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Items: 1 to 50 of 72

1.

Inhale, exhale: Probing the inside-out mechanism of nicotine addiction using novel fluorescent sensors.

McManus OB, Werley CA, Dempsey GT.

J Gen Physiol. 2019 Jun 3;151(6):714-717. doi: 10.1085/jgp.201912325. Epub 2019 Mar 22. No abstract available.

PMID:
30902836
2.

Simultaneous voltage and calcium imaging and optogenetic stimulation with high sensitivity and a wide field of view.

Nguyen C, Upadhyay H, Murphy M, Borja G, Rozsahegyi EJ, Barnett A, Brookings T, McManus OB, Werley CA.

Biomed Opt Express. 2019 Jan 23;10(2):789-806. doi: 10.1364/BOE.10.000789. eCollection 2019 Feb 1.

3.

All-Optical Electrophysiology for Disease Modeling and Pharmacological Characterization of Neurons.

Werley CA, Brookings T, Upadhyay H, Williams LA, McManus OB, Dempsey GT.

Curr Protoc Pharmacol. 2017 Sep 11;78:11.20.1-11.20.24. doi: 10.1002/cpph.25.

4.

Pyrazolopyrimidines as Potent Stimulators for Transient Receptor Potential Canonical 3/6/7 Channels.

Qu C, Ding M, Zhu Y, Lu Y, Du J, Miller M, Tian J, Zhu J, Xu J, Wen M, Er-Bu A, Wang J, Xiao Y, Wu M, McManus OB, Li M, Wu J, Luo HR, Cao Z, Shen B, Wang H, Zhu MX, Hong X.

J Med Chem. 2017 Jun 8;60(11):4680-4692. doi: 10.1021/acs.jmedchem.7b00304. Epub 2017 Apr 28.

5.

Identification and optimization of 2-aminobenzimidazole derivatives as novel inhibitors of TRPC4 and TRPC5 channels.

Zhu Y, Lu Y, Qu C, Miller M, Tian J, Thakur DP, Zhu J, Deng Z, Hu X, Wu M, McManus OB, Li M, Hong X, Zhu MX, Luo HR.

Br J Pharmacol. 2015 Jul;172(14):3495-509. doi: 10.1111/bph.13140. Epub 2015 May 11.

6.

Identification and characterization of ML352: a novel, noncompetitive inhibitor of the presynaptic choline transporter.

Ennis EA, Wright J, Retzlaff CL, McManus OB, Lin Z, Huang X, Wu M, Li M, Daniels JS, Lindsley CW, Hopkins CR, Blakely RD.

ACS Chem Neurosci. 2015 Mar 18;6(3):417-27. doi: 10.1021/cn5001809. Epub 2015 Feb 2.

7.

An old probe sheds new light on BK channel pore structure.

McManus OB, Rothberg BS.

J Gen Physiol. 2014 Dec;144(6):499-501. doi: 10.1085/jgp.201411306. Epub 2014 Nov 10. No abstract available.

8.

Discovery and characterization of 2-(cyclopropanesulfonamido)-N-(2-ethoxyphenyl)benzamide, ML382: a potent and selective positive allosteric modulator of MrgX1.

Wen W, Wang Y, Li Z, Tseng PY, McManus OB, Wu M, Li M, Lindsley CW, Dong X, Hopkins CR.

ChemMedChem. 2015 Jan;10(1):57-61. doi: 10.1002/cmdc.201402277. Epub 2014 Sep 10.

9.

Potent and selective inhibitors of the TASK-1 potassium channel through chemical optimization of a bis-amide scaffold.

Flaherty DP, Simpson DS, Miller M, Maki BE, Zou B, Shi J, Wu M, McManus OB, Aubé J, Li M, Golden JE.

Bioorg Med Chem Lett. 2014 Aug 15;24(16):3968-73. doi: 10.1016/j.bmcl.2014.06.032. Epub 2014 Jun 19.

10.

Improved Cav2.2 Channel Inhibitors through a gem-Dimethylsulfone Bioisostere Replacement of a Labile Sulfonamide.

Shao PP, Ye F, Chakravarty PK, Herrington JB, Dai G, Bugianesi RM, Haedo RJ, Swensen AM, Warren VA, Smith MM, Garcia ML, McManus OB, Lyons KA, Li X, Green M, Jochnowitz N, McGowan E, Mistry S, Sun SY, Abbadie C, Kaczorowski GJ, Duffy JL.

