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Items: 1 to 50 of 159

1.

Modeling and mutational analysis of the binding mode for the multimodal antidepressant drug vortioxetine to the human 5-HT3A receptor.

Ladefoged LK, Munro L, Pedersen AJ, Balle T, Bang-Andersen B, Lummis SCR, Schiott B, Kristensen AS.

Mol Pharmacol. 2018 Sep 26. pii: mol.118.113530. doi: 10.1124/mol.118.113530. [Epub ahead of print]

2.

The roles of aromatic residues in the glycine receptor transmembrane domain.

Tang B, Lummis SCR.

BMC Neurosci. 2018 Sep 6;19(1):53. doi: 10.1186/s12868-018-0454-8.

3.

Identification of Novel Functionally Important Aromatic Residue Interactions in the Extracellular Domain of the Glycine Receptor.

Tang B, Devenish SO, Lummis SCR.

Biochemistry. 2018 Jul 10;57(27):4029-4035. doi: 10.1021/acs.biochem.8b00425. Epub 2018 Jun 27.

PMID:
29947514
4.

Multiple regions in the extracellular domain of the glycine receptor determine receptor activity.

Tang B, Lummis SCR.

J Biol Chem. 2018 Sep 7;293(36):13889-13896. doi: 10.1074/jbc.RA118.003088. Epub 2018 Jun 25.

5.

Probing Proline Residues in the Prokaryotic Ligand-Gated Ion Channel, ELIC.

Mosesso R, Dougherty DA, Lummis SCR.

Biochemistry. 2018 Jul 10;57(27):4036-4043. doi: 10.1021/acs.biochem.8b00379. Epub 2018 Jun 21.

PMID:
29927250
6.

Characterization of a 5-HT3-ELIC Chimera Revealing the Sites of Action of Modulators.

Price KL, Lummis SCR.

ACS Chem Neurosci. 2018 Jun 20;9(6):1409-1415. doi: 10.1021/acschemneuro.8b00028. Epub 2018 Mar 6.

PMID:
29508995
7.

Aromatic Residues in the Fourth Transmembrane-Spanning Helix M4 Are Important for GABAρ Receptor Function.

Cory-Wright J, Alqazzaz M, Wroe F, Jeffreys J, Zhou L, Lummis SCR.

ACS Chem Neurosci. 2018 Feb 21;9(2):284-290. doi: 10.1021/acschemneuro.7b00315. Epub 2017 Nov 9.

PMID:
29120166
8.

Unexpected resilience of a seagrass system exposed to global stressors.

Hughes BB, Lummis SC, Anderson SC, Kroeker KJ.

Glob Chang Biol. 2018 Jan;24(1):224-234. doi: 10.1111/gcb.13854. Epub 2017 Sep 13.

PMID:
28752587
9.

The Proton Responsiveness in the Extracellular Domain of GLIC Differs in the Presence of the ELIC Transmembrane Domain.

Alqazzaz MA, Price KL, Lummis SCR.

Biochemistry. 2017 Apr 18;56(15):2134-2138. doi: 10.1021/acs.biochem.6b00900. Epub 2017 Apr 6.

PMID:
28383883
10.

Subtle Differences among 5-HT3AC, 5-HT3AD, and 5-HT3AE Receptors Are Revealed by Partial Agonists.

Price KL, Hirayama Y, Lummis SCR.

ACS Chem Neurosci. 2017 May 17;8(5):1085-1091. doi: 10.1021/acschemneuro.6b00416. Epub 2017 Apr 3.

PMID:
28367632
11.

Crotonic Acid Blocks the Gloeobacter Ligand-Gated Ion Channel (GLIC) via the Extracellular Domain.

Alqazzaz MA, Price KL, Lummis SC.

Biochemistry. 2016 Oct 14. [Epub ahead of print]

PMID:
27739668
12.

Palonosetron-5-HT3 Receptor Interactions As Shown by a Binding Protein Cocrystal Structure.

Price KL, Lillestol RK, Ulens C, Lummis SC.

ACS Chem Neurosci. 2016 Dec 21;7(12):1641-1646. doi: 10.1021/acschemneuro.6b00132. Epub 2016 Sep 22.

13.

Perturbation of Critical Prolines in Gloeobacter violaceus Ligand-gated Ion Channel (GLIC) Supports Conserved Gating Motions among Cys-loop Receptors.

