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1

Cato, Laura, Antje Neeb, Myles Brown, and Andrew C. B. Cato. "Control of Steroid Receptor Dynamics and Function by Genomic Actions of the Cochaperones p23 and Bag-1L." Nuclear Receptor Signaling 12, no. 1 (2014): nrs.12005. http://dx.doi.org/10.1621/nrs.12005.

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Molecular chaperones encompass a group of unrelated proteins that facilitate the correct assembly and disassembly of other macromolecular structures of which they themselves do not remain a part. Chaperones associate with a large and diverse set of cofactors termed cochaperones that regulate their function and specificity. Chaperones and cochaperones regulate the activity of several classes of signaling molecules, including steroid receptors. Upon binding ligand, steroid receptors interact with discrete nucleotide sequences within the nucleus to control the expression of diverse physiological
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2

Ben-Shlomo, Izhar, Rami Rauch, Orna Avsian-Kretchmer, and Aaron J. W. Hsueh. "Matching Receptome Genes with Their Ligands for Surveying Paracrine/Autocrine Signaling Systems." Molecular Endocrinology 21, no. 8 (2007): 2009–14. http://dx.doi.org/10.1210/me.2007-0087.

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Abstract Sequencing of genomes from diverse organisms facilitates studies on the repertoire of genes involved in intercellular signaling. Extending previous efforts to annotate most human plasma membrane receptors in the Human Plasma Membrane Receptome database, we matched cognate ligands with individual receptors by surveying the published literature. In the updated online database we called “liganded receptome,” users can search for individual ligands or receptors to reveal their pairing partners and browse through receptor or ligand families to identify relationships between ligands and rec
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3

YOSHINO, T. P., J. P. BOYLE, and J. E. HUMPHRIES. "Receptor–ligand interactions and cellular signalling at the host–parasite interface." Parasitology 123, no. 7 (2001): 143–57. http://dx.doi.org/10.1017/s0031182001007685.

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Although the effects of trematode infection on snail host physiology or host responses on parasite development have been well described in the literature, very little is known regarding the underlying mechanisms and specific molecules responsible for mediating those effects. It is presumed that many host–parasite interactions are communicated through receptor-mediated events, in particular those involving haemocytic immune responses to invading parasites, larval motility and migration through host tissues, and larval acquisition of host molecules either as nutrients or critical developmental f
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4

Thambidurai, Yuvarani, Sudarsanam Durairaj, Siddhardha Solosan S, Sewali Ghosh, and Habeeb Shaik Mohideen. "Binding Potential of Dysidea Herbacea Derived Small Molecules to Breast Cancer Implicating Targets Estrogen and Epidermal Growth Factor Receptors." Biomedical and Pharmacology Journal 14, no. 01 (2021): 391–402. http://dx.doi.org/10.13005/bpj/2139.

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Identifying new targets and new drugs has always been a daunting task, especially in cancer research. This studyexamines the binding interaction and the drug-likeness properties of small molecules derived from marine sponge Dysideaherbacea to breast cancer receptors: epidermal growth factor receptor and estrogen receptor. The receptor’s interaction with the ligand was evaluated using the Schrodinger Glide package, and affinities were assessed based on the glide score. Ligand molecules that have higher binding affinity were evaluated further for their ADMET properties using Molinspiration.We fo
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Altenbach, Denise, and Silke Robatzek. "Pattern Recognition Receptors: From the Cell Surface to Intracellular Dynamics." Molecular Plant-Microbe Interactions® 20, no. 9 (2007): 1031–39. http://dx.doi.org/10.1094/mpmi-20-9-1031.

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Detection of potentially infectious microorganisms is essential for plant immunity. Microbial communities growing on plant surfaces are constantly monitored according to their conserved microbe-associated molecular patterns (MAMPs). In recent years, several pattern-recognition receptors, including receptor-like kinases and receptor-like proteins, and their contribution to disease resistance have been described. MAMP signaling must be carefully controlled and seems to involve receptor endocytosis. As a further surveillance layer, plants are able to specifically recognize microbial effector mole
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6

Brown, Michael, Michael Webb, Elsa Phillips, Elizabeth Skidmore, and Peter McIntyre. "Molecular studies on kinin receptors." Canadian Journal of Physiology and Pharmacology 73, no. 7 (1995): 780–86. http://dx.doi.org/10.1139/y95-105.