ACS Med Chem Lett. 2013 Sep 8;4(11):1064-8. doi: 10.1021/ml4002612. eCollection 2013 Nov 14.

11.

HTS assays for developing the molecular pharmacology of ion channels.

McManus OB.

Curr Opin Pharmacol. 2014 Apr;15:91-6. doi: 10.1016/j.coph.2014.01.004. Epub 2014 Feb 18. Review.

PMID:
24556186
12.

ML365: Development of Bis-Amides as Selective Inhibitors of the KCNK3/TASK1 Two Pore Potassium Channel.

Zou B, Flaherty DP, Simpson DS, Maki BE, Miller MR, Shi J, Wu M, McManus OB, Golden JE, Aubé J, Li M.

Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2010-.
2013 Apr 15 [updated 2013 Nov 14].

13.

Reversible inhibitors of regulators of G-protein signaling identified in a high-throughput cell-based calcium signaling assay.

Storaska AJ, Mei JP, Wu M, Li M, Wade SM, Blazer LL, Sjögren B, Hopkins CR, Lindsley CW, Lin Z, Babcock JJ, McManus OB, Neubig RR.

Cell Signal. 2013 Dec;25(12):2848-55. doi: 10.1016/j.cellsig.2013.09.007. Epub 2013 Sep 14.

14.

Identification of a novel, small molecule activator of KCNQ1 channels.

Yu H, Lin Z, Xu K, Huang X, Long S, Wu M, McManus OB, Le Engers J, Mattmann ME, Engers DW, Le UM, Lindsley CW, Hopkins CR, Li M.

Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2010-.
2011 Dec 16 [updated 2013 Mar 7].

15.

Identification of a novel, small molecule inhibitor of KCNQ2 channels.

Yu H, Xu K, Zou B, Wu M, McManus OB, Le Engers J, Cheung YY, Salovich JM, Hopkins CR, Lindsley CW, Li M.

Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2010-.
2011 Oct 28 [updated 2013 Feb 25].

16.

Development of a Selective Chemical Inhibitor for the Two-Pore Potassium Channel, KCNK9.

Miller MR, Zou B, Shi J, Flaherty DP, Simpson DS, Yao T, Maki BE, Day VW, Douglas JT, Wu M, McManus OB, Golden JE, Aubé J, Li M.

Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2010-.
2012 Apr 16 [updated 2013 Feb 28].

17.

A small molecule activator of KCNQ2 and KCNQ4 channels.

Yu H, Wu M, Hopkins C, Engers J, Townsend S, Lindsley C, McManus OB, Li M.

Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2010-.
2011 Mar 29 [updated 2013 Feb 28].

18.

Dynamic subunit stoichiometry confers a progressive continuum of pharmacological sensitivity by KCNQ potassium channels.

Yu H, Lin Z, Mattmann ME, Zou B, Terrenoire C, Zhang H, Wu M, McManus OB, Kass RS, Lindsley CW, Hopkins CR, Li M.

Proc Natl Acad Sci U S A. 2013 May 21;110(21):8732-7. doi: 10.1073/pnas.1300684110. Epub 2013 May 6.

19.

Aminopiperidine sulfonamide Cav2.2 channel inhibitors for the treatment of chronic pain.

Shao PP, Ye F, Chakravarty PK, Varughese DJ, Herrington JB, Dai G, Bugianesi RM, Haedo RJ, Swensen AM, Warren VA, Smith MM, Garcia ML, McManus OB, Lyons KA, Li X, Green M, Jochnowitz N, McGowan E, Mistry S, Sun SY, Abbadie C, Kaczorowski GJ, Duffy JL.

J Med Chem. 2012 Nov 26;55(22):9847-55. doi: 10.1021/jm301056k. Epub 2012 Nov 12.

PMID:
23098566
20.

Ion Channel Screening.

McManus OB, Garcia ML, Weaver D, Bryant M, Titus S, Herrington JB.

In: Sittampalam GS, Coussens NP, Brimacombe K, Grossman A, Arkin M, Auld D, Austin C, Baell J, Bejcek B, Caaveiro JMM, Chung TDY, Dahlin JL, Devanaryan V, Foley TL, Glicksman M, Hall MD, Haas JV, Inglese J, Iversen PW, Kahl SD, Kales SC, Lal-Nag M, Li Z, McGee J, McManus O, Riss T, Trask OJ Jr., Weidner JR, Wildey MJ, Xia M, Xu X, editors. Assay Guidance Manual [Internet]. Bethesda (MD): Eli Lilly & Company and the National Center for Advancing Translational Sciences; 2004-.
2012 Oct 1.