Rienzo M, Rocchi AR, Threatt SD, Dougherty DA, Lummis SC.

J Biol Chem. 2016 Mar 18;291(12):6272-80. doi: 10.1074/jbc.M115.694372. Epub 2015 Dec 14.

14.

The nicotinic α6 subunit gene determines variability in chronic pain sensitivity via cross-inhibition of P2X2/3 receptors.

Wieskopf JS, Mathur J, Limapichat W, Post MR, Al-Qazzaz M, Sorge RE, Martin LJ, Zaykin DV, Smith SB, Freitas K, Austin JS, Dai F, Zhang J, Marcovitz J, Tuttle AH, Slepian PM, Clarke S, Drenan RM, Janes J, Al Sharari S, Segall SK, Aasvang EK, Lai W, Bittner R, Richards CI, Slade GD, Kehlet H, Walker J, Maskos U, Changeux JP, Devor M, Maixner W, Diatchenko L, Belfer I, Dougherty DA, Su AI, Lummis SC, Imad Damaj M, Lester HA, Patapoutian A, Mogil JS.

Sci Transl Med. 2015 May 13;7(287):287ra72. doi: 10.1126/scitranslmed.3009986.

15.

5-HT3 Receptor Brain-Type B-Subunits are Differentially Expressed in Heterologous Systems.

Corradi J, Thompson AJ, McGonigle I, Price KL, Bouzat C, Lummis SC.

ACS Chem Neurosci. 2015 Jul 15;6(7):1158-64. doi: 10.1021/acschemneuro.5b00080. Epub 2015 May 7.

16.

Probing residues in the pore-forming (M2) domain of the Cys-loop receptor homologue GLIC reveals some unusual features.

Alqazzaz MA, Lummis SC.

Mol Membr Biol. 2015;32(1):26-31. doi: 10.3109/09687688.2015.1023377. Epub 2015 Apr 13.

PMID:
25865129
17.

Varenicline Interactions at the 5-HT3 Receptor Ligand Binding Site are Revealed by 5-HTBP.

Price KL, Lillestol RK, Ulens C, Lummis SC.

ACS Chem Neurosci. 2015 Jul 15;6(7):1151-7. doi: 10.1021/cn500369h. Epub 2015 Feb 19.

18.

Disturbed neuronal ER-Golgi sorting of unassembled glycine receptors suggests altered subcellular processing is a cause of human hyperekplexia.

Schaefer N, Kluck CJ, Price KL, Meiselbach H, Vornberger N, Schwarzinger S, Hartmann S, Langlhofer G, Schulz S, Schlegel N, Brockmann K, Lynch B, Becker CM, Lummis SC, Villmann C.

J Neurosci. 2015 Jan 7;35(1):422-37. doi: 10.1523/JNEUROSCI.1509-14.2015.

19.

Structural requirements in the transmembrane domain of GLIC revealed by incorporation of noncanonical histidine analogs.

Rienzo M, Lummis SC, Dougherty DA.

Chem Biol. 2014 Dec 18;21(12):1700-6. doi: 10.1016/j.chembiol.2014.10.019.

20.

An atypical residue in the pore of Varroa destructor GABA-activated RDL receptors affects picrotoxin block and thymol modulation.

Price KL, Lummis SC.

Insect Biochem Mol Biol. 2014 Dec;55:19-25. doi: 10.1016/j.ibmb.2014.10.002. Epub 2014 Oct 18.

21.

Phenylalanine in the pore of the Erwinia ligand-gated ion channel modulates picrotoxinin potency but not receptor function.

Thompson AJ, Alqazzaz M, Price KL, Weston DA, Lummis SC.

Biochemistry. 2014 Oct 7;53(39):6183-8. doi: 10.1021/bi5008035. Epub 2014 Sep 19.

22.

The prokaryote ligand-gated ion channel ELIC captured in a pore blocker-bound conformation by the Alzheimer's disease drug memantine.

Ulens C, Spurny R, Thompson AJ, Alqazzaz M, Debaveye S, Han L, Price K, Villalgordo JM, Tresadern G, Lynch JW, Lummis SC.

Structure. 2014 Oct 7;22(10):1399-407. doi: 10.1016/j.str.2014.07.013. Epub 2014 Sep 4.

23.

The binding characteristics and orientation of a novel radioligand with distinct properties at 5-HT3A and 5-HT3AB receptors.

Thompson AJ, Verheij MH, Verbeek J, Windhorst AD, de Esch IJ, Lummis SC.