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We describe the results of functional studies on DNA clones encoding functional bradykinin receptors derived from human, rat, and mouse sources and including both genomic and complementary DNA clones. In both the Xenopus oocyte and the COS cell expression systems, the receptors from human and rat showed the pharmacological properties of B2 receptors, but receptors from mouse displayed both B1- and B2-like pharmacological properties. We further investigated the molecular relationship between the B1 and B2 receptor subtypes expressed by a human fibroblast cell line, and we demonstrate that these
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7

Walker, R. J., and L. Holden-Dye. "Evolutionary aspects of transmitter molecules, their receptors and channels." Parasitology 102, S1 (1991): S7—S29. http://dx.doi.org/10.1017/s0031182000073261.

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Classical transmitters are present in all phyla that have been studied; however, our detailed understanding of the process of neurotransmission in these phyla is patchy and has centred on those neurotransmitter receptor mechanisms which are amenable to study with the tools available at the time, for example, high-affinity ligands, tissues with high density of receptor protein, suitable electrophysio-logical recording systems. Studies also clearly show that many neurones exhibit co-localization of classical transmitters and neuropeptides. However, the physiological implications of this co-local
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8

Molteni, Monica, Annalisa Bosi, and Carlo Rossetti. "Natural Products with Toll-Like Receptor 4 Antagonist Activity." International Journal of Inflammation 2018 (2018): 1–9. http://dx.doi.org/10.1155/2018/2859135.

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Toll-Like Receptors (TLRs) are the innate immunity receptors that play an activating role when interacting with molecules released by bacteria and viruses (PAMPs, pathogen-associated molecular patterns) or with molecules released by injured cells and tissues (DAMPs, danger-associated molecular patterns). TLR triggering leads to the induction of proinflammatory cytokines and chemokines, driving the activation of both innate and adaptive immunity. In particular, Toll-Like Receptor 4 (TLR4) has been described to be involved in the inflammatory processes observed in several pathologies (such as is
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9

Brown, E. J., and J. L. Goodwin. "Fibronectin receptors of phagocytes. Characterization of the Arg-Gly-Asp binding proteins of human monocytes and polymorphonuclear leukocytes." Journal of Experimental Medicine 167, no. 3 (1988): 777–93. http://dx.doi.org/10.1084/jem.167.3.777.

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We have defined the cell surface molecules of human monocytes and PMN that bind to the chymotryptic cell binding domain of Fn and to a synthetic peptide, KYAVTGRGDS, based on the sequence of Fn, by affinity chromatography. Monocytes express two receptors that differ in their affinity for CBD-Sepharose and peptide-Sepharose, but that both recognize the RGD sequence. Only a single receptor is purified from PMN, which resembles the monocyte surface molecule that binds to peptide-Sepharose. These receptors are not part of the Mac-1, LFA-1, p(150,95) family, but do have homology to the platelet Fn
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10

Breyer, M. D., H. R. Jacobson, and R. M. Breyer. "Functional and molecular aspects of renal prostaglandin receptors." Journal of the American Society of Nephrology 7, no. 1 (1996): 8–17. http://dx.doi.org/10.1681/asn.v718.

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The diverse intrarenal effects of the prostaglandins (PG) are mediated by distinct guanine nucleotide regulatory protein (G-protein)-coupled receptors. The cDNA for these receptors have been cloned, their signal transduction mechanisms determined, and their intrarenal distribution mapped. PGE2, the major intrarenal prostaglandin, interacts with at least three distinct E-prostanoid (EP) receptors that are highly expressed in specific regions of the kidney. Each EP receptor not only selectively binds PGE2, but also preferentially couples to different signal transduction pathways, including: stim
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11

Thomas, Lance R., Ronald L. Johnson, John C. Reed, and Andrew Thorburn. "The C-terminal Tails of Tumor Necrosis Factor-related Apoptosis-inducing Ligand (TRAIL) and Fas Receptors Have Opposing Functions in Fas-associated Death Domain (FADD) Recruitment and Can Regulate Agonist-specific Mechanisms of Receptor Activation." Journal of Biological Chemistry 279, no. 50 (2004): 52479–86. http://dx.doi.org/10.1074/jbc.m409578200.

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Members of the tumor necrosis factor (TNF) superfamily of receptors such as Fas/CD95 and the TNF-related apoptosis-inducing ligand (TRAIL) receptors DR4 and DR5 induce apoptosis by recruiting adaptor molecules and caspases. The central adaptor molecule for these receptors is a death domain-containing protein, FADD, which binds to the activated receptor via death domain-death domain interactions. Here, we show that in addition to the death domain, the C-terminal tails of DR4 and DR5 positively regulate FADD binding, caspase activation and apoptosis. In contrast, the corresponding region in the
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12

Castaño, Andrea, and Margarita María Velásquez. "Psoriasis pustulosa generalizada: de la inmunopatogénesis a la clínica." Revista de la Asociación Colombiana de Dermatología y Cirugía Dermatológica 25, no. 2 (2017): 130–42. http://dx.doi.org/10.29176/2590843x.9.