21.

Identification of (R)-N-(4-(4-methoxyphenyl)thiazol-2-yl)-1-tosylpiperidine-2-carboxamide, ML277, as a novel, potent and selective K(v)7.1 (KCNQ1) potassium channel activator.

Mattmann ME, Yu H, Lin Z, Xu K, Huang X, Long S, Wu M, McManus OB, Engers DW, Le UM, Li M, Lindsley CW, Hopkins CR.

Bioorg Med Chem Lett. 2012 Sep 15;22(18):5936-41. doi: 10.1016/j.bmcl.2012.07.060. Epub 2012 Aug 2.

23.

Modulation of hERG potassium channel gating normalizes action potential duration prolonged by dysfunctional KCNQ1 potassium channel.

Zhang H, Zou B, Yu H, Moretti A, Wang X, Yan W, Babcock JJ, Bellin M, McManus OB, Tomaselli G, Nan F, Laugwitz KL, Li M.

Proc Natl Acad Sci U S A. 2012 Jul 17;109(29):11866-71. doi: 10.1073/pnas.1205266109. Epub 2012 Jun 28.

24.

Asymmetric synthesis and evaluation of a hydroxyphenylamide voltage-gated sodium channel blocker in human prostate cancer xenografts.

Davis GC, Kong Y, Paige M, Li Z, Merrick EC, Hansen T, Suy S, Wang K, Dakshanamurthy S, Cordova A, McManus OB, Williams BS, Chruszcz M, Minor W, Patel MK, Brown ML.

Bioorg Med Chem. 2012 Mar 15;20(6):2180-8. doi: 10.1016/j.bmc.2011.08.061. Epub 2011 Sep 1.

25.

Selective, direct activation of high-conductance, calcium-activated potassium channels causes smooth muscle relaxation.

Ponte CG, McManus OB, Schmalhofer WA, Shen DM, Dai G, Stevenson A, Sur S, Shah T, Kiss L, Shu M, Doherty JB, Nargund R, Kaczorowski GJ, Suarez-Kurtz G, Garcia ML.

Mol Pharmacol. 2012 Apr;81(4):567-77. doi: 10.1124/mol.111.075853. Epub 2012 Jan 12.

PMID:
22241372
26.

Characterization of the substituted N-triazole oxindole TROX-1, a small-molecule, state-dependent inhibitor of Ca(V)2 calcium channels.

Swensen AM, Herrington J, Bugianesi RM, Dai G, Haedo RJ, Ratliff KS, Smith MM, Warren VA, Arneric SP, Eduljee C, Parker D, Snutch TP, Hoyt SB, London C, Duffy JL, Kaczorowski GJ, McManus OB.

Mol Pharmacol. 2012 Mar;81(3):488-97. doi: 10.1124/mol.111.075226. Epub 2011 Dec 21.

PMID:
22188924
27.

Discovery, Synthesis, and Structure Activity Relationship of a Series of N-Aryl- bicyclo[2.2.1]heptane-2-carboxamides: Characterization of ML213 as a Novel KCNQ2 and KCNQ4 Potassium Channel Opener.

Yu H, Wu M, Townsend SD, Zou B, Long S, Daniels JS, McManus OB, Li M, Lindsley CW, Hopkins CR.

ACS Chem Neurosci. 2011 Oct 19;2(10):572-577.

28.

Novel Chemical Inhibitor of TRPC4 Channels.

Miller MR, Shi J, Wu M, Engers J, Hopkins CR, Lindsley CW, Salovich JM, Zhu Y, Tian JB, Zhu MX, McManus OB, Li M.

Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2010-.
2010 Dec 15 [updated 2011 May 26].

29.

Identification of novel and selective Kv2 channel inhibitors.

Herrington J, Solly K, Ratliff KS, Li N, Zhou YP, Howard A, Kiss L, Garcia ML, McManus OB, Deng Q, Desai R, Xiong Y, Kaczorowski GJ.

Mol Pharmacol. 2011 Dec;80(6):959-64. doi: 10.1124/mol.111.074831. Epub 2011 Sep 26.

PMID:
21948463
30.

Selective inhibition of the K(ir)2 family of inward rectifier potassium channels by a small molecule probe: the discovery, SAR, and pharmacological characterization of ML133.

Wang HR, Wu M, Yu H, Long S, Stevens A, Engers DW, Sackin H, Daniels JS, Dawson ES, Hopkins CR, Lindsley CW, Li M, McManus OB.

