Search Results - (Author, Cooperation:J. R. Traynor)
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1Latest Papers from Table of Contents or Articles in PressW. Huang ; A. Manglik ; A. J. Venkatakrishnan ; T. Laeremans ; E. N. Feinberg ; A. L. Sanborn ; H. E. Kato ; K. E. Livingston ; T. S. Thorsen ; R. C. Kling ; S. Granier ; P. Gmeiner ; S. M. Husbands ; J. R. Traynor ; W. I. Weis ; J. Steyaert ; R. O. Dror ; B. K. Kobilka
Nature Publishing Group (NPG)
Published 2015Staff ViewPublication Date: 2015-08-08Publisher: Nature Publishing Group (NPG)Print ISSN: 0028-0836Electronic ISSN: 1476-4687Topics: BiologyChemistry and PharmacologyMedicineNatural Sciences in GeneralPhysicsKeywords: Allosteric Regulation ; Animals ; Binding Sites ; Crystallography, X-Ray ; Heterotrimeric GTP-Binding Proteins/chemistry/metabolism ; Mice ; Models, Molecular ; Molecular Dynamics Simulation ; Morphinans/chemistry/metabolism/pharmacology ; Protein Stability/drug effects ; Protein Structure, Tertiary ; Pyrroles/chemistry/metabolism/pharmacology ; Receptor, Muscarinic M2/chemistry ; Receptors, Adrenergic, beta-2/chemistry ; Receptors, Opioid, mu/agonists/*chemistry/*metabolism ; Single-Chain Antibodies/chemistry/pharmacology ; Structure-Activity RelationshipPublished by: -
2Latest Papers from Table of Contents or Articles in PressLivingston, K. E., Stanczyk, M. A., Burford, N. T., Alt, A., Canals, M., Traynor, J. R.
The American Society for Pharmacology and Experimental Therapeutics (ASPET)
Published 2018Staff ViewPublication Date: 2018-01-13Publisher: The American Society for Pharmacology and Experimental Therapeutics (ASPET)Print ISSN: 0026-895XElectronic ISSN: 1521-0111Topics: Chemistry and PharmacologyMedicinePublished by: -
3Articles: DFG German National LicensesStaff View
ISSN: 1471-4159Source: Blackwell Publishing Journal Backfiles 1879-2005Topics: MedicineNotes: Abstract: The binding of the unselective opioid antagonist [3H]diprenorphine to homogenates prepared from rat brain and from guinea-pig brain and cerebellum has been studied in HEPES buffer containing 10 mM Mg2+ ions. Sequential displacement of bound [3H]diprenorphine by ligands with selectivity for μ-, 8- δ, and k-opioid receptors uncovers the multiple components of binding. In the presence of cold ligands that occupy all μ-, δ-, and k-sites, opioid binding still remains. This binding represents 20% of total specific sites and is displaced by naloxone. The nature of these undefined opioid binding sites is discussed.Type of Medium: Electronic ResourceURL: -
4Articles: DFG German National LicensesRodriguez, F. D. ; Bardaji, E. ; Traynor, J. R.
Oxford, UK : Blackwell Publishing Ltd
Published 1992Staff ViewISSN: 1471-4159Source: Blackwell Publishing Journal Backfiles 1879-2005Topics: MedicineNotes: Abstract: The effects of MgCl2 on the binding of tritiated ligands to opioid binding sites in homogenates of guinea-pig brain in HEPES buffer have been studied. The binding of tritiated μ-, δ, and κ-opioid agonists was promoted in a concentration-dependent manner over a range of MgCl2 concentrations from 0.1 mM to 10 mM, as was binding of the nonselective antagonists [3H]diprenorphine and [3H]naloxone. At concentrations of MgCl2 above 10 mM reversal of this effect was observed. The effects of MgCl2 on binding parameters differed at each site. The promoting effects of MgCl2 were mimicked by MnCl2, CaCl2, and MgSO4, but CoCl2 and ZnCl2 were inhibitory. Following treatment of guinea-pig brain synaptosomes at pH 11.5 to eliminate G proteins, the binding of the μ-opioid agonist [3H][D-Ala2, MePhe4, Gly-ol5]enkephalin and [3H]naloxone was much reduced but binding of [3H]diprenorphine was unaffected. Under these conditions MgCl2 still promoted binding of [3H]diprenorphine. The results suggest that Mg2+ ions promote binding by an action at the opioid receptor, even in the absence of G protein, and that opioid antagonists may differ in their recognition of opioid receptor binding sites.Type of Medium: Electronic ResourceURL: -
5Articles: DFG German National LicensesStaff View
ISSN: 1471-4159Source: Blackwell Publishing Journal Backfiles 1879-2005Topics: MedicineNotes: [3H]Dynorphin A(1–8) is readily metabolised by rat lumbosacral spinal cord tissue in vitro, affording a variety of products including a significant amount (20% recovered activity) of [3H][Leu5]enkephalin. In the presence of the peptidase inhibitors bestatin, captopril, thiorphan, and leucylleucine, [3H][Leu5]enkephalin was the major metabolic product, accounting for 60% of recovered activity. Production of [3H][Leu5]enkephalin was seen across all gross brain regions. The enzyme responsible for the cleavage has an optimal substrate length of 8–13 amino acids and is inhibited b N-[1-(RS)-carboxy-2-phenylethyl]-Ala-Ala-Phe-p-aminobenzoate, a site-directed inhibitor of the metalloendopeptidase EC 3.4.24.15. However the enzymic breakdown also has properties in common with involvement of endo-oligopeptidase A. Possible consequences of the formation of [Leu5]enkephalin from the smaller dynorphins are discussed.Type of Medium: Electronic ResourceURL: -
6Articles: DFG German National LicensesStaff View
ISSN: 0030-493XKeywords: Chemistry ; Analytical Chemistry and SpectroscopySource: Wiley InterScience Backfile Collection 1832-2000Topics: Chemistry and PharmacologyNotes: The mass spectra of eight pyrrolo[1,2-a][1,3,5]triazie-2,4(1H, 3H)-diones have been examined. An unusual feature in the fragmentation of those compounds having a 7-alkoxycarbonyl function, namely loss of the whole ester grouping with concomitant hydrogen rearrangement, is discussed.Additional Material: 1 Tab.Type of Medium: Electronic ResourceURL: