. G protein–coupled receptors are found only ineukaryotes, including yeast, choanof

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2

Jaremko, William J., Zhen Huang, Wei Wen, Andrew Wu, Nicholas Karl, and Li Niu. "Identification and characterization of RNA aptamers: A long aptamer blocks the AMPA receptor and a short aptamer blocks both AMPA and kainate receptors." Journal of Biological Chemistry 292, no. 18 (2017): 7338–47. http://dx.doi.org/10.1074/jbc.m116.774752.

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AMPA and kainate receptors, along with NMDA receptors, represent different subtypes of glutamate ion channels. AMPA and kainate receptors share a high degree of sequence and structural similarities, and excessive activity of these receptors has been implicated in neurological diseases such as epilepsy. Therefore, blocking detrimental activity of both receptor types could be therapeutically beneficial. Here, we report the use of an in vitro evolution approach involving systematic evolution of ligands by exponential enrichment with a single AMPA receptor target (i.e. GluA1/2R) to isolate RNA apt

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3

Santiago, Luis, and Ravinder Abrol. "Understanding G Protein Selectivity of Muscarinic Acetylcholine Receptors Using Computational Methods." International Journal of Molecular Sciences 20, no. 21 (2019): 5290. http://dx.doi.org/10.3390/ijms20215290.

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The neurotransmitter molecule acetylcholine is capable of activating five muscarinic acetylcholine receptors, M1 through M5, which belong to the superfamily of G-protein-coupled receptors (GPCRs). These five receptors share high sequence and structure homology; however, the M1, M3, and M5 receptor subtypes signal preferentially through the Gαq/11 subset of G proteins, whereas the M2 and M4 receptor subtypes signal through the Gαi/o subset of G proteins, resulting in very different intracellular signaling cascades and physiological effects. The structural basis for this innate ability of the M1

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4

Steverding, Dietmar. "Cycle Numbers of Cell Surface Recycling Receptors." Receptors 2, no. 2 (2023): 160–65. http://dx.doi.org/10.3390/receptors2020010.

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The cycle number (nc) of a recycling receptor is defined as the average number of round trips (cell surface–endosome–cell surface) the receptor can make before it is degraded. This characteristic parameter of recycling receptors can be easily determined from the receptor’s half-life (t½, the time in which 50% of the receptor is degraded) and cycling time (Tc, the time a receptor needs to complete a round trip). Relationship analyses revealed that nc increases linearly with increasing t½ and decreases exponentially with increasing Tc. For commonly observed t½ and Tc values, it was calculated th

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Melkes, Barbora, Vendula Markova, Lucie Hejnova та Jiri Novotny. "β-Arrestin 2 and ERK1/2 Are Important Mediators Engaged in Close Cooperation between TRPV1 and µ-Opioid Receptors in the Plasma Membrane". International Journal of Molecular Sciences 21, № 13 (2020): 4626. http://dx.doi.org/10.3390/ijms21134626.

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The interactions between TRPV1 and µ-opioid receptors (MOR) have recently attracted much attention because these two receptors play important roles in pain pathways and can apparently modulate each other’s functioning. However, the knowledge about signaling interactions and crosstalk between these two receptors is still limited. In this study, we investigated the mutual interactions between MOR and TRPV1 shortly after their activation in HEK293 cells expressing these two receptors. After activation of one receptor we observed significant changes in the other receptor’s lateral mobility and vic

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6

Jia, Huilin, Xingli He, Tengfei Jiang, and Fanzhi Kong. "Roles of Bile Acid-Activated Receptors in Monocytes-Macrophages and Dendritic Cells." Cells 14, no. 12 (2025): 920. https://doi.org/10.3390/cells14120920.

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Bile acids (BAs), essential for lipid metabolism and fat-soluble vitamin absorption, also act as signaling molecules that regulate immune homeostasis. This review focuses on the roles of four key BA-activated receptors, farnesoid X receptor (FXR), G protein-coupled bile acid receptor 1 (GPBAR1), liver X receptors (LXRs), and vitamin D receptor (VDR), in modulating the functions of monocytes-macrophages, and dendritic cells (DCs). The biological synthesis, transport, and metabolism of BAs were discussed and highlighted the feedback mechanisms regulating the synthesis and enterohepatic circulati

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Roddey, J. C., and G. A. Jacobs. "Information theoretic analysis of dynamical encoding by filiform mechanoreceptors in the cricket cercal system." Journal of Neurophysiology 75, no. 4 (1996): 1365–76. http://dx.doi.org/10.1152/jn.1996.75.4.1365.

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1. The stimulus/response properties of 20 mechanosensory receptors in the cricket cercal sensory system were studied using electrophysiological techniques. These receptors innervated filiform hairs of various lengths and directional selectivities. Previous studies have characterized the sensitivity of such cells to the direction of air currents and to the amplitude of sinusoidal stimuli. In the experiments reported here, the quantity and quality of information encoded in the receptors' elicited responses about the dynamics of more complex air current waveforms were characterized. 2. Based on a

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8

Xie, Peng, Junjie Zhang, Baiyu Chen, et al. "Computational Methods for Understanding the Selectivity and Signal Transduction Mechanism of Aminomethyl Tetrahydronaphthalene to Opioid Receptors." Molecules 27, no. 7 (2022): 2173. http://dx.doi.org/10.3390/molecules27072173.

