• The ability of organisms, or individual cells, to react to external chemical signals, which are detected and transduced by cell-surface receptors, is crucial for their survival. (epfl.ch)
  • The results of this study support accumulating data on the role of the delta opioid receptor ligand met-enkephalin in the pathogenesis of hepatic encephalopathy, and provide a rationale for the use of opioid receptor antagonists in the treatment of hepatic encephalopathy. (ovid.com)
  • In addition to the Frizzleds, members of the LRP family (represented by the arrow gene in Drosophila) are also necessary for Wnt signal transduction and have been postulated to act as co-receptors. (stanford.edu)
  • The aim of this chapter is to address the key steps involved in the cellular pathway of ligand-functionalized probes for cancer targeting. (springer.com)
  • Combinatorial genetics can provide almost unlimited numbers of mutant receptor proteins and combinatorial chemistry can produce large libraries of potential therapeutic compounds that act on these membrane receptors. (epfl.ch)
  • As proteins sometimes rearrange slightly around a small molecule, we've allowed for some flexibility in the protein, but as we'd like for you to focus on how the ligand binds, you'll get a penalty if the protein moves too far from the starting model. (fold.it)
  • The second is that proteins sometimes flex and move a little when ligands bind, so even if we had a perfect structure we would need to accommodate that. (fold.it)
  • Secreted Wnt proteins have numerous signaling functions during development, mediated by Frizzled molecules that act as Wnt receptors on the cell surface. (stanford.edu)
  • Both CB 1 and CB 2 receptors are coupled through G i/o proteins, negatively to adenylyl cyclase and positively to mitogen-activated protein kinase. (420magazine.com)
  • 1,14 In addition, CB 1 receptors are coupled to ion channels through G i/o proteins, positively toA-type and inwardly rectifying potassium channels and negatively to N-type and P/Q-type calcium channels. (420magazine.com)
  • 1,13,14 CB 1 receptors can also couple to G s proteins to activate adenylyl cyclase, 15-17 the extent to which this occurs possibly being determined by the location of these receptors or by cross-talk between CB 1 receptors and co localised G-protein-coupled non-CB 1 N -oleoyl dopamine (OLDA) (Figures 2 and 3). (420magazine.com)
  • 15,16,18,19 It may also be that CB 1 receptors can exist as two distinct subpopulations, one coupled to G i/o proteins and the other to G s . 15 Details of additional signalling mechanisms that have been proposed for cannabinoid CB 1 and CB 2 receptors can be found elsewhere. (420magazine.com)
  • This describes a ligand binding domain and includes extracellular ligand binding domains of a wide range of receptors, as well as the bacterial amino acid binding proteins of known structure [ PMID: 8011339 ]. (ebi.ac.uk)
  • Mutational analysis of the glycine-binding site of the NMDA receptor: structural similarity with bacterial amino acid-binding proteins. (ebi.ac.uk)
  • They are hologram QSAR (HQSAR), receptor surface model (RSM), comparative molecular field analysis (CoMFA), and applications of genetic neural network to similarity matrix (SM/GNN) or conventional descriptors (C2GNN). (springer.com)
  • NFkappaB, a key link between inflammation and cancer, regulates dual activities of death ligands, depending on molecular signals in the tumor microenvironment. (biomedsearch.com)
  • Despite the physiological and clinical importance of GLP-1, molecular interaction with the GLP-1 receptor (GLP1R) is not well understood. (frontiersin.org)
  • Six crystal structures were used as templates for docking and ligand-based modeling approaches (two-, three-, four- and five-dimensional analyses). (biomedsearch.com)
  • Docking of ligands to the PXR structure co-crystallized with hyperforin had the best statistics for this method. (biomedsearch.com)
  • Binding mode of the cocrystallized ligand 6 (A) and the predicted binding modes of the seven ligands discovered in the docking screen (B−H). The A 2A AR binding site is shown in white ribbons with the side chains of Glu169 and Asn253 in sticks. (nih.gov)
  • In (B−H), the crystallographic ligand is shown using blue lines and the docking poses for the ligands are depicted with orange carbon atoms. (nih.gov)
  • These receptors perceive signaling ligands, EPF1 and EPF2, which are secreted from neighboring stomatal precursors ( 7 ⇓ ⇓ - 10 , 22 ). (pnas.org)
  • Here, we report that EPF1 and its primary receptor ERECTA-LIKE1 (ERL1) target MUTE, a transcription factor specifying the proliferation-to-differentiation switch within the stomatal cell lineages. (elifesciences.org)
  • Click on one of the chemokine subfamilies shown in the Explore Pathways box below to see the specific chemokines that belong to each group, their receptors, and the different immune cell types that have been shown to express the chemokine receptors. (rndsystems.com)
  • Because VAPs have a MSP domain and MSPs are ligands for Eph homologs in Caenorhabditis elegans , the authors performed genetic experiments that placed dVAP and Eph in common developmental pathways in flies and placed VPR-1, the C. elegans VAP homolog, and VAB-1, the C. elegans Eph receptor, in common pathways in worms. (sciencemag.org)
  • Loss of function in the Arabidopsis ERECTA ( ER ) receptor-kinase gene confers characteristic compact inflorescence architecture, but its underlying signaling pathways remain unknown. (pnas.org)
  • The calculated binding affinities quantitatively agree with experimental studies for cholera toxin (n = 5) and anthrax receptor (n = 7) and allow to predict optimal core size and optimal linker length. (uio.no)
  • Binding potential Patlak plot Scatchard plot D.A. Lauffenburger and J.J. Linderman (1993) Receptors: Models for Binding, Trafficking, and Signaling, Oxford University Press. (wikipedia.org)