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El síndrome DITRA (Interleukin-36-Receptor Antagonist Deficiency) es una enfermedad autoinflamatoria debida a mutaciones del gen IL36RN que producen deficiencia del antagonista del receptor de la IL-36, lo que induce una cascada inflamatoria que lleva a un cuadro clínico grave de psoriasis pustulosa generalizada. Ante desencadenantes externos, como los componentes de agentes infecciosos que son activadores de los receptores de inmunidad innata, denominados PAMP (Pathogen-Associated Molecular Patterns), o los asociados a estrés celular, llamados DAMP (Damage-Associated Molecular Patterns), se a
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13

Naval, Javier, Diego de Miguel, Ana Gallego-Lleyda, Alberto Anel, and Luis Martinez-Lostao. "Importance of TRAIL Molecular Anatomy in Receptor Oligomerization and Signaling. Implications for Cancer Therapy." Cancers 11, no. 4 (2019): 444. http://dx.doi.org/10.3390/cancers11040444.

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(TNF)-related apoptosis-inducing ligand (TRAIL) is able to activate the extrinsic apoptotic pathway upon binding to DR4/TRAIL-R1 and/or DR5/TRAIL-R2 receptors. Structural data indicate that TRAIL functions as a trimer that can engage three receptor molecules simultaneously, resulting in receptor trimerization and leading to conformational changes in TRAIL receptors. However, receptor conformational changes induced by the binding of TRAIL depend on the molecular form of this death ligand, and not always properly trigger the apoptotic cascade. In fact, TRAIL exhibits a much stronger pro-apoptoti
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14

Hay, D. L., G. Christopoulos, A. Christopoulos, and P. M. Sexton. "Amylin receptors: molecular composition and pharmacology." Biochemical Society Transactions 32, no. 5 (2004): 865–67. http://dx.doi.org/10.1042/bst0320865.

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Several receptors which bind the hormone AMY (amylin) with high affinity have now been identified. The minimum binding unit is composed of the CT (calcitonin) receptor at its core, plus a RAMP (receptor activity modifying protein). The receptors have been named AMY1(a), AMY2(a) and AMY3(a) in accordance with the association of the CT receptor (CT(a)) with RAMP1, RAMP2 and RAMP3 respectively. The challenge is now to determine the localization and pharmacological nature of each of these receptors. Recent attempts to achieve these aims will be briefly discussed.
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15

Kazantseva, Z. I. "Phosphorylated thiacalixarenes as molecular receptors for QCM sensors of volatile compounds." Functional materials 24, no. 4 (2017): 599–606. http://dx.doi.org/10.15407/fm24.04.599.

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16

Virovets, A. V., V. A. Blatov, and A. P. Shevchenko. "Methods of crystallochemical analysis of supramolecular complexes by means of Voronoi–Dirichlet polyhedra: a study of cucurbituril host–guest compounds." Acta Crystallographica Section B Structural Science 60, no. 3 (2004): 350–57. http://dx.doi.org/10.1107/s0108768104005051.

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Crystallochemical analysis methods based on the Voronoi–Dirichlet partition of crystal space are extended to supramolecular complexes of any complexity. The sizes and shapes of receptor cavities and substrate molecules are shown to be successfully estimated as volumes and the second moments of inertia of the corresponding molecular Voronoi–Dirichlet polyhedra. To predict which organic substrates can occupy the receptor cavity a mini-expert system known as MOLVOL was created, comprising a database on completely determined crystal structures of almost 60 000 organic molecular compounds. Using th
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17

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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18

Abdul Malik, Nurul Azmina, Ilakiya Sharanee Kumar, and Kalaivani Nadarajah. "Elicitor and Receptor Molecules: Orchestrators of Plant Defense and Immunity." International Journal of Molecular Sciences 21, no. 3 (2020): 963. http://dx.doi.org/10.3390/ijms21030963.