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Opioid receptors are members of the group of G protein-couple receptors, which have been proven to be effective targets for treating severe pain. The interactions between the opioid receptors and corresponding ligands and the receptor’s activation by different agonists have been among the most important fields in opioid research. In this study, with compound M1, an active metabolite of tramadol, as the clue compound, several aminomethyl tetrahydronaphthalenes were designed, synthesized and assayed upon opioid receptors. With the resultant compounds FW-AII-OH-1 (Ki = 141.2 nM for the κ opioid r

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9

Wicher, Dieter, and Fabio Miazzi. "Functional properties of insect olfactory receptors: ionotropic receptors and odorant receptors." Cell and Tissue Research 383, no. 1 (2021): 7–19. http://dx.doi.org/10.1007/s00441-020-03363-x.

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AbstractThe majority of insect olfactory receptors belong to two distinct protein families, the ionotropic receptors (IRs), which are related to the ionotropic glutamate receptor family, and the odorant receptors (ORs), which evolved from the gustatory receptor family. Both receptor types assemble to heteromeric ligand-gated cation channels composed of odor-specific receptor proteins and co-receptor proteins. We here present in short the current view on evolution, function, and regulation of IRs and ORs. Special attention is given on how their functional properties can meet the environmental a

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10

Wajant, Harald. "Death receptors." Essays in Biochemistry 39 (October 1, 2003): 53–71. http://dx.doi.org/10.1042/bse0390053.

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Death receptors [Fas/Apo-1/CD95, TNF-R1 [tumour necrosis factor (TNF) receptor 1], DR3 [death receptor 3], TRAIL-R1 [TNF-related apoptosis-inducing ligand receptor 1], TRAIL-R2, DR6, p75-NGFR [p75-nerve growth factor receptor], EDAR [ectodermal dysplasia receptor]] form a subgroup of the TNF-R superfamily that can induce apoptosis (programmed cell death) via a conserved cytoplasmic signalling module termed the death domain. Although death receptors have been recognized mainly as apoptosis inducers, there is growing evidence that these receptors also fulfil a variety of nonapoptotic functions.

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11

Christopoulos, A., L. T. May, V. A. Avlani, and P. M. Sexton. "G-protein-coupled receptor allosterism: the promise and the problem(s)." Biochemical Society Transactions 32, no. 5 (2004): 873–77. http://dx.doi.org/10.1042/bst0320873.

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Allosteric modulators of G-protein-coupled receptors interact with binding sites that are topographically distinct from the orthosteric site recognized by the receptor's endogenous agonist. Allosteric ligands offer a number of advantages over orthosteric drugs, including the potential for greater receptor subtype selectivity and a more ‘physiological’ regulation of receptor activity. However, the manifestations of allosterism at G-protein-coupled receptors are quite varied, and significant challenges remain for the optimization of screening methods to ensure the routine detection and validatio

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12

Rossokhin, Alexey V., та Irina N. Sharonova. "Structural pharmacology of GABAА receptors". Annals of Clinical and Experimental Neurology 15, № 4 (2021): 44–53. http://dx.doi.org/10.54101/acen.2021.4.5.

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Gamma-aminobutyric acid (GABA) is the main inhibitory neurotransmitter in the mammalian central nervous system (CNS), activating the inotropic type A receptors (GABAА receptors) to provide fast inhibition. GABAА receptors are the main target for various groups of drugs that are widely used in the treatment of CNS disorders. This review examines the relationship between the physiological effects of GABAА receptor activation and modulation by various substances (including medicinal compounds), the receptor's structure, and the interaction of these substances with specific modulatory sites.

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13

Trebesova, Hanna, Guendalina Olivero, Mario Marchi та Massimo Grilli. "The Anti-Aggregative Peptide KLVFF Mimics Aβ1-40 in the Modulation of Nicotinic Receptors: Implications for Peptide-Based Therapy". Biomedicines 10, № 9 (2022): 2231. http://dx.doi.org/10.3390/biomedicines10092231.

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In recent years, the inhibition of beta-amyloid (Aβ) aggregation has emerged as a potential strategy for Alzheimer’s disease. KLVFF, a small peptide corresponding to the aminoacidic sequence 16-20 of Aβ, reduces Aβ fibrillation dose dependently. Therefore, the toxic and functional characterization of its brain activity is fundamental for clarifying its potential therapeutic role. Accordingly, we studied the modulatory role of KLVFF on the cholinergic receptors regulating dopamine and noradrenaline release in rat synaptosomes. Nicotinic receptors on dopaminergic nerve terminals in the nucleus a

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14

Okusa, Mark D., Liping Huang, Akemi Momose-Hotokezaka, Long P. Huynh, and Amy J. Mangrum. "Regulation of adenylyl cyclase in polarized renal epithelial cells by G protein-coupled receptors." American Journal of Physiology-Renal Physiology 273, no. 6 (1997): F883—F891. http://dx.doi.org/10.1152/ajprenal.1997.273.6.f883.

