... have remained intractable to therapeutic antibodies due to complexity of the target molecules. These complex target molecules include G-protein-coupled receptors and ion channels which represent a large potential target class for therapeutic intervention with monoclonal antibodies. Although...

...Sophie Mary; Jean-Alain Fehrentz; Marjorie Damian; Pascal Verdié; Jean Martinez; Jacky Marie; Jean-Louis Banères The dynamic character of GPCRs (G-protein-coupled receptors) is essential to their function. However, the details of how ligands and signalling proteins stabilize a receptor conformation...

...Robert M. Cooke; Markus Koglin; James C. Errey; Fiona H. Marshall Since the publication of the first X-ray structure of a GPCR (G-protein couple receptor) in 2000, the rate at which subsequent ones have appeared has steadily increased. This has required the development of new methodology...

...Martin Cottet; Orestis Faklaris; Amadine Falco; Eric Trinquet; Jean-Philippe Pin; Bernard Mouillac; Thierry Durroux Fluorescent ligands for GPCRs (G-protein-coupled receptors) have been synthesized for a long time but their use was usually restricted to receptor localization in the cell...

[email protected] ). 24 9 2012 © The Authors Journal compilation © 2013 Biochemical Society 2013 allosteric modulation biased signalling G-protein-coupled receptor glucagon-like peptide-1 receptor glucagon-like peptide-1 probe-dependence Type 2 DM (diabetes mellitus) is a global...

... sphingosine kinase, S1P lyase and S1P phosphatases. S1P binds to cell-surface G-protein-coupled receptors (S1P 1 –S1P 5 ) to elicit cell responses and can also regulate, by direct binding, a number of intracellular targets such as HDAC (histone deacetylase) 1/2 to induce epigenetic regulation. S1P is involved...

... system Cx43 connexin43 DEP dishevelled, Egl-10, pleckstrin Epac exchange protein directly activated by cAMP ERK extracellular-signal-regulated kinase GEF guanine-nucleotide-exchange factor GJ gap junction GRK2 G-protein-coupled receptor kinase 2 G s PCR G s...

...D.K. Covington; C.A. Briscoe; A.J. Brown; C.K. Jayawickreme Recent deorphanization efforts have paired the G-protein-coupled receptors GPR40, GPR41 and GPR43 with fatty acids as endogenous ligands. While carboxylic acids have been historically known to serve as fuel sources and biomarkers...

... Châtenay-Malabry Cedex, France (email [email protected] ). 3 4 2006 © 2006 The Biochemical Society 2006 adrenergic receptor cAMP cardiac myocyte cyclic nucleotide-gated channel (CNG channel) G-protein-coupled receptor phosphodiesterase (PDE) Early...

... membrane Na + /glucose cotransporter, SGLT1. The experimental evidence suggests that luminal sugar is sensed by a glucose sensor residing on the luminal membrane of the gut epithelium and linked to a G-protein-coupled receptor, cAMP/PKA (protein kinase A) pathway, resulting ultimately in modulation...

... receptor (CaR). CaR belongs to the ‘family C’ of G-protein-coupled receptors and was the first G-protein-coupled receptor to be identified to have an inorganic cation, calcium, as its ligand. While calcium is the physiological agonist of the receptor, several other polyvalent cations and polycations can...

... and the approaches that have been applied to monitoring the selectivity and the basis of α 1 -adrenoceptor dimerization are discussed. adrenaline adrenoceptor dimerization G-protein-coupled receptor Signalling Outwards and Inwards: A Focus Topic at BioScience2004, held at SECC Glasgow, U.K., 18–22 July...

...G. Milligan; H. Murdoch; E. Kellett; J.H. White; G.-J. Feng A substantial number of G-protein-coupled receptor-interacting proteins have been identified initially by the use of yeast two-hybrid screens. Using the C-terminal tail of both opioid receptors and the melanin concentrating hormone...

...T. Okada G-protein-coupled receptors constitute the largest transmembrane receptor family in human. They are generally activated on binding their specific ligands at the extracellular side of membranes. The signal carried by an agonist is then transmitted to the intracellular side through...

...A. Christopoulos; L.T. May; V.A. Avlani; P.M. Sexton 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...

... of the NMDAR to allow either rapid cAMP-dependent potentiation of NMDA transmission [ 18 – 21 ] or cAMP-independent inhibition of NMDA currents [ 22 ]. desensitization G-protein-coupled receptor ligand-gated channel oligomerization postsynaptic density striatum DA (dopamine) controls key...

...M. Bhattacharya; A.V. Babwah; S.S.G. Ferguson Heterotrimeric GPCRs (G-protein-coupled receptors) form the largest group of integral membrane receptor proteins and mediate diverse physiological processes. In addition to signalling via heterotrimeric G-proteins, GPCRs can also signal by interacting...

... of detectable hetero-oligomerization among α 2A -AR and MOR after overexpression in fibroblasts or primary cultures of hippocampal or spinal cord neurons. An emerging literature has demonstrated the homo- and hetero-oligomerization of GPCRs (G-protein-coupled receptors). In some cases, formation...

...A.B. Tobin; D.C. Budd It is now clear that G-protein-coupled receptors can regulate programmed cell death (apoptosis) through a variety of mechanisms that are dependent on cell type and receptor subtype. Here we present evidence that the G q/11 -coupled subtypes of the muscarinic receptor family...

... and is likely to operate via a G-protein-coupled receptor and cAMP/protein kinase A signalling cascade. Introduction Sensing nutrients is a fundamental challenge for all living cells. It is important for the intestinal epithelial cells, enterocytes, which are exposed from the luminal domain to an environment...

... of a family of related G-protein-coupled receptors (GPCRs) that are activated by vasopressin, oxytocin (OT) and related peptides. A segment of the N-terminus that was required for agonist binding, but not antagonist binding, was identified by characterizing truncated V 1a R constructs. Site-directed...

...-mail [email protected] Signalling the Future, a Biochemical Society-sponsored meeting held at University of Liverpool, Liverpool, 4–6 September 2002 6 September 2002 Copyright 2003 Biochemical Society 2003 G-protein-coupled receptor olfactory neuron second messenger...

... 6 September 2002 Copyright 2003 Biochemical Society 2003 G-protein G-protein-coupled receptor rhodopsin Abbreviations used: ACh, acetylcholine; mAChR, muscarinic acetylcholine receptor; NMS, N -methyl scopolamine; TM, transmembrane. Signalling the Future 29 Structure...