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Pathogen-associated molecular patterns (PAMPs), microbe-associated molecular patterns (MAMPs), herbivore-associated molecular patterns (HAMPs), and damage-associated molecular patterns (DAMPs) are molecules produced by microorganisms and insects in the event of infection, microbial priming, and insect predation. These molecules are then recognized by receptor molecules on or within the plant, which activates the defense signaling pathways, resulting in plant’s ability to overcome pathogenic invasion, induce systemic resistance, and protect against insect predation and damage. These small molec
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19

Drummond, Heather A. "What Evolutionary Evidence Implies About the Identity of the Mechanoelectrical Couplers in Vascular Smooth Muscle Cells." Physiology 36, no. 5 (2021): 292–306. http://dx.doi.org/10.1152/physiol.00008.2021.

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Loss of pressure-induced vasoconstriction increases susceptibility to renal and cerebral vascular injury. Favored paradigms underlying initiation of the response include transient receptor potential channels coupled to G protein-coupled receptors or integrins as transducers. Degenerin channels may also mediate the response. This review addresses the 1) evolutionary role of these molecules in mechanosensing, 2) limitations to identifying mechanosensitive molecules, and 3) paradigm shifting molecular model for a VSMC mechanosensor.
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20

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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Vila-Viçosa, Diogo, Oscar Francesconi, and Miguel Machuqueiro. "Why a diaminopyrrolic tripodal receptor binds mannosides in acetonitrile but not in water?" Beilstein Journal of Organic Chemistry 10 (July 3, 2014): 1513–23. http://dx.doi.org/10.3762/bjoc.10.156.

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Intermolecular interactions involving carbohydrates and their natural receptors play important roles in several biological processes. The development of synthetic receptors is very useful to study these recognition processes. Recently, it was synthetized a diaminopyrrolic tripodal receptor that is selective for mannosides, which are obtained from mannose, a sugar with significant relevance in living systems. However, this receptor is significantly more active in acetonitrile than in water. In this work, we performed several molecular dynamics and constant-pH molecular dynamics simulations in a
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Brooks, Charles L. "Molecular Mechanisms of Prolactin and Its Receptor." Endocrine Reviews 33, no. 4 (2012): 504–25. http://dx.doi.org/10.1210/er.2011-1040.

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Prolactin and the prolactin receptors are members of a family of hormone/receptor pairs which include GH, erythropoietin, and other ligand/receptor pairs. The mechanisms of these ligand/receptor pairs have broad similarities, including general structures, ligand/receptor stoichiometries, and activation of several common signaling pathways. But significant variations in the structural and mechanistic details are present among these hormones and their type 1 receptors. The prolactin receptor is particularly interesting because it can be activated by three sequence-diverse human hormones: prolact
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Livingstone, C. D., P. G. Strange, and L. H. Naylor. "Molecular modelling of D2-like dopamine receptors." Biochemical Journal 287, no. 1 (1992): 277–82. http://dx.doi.org/10.1042/bj2870277.

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Three-dimensional computer models of the rat D2, D3 and D4 dopamine receptor subtypes have been constructed based on the diffraction co-ordinates for bacteriorhodopsin, another membrane-bound protein containing seven transmembrane domains presumed to be arranged in a similar spatial orientation. Models were assembled by aligning the putative transmembrane domains of the dopamine receptors with those of bacteriorhodopsin using sequence similarities, and then superimposing these modelled alpha-helices on to the bacteriorhodopsin-derived co-ordinates. These models explore the potential hydrogen b
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Blenau, Wolfgang, Joana Alessandra Wilms, Sabine Balfanz та Arnd Baumann. "AmOctα2R: Functional Characterization of a Honeybee Octopamine Receptor Inhibiting Adenylyl Cyclase Activity". International Journal of Molecular Sciences 21, № 24 (2020): 9334. http://dx.doi.org/10.3390/ijms21249334.

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The catecholamines norepinephrine and epinephrine are important regulators of vertebrate physiology. Insects such as honeybees do not synthesize these neuroactive substances. Instead, they use the phenolamines tyramine and octopamine for similar physiological functions. These biogenic amines activate specific members of the large protein family of G protein-coupled receptors (GPCRs). Based on molecular and pharmacological data, insect octopamine receptors were classified as either α- or β-adrenergic-like octopamine receptors. Currently, one α- and four β-receptors have been molecularly and pha
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25

Al-Hasani, Ream, and Michael R. Bruchas. "Molecular Mechanisms of Opioid Receptor-dependent Signaling and Behavior." Anesthesiology 115, no. 6 (2011): 1363–81. http://dx.doi.org/10.1097/aln.0b013e318238bba6.

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Opioid receptors have been targeted for the treatment of pain and related disorders for thousands of years and remain the most widely used analgesics in the clinic. Mu (μ), kappa (κ), and delta (δ) opioid receptors represent the originally classified receptor subtypes, with opioid receptor like-1 (ORL1) being the least characterized. All four receptors are G-protein coupled and activate inhibitory G proteins. These receptors form homo- and heterodimeric complexes and signal to kinase cascades and scaffold a variety of proteins.The authors discuss classic mechanisms and developments in understa
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Najmabadi, Peyman, Kwang-Seuk Ko, James J. La Clair, and Michael D. Burkart. "A Method for Fabrication of Polycarbonate-Based Bioactive Platforms." JALA: Journal of the Association for Laboratory Automation 13, no. 5 (2008): 284–88. http://dx.doi.org/10.1016/j.jala.2008.07.003.

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Surface-based assays have been used extensively for the functional and structural analysis of biomolecules such as DNA or proteins. These experiments are established by the analysis of binding between acceptor molecules and immobilized receptors on a platform. Site-specific printing of receptor molecules on gold, glass, or polycarbonate (PC) surfaces is conventionally performed by the chemical derivatization of a surface, priming it to covalently bind to subsequently deposited receptor molecules. Unlike conventional methods, we have developed a new fabrication method for bioactive PC surfaces
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Clarke, David T., and Marisa L. Martin-Fernandez. "A Brief History of Single-Particle Tracking of the Epidermal Growth Factor Receptor." Methods and Protocols 2, no. 1 (2019): 12. http://dx.doi.org/10.3390/mps2010012.

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Single-particle tracking (SPT) has been used and developed over the last 25 years as a method to investigate molecular dynamics, structure, interactions, and function in the cellular context. SPT is able to show how fast and how far individual molecules move, identify different dynamic populations, measure the duration and strength of intermolecular interactions, and map out structures on the nanoscale in cells. In combination with other techniques such as macromolecular crystallography and molecular dynamics simulation, it allows us to build models of complex structures, and develop and test
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Hercus, Timothy R., Daniel Thomas, Mark A. Guthridge, et al. "The granulocyte-macrophage colony-stimulating factor receptor: linking its structure to cell signaling and its role in disease." Blood 114, no. 7 (2009): 1289–98. http://dx.doi.org/10.1182/blood-2008-12-164004.

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AbstractAlready 20 years have passed since the cloning of the granulocyte-macrophage colony-stimulating factor (GM-CSF) receptor α-chain, the first member of the GM-CSF/interleukin (IL)–3/IL-5 family of hemopoietic cytokine receptors to be molecularly characterized. The intervening 2 decades have uncovered a plethora of biologic functions transduced by the GM-CSF receptor (pleiotropy) and revealed distinct signaling networks that couple the receptor to biologic outcomes. Unlike other hemopoietin receptors, the GM-CSF receptor has a significant nonredundant role in myeloid hematologic malignanc
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29

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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Hébert, Terence E., and Michel Bouvier. "Structural and functional aspects of G protein-coupled receptor oligomerization." Biochemistry and Cell Biology 76, no. 1 (1998): 1–11. http://dx.doi.org/10.1139/o98-012.

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G protein-coupled receptors (GPCRs) represent the single largest family of cell surface receptors involved in signal transduction. It is estimated that several hundred distinct members of this receptor family in humans direct responses to a wide variety of chemical transmitters, including biogenic amines, amino acids, peptides, lipids, nucleosides, and large polypeptides. These transmembrane receptors are key controllers of such diverse physiological processes as neurotransmission, cellular metabolism, secretion, cellular differentiation, and growth as well as inflammatory and immune responses
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Sykiotis, Gerasimos, and Athanasios Papavassiliou. "Molecular mechanisms of transcriptional regulation by nuclear receptors. Perspectives for therapeutic implications." HORMONES 1, no. 2 (2002): 69–75. http://dx.doi.org/10.14310/horm.2002.1154.

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32

Coller, B. S. "Activation affects access to the platelet receptor for adhesive glycoproteins." Journal of Cell Biology 103, no. 2 (1986): 451–56. http://dx.doi.org/10.1083/jcb.103.2.451.

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Blood platelets have a receptor for macromolecular adhesive glycoproteins, located on a heteroduplex membrane glycoprotein complex (GPIIb/IIIa) that only becomes "exposed" when platelets are activated. Binding of the adhesive glycoproteins, in particular fibrinogen, to the receptor is required for platelet aggregation, which in turn is required to arrest bleeding. A murine monoclonal antibody whose rate of binding to the receptor is affected by platelet activation was both cross-linked and fragmented to assess the effects of changes in molecular size on its rate of binding to unactivated and a
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Bettler, Bernhard, Klemens Kaupmann, Johannes Mosbacher, and Martin Gassmann. "Molecular Structure and Physiological Functions of GABAB Receptors." Physiological Reviews 84, no. 3 (2004): 835–67. http://dx.doi.org/10.1152/physrev.00036.2003.