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We employed two guanine nucleotide binding protein (G protein)-coupled receptors known to be targeted to opposite domains in renal epithelial cells to test the hypothesis that the polarized receptor expression of receptors regulates the activity of the receptor’s effector molecule, adenylyl cyclase. We used LLC-PK1 cells stably transfected with cDNA encoding the α2B-adrenergic receptor (α2B-AR) or A1-adenosine receptor (A1-AdR). Immunohistochemistry and Western blot analysis confirmed the basolateral and apical expression of α2B-ARs and A1-AdRs, respectively. Adenylyl cyclase activity was asse

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15

Wank, S. A. "Cholecystokinin receptors." American Journal of Physiology-Gastrointestinal and Liver Physiology 269, no. 5 (1995): G628—G646. http://dx.doi.org/10.1152/ajpgi.1995.269.5.g628.

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The cholecystokinin (CCK) and gastrin families of peptides act as hormones and neuropeptides on central and peripheral CCK receptors to mediate secretion and motility in the gastrointestinal (GI) tract in the physiological response to a normal meal. CCK and its receptors are also widely distributed in the central nervous system (CNS) and contribute to the regulation of satiety, anxiety, analgesia, and dopamine-mediated behavior. Although the wide distribution, myriad number of functions, and reported pharmacological heterogeneity of CCK receptors would suggest a large number of receptor subtyp

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16

Gado, Francesca, Serena Meini, Simone Bertini, Maria Digiacomo, Marco Macchia, and Clementina Manera. "Allosteric modulators targeting cannabinoid cb1 and cb2 receptors: implications for drug discovery." Future Medicinal Chemistry 11, no. 15 (2019): 2019–37. http://dx.doi.org/10.4155/fmc-2019-0005.

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Allosteric modulators of cannabinoid receptors hold great therapeutic potential, as they do not possess intrinsic efficacy, but instead enhance or diminish the receptor's response of orthosteric ligands allowing for the tempering of cannabinoid receptor signaling without the desensitization, tolerance and dependence. Allosteric modulators of cannabinoid receptors have numerous advantages over the orthosteric ligands such as higher receptor type selectivity, probe dependence and biased signaling, so they have a great potential to separate the therapeutic benefits from side effects own of orthos

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17

Doukhanina, Elena V., Nestor R. Apuya, Hye-Dong Yoo, et al. "Expression of Human Nuclear Receptors in Plants for the Discovery of Plant-Derived Ligands." Journal of Biomolecular Screening 12, no. 3 (2007): 385–95. http://dx.doi.org/10.1177/1087057107299255.

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Plants have the potential to produce a wide array of secondary metabolites that have utility as drugs to treat human diseases. To tap this potential, functional human nuclear receptors have been expressed in plants to create in planta screening assays as a tool to discover natural product ligands. Assays have been designed and validated using 3 nuclear receptors: the estrogen receptor (ER), the androgen receptor (AR), and the heterodimeric retinoid X receptor-α plus thyroid hormone receptorβ (RXRA/THRB). Nuclear receptor—reporter constructs have been expressed in plants to detect the presence

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18

Ide, Hiroki, and Hiroshi Miyamoto. "Steroid Hormone Receptor Signals as Prognosticators for Urothelial Tumor." Disease Markers 2015 (2015): 1–12. http://dx.doi.org/10.1155/2015/840640.

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There is a substantial amount of preclinical or clinical evidence suggesting that steroid hormone receptor-mediated signals play a critical role in urothelial tumorigenesis and tumor progression. These receptors include androgen receptor, estrogen receptors, glucocorticoid receptor, progesterone receptor, vitamin D receptor, retinoid receptors, peroxisome proliferator-activated receptors, and others including orphan receptors. In particular, studies using urothelial cancer tissue specimens have demonstrated that elevated or reduced expression of these receptors as well as alterations of their

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19

Ayyad, Rezk R., Ahmed M. Mansour, Ahmed M. Nejm, Yasser Abdel Allem Hassan, and Ahmed R. Ayyad. "The Direct Cholinomimetics and Cholinergic Blocking Agents Depend on Stereo Specificity of Cholinergic Receptors." Current Research in Medical Sciences 3, no. 2 (2024): 1–7. http://dx.doi.org/10.56397/crms.2024.06.01.

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The cholinergic receptors are the site of action of acetylcholine (Ach) and acetylcholine like substance and anti-cholinergic agents, these receptors either muscarinic receptors or nicotinic receptors the exactly difference between them the area of receptor, where the muscarinic receptor is short than nicotinic receptor (nearly 4.5 and 6 Angstrom, respectively) and the muscarine act on muscarinic receptors and nicotine act on nicotinic receptors. The direct cholinomimetics and cholinergic blocking agents are characterized by chemical features adjustment with these receptors. This can be explai

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20

Johnson, L. S., K. W. Dunn, B. Pytowski, and T. E. McGraw. "Endosome acidification and receptor trafficking: bafilomycin A1 slows receptor externalization by a mechanism involving the receptor's internalization motif." Molecular Biology of the Cell 4, no. 12 (1993): 1251–66. http://dx.doi.org/10.1091/mbc.4.12.1251.