Neuropharmacology. 2014 Nov;86:378-88. doi: 10.1016/j.neuropharm.2014.08.008. Epub 2014 Aug 28.

24.

The Concise Guide to PHARMACOLOGY 2013/14: overview.

Alexander SP, Benson HE, Faccenda E, Pawson AJ, Sharman JL, McGrath JC, Catterall WA, Spedding M, Peters JA, Harmar AJ; CGTP Collaborators, Abul-Hasn N, Anderson CM, Anderson CM, Araiksinen MS, Arita M, Arthofer E, Barker EL, Barratt C, Barnes NM, Bathgate R, Beart PM, Belelli D, Bennett AJ, Birdsall NJ, Boison D, Bonner TI, Brailsford L, Bröer S, Brown P, Calo G, Carter WG, Catterall WA, Chan SL, Chao MV, Chiang N, Christopoulos A, Chun JJ, Cidlowski J, Clapham DE, Cockcroft S, Connor MA, Cox HM, Cuthbert A, Dautzenberg FM, Davenport AP, Dawson PA, Dent G, Dijksterhuis JP, Dollery CT, Dolphin AC, Donowitz M, Dubocovich ML, Eiden L, Eidne K, Evans BA, Fabbro D, Fahlke C, Farndale R, Fitzgerald GA, Fong TM, Fowler CJ, Fry JR, Funk CD, Futerman AH, Ganapathy V, Gaisnier B, Gershengorn MA, Goldin A, Goldman ID, Gundlach AL, Hagenbuch B, Hales TG, Hammond JR, Hamon M, Hancox JC, Hauger RL, Hay DL, Hobbs AJ, Hollenberg MD, Holliday ND, Hoyer D, Hynes NA, Inui KI, Ishii S, Jacobson KA, Jarvis GE, Jarvis MF, Jensen R, Jones CE, Jones RL, Kaibuchi K, Kanai Y, Kennedy C, Kerr ID, Khan AA, Klienz MJ, Kukkonen JP, Lapoint JY, Leurs R, Lingueglia E, Lippiat J, Lolait SJ, Lummis SC, Lynch JW, MacEwan D, Maguire JJ, Marshall IL, May JM, McArdle CA, McGrath JC, Michel MC, Millar NS, Miller LJ, Mitolo V, Monk PN, Moore PK, Moorhouse AJ, Mouillac B, Murphy PM, Neubig RR, Neumaier J, Niesler B, Obaidat A, Offermanns S, Ohlstein E, Panaro MA, Parsons S, Pwrtwee RG, Petersen J, Pin JP, Poyner DR, Prigent S, Prossnitz ER, Pyne NJ, Pyne S, Quigley JG, Ramachandran R, Richelson EL, Roberts RE, Roskoski R, Ross RA, Roth M, Rudnick G, Ryan RM, Said SI, Schild L, Sanger GJ, Scholich K, Schousboe A, Schulte G, Schulz S, Serhan CN, Sexton PM, Sibley DR, Siegel JM, Singh G, Sitsapesan R, Smart TG, Smith DM, Soga T, Stahl A, Stewart G, Stoddart LA, Summers RJ, Thorens B, Thwaites DT, Toll L, Traynor JR, Usdin TB, Vandenberg RJ, Villalon C, Vore M, Waldman SA, Ward DT, Willars GB, Wonnacott SJ, Wright E, Ye RD, Yonezawa A, Zimmermann M.

Br J Pharmacol. 2013 Dec;170(8):1449-58. doi: 10.1111/bph.12444.

25.

Insights into the binding of GABA to the insect RDL receptor from atomistic simulations: a comparison of models.

Comitani F, Cohen N, Ashby J, Botten D, Lummis SC, Molteni C.

J Comput Aided Mol Des. 2014 Jan;28(1):35-48. doi: 10.1007/s10822-013-9704-0. Epub 2014 Jan 18.

26.

GABA(A) receptor modulation by terpenoids from Sideritis extracts.

Kessler A, Sahin-Nadeem H, Lummis SC, Weigel I, Pischetsrieder M, Buettner A, Villmann C.

Mol Nutr Food Res. 2014 Apr;58(4):851-62. doi: 10.1002/mnfr.201300420. Epub 2013 Nov 24.

27.

Exploring a potential palonosetron allosteric binding site in the 5-HT(3) receptor.