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GABAB receptors are broadly expressed in the nervous system and have been implicated in a wide variety of neurological and psychiatric disorders. The cloning of the first GABAB receptor cDNAs in 1997 revived interest in these receptors and their potential as therapeutic targets. With the availability of molecular tools, rapid progress was made in our understanding of the GABAB system. This led to the surprising discovery that GABAB receptors need to assemble from distinct subunits to function and provided exciting new insights into the structure of G protein-coupled receptors (GPCRs) in genera
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Koehler, Melanie, Anny Fis, Hermann J. Gruber, and Peter Hinterdorfer. "AFM-Based Force Spectroscopy Guided by Recognition Imaging: A New Mode for Mapping and Studying Interaction Sites at Low Lateral Density." Methods and Protocols 2, no. 1 (2019): 6. http://dx.doi.org/10.3390/mps2010006.

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Ligand binding to receptors is one of the most important regulatory elements in biology as it is the initiating step in signaling pathways and cascades. Thus, precisely localizing binding sites and measuring interaction forces between cognate receptor–ligand pairs leads to new insights into the molecular recognition involved in these processes. Here we present a detailed protocol about applying a technique, which combines atomic force microscopy (AFM)-based recognition imaging and force spectroscopy for studying the interaction between (membrane) receptors and ligands on the single molecule le
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Boncompain, Gaelle, Floriane Herit, Sarah Tessier, et al. "Targeting CCR5 trafficking to inhibit HIV-1 infection." Science Advances 5, no. 10 (2019): eaax0821. http://dx.doi.org/10.1126/sciadv.aax0821.

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Using a cell-based assay monitoring differential protein transport in the secretory pathway coupled to high-content screening, we have identified three molecules that specifically reduce the delivery of the major co-receptor for HIV-1, CCR5, to the plasma membrane. They have no effect on the closely related receptors CCR1 and CXCR4. These molecules are also potent in primary macrophages as they markedly decrease HIV entry. At the molecular level, two of these molecules inhibit the critical palmitoylation of CCR5 and thereby block CCR5 in the early secretory pathway. Our results open a clear th
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Such, Justyna, Krzysztof Jóźwiak, and Artur Wnorowski. "(R,R′)-4′-methoxy-1-naphthylfenoterol as a new multi-target compound of antitumorigenic properties." Postępy Polskiej Medycyny i Farmacji 5 (June 26, 2017): 9–15. http://dx.doi.org/10.5604/01.3001.0011.6190.

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Targeted therapies are based on the use of compounds that inhibit a specific target molecule within the tissue of interest. The recent advances in the molecular etiology of cancer significantly shifted the therapeutic approach from nonspecific cytotoxic agents towards molecules directed either at individual receptors or acting simultaneously on multiple molecular targets. This article is an overview of recent literature on (R,R′)-4′-methoxy-1-naphthylfenoterol (MNF), a novel bifunctional ligand that activates β2 adrenergic receptor (β2AR) and blocks GPR55 receptor. These two activities are imp
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Bennett, Maxwell. "Positive and Negative Symptoms in Schizophrenia: The NMDA Receptor Hypofunction Hypothesis, Neuregulin/ErbB4 and Synapse Regression." Australian & New Zealand Journal of Psychiatry 43, no. 8 (2009): 711–21. http://dx.doi.org/10.1080/00048670903001943.

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Carlsson has put forward the hypothesis that the positive and negative symptoms of schizophrenia are due to failure of mesolimbic and mesocortical projections consequent on hypofunction of the glutamate N-methyl-d-aspartate (NMDA) receptor. The hypothesis has been recently emphasized in this Journal that the loss of synaptic spines with NMDA receptors, which can be precipitated by stress, can explain the emergence of positive symptoms such as hallucinations and that this synapse regression involves molecules such as neuregulin and its receptor ErbB4 that have been implicated in schizophrenia.
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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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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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Lakshmi, Sowmya P., Aravind T. Reddy, Asoka Banno, and Raju C. Reddy. "Molecular, chemical, and structural characterization of prostaglandin A2 as a novel agonist for Nur77." Biochemical Journal 476, no. 19 (2019): 2757–67. http://dx.doi.org/10.1042/bcj20190253.