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To examine the relationship between endosome acidification and receptor trafficking, transferrin receptor trafficking was characterized in Chinese hamster ovary cells in which endosome acidification was blocked by treatment with the specific inhibitor of the vacuolar H(+)-ATPase, bafilomycin A1. Elevating endosome pH slowed the receptor externalization rate to approximately one-half of control but did not affect receptor internalization kinetics. The slowed receptor externalization required the receptor's cytoplasmic domain and was largely eliminated by substitutions replacing either of two ar

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21

Mao, S. Y., J. R. Pfeiffer, J. M. Oliver, and H. Metzger. "Effects of subunit mutation on the localization to coated pits and internalization of cross-linked IgE-receptor complexes." Journal of Immunology 151, no. 5 (1993): 2760–74. http://dx.doi.org/10.4049/jimmunol.151.5.2760.

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Abstract IgE receptors of mast cells, Fc epsilon RI, localize to coated pits and internalize after cross-linking. We investigated whether any one of the receptor's four distinctive cytoplasmic domains regulates these phenomena. COS cells, which lack Fc epsilon RI entirely, and P815 mouse mastocytoma cells that lack the alpha and beta subunits of the tetrameric Fc epsilon RI (alpha beta gamma 2), were transfected with wild-type, incomplete, or variant Fc epsilon RI. IgE-receptor complexes were observed by electron microscopy. Before cross-linking with anti-IgE gold particles, receptors were not

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22

Liu, Xiangyu, Ali Masoudi, Alem W. Kahsai та ін. "Mechanism of β2AR regulation by an intracellular positive allosteric modulator". Science 364, № 6447 (2019): 1283–87. http://dx.doi.org/10.1126/science.aaw8981.

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Drugs targeting the orthosteric, primary binding site of G protein–coupled receptors are the most common therapeutics. Allosteric binding sites, elsewhere on the receptors, are less well-defined, and so less exploited clinically. We report the crystal structure of the prototypic β2-adrenergic receptor in complex with an orthosteric agonist and compound-6FA, a positive allosteric modulator of this receptor. It binds on the receptor’s inner surface in a pocket created by intracellular loop 2 and transmembrane segments 3 and 4, stabilizing the loop in an α-helical conformation required to engage

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23

Jose, P. A., J. R. Raymond, M. D. Bates, A. Aperia, R. A. Felder, and R. M. Carey. "The renal dopamine receptors." Journal of the American Society of Nephrology 2, no. 8 (1992): 1265–78. http://dx.doi.org/10.1681/asn.v281265.

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Dopamine is an endogenous catecholamine that modulates many functions including behavior, movement, nerve conduction, hormone synthesis and release, blood pressure, and ion fluxes. Dopamine receptors in the brain have been classically divided into D1 and D2 subtypes, based on pharmacological data. However, molecular biology techniques have identified many more dopamine receptor subtypes. Several of the receptors cloned from the brain correspond to the classically described D1 and D2 receptors. Several D1 receptor subtypes have been cloned (D1A, D1B, and D5) and are each coupled to the stimulat

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Cato, A. C., and H. Ponta. "Different regions of the estrogen receptor are required for synergistic action with the glucocorticoid and progesterone receptors." Molecular and Cellular Biology 9, no. 12 (1989): 5324–30. http://dx.doi.org/10.1128/mcb.9.12.5324-5330.1989.

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Estrogen and progesterone or estrogen and glucocorticoid receptors functionally cooperate in gene activation if their cognate binding sites are close to one another. These interactions have been described as synergism of action of the steroid receptors. The mechanism by which synergism is achieved is not clear, although protein-protein interaction of the receptors is one of the favorite models. In transfection experiments with receptor expression vectors and a reporter gene containing estrogen and progesterone-glucocorticoid receptor binding sites, we have examined the effects that different p

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Cato, A. C., and H. Ponta. "Different regions of the estrogen receptor are required for synergistic action with the glucocorticoid and progesterone receptors." Molecular and Cellular Biology 9, no. 12 (1989): 5324–30. http://dx.doi.org/10.1128/mcb.9.12.5324.

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Estrogen and progesterone or estrogen and glucocorticoid receptors functionally cooperate in gene activation if their cognate binding sites are close to one another. These interactions have been described as synergism of action of the steroid receptors. The mechanism by which synergism is achieved is not clear, although protein-protein interaction of the receptors is one of the favorite models. In transfection experiments with receptor expression vectors and a reporter gene containing estrogen and progesterone-glucocorticoid receptor binding sites, we have examined the effects that different p

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26

Mattová, Simona, and Terézia Kisková. "P2X receptory a ich možné využitie pri liečbe rakoviny." Laboratórna Diagnostika XXIX, no. 1/2024 (2024): 70–75. https://doi.org/10.5281/zenodo.12531964.