Del Cadia M, De Rienzo F, Weston DA, Thompson AJ, Menziani MC, Lummis SC.

Bioorg Med Chem. 2013 Dec 1;21(23):7523-8. doi: 10.1016/j.bmc.2013.09.028. Epub 2013 Sep 20.

28.

A single channel mutation alters agonist efficacy at 5-HT3A and 5-HT3AB receptors.

Thompson AJ, Lummis SC.

Br J Pharmacol. 2013 Sep;170(2):391-402. doi: 10.1111/bph.12287.

29.

Agonists and antagonists induce different palonosetron dissociation rates in 5-HT₃A and 5-HT₃AB receptors.

Lummis SC, Thompson AJ.

Neuropharmacology. 2013 Oct;73:241-6. doi: 10.1016/j.neuropharm.2013.05.010. Epub 2013 Jun 5.

30.

Structure-activity relationships of quinoxaline-based 5-HT3A and 5-HT3AB receptor-selective ligands.

Thompson AJ, Verheij MH, van Muijlwijk-Koezen JE, Lummis SC, Leurs R, de Esch IJ.

ChemMedChem. 2013 Jun;8(6):946-55. doi: 10.1002/cmdc.201300032. Epub 2013 May 2.

31.

Discriminating between 5-HT₃A and 5-HT₃AB receptors.

Thompson AJ, Lummis SC.

Br J Pharmacol. 2013 Jun;169(4):736-47. doi: 10.1111/bph.12166. Review.

32.

Multisite binding of a general anesthetic to the prokaryotic pentameric Erwinia chrysanthemi ligand-gated ion channel (ELIC).

Spurny R, Billen B, Howard RJ, Brams M, Debaveye S, Price KL, Weston DA, Strelkov SV, Tytgat J, Bertrand S, Bertrand D, Lummis SC, Ulens C.

J Biol Chem. 2013 Mar 22;288(12):8355-64. doi: 10.1074/jbc.M112.424507. Epub 2013 Jan 30.

33.

GABA binding to an insect GABA receptor: a molecular dynamics and mutagenesis study.

Ashby JA, McGonigle IV, Price KL, Cohen N, Comitani F, Dougherty DA, Molteni C, Lummis SC.

Biophys J. 2012 Nov 21;103(10):2071-81. doi: 10.1016/j.bpj.2012.10.016. Epub 2012 Nov 20.

34.

Structural basis of ligand recognition in 5-HT3 receptors.

Kesters D, Thompson AJ, Brams M, van Elk R, Spurny R, Geitmann M, Villalgordo JM, Guskov A, Danielson UH, Lummis SC, Smit AB, Ulens C.

EMBO Rep. 2013 Jan;14(1):49-56. doi: 10.1038/embor.2012.189. Epub 2012 Nov 30.

35.

Biolistic transfection of neurons in organotypic brain slices.

O'Brien JA, Lummis SC.

Methods Mol Biol. 2013;940:157-66. doi: 10.1007/978-1-62703-110-3_13.

PMID:
23104341
36.

5-HT(3) receptors.

Lummis SC.

J Biol Chem. 2012 Nov 23;287(48):40239-45. doi: 10.1074/jbc.R112.406496. Epub 2012 Oct 4. Review.

37.

Pentameric ligand-gated ion channel ELIC is activated by GABA and modulated by benzodiazepines.

Spurny R, Ramerstorfer J, Price K, Brams M, Ernst M, Nury H, Verheij M, Legrand P, Bertrand D, Bertrand S, Dougherty DA, de Esch IJ, Corringer PJ, Sieghart W, Lummis SC, Ulens C.

Proc Natl Acad Sci U S A. 2012 Oct 30;109(44):E3028-34. doi: 10.1073/pnas.1208208109. Epub 2012 Oct 3.

38.

Design, synthesis, and structure-activity relationships of highly potent 5-HT₃ receptor ligands.

Verheij MH, Thompson AJ, van Muijlwijk-Koezen JE, Lummis SC, Leurs R, de Esch IJ.

J Med Chem. 2012 Oct 25;55(20):8603-14. doi: 10.1021/jm300801u. Epub 2012 Oct 12.

39.

Identification of novel α7 nicotinic receptor ligands by in silico screening against the crystal structure of a chimeric α7 receptor ligand binding domain.

Akdemir A, Edink E, Thompson AJ, Lummis SC, Kooistra AJ, de Graaf C, de Esch IJ.

