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Identification of aurintricarboxylic acid as a potent allosteric antagonist of P2X1 and P2X3 receptors.

Obrecht AS, Urban N, Schaefer M, Röse A, Kless A, Meents JE, Lampert A, Abdelrahman A, Müller CE, Schmalzing G, Hausmann R.

Neuropharmacology. 2019 Nov 1;158:107749. doi: 10.1016/j.neuropharm.2019.107749. Epub 2019 Aug 25.


Author Correction: The ASIC3/P2X3 cognate receptor is a pain-relevant and ligand-gated cationic channel.

Stephan G, Huang L, Tang Y, Vilotti S, Fabbretti E, Yu Y, Nörenberg W, Franke H, Gölöncsér F, Sperlágh B, Dopychai A, Hausmann R, Schmalzing G, Rubini P, Illes P.

Nat Commun. 2018 Aug 17;9(1):3351. doi: 10.1038/s41467-018-05621-7.


Loss-of-function of Nav1.8/D1639N linked to human pain can be rescued by lidocaine.

Kaluza L, Meents JE, Hampl M, Rösseler C, Hautvast PAI, Detro-Dassen S, Hausmann R, Schmalzing G, Lampert A.

Pflugers Arch. 2018 Dec;470(12):1787-1801. doi: 10.1007/s00424-018-2189-x. Epub 2018 Aug 11.


β-Nicotinamide Adenine Dinucleotide (β-NAD) Inhibits ATP-Dependent IL-1β Release from Human Monocytic Cells.

Hiller SD, Heldmann S, Richter K, Jurastow I, Küllmar M, Hecker A, Wilker S, Fuchs-Moll G, Manzini I, Schmalzing G, Kummer W, Padberg W, McIntosh JM, Damm J, Zakrzewicz A, Grau V.

Int J Mol Sci. 2018 Apr 10;19(4). pii: E1126. doi: 10.3390/ijms19041126.


The ASIC3/P2X3 cognate receptor is a pain-relevant and ligand-gated cationic channel.

Stephan G, Huang L, Tang Y, Vilotti S, Fabbretti E, Yu Y, Nörenberg W, Franke H, Gölöncsér F, Sperlágh B, Dopychai A, Hausmann R, Schmalzing G, Rubini P, Illes P.

Nat Commun. 2018 Apr 10;9(1):1354. doi: 10.1038/s41467-018-03728-5. Erratum in: Nat Commun. 2018 Aug 17;9(1):3351.


The Elusive P2X7 Macropore.

Di Virgilio F, Schmalzing G, Markwardt F.

Trends Cell Biol. 2018 May;28(5):392-404. doi: 10.1016/j.tcb.2018.01.005. Epub 2018 Feb 10. Review.


Interaction of Purinergic P2X4 and P2X7 Receptor Subunits.

Schneider M, Prudic K, Pippel A, Klapperstück M, Braam U, Müller CE, Schmalzing G, Markwardt F.

Front Pharmacol. 2017 Nov 22;8:860. doi: 10.3389/fphar.2017.00860. eCollection 2017.


Localization of the gate and selectivity filter of the full-length P2X7 receptor.

Pippel A, Stolz M, Woltersdorf R, Kless A, Schmalzing G, Markwardt F.

Proc Natl Acad Sci U S A. 2017 Mar 14;114(11):E2156-E2165. doi: 10.1073/pnas.1610414114. Epub 2017 Feb 24.


The protective effect of resveratrol in the transmission of neuropathic pain mediated by the P2X7 receptor in the dorsal root ganglia.

Xie J, Liu S, Wu B, Li G, Rao S, Zou L, Yi Z, Zhang C, Jia T, Zhao S, Schmalzing G, Hausmann R, Nie H, Li G, Liang S.

Neurochem Int. 2017 Feb;103:24-35. doi: 10.1016/j.neuint.2016.12.006. Epub 2016 Dec 24.


Inter-subunit disulfide locking of the human P2X3 receptor elucidates ectodomain movements associated with channel gating.

Stephan G, Kowalski-Jahn M, Zens C, Schmalzing G, Illes P, Hausmann R.

Purinergic Signal. 2016 Jun;12(2):221-33. doi: 10.1007/s11302-016-9496-5. Epub 2016 Jan 29.


Impaired surface membrane insertion of homo- and heterodimeric human muscle chloride channels carrying amino-terminal myotonia-causing mutations.

Ronstedt K, Sternberg D, Detro-Dassen S, Gramkow T, Begemann B, Becher T, Kilian P, Grieschat M, Machtens JP, Schmalzing G, Fischer M, Fahlke C.

Sci Rep. 2015 Oct 27;5:15382. doi: 10.1038/srep15382.


Flexible subunit stoichiometry of functional human P2X2/3 heteromeric receptors.

Kowalski M, Hausmann R, Schmid J, Dopychai A, Stephan G, Tang Y, Schmalzing G, Illes P, Rubini P.

Neuropharmacology. 2015 Dec;99:115-30. doi: 10.1016/j.neuropharm.2015.07.008. Epub 2015 Jul 13.


Homodimeric anoctamin-1, but not homodimeric anoctamin-6, is activated by calcium increases mediated by the P2Y1 and P2X7 receptors.

Stolz M, Klapperstück M, Kendzierski T, Detro-Dassen S, Panning A, Schmalzing G, Markwardt F.

Pflugers Arch. 2015 Oct;467(10):2121-40. doi: 10.1007/s00424-015-1687-3. Epub 2015 Jan 17.


Conformational flexibility of the agonist binding jaw of the human P2X3 receptor is a prerequisite for channel opening.

Kowalski M, Hausmann R, Dopychai A, Grohmann M, Franke H, Nieber K, Schmalzing G, Illes P, Riedel T.

Br J Pharmacol. 2014 Nov;171(22):5093-112. doi: 10.1111/bph.12830. Epub 2014 Sep 5.


A hydrophobic residue in position 15 of the rP2X3 receptor slows desensitization and reveals properties beneficial for pharmacological analysis and high-throughput screening.

Hausmann R, Bahrenberg G, Kuhlmann D, Schumacher M, Braam U, Bieler D, Schlusche I, Schmalzing G.

Neuropharmacology. 2014 Apr;79:603-15. doi: 10.1016/j.neuropharm.2014.01.010. Epub 2014 Jan 19.


Characterization of SLCO5A1/OATP5A1, a solute carrier transport protein with non-classical function.

Sebastian K, Detro-Dassen S, Rinis N, Fahrenkamp D, Müller-Newen G, Merk HF, Schmalzing G, Zwadlo-Klarwasser G, Baron JM.

PLoS One. 2013 Dec 20;8(12):e83257. doi: 10.1371/journal.pone.0083257. eCollection 2013.


Salt bridge switching from Arg290/Glu167 to Arg290/ATP promotes the closed-to-open transition of the P2X2 receptor.

Hausmann R, Günther J, Kless A, Kuhlmann D, Kassack MU, Bahrenberg G, Markwardt F, Schmalzing G.

Mol Pharmacol. 2013 Jan;83(1):73-84. doi: 10.1124/mol.112.081489. Epub 2012 Oct 5.


P2X1 and P2X2 receptors in the central nervous system as possible drug targets.

Hausmann R, Schmalzing G.

CNS Neurol Disord Drug Targets. 2012 Sep;11(6):675-86. Review.


Positive allosteric modulation by ivermectin of human but not murine P2X7 receptors.

Nörenberg W, Sobottka H, Hempel C, Plötz T, Fischer W, Schmalzing G, Schaefer M.

Br J Pharmacol. 2012 Sep;167(1):48-66. doi: 10.1111/j.1476-5381.2012.01987.x.


ATP binding site mutagenesis reveals different subunit stoichiometry of functional P2X2/3 and P2X2/6 receptors.

Hausmann R, Bodnar M, Woltersdorf R, Wang H, Fuchs M, Messemer N, Qin Y, Günther J, Riedel T, Grohmann M, Nieber K, Schmalzing G, Rubini P, Illes P.

J Biol Chem. 2012 Apr 20;287(17):13930-43. doi: 10.1074/jbc.M112.345207. Epub 2012 Feb 29.


The effect of anions on the human P2X7 receptor.

Kubick C, Schmalzing G, Markwardt F.

Biochim Biophys Acta. 2011 Dec;1808(12):2913-22. doi: 10.1016/j.bbamem.2011.08.017. Epub 2011 Aug 19.


A Single phenylalanine residue in the main intracellular loop of α1 γ-aminobutyric acid type A and glycine receptors influences their sensitivity to propofol.

Moraga-Cid G, Yevenes GE, Schmalzing G, Peoples RW, Aguayo LG.

Anesthesiology. 2011 Sep;115(3):464-73. doi: 10.1097/ALN.0b013e31822550f7.


Robust post-translocational N-glycosylation at the extreme C-terminus of membrane and secreted proteins in Xenopus laevis oocytes and HEK293 cells.