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<strong>Súhrn</strong> Rakovina patrí medzi závažné a rozmanité ochorenie, ktoré je jednou z hlavných príčin úmrtnosti na celom svete. V súčasnosti sa v boji proti rakovine využívajú liečebné postupy, medzi ktoré patrí chemoterapia, ožarovanie, cielená liečba a imunoterapia. Tieto liečebné postupy v&scaron;ak nie sú vždy dostačujúce, pričom najväč&scaron;í problém predstavuje rezistencia na liečbu. Je preto potrebn&eacu

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27

Ecke, Denise, Theodor Hanck, Mohan E. Tulapurkar, et al. "Hetero-oligomerization of the P2Y11 receptor with the P2Y1 receptor controls the internalization and ligand selectivity of the P2Y11 receptor." Biochemical Journal 409, no. 1 (2007): 107–16. http://dx.doi.org/10.1042/bj20070671.

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Nucleotides signal through purinergic receptors such as the P2 receptors, which are subdivided into the ionotropic P2X receptors and the metabotropic P2Y receptors. The diversity of functions within the purinergic receptor family is required for the tissue-specificity of nucleotide signalling. In the present study, hetero-oligomerization between two metabotropic P2Y receptor subtypes is established. These receptors, P2Y1 and P2Y11, were found to associate together when co-expressed in HEK293 cells. This association was detected by co-pull-down, immunoprecipitation and FRET (fluorescence resona

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28

Stephenson, F. A. "Structure and trafficking of NMDA and GABAA receptors." Biochemical Society Transactions 34, no. 5 (2006): 877–81. http://dx.doi.org/10.1042/bst0340877.

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The fidelity of synaptic function is dependent on the expression of the appropriate neurotransmitter receptor subtype, the targeting and trafficking of receptors to synapses as well as the regulation of the actual number of receptors at synapses. GABAA (γ-aminobutyric acid type A) receptors and NMDA (N-methyl-D-aspartate) receptors are both examples of ligand-gated, heteromeric neurotransmitter receptors whose cell-surface expression is dynamic and tightly regulated. NMDA receptors are localized at excitatory synapses. These synapses are highly structured but dynamic, with the interplay betwee

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Srejovic, Ivan, Vladimir Jakovljevic, Vladimir Zivkovic, and Dragan Djuric. "Possible Role of N-Methyl-D-Aspartate Receptors in Physiology and Pathophysiology of Cardiovascular System." Serbian Journal of Experimental and Clinical Research 20, no. 1 (2019): 3–13. http://dx.doi.org/10.1515/sjecr-2017-0010.

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Abstract N-methyl-D-aspartate (NMDA) receptors belong to ionotropic glutamate receptor family, together with α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptors, kainite receptors and δ-receptors. All of these receptors are tetramers composed of four subunits. NMDA receptors have several unique features in relation to other ionotropic glutamate receptors: requirement for simultaneous action of two coagonists, glutamate and glycine; dual control of receptor activation, ligand-dependent (by glutamate and glycine) and voltage-dependent (Mg2+ block) control; and influx of conside

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Baker, ME. "Adrenal and sex steroid receptor evolution: environmental implications." Journal of Molecular Endocrinology 26, no. 2 (2001): 119–25. http://dx.doi.org/10.1677/jme.0.0260119.

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The nuclear receptor family responds to a diverse group of ligands, including steroids, retinoids, thyroid hormone, prostaglandins and fatty acids. Previous sequence analyses of adrenal and sex steroid receptors indicate that they form a clade separate from other nuclear receptors. However, the relationships of adrenal and sex steroid receptors to each other and to their ancestors are not fully understood. We have used new information from androgen, estrogen, mineralocorticoid and progesterone receptors in fish to better resolve the phylogeny of adrenal and sex steroid receptors. Sequence dive

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del Mármol, Josefina, Mackenzie A. Yedlin, and Vanessa Ruta. "The structural basis of odorant recognition in insect olfactory receptors." Nature 597, no. 7874 (2021): 126–31. http://dx.doi.org/10.1038/s41586-021-03794-8.

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AbstractOlfactory systems must detect and discriminate amongst an enormous variety of odorants1. To contend with this challenge, diverse species have converged on a common strategy in which odorant identity is encoded through the combinatorial activation of large families of olfactory receptors1–3, thus allowing a finite number of receptors to detect a vast chemical world. Here we offer structural and mechanistic insight into how an individual olfactory receptor can flexibly recognize diverse odorants. We show that the olfactory receptor MhOR5 from the jumping bristletail4Machilis hrabei assem

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Sheppard, Karen E. "II. Intestinal corticosteroid receptors." American Journal of Physiology-Gastrointestinal and Liver Physiology 282, no. 5 (2002): G742—G746. http://dx.doi.org/10.1152/ajpgi.00531.2001.

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Two corticosteroid receptors have been cloned; they are the glucocorticoid receptor and the mineralocorticoid receptor. These receptors are members of the steroid/thyroid/retinoid receptor family of nuclear transactivating factors, which are characterized by two highly conserved zinc fingers in the central DNA binding domain, a COOH-terminal domain that encompasses the ligand binding site, and a variable NH2-terminal domain. In addition to these cloned receptors, other corticosteroid receptors have recently been identified in intestine. Steroid binding studies have identified two novel putativ

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Cottrell, Jeffrey R., Gilles R. Dubé, Christophe Egles, and Guosong Liu. "Distribution, Density, and Clustering of Functional Glutamate Receptors Before and After Synaptogenesis in Hippocampal Neurons." Journal of Neurophysiology 84, no. 3 (2000): 1573–87. http://dx.doi.org/10.1152/jn.2000.84.3.1573.