Bioorg Med Chem. 2012 Oct 1;20(19):5992-6002. doi: 10.1016/j.bmc.2012.06.054. Epub 2012 Jul 11.

40.

Mixed antagonistic effects of the ginkgolides at recombinant human ρ1 GABAC receptors.

Huang SH, Lewis TM, Lummis SC, Thompson AJ, Chebib M, Johnston GA, Duke RK.

Neuropharmacology. 2012 Nov;63(6):1127-39. doi: 10.1016/j.neuropharm.2012.06.067. Epub 2012 Jul 22.

41.

The pharmacological profile of ELIC, a prokaryotic GABA-gated receptor.

Thompson AJ, Alqazzaz M, Ulens C, Lummis SC.

Neuropharmacology. 2012 Sep;63(4):761-7. doi: 10.1016/j.neuropharm.2012.05.027. Epub 2012 Jun 4.

42.

Azemiopsin from Azemiops feae viper venom, a novel polypeptide ligand of nicotinic acetylcholine receptor.

Utkin YN, Weise C, Kasheverov IE, Andreeva TV, Kryukova EV, Zhmak MN, Starkov VG, Hoang NA, Bertrand D, Ramerstorfer J, Sieghart W, Thompson AJ, Lummis SC, Tsetlin VI.

J Biol Chem. 2012 Aug 3;287(32):27079-86. doi: 10.1074/jbc.M112.363051. Epub 2012 May 21.

43.

Multiple Tyrosine Residues Contribute to GABA Binding in the GABA(C) Receptor Binding Pocket.

Lummis SC, Harrison NJ, Wang J, Ashby JA, Millen KS, Beene DL, Dougherty DA.

ACS Chem Neurosci. 2012 Mar 21;3(3):186-192. Epub 2011 Dec 15.

44.

VUF10166, a novel compound with differing activities at 5-HT₃A and 5-HT₃AB receptors.

Thompson AJ, Verheij MH, de Esch IJ, Lummis SC.

J Pharmacol Exp Ther. 2012 May;341(2):350-9. doi: 10.1124/jpet.111.190769. Epub 2012 Feb 3.

45.

A single amino acid determines the toxicity of Ginkgo biloba extracts.

Thompson AJ, McGonigle I, Duke R, Johnston GA, Lummis SC.

FASEB J. 2012 May;26(5):1884-91. doi: 10.1096/fj.11-192765. Epub 2012 Jan 17.

46.

Cys-loop receptor channel blockers also block GLIC.

Alqazzaz M, Thompson AJ, Price KL, Breitinger HG, Lummis SC.

Biophys J. 2011 Dec 21;101(12):2912-8. doi: 10.1016/j.bpj.2011.10.055. Epub 2011 Dec 20.

47.

High-affinity fluorescent ligands for the 5-HT(3) receptor.

Simonin J, Vernekar SK, Thompson AJ, Hothersall JD, Connolly CN, Lummis SC, Lochner M.

Bioorg Med Chem Lett. 2012 Jan 15;22(2):1151-5. doi: 10.1016/j.bmcl.2011.11.097. Epub 2011 Dec 1.

48.

Two amino acid residues contribute to a cation-π binding interaction in the binding site of an insect GABA receptor.

Lummis SC, McGonigle I, Ashby JA, Dougherty DA.

J Neurosci. 2011 Aug 24;31(34):12371-6. doi: 10.1523/JNEUROSCI.1610-11.2011.

49.

Fragment library screening reveals remarkable similarities between the G protein-coupled receptor histamine H₄ and the ion channel serotonin 5-HT₃A.

Verheij MH, de Graaf C, de Kloe GE, Nijmeijer S, Vischer HF, Smits RA, Zuiderveld OP, Hulscher S, Silvestri L, Thompson AJ, van Muijlwijk-Koezen JE, Lummis SC, Leurs R, de Esch IJ.

Bioorg Med Chem Lett. 2011 Sep 15;21(18):5460-4. doi: 10.1016/j.bmcl.2011.06.123. Epub 2011 Jul 2.

50.

Varenicline is a potent agonist of the human 5-hydroxytryptamine3 receptor.

Lummis SC, Thompson AJ, Bencherif M, Lester HA.

J Pharmacol Exp Ther. 2011 Oct;339(1):125-31. doi: 10.1124/jpet.111.185306. Epub 2011 Jul 20.

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