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  • Antagonists
  • 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)
  • bind
  • none of them can reliably predict binding affinities, although many have proven successful at distinguishing low-likelihood ligands from those more likely to bind. (pnas.org)
  • 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)
  • During the past decade, more than half a dozen chemically distinct (that is, unrelated to 1,4-BDZ) structures have been reported to bind with high affinities to these BDZ receptors (BDZR), with at least as many compounds reported to possess anticonflict (and/or anxiolytic) actions devoid of significant hypnotic and/or myorelaxant potential (reviewed in Skolnick and Paul, 1988). (springer.com)
  • However, the terminology of 1,25-dihydroxyvitamin D, or 1,25(OH)2D, is often used to refer to both types of active forms of vitamin D. Indeed, both bind to the vitamin D receptor and produce biological effects. (wikipedia.org)
  • protein
  • Aminergic G protein-coupled receptors (GPCRs) have been a major focus of pharmaceutical research for many years. (pnas.org)
  • (pnas.org)
  • Looking for ligand variation, not protein variation. (fold.it)
  • The ligand was arbitrarily placed in the protein with an arbitrary conformation, and we hope that players can find where it should go. (fold.it)
  • 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)
  • Since then, advances in protein expression, structure determination methods and functional assays have enabled us to define the molecular basis of the core receptor/ligand interaction and given new insights into the architecture of the Notch complex at the cell surface. (springer.com)
  • Ligand-dependent nuclear receptor-interacting factor 1 (LRIF1) also known as receptor-interacting factor 1 (RIF1) is a protein that in humans is encoded by the C1orf103 gene. (wikipedia.org)
  • This stimulates ligand-induced dimerization, activating the intrinsic protein-tyrosine kinase activity of the receptor (see the second diagram). (wikipedia.org)
  • potent
  • 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)
  • complementarity
  • Here we explore whether novel chemotypes may be discovered for the A(2A) adenosine receptor, based on complementarity to its recently determined structure. (nih.gov)
  • adult
  • A) Under favorable conditions, cholesterol is converted into ligands of the nuclear hormone receptor DAF-12, triggering development to adult worms. (nih.gov)
  • lipid
  • 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)
  • Binding
  • 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)
  • Strategies that may reduce the immunogenicity of CAR T cells are humanization of the scFv and the use of naturally occurring receptor ligands as antigen-binding domains. (mdpi.com)
  • Gottschalk, S. Foreign or Domestic CARs: Receptor Ligands as Antigen-Binding Domains. (mdpi.com)
  • 2014. "Foreign or Domestic CARs: Receptor Ligands as Antigen-Binding Domains. (mdpi.com)
  • Furthermore, structure determination of O -glycosylated variants of Notch alone or in complex with receptor fragments, has shown that these sugars contribute directly to the binding interface, as well as to stabilizing intra-molecular domain structure, providing some mechanistic insights into the observed modulatory effects of O -glycosylation on Notch activity. (springer.com)
  • Chillakuri CR, Sheppard D, Lea SM, Handford PA (2012) Notch receptor-ligand binding and activation: insights from molecular studies. (springer.com)
  • It is largely related to menstrual and estrous and its biological function is mediated by binding to two receptors: Estrogen Receptor alpha (ERα) and Estrogen Receptor beta (ERβ). (wikipedia.org)
  • targets
  • The recently determined X-ray structure of the β 2 -adrenergic receptor offers an opportunity to investigate the advantages and limitations inherent in a structure-based approach to ligand discovery against this and related GPCR targets. (pnas.org)
  • vertebrate
  • The development and lifespan of C. elegans are controlled by the nuclear hormone receptor DAF-12, an important model for the vertebrate vitamin D and liver X receptors. (nih.gov)
  • structures
  • Due partly to the lack of reliable receptor structures, drug discovery efforts have been largely ligand-based. (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)
  • Only a few different classes of structures are currently known as ligands for the GABA recognition site on the GABA-A receptor complex, reflecting the very strict structural requirements for GABA-A receptor recognition and activation. (eurekaselect.com)
  • suggests
  • Recent evidence suggests that imidazoline I-2 receptor ligands are suitable for combination therapy with opioids. (rti.org)
  • Quantitative analysis of the antihyperalgesic and response rate-suppressing effects suggests that I-2 receptor ligands are not well suited to combination therapy with acetaminophen. (rti.org)
  • neurological
  • In pursuit of neurological therapies, the opioid system, specifically delta opioid receptors and delta opioid peptides, demonstrates promising therapeutic potential for stroke, Parkinson's disease, and other degenerative neurological conditions. (mdpi.com)
  • enables
  • The ability of ligands to differentially regulate the activity of signaling pathways coupled to a receptor potentially enables researchers to optimize therapeutically relevant efficacies, while minimizing activity at pathways that lead to adverse effects. (ku.edu)
  • structural
  • These data suggest that the efficacy for specific signaling pathways can be finely tuned by structural modifications to a given ligand. (ku.edu)
  • human
  • In the previous puzzle, we asked you to model the structure of the human Y1 neuropeptide receptor. (fold.it)
  • delta
  • Recent studies offer strong evidence in support of the therapeutic use of delta opioid receptors, and provide insights into the underlying mechanisms of action. (mdpi.com)
  • Delta opioid receptors have been shown to confer protective effects by mediating ionic homeostasis and activating endogenous neuroprotective pathways. (mdpi.com)