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Postsynaptic differentiation during glutamatergic synapse formation is poorly understood. Using a novel biophysical approach, we have investigated the distribution and density of functional glutamate receptors and characterized their clustering during synaptogenesis in cultured hippocampal neurons. We found that functional α-amino-3-hydroxy-5-methyl-4-isoxazolpropionate (AMPA) and N-methyl-d-aspartate (NMDA) receptors are evenly distributed in the dendritic membrane before synaptogenesis with an estimated density of 3 receptors/μm2. Following synaptogenesis, functional AMPA and NMDA receptors

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Althumairy, Duaa, Xiaoping Zhang, Nicholas Baez, et al. "Glycoprotein G-protein Coupled Receptors in Disease: Luteinizing Hormone Receptors and Follicle Stimulating Hormone Receptors." Diseases 8, no. 3 (2020): 35. http://dx.doi.org/10.3390/diseases8030035.

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Signal transduction by luteinizing hormone receptors (LHRs) and follicle-stimulating hormone receptors (FSHRs) is essential for the successful reproduction of human beings. Both receptors and the thyroid-stimulating hormone receptor are members of a subset of G-protein coupled receptors (GPCRs) described as the glycoprotein hormone receptors. Their ligands, follicle-stimulating hormone (FSH) and luteinizing hormone (LH) and a structurally related hormone produced in pregnancy, human chorionic gonadotropin (hCG), are large protein hormones that are extensively glycosylated. Although the primary

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Soos, M. A., and K. Siddle. "Immunological relationships between receptors for insulin and insulin-like growth factor I. Evidence for structural heterogeneity of insulin-like growth factor I receptors involving hybrids with insulin receptors." Biochemical Journal 263, no. 2 (1989): 553–63. http://dx.doi.org/10.1042/bj2630553.

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The receptors for insulin and insulin-like growth factor-I (IGF-I) are closely related in primary sequence and overall structure. We have examined the immunological relationships between these receptors by testing the reactivity of anti-(insulin receptor) monoclonal antibodies with IGF-I receptors in various tissues and cell lines. Antibodies for six distinct epitopes reacted with a subfraction of IGF-I receptors, as shown by inhibition of 125I-IGF-I binding, precipitation of 125I-IGF-I-receptor complexes or immunodepletion of receptor from tissue extracts before binding assays. Both immunorea

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Khatri, Shailesh N., Wan-Chen Wu, Ying Yang, and Jason R. Pugh. "Direction of action of presynaptic GABAA receptors is highly dependent on the level of receptor activation." Journal of Neurophysiology 121, no. 5 (2019): 1896–905. http://dx.doi.org/10.1152/jn.00779.2018.

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Many synapses, including parallel fiber synapses in the cerebellum, express presynaptic GABAA receptors. However, reports of the functional consequences of presynaptic GABAA receptor activation are variable across synapses, from inhibition to enhancement of transmitter release. We find that presynaptic GABAA receptor function is bidirectional at parallel fiber synapses depending on GABA concentration and modulation of GABAA receptors in mice. Activation of GABAA receptors by low GABA concentrations enhances glutamate release, whereas activation of receptors by higher GABA concentrations inhibi

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Wetter, Justin A., Chetana Revankar та Bonnie J. Hanson. "Utilization of the TangoTM β-Arrestin Recruitment Technology for Cell-Based EDG Receptor Assay Development and Interrogation". Journal of Biomolecular Screening 14, № 9 (2009): 1134–41. http://dx.doi.org/10.1177/1087057109343809.

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Cellular assay development for the endothelial differentiation gene (EDG) family of G-protein-coupled receptors (GPCRs) and related lysophospholipid (LP) receptors is complicated by endogenous receptor expression and divergent receptor signaling. Endogenously expressed LP receptors exist in most tissue culture cell lines. these LP receptors, along with other endogenously expressed GPCRs, contribute to off-target signaling that can complicate interpretation of second-messenger-based cellular assay results. these receptors also activate a diverse and divergent set of cellular signaling pathways,

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Waage, A., N. Liabakk, E. Lien, J. Lamvik, and T. Espevik. "p55 and p75 tumor necrosis factor receptors in patients with chronic lymphocytic leukemia." Blood 80, no. 10 (1992): 2577–83. http://dx.doi.org/10.1182/blood.v80.10.2577.2577.

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Abstract We studied the expression of the two tumor necrosis factor (TNF) receptors, p55 and p75, on B cells from patients with chronic lymphocytic leukemia (CLL), and the presence of soluble TNF receptors in serum. Expression of membrane-associated receptors was quantified by double labeling of peripheral blood mononuclear cells (PBMC) with monoclonal antibodies against CD19 and p55/p75 TNF receptors and flow cytometry. A high fraction of the CD19+ cells expressed the p55 receptor (44% +/- 34% [SD]) and p75 receptor (61% +/- 31%). In healthy controls, 0% to 1% of the CD19+ cells expressed the

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Waage, A., N. Liabakk, E. Lien, J. Lamvik, and T. Espevik. "p55 and p75 tumor necrosis factor receptors in patients with chronic lymphocytic leukemia." Blood 80, no. 10 (1992): 2577–83. http://dx.doi.org/10.1182/blood.v80.10.2577.bloodjournal80102577.