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Abstract Nur77 is a transcription factor belonging to the NR4A subfamily of nuclear hormone receptors. Upon induction, Nur77 modulates the expression of its target genes and controls a variety of biological and pathophysiological processes. Prior research that revealed a structurally atypical ligand-binding domain (LBD) and failed to locate an endogenous ligand had led to a classification of Nur77 as an orphan receptor. However, several more recent studies indicate that small synthetic molecules and unsaturated fatty acids can bind to Nur77. Discovery of additional endogenous ligands will faci
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Mahmod Al-Qattan, Mohammed Nooraldeen, and Mohd Nizam Mordi. "Molecular Basis of Modulating Adenosine Receptors Activities." Current Pharmaceutical Design 25, no. 7 (2019): 817–31. http://dx.doi.org/10.2174/1381612825666190304122624.

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Modulating cellular processes through extracellular chemical stimuli is medicinally an attractive approach to control disease conditions. GPCRs are the most important group of transmembranal receptors that produce different patterns of activations using intracellular mediators (such as G-proteins and Beta-arrestins). Adenosine receptors (ARs) belong to GPCR class and are divided into A1AR, A2AAR, A2BAR and A3AR. ARs control different physiological activities thus considered valuable target to control neural, heart, inflammatory and other metabolic disorders. Targeting ARs using small molecules
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Indik, ZK, JG Park, S. Hunter, and AD Schreiber. "The molecular dissection of Fc gamma receptor mediated phagocytosis." Blood 86, no. 12 (1995): 4389–99. http://dx.doi.org/10.1182/blood.v86.12.4389.bloodjournal86124389.

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Because hematopoietic cells express multiple Fc gamma receptor isoforms, the role of the individual Fc gamma receptors in phagocytosis has been difficult to define. Transfection of Fc gamma receptors into COS-1 cells, which lack endogeneous Fc gamma receptors but have phagocytic potential, has proved valuable for the study of individual Fc gamma receptor function. Using this model system, we have established that a single class of human Fc gamma receptor mediates phagocytosis in the absence of other Fc receptors and that isoforms from each Fc gamma receptor class mediate phagocytosis, although
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Bagnato, Anna, Francesca Spinella, and Laura Rosanò. "The endothelin axis in cancer: the promise and the challenges of molecularly targeted therapyThis article is one of a selection of papers published in the special issue (part 2 of 2) on Forefronts in Endothelin." Canadian Journal of Physiology and Pharmacology 86, no. 8 (2008): 473–84. http://dx.doi.org/10.1139/y08-058.

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The endothelin (ET) axis, which includes ET-1, ET-2, ET-3, and 2 G protein-coupled receptor subtypes, ETAR and ETBR, promotes growth and progression of a variety of tumors, such as prostatic, ovarian, renal, pulmonary, colorectal, cervical, breast, lung, bladder, endometrial carcinoma, Kaposi’s sarcoma, brain tumors, and melanoma. Acting on selective receptors, ET-1 regulates mitogenesis, cell survival, angiogenesis, bone remodeling, stimulation of nociceptors, tumor-infiltrating immune cells, epithelial-to-mesenchymal transition, invasion, and metastatic dissemination. At the molecular level,
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McQuaid, Fiona, and J. Alexandra Rowe. "Rosetting revisited: a critical look at the evidence for host erythrocyte receptors in Plasmodium falciparum rosetting." Parasitology 147, no. 1 (2019): 1–11. http://dx.doi.org/10.1017/s0031182019001288.

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AbstractMalaria remains a major cause of mortality in African children, with no adjunctive treatments currently available to ameliorate the severe clinical forms of the disease. Rosetting, the adhesion of infected erythrocytes (IEs) to uninfected erythrocytes, is a parasite phenotype strongly associated with severe malaria, and hence is a potential therapeutic target. However, the molecular mechanisms of rosetting are complex and involve multiple distinct receptor–ligand interactions, with some similarities to the diverse pathways involved in P. falciparum erythrocyte invasion. This review sum
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Hess, J. Fred, Patricia J. Hey, Tsing-Bau Chen, et al. "Molecular Cloning and Pharmacological Characterization of the Canine B1 and B2 Bradykinin Receptors." Biological Chemistry 382, no. 1 (2001): 123–29. http://dx.doi.org/10.1515/bc.2001.018.