Pult F, Fallah G, Braam U, Detro-Dassen S, Niculescu C, Laube B, Schmalzing G.

Glycobiology. 2011 Sep;21(9):1147-60. doi: 10.1093/glycob/cwr013. Epub 2011 Feb 8.


Discovery of potent competitive antagonists and positive modulators of the P2X2 receptor.

Baqi Y, Hausmann R, Rosefort C, Rettinger J, Schmalzing G, Müller CE.

J Med Chem. 2011 Feb 10;54(3):817-30. Epub 2011 Jan 5.


Molecular determinants of potent P2X2 antagonism identified by functional analysis, mutagenesis, and homology docking.

Wolf C, Rosefort C, Fallah G, Kassack MU, Hamacher A, Bodnar M, Wang H, Illes P, Kless A, Bahrenberg G, Schmalzing G, Hausmann R.

Mol Pharmacol. 2011 Apr;79(4):649-61. doi: 10.1124/mol.110.068700. Epub 2010 Dec 29.


Amino acid residues constituting the agonist binding site of the human P2X3 receptor.

Bodnar M, Wang H, Riedel T, Hintze S, Kato E, Fallah G, Gröger-Arndt H, Giniatullin R, Grohmann M, Hausmann R, Schmalzing G, Illes P, Rubini P.

J Biol Chem. 2011 Jan 28;286(4):2739-49. doi: 10.1074/jbc.M110.167437. Epub 2010 Nov 22.


TMEM16A(a)/anoctamin-1 shares a homodimeric architecture with CLC chloride channels.

Fallah G, Römer T, Detro-Dassen S, Braam U, Markwardt F, Schmalzing G.

Mol Cell Proteomics. 2011 Feb;10(2):M110.004697. doi: 10.1074/mcp.M110.004697. Epub 2010 Oct 25.


Ectopic vesicular neurotransmitter release along sensory axons mediates neurovascular coupling via glial calcium signaling.

Thyssen A, Hirnet D, Wolburg H, Schmalzing G, Deitmer JW, Lohr C.

Proc Natl Acad Sci U S A. 2010 Aug 24;107(34):15258-63. doi: 10.1073/pnas.1003501107. Epub 2010 Aug 9.


Trophic activity of a naturally occurring truncated isoform of the P2X7 receptor.

Adinolfi E, Cirillo M, Woltersdorf R, Falzoni S, Chiozzi P, Pellegatti P, Callegari MG, Sandonà D, Markwardt F, Schmalzing G, Di Virgilio F.

FASEB J. 2010 Sep;24(9):3393-404. doi: 10.1096/fj.09-153601. Epub 2010 May 7.


Effects of protons on macroscopic and single-channel currents mediated by the human P2X7 receptor.

Flittiger B, Klapperstück M, Schmalzing G, Markwardt F.

Biochim Biophys Acta. 2010 May;1798(5):947-57. doi: 10.1016/j.bbamem.2010.01.023. Epub 2010 Feb 4.


An intramembrane aromatic network determines pentameric assembly of Cys-loop receptors.

Haeger S, Kuzmin D, Detro-Dassen S, Lang N, Kilb M, Tsetlin V, Betz H, Laube B, Schmalzing G.

Nat Struct Mol Biol. 2010 Jan;17(1):90-8. doi: 10.1038/nsmb.1721. Epub 2009 Dec 20.


NF546 [4,4'-(carbonylbis(imino-3,1-phenylene-carbonylimino-3,1-(4-methyl-phenylene)-carbonylimino))-bis(1,3-xylene-alpha,alpha'-diphosphonic acid) tetrasodium salt] is a non-nucleotide P2Y11 agonist and stimulates release of interleukin-8 from human monocyte-derived dendritic cells.

Meis S, Hamacher A, Hongwiset D, Marzian C, Wiese M, Eckstein N, Royer HD, Communi D, Boeynaems JM, Hausmann R, Schmalzing G, Kassack MU.

J Pharmacol Exp Ther. 2010 Jan;332(1):238-47. doi: 10.1124/jpet.109.157750. Epub 2009 Oct 8.


Cross-inhibition between native and recombinant TRPV1 and P2X(3) receptors.

Stanchev D, Blosa M, Milius D, Gerevich Z, Rubini P, Schmalzing G, Eschrich K, Schaefer M, Wirkner K, Illes P.

Pain. 2009 May;143(1-2):26-36. doi: 10.1016/j.pain.2009.01.006. Epub 2009 Feb 14.