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We studied the expression of the two tumor necrosis factor (TNF) receptors, p55 and p75, on B cells from patients with chronic lymphocytic leukemia (CLL), and the presence of soluble TNF receptors in serum. Expression of membrane-associated receptors was quantified by double labeling of peripheral blood mononuclear cells (PBMC) with monoclonal antibodies against CD19 and p55/p75 TNF receptors and flow cytometry. A high fraction of the CD19+ cells expressed the p55 receptor (44% +/- 34% [SD]) and p75 receptor (61% +/- 31%). In healthy controls, 0% to 1% of the CD19+ cells expressed the p55 rece

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Johnstone, Elizabeth K. M., and Kevin D. G. Pfleger. "Profiling novel pharmacology of receptor complexes using Receptor-HIT." Biochemical Society Transactions 49, no. 4 (2021): 1555–65. http://dx.doi.org/10.1042/bst20201110.

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Many receptors are able to undergo heteromerisation, leading to the formation of receptor complexes that may have pharmacological profiles distinct from those of the individual receptors. As a consequence of this, receptor heteromers can be classed as new drug targets, with the potential for achieving greater specificity and selectivity over targeting their constituent receptors. We have developed the Receptor-Heteromer Investigation Technology (Receptor-HIT), which enables the detection of receptor heteromers using a proximity-based reporter system such as bioluminescence resonance energy tra

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Anders, Robert A., Sandra L. Arline, Jules J. E. Doré та Edward B. Leof. "Distinct Endocytic Responses of Heteromeric and Homomeric Transforming Growth Factor β Receptors". Molecular Biology of the Cell 8, № 11 (1997): 2133–43. http://dx.doi.org/10.1091/mbc.8.11.2133.

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Transforming growth factor β (TGFβ) family ligands initiate a cascade of events capable of modulating cellular growth and differentiation. The receptors responsible for transducing these cellular signals are referred to as the type I and type II TGFβ receptors. Ligand binding to the type II receptor results in the transphosphorylation and activation of the type I receptor. This heteromeric complex then propagates the signal(s) to downstream effectors. There is presently little data concerning the fate of TGFβ receptors after ligand binding, with conflicting reports indicating no change or decr

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Agnati, Luigi F., Giuseppina Leo, Susanna Genedani, Diego Guidolin, Nicola Andreoli, and Kjell Fuxe. "Possible Relevance of Receptor-Receptor Interactions between Viral- and Host-Coded Receptors for Viral-Induced Disease." Scientific World JOURNAL 7 (2007): 1073–81. http://dx.doi.org/10.1100/tsw.2007.166.

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It has been demonstrated that some viruses, such as the cytomegalovirus, code for G-protein coupled receptors not only to elude the immune system, but also to redirect cellular signaling in the receptor networks of the host cells. In view of the existence of receptor-receptor interactions, the hypothesis is introduced that these viral-coded receptors not only operate as constitutively active monomers, but also can affect other receptor function by interacting with receptors of the host cell. Furthermore, it is suggested that viruses could also insert not single receptors (monomers), but cluste

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Kashles, O., Y. Yarden, R. Fischer, A. Ullrich, and J. Schlessinger. "A dominant negative mutation suppresses the function of normal epidermal growth factor receptors by heterodimerization." Molecular and Cellular Biology 11, no. 3 (1991): 1454–63. http://dx.doi.org/10.1128/mcb.11.3.1454-1463.1991.

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Recent studies provide evidence that defective receptors can function as a dominant negative mutation suppressing the action of wild-type receptors. This causes various diminished responses in cell culture and developmental disorders in murine embryogenesis. Here, we describe a model system and a potential mechanism underlying the dominant suppressing response caused by defective epidermal growth factor (EGF) receptors. We used cultured 3T3 cells coexpressing human wild-type receptors and an inactive deletion mutant lacking most of the cytoplasmic domain. When expressed alone, EGF was able to

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Kashles, O., Y. Yarden, R. Fischer, A. Ullrich, and J. Schlessinger. "A dominant negative mutation suppresses the function of normal epidermal growth factor receptors by heterodimerization." Molecular and Cellular Biology 11, no. 3 (1991): 1454–63. http://dx.doi.org/10.1128/mcb.11.3.1454.

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Recent studies provide evidence that defective receptors can function as a dominant negative mutation suppressing the action of wild-type receptors. This causes various diminished responses in cell culture and developmental disorders in murine embryogenesis. Here, we describe a model system and a potential mechanism underlying the dominant suppressing response caused by defective epidermal growth factor (EGF) receptors. We used cultured 3T3 cells coexpressing human wild-type receptors and an inactive deletion mutant lacking most of the cytoplasmic domain. When expressed alone, EGF was able to

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Wang, Kemo, and Jian Liu. "Needling Sensation Receptor of an Acupoint Supplied by the Median Nerve - Studies of their Electro-Physiological Characteristics." American Journal of Chinese Medicine 17, no. 03n04 (1989): 145–55. http://dx.doi.org/10.1142/s0192415x89000231.