  • We find support for the hypothesis that, with the exception of RLN, which has undergone strong positive selection in mammalian lineages, the ligand and receptor genes shared between mammals and teleosts appear to have similar pairings. (hindawi.com)
  • Slightly better success has been achieved with ligand-based modeling methods including quantitative structure-activity relationship (QSAR) analysis, pharmacophore modeling and machine learning. (biomedsearch.com)
  • Five of the methods involve quantitative structure-activity relationships (QSAR) based on the 2D or 3D structures of the GP ligands alone. (springer.com)
  • In this review we evaluate our data in comparison to the theoretical and experimental aspects of developing selective and sensitive imaging ligands for in vivo imaging. (ingentaconnect.com)
  • Fig. 1 Natural RXRA ligands in mouse hematopoietic cells in vivo. (sciencemag.org)
  • Using an alkaline phosphatase-tagged Mob-5 as ligand, a putative Mob-5 receptor was identified on the cell surface of oncogenic ras transformed cells. (nih.gov)
  • Thus, the Mob-5/Mob-5 receptor may represent a novel putative autocrine loop coordinately activated by ras oncogenes. (nih.gov)
  • Jones DT, Trowbridge IS, Harris AL (2006) Effects of transferrin receptor blockade on cancer cell proliferation and hypoxia-inducible factor function and their differential regulation by ascorbate. (springer.com)
  • Sommer S, Fuqua SA (2001) Estrogen receptor and breast cancer. (springer.com)
  • This effect, unlike that of 17 beta-estradiol (E2), was not influenced by a pure antiestrogen, ICI 182780, suggesting that the THC-induced uterine lactoferrin gene expression does not involve estrogen receptors. (pnas.org)
  • The first is that predicted structures tend to be a little bit inaccurate, and adding a ligand might give additional information which can help correct some of the minor inaccuracies. (fold.it)
  • Despite this bias, many of the most potent new ligands were novel, dissimilar from known ligands, providing new lead structures for modulation of this medically important target. (nih.gov)
  • Ligand-free and -bound structures of the binding protein (LivJ) of the Escherichia coli ABC leucine/isoleucine/valine transport system: trajectory and dynamics of the interdomain rotation and ligand specificity. (ebi.ac.uk)
  • X-ray structures of the leucine-binding protein illustrate conformational changes and the basis of ligand specificity. (ebi.ac.uk)
  • Fuqua SA, Cui Y, Lee AV, Osborne CK, Horwitz KB (2005) Insights into the role of progesterone receptors in breast cancer. (springer.com)
  • As the goal of the puzzle was primarily to find the position and orientation of the ligand, and not the internal structure of the protein, providing an optimized protein with structural restrictions was deliberate, so that players could focus on the ligand position, rather than having to re-optimize the protein structure. (fold.it)
  • To clarify on the background, we know the structure of the ligand and that it binds the protein, but we really don't know exactly where it binds, or how it binds, or the internal conformation it takes when it binds. (fold.it)
  • The MSP domain of hVAP also competed with EphrinB2 for binding to EphA4 in a dose-dependent manner, suggesting that VAPs may serve as Eph ligands in mammals as well. (sciencemag.org)
  • Relaxin-like peptides (RLN/INSL) play diverse roles in reproductive and neuroendocrine processes in placental mammals and are functionally associated with two distinct types of receptors (RXFP) for each respective function. (hindawi.com)
  • Teleosts preferentially retained duplicates of genes putatively involved in neuroendocrine regulation, harboring a total of 10-11 receptors and 6 ligand genes, while most mammals have equal numbers of ligands and receptors. (hindawi.com)
  • Ligands consist of a geometrically matching rigid polygonal core to which monovalent ligand units are attached via flexible linker polymers, closely mimicking existing experimental designs. (uio.no)
  • Despite the evolutionary conservation, the mode of ligand binding by CDON/Ihog and BOC/Boi is distinct in vertebrates and invertebrates. (reactome.org)
  • We propose that the uterus is a new target for cannabinoid ligand-receptor signaling. (pnas.org)
  • Here we report that proper inflorescence architecture in Arabidopsis can be specified by intertissue layer communication between the phloem and the endodermis mediated by ER and its signaling ligands, EPFL4 and EPFL6, 2 of the 11 members of the EPFL family of secreted cysteine-rich peptides (CRPs) ( 9 , 14 , 15 ). (pnas.org)
  • In the absence of ligand, PTCH is localized in the cilium, while SMO is largely concentrated in intracellular compartments. (reactome.org)
  • The delivery system comprises a mixture of cationic lipid in combination with a receptor ligand and is particularly suited for intracellular delivery of polynucleotides. (google.com)
  • CB 2 receptors are located predominantly in immune cells both within and outside the central nervous system, the functions of these receptors including modulation of cytokine release and of immune cell migration. (420magazine.com)
  • Although these ligands have had and still have important roles in elucidating physiological and pathophysiological properties of mGluRs, their poor selectivity within group presupposes some knowledge of complexity. (ingentaconnect.com)
  • The cloning of these receptors prompted the development of mice from which cannabinoid CB 1 and/or CB 2 receptors have been genetically deleted and these transgenic animals, particularly CB 1 knockout mice, are now widely used to explore the physiological and pathological functions of cannabinoid receptors. (420magazine.com)
  • These receptors are the targets of the majority of clinically used medicines. (epfl.ch)
  • In the previous puzzle, we asked you to model the structure of the human Y1 neuropeptide receptor. (fold.it)
  • Thus in some peripheral tissues, discrete regions such as nerve terminals that form only a small part of the total tissue mass are known to be densely populated with CB 1 receptors. (420magazine.com)