A selective G betagamma-linked intracellular mechanism for modulation of a ligand-gated ion channel by ethanol.

Yevenes GE, Moraga-Cid G, Peoples RW, Schmalzing G, Aguayo LG.

Proc Natl Acad Sci U S A. 2008 Dec 23;105(51):20523-8. doi: 10.1073/pnas.0806257105. Epub 2008 Dec 12.


The P2X7 carboxyl tail is a regulatory module of P2X7 receptor channel activity.

Becker D, Woltersdorf R, Boldt W, Schmitz S, Braam U, Schmalzing G, Markwardt F.

J Biol Chem. 2008 Sep 12;283(37):25725-34. doi: 10.1074/jbc.M803855200. Epub 2008 Jul 10.


Lack of evidence for direct phosphorylation of recombinantly expressed P2X(2) and P2X (3) receptors by protein kinase C.

Franklin C, Braam U, Eisele T, Schmalzing G, Hausmann R.

Purinergic Signal. 2007 Sep;3(4):377-88. doi: 10.1007/s11302-007-9067-x. Epub 2007 Sep 6.


Conserved dimeric subunit stoichiometry of SLC26 multifunctional anion exchangers.

Detro-Dassen S, Schänzler M, Lauks H, Martin I, zu Berstenhorst SM, Nothmann D, Torres-Salazar D, Hidalgo P, Schmalzing G, Fahlke C.

J Biol Chem. 2008 Feb 15;283(7):4177-88. Epub 2007 Dec 11.


Exploring fluorescence antibunching in solution to determine the stoichiometry of molecular complexes.

Sýkora J, Kaiser K, Gregor I, Bönigk W, Schmalzing G, Enderlein J.

Anal Chem. 2007 Jun 1;79(11):4040-9. Epub 2007 May 8.


Kinetics of P2X7 receptor-operated single channels currents.

Riedel T, Lozinsky I, Schmalzing G, Markwardt F.

Biophys J. 2007 Apr 1;92(7):2377-91. Epub 2006 Dec 22.


Molecular basis of gephyrin clustering at inhibitory synapses: role of G- and E-domain interactions.

Saiyed T, Paarmann I, Schmitt B, Haeger S, Sola M, Schmalzing G, Weissenhorn W, Betz H.

J Biol Chem. 2007 Feb 23;282(8):5625-32. Epub 2006 Dec 20.


Characterization of the Interleukin (IL)-6 Inhibitor IL-6-RFP: fused receptor domains act as high affinity cytokine-binding proteins.

Metz S, Wiesinger M, Vogt M, Lauks H, Schmalzing G, Heinrich PC, Müller-Newen G.

J Biol Chem. 2007 Jan 12;282(2):1238-48. Epub 2006 Nov 3.


Molecular determinants for G protein betagamma modulation of ionotropic glycine receptors.

Yevenes GE, Moraga-Cid G, Guzmán L, Haeger S, Oliveira L, Olate J, Schmalzing G, Aguayo LG.

J Biol Chem. 2006 Dec 22;281(51):39300-7. Epub 2006 Oct 12.


P2X5 subunit assembly requires scaffolding by the second transmembrane domain and a conserved aspartate.

Duckwitz W, Hausmann R, Aschrafi A, Schmalzing G.

J Biol Chem. 2006 Dec 22;281(51):39561-72. Epub 2006 Sep 25.


Synthesis and structure-activity relationships of suramin-derived P2Y11 receptor antagonists with nanomolar potency.

Ullmann H, Meis S, Hongwiset D, Marzian C, Wiese M, Nickel P, Communi D, Boeynaems JM, Wolf C, Hausmann R, Schmalzing G, Kassack MU.

J Med Chem. 2005 Nov 3;48(22):7040-8.


The beta subunit determines the ligand binding properties of synaptic glycine receptors.

Grudzinska J, Schemm R, Haeger S, Nicke A, Schmalzing G, Betz H, Laube B.

Neuron. 2005 Mar 3;45(5):727-39.


Profiling at recombinant homomeric and heteromeric rat P2X receptors identifies the suramin analogue NF449 as a highly potent P2X1 receptor antagonist.

Rettinger J, Braun K, Hochmann H, Kassack MU, Ullmann H, Nickel P, Schmalzing G, Lambrecht G.

Neuropharmacology. 2005 Mar;48(3):461-8.


Dissecting individual current components of co-expressed human P2X1 and P2X7 receptors.

Seyffert C, Schmalzing G, Markwardt F.

Curr Top Med Chem. 2004;4(16):1719-30.


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