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We classified 50 receptor units from 10 acupoints supplied by the medium nerve. It was found that the needling stimulation mostly excited slowly adapting receptors and that the classification of acupoint receptors related closely to their location. For example, the Shanyang, Zhongchong, Shaoshang acupoints in the skin needling sensation receptors are touch or pressure receptor units; the receptors of Neiguan, Yuji, etc.; the acupoints located in deep tissue with abundant muscles, are mostly muscle spindles; the Daling acupoint might be a colgi tendon and/or pressure receptor unit. Besides a si

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Woodcock, E. A., S. L. Land, R. K. Andrews, M. Linsenmeyer, and D. M. Woodcock. "A low-affinity, low-molecular-mass endothelin-A receptor in neonatal rat heart." Biochemical Journal 304, no. 1 (1994): 113–19. http://dx.doi.org/10.1042/bj3040113.

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Endothelin receptors with endothelin-A (ETa) specificity were present in neonatal rat ventricle. However, in both receptor-binding studies and studies of inositol phosphate accumulation, these receptors had lower affinity for endothelin-1 than ETa receptors on isolated neonatal cardiomyocytes or adult left atria. Receptors in the three myocardial preparations were cross-linked to 125I-endothelin-1 and their molecular masses measured using SDS/PAGE. Receptors on left atria and neonatal cardiomyocytes had the expected molecular mass of 48 kDa, whereas the receptors in neonatal ventricle were sma

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Salmon, J. E., N. Brogle, C. Brownlie, et al. "Human mononuclear phagocytes express adenosine A1 receptors. A novel mechanism for differential regulation of Fc gamma receptor function." Journal of Immunology 151, no. 5 (1993): 2775–85. http://dx.doi.org/10.4049/jimmunol.151.5.2775.

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Abstract Using monoclonal anti-adenosine A1 receptor antibodies that bind the A1 receptor ligand binding site, we demonstrate that A1 receptors are expressed on cultured monocytes and rheumatoid synovial fluid mononuclear phagocytes. This finding is associated with the acquisition of reactivity with selective adenosine A1 receptor agonists and is temporally coordinated with the induction of adenosine A2 receptors on cultured monocytes. In a rapid, concentration-dependent fashion, these two distinct adenosine receptors modulate Fc gamma receptor-mediated phagocytosis, a response critical to the

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Yuzaki, Michisuke, and John A. Connor. "Characterization of l-Homocysteate–Induced Currents in Purkinje Cells From Wild-Type and NMDA Receptor Knockout Mice." Journal of Neurophysiology 82, no. 5 (1999): 2820–26. http://dx.doi.org/10.1152/jn.1999.82.5.2820.

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l-Homocysteic acid (HCA), an endogenous excitatory amino acid in the mammalian CNS, potently activates N-methyl-d-aspartate (NMDA) receptors in hippocampal neurons. However, the responses to HCA in Purkinje cells, which lack functional NMDA receptors, have been largely unexplored: HCA may activate conventional non-NMDA receptors by its mixed agonistic action on both NMDA and non-NMDA receptors, or it may activate a novel non-NMDA receptor that has high affinity for HCA. To test these possibilities, we compared the responses to HCA in cultured Purkinje cells with those in hippocampal neurons by

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Barinov, Edward F., Dina I. Giller, Sabina A. Akhundova, Alina S. Yureva, and Bogdan P. Tereshchuk. "Efficiency of platelet aggregation with different sensitivity of cyclooxygenase to non-steroid anti-inflammatory drugs in patients with nephrolithiasis." Saratov Journal of Medical Scientific Research 20, no. 1 (2024): 97–102. http://dx.doi.org/10.15275/ssmj2001097.

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Objective: to establish the dependence of thrombocyte (Tc) aggregation efficiency on crosstalk-signaling pathways associated with stimulation of TR-receptor and purine P2-receptors, with different cyclooxygenase (COX) activity against the background of non-steroidal anti-inflammatory drugs (NSAIDs) administration in patients with nephrolithiasis (NLT). Material and methods. The study was prospective and included 60 patients with NLT who received non-steroid anti-inflammatory drugs (NSAIDs) for analgesia as part of lithokinetic therapy (LKT). The cohort of patients was divided into two groups,

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Sigel, E., R. Baur, N. Boulineau, and F. Minier. "Impact of subunit positioning on GABAA receptor function." Biochemical Society Transactions 34, no. 5 (2006): 868–71. http://dx.doi.org/10.1042/bst0340868.

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The major isoforms of the GABAA (γ-aminobutyric acid type A) receptor are composed of two α, two β and one γ subunit. Thus α and β subunits occur twice in the receptor pentamer. As it is well documented that different isoforms of α and β subunits can co-exist in the same pentamer, the question is raised whether the relative position of a subunit isoform affects the functional properties of the receptor. We have used subunit concatenation to engineer receptors of well-defined subunit arrangement to study this question. Although all five subunits may be concatenated, we have focused on the combi

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