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Abstract The dog is a valuable animal model in the study of the physiological role of both the B1 and B2 bradykinin receptors. To more thoroughly characterize the pharmacological properties of the canine kinin receptors we isolated the cDNA sequence encoding the B1 and B2 bradykinin receptor subtypes and overexpressed them in Chinese hamster ovary (CHO) cells. The cDNA sequence of the canine B1 bradykinin receptor encodes a protein comprised of 350 amino acids that is 76% identical to the human B1 bradykinin receptor. The cDNA sequence of the canine B2 bradykinin receptor encodes a protein of
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Putri, Deby Kania Tri, Indah Listiana Kriswandini, and Muhammad Luthfi. "Characterization of Streptococcus sanguis molecular receptors for Streptococcus mutans binding molecules." Dental Journal (Majalah Kedokteran Gigi) 49, no. 4 (2016): 213. http://dx.doi.org/10.20473/j.djmkg.v49.i4.p213-216.

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Background: Dental caries is a major problem in oral cavity. If dental caries causes cavity, the structure of dental hard tissue will not be reversible because of damage in the structure of the hard tissue. The early pathogenesis mechanism of dental caries is an adhesion interaction between cariogenic Streptococcus mutans microorganisms and tooth surface pellicles. The attachment involves a specific molecular component interaction between the bacterial complement molecules and the surface of the host. Streptococcus sanguis as a dominant ecology at the beginning of bacterial plaque aggregation
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Molteni, Monica, Sabrina Gemma, and Carlo Rossetti. "The Role of Toll-Like Receptor 4 in Infectious and Noninfectious Inflammation." Mediators of Inflammation 2016 (2016): 1–9. http://dx.doi.org/10.1155/2016/6978936.

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Toll-like receptor 4 (TLR4) belongs to the family of pattern recognition receptors (PRRs). They are highly conserved receptors that recognize conserved pathogen-associated molecular patterns (PAMPs), thus representing the first line of defense against infections. TLR4 has been long recognized as the sensing receptor for gram-negative lipopolysaccharide (LPS). In addition, it also binds endogenous molecules produced as a result of tissue injury. Hence, TLR4 represents a key receptor on which both infectious and noninfectious stimuli converge to induce a proinflammatory response. TLR4-mediated i
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BREDESEN, DALE E., PATRICK MEHLEN, and SHAHROOZ RABIZADEH. "Apoptosis and Dependence Receptors: A Molecular Basis for Cellular Addiction." Physiological Reviews 84, no. 2 (2004): 411–30. http://dx.doi.org/10.1152/physrev.00027.2003.

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Bredesen, Dale E., Patrick Mehlen, and Shahrooz Rabizadeh. Apoptosis and Dependence Receptors: A Molecular Basis for Cellular Addiction. Physiol Rev 84: 411–430, 2004; 10.1152/physrev.00027.2003.—Classical signal transduction is initiated by ligand-receptor interactions. We have described an alternative form of signal transduction that is initiated by the withdrawal of ligands from specific receptors referred to as dependence receptors. This process is widespread, featuring in developmental cell death, carcinogenesis (especially metastasis), neurodegeneration, and possibly subapoptotic events
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Choi, Kyung M. "Microfluidic Approach for the Synthesis of Micro- or Nanosized Molecularly Imprinted Polymer Particles." Research Letters in Materials Science 2008 (2008): 1–3. http://dx.doi.org/10.1155/2008/458158.

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Molecularly imprinted polymers (MIPs) have specific molecular recognition sites for chemical detection.High affinity receptors can increase the sensitivity of sensors/devices. The synthesis of micro- or nanosized MIP's particles is desirable to improve the sensitivity since MIP's particle sizes are inversely proportional to the affinity between receptors and template molecules. To synthesize nano- or microsized MIPs particles, we demonstrate here a novel microfluidic approach, which presents continuous and uniform MIP's particle generation.
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Derby, C. D., H. S. Cate, and L. R. Gentilcore. "Perireception in olfaction: molecular mass sieving by aesthetasc sensillar cuticle determines odorant access to receptor sites in the Caribbean spiny lobster Panulirus argus." Journal of Experimental Biology 200, no. 15 (1997): 2073–81. http://dx.doi.org/10.1242/jeb.200.15.2073.

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The responsiveness of chemoreceptor neurons depends on a combination of perireceptor and receptor events. Olfactory neurons of crustaceans are packaged into distinctive cuticular sensilla called aesthetascs. The cuticle of aesthetascs is thin and permeable, even though it does not contain any obvious surface pores or pore tubules. This suggests that this 'spongy' aesthetasc cuticle may act as a molecular sieve that restricts large odorant molecules from entering the sensilla and binding to the olfactory neurons. We examined whether this is so for the aesthetasc cuticle of the Caribbean spiny l
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