ACS Chem Biol. 2011 Aug 19;6(8):845-56. doi: 10.1021/cb200146a. Epub 2011 Jun 13.

31.

A potent and selective small molecule Kir2.1 inhibitor.

Wu M, Wang H, Yu H, Makhina E, Xu J, Dawson ES, Hopkins CR, Lindsley CW, McManus OB, Li M.

Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2010-.
2010 Feb 26 [updated 2010 Oct 20].

32.

A potent and selective indole N-type calcium channel (Ca(v)2.2) blocker for the treatment of pain.

Tyagarajan S, Chakravarty PK, Park M, Zhou B, Herrington JB, Ratliff K, Bugianesi RM, Williams B, Haedo RJ, Swensen AM, Warren VA, Smith M, Garcia M, Kaczorowski GJ, McManus OB, Lyons KA, Li X, Madeira M, Karanam B, Green M, Forrest MJ, Abbadie C, McGowan E, Mistry S, Jochnowitz N, Duffy JL.

Bioorg Med Chem Lett. 2011 Jan 15;21(2):869-73. doi: 10.1016/j.bmcl.2010.11.067. Epub 2010 Nov 21.

PMID:
21195616
33.

Profiling diverse compounds by flux- and electrophysiology-based primary screens for inhibition of human Ether-à-go-go related gene potassium channels.

Zou B, Yu H, Babcock JJ, Chanda P, Bader JS, McManus OB, Li M.

Assay Drug Dev Technol. 2010 Dec;8(6):743-54. doi: 10.1089/adt.2010.0339.

34.

Analgesic effects of a substituted N-triazole oxindole (TROX-1), a state-dependent, voltage-gated calcium channel 2 blocker.

Abbadie C, McManus OB, Sun SY, Bugianesi RM, Dai G, Haedo RJ, Herrington JB, Kaczorowski GJ, Smith MM, Swensen AM, Warren VA, Williams B, Arneric SP, Eduljee C, Snutch TP, Tringham EW, Jochnowitz N, Liang A, Euan MacIntyre D, McGowan E, Mistry S, White VV, Hoyt SB, London C, Lyons KA, Bunting PB, Volksdorf S, Duffy JL.

J Pharmacol Exp Ther. 2010 Aug;334(2):545-55. doi: 10.1124/jpet.110.166363. Epub 2010 May 3.

PMID:
20439438
35.

Positive allosteric interaction of structurally diverse T-type calcium channel antagonists.

Uebele VN, Nuss CE, Fox SV, Garson SL, Cristescu R, Doran SM, Kraus RL, Santarelli VP, Li Y, Barrow JC, Yang ZQ, Schlegel KA, Rittle KE, Reger TS, Bednar RA, Lemaire W, Mullen FA, Ballard JE, Tang C, Dai G, McManus OB, Koblan KS, Renger JJ.

Cell Biochem Biophys. 2009;55(2):81-93. doi: 10.1007/s12013-009-9057-4. Epub 2009 Jul 7.

PMID:
19582593
36.

An automated electrophysiology serum shift assay for K(V) channels.

Ratliff KS, Petrov A, Eiermann GJ, Deng Q, Green MD, Kaczorowski GJ, McManus OB, Herrington J.

Assay Drug Dev Technol. 2008 Apr;6(2):243-53. doi: 10.1089/adt.2008.128.

PMID:
18471078
37.

A high-throughput assay for evaluating state dependence and subtype selectivity of Cav2 calcium channel inhibitors.

Dai G, Haedo RJ, Warren VA, Ratliff KS, Bugianesi RM, Rush A, Williams ME, Herrington J, Smith MM, McManus OB, Swensen AM.

Assay Drug Dev Technol. 2008 Apr;6(2):195-212. doi: 10.1089/adt.2008.136.

PMID:
18471074
38.

Ion channels as drug targets: the next GPCRs.

Kaczorowski GJ, McManus OB, Priest BT, Garcia ML.

J Gen Physiol. 2008 May;131(5):399-405. doi: 10.1085/jgp.200709946. Epub 2008 Apr 14. No abstract available.

39.

Automated electrophysiology in drug discovery.

Priest BT, Swensen AM, McManus OB.

Curr Pharm Des. 2007;13(23):2325-37. Review.

PMID:
17692004
40.

Blockers of the delayed-rectifier potassium current in pancreatic beta-cells enhance glucose-dependent insulin secretion.

Herrington J, Zhou YP, Bugianesi RM, Dulski PM, Feng Y, Warren VA, Smith MM, Kohler MG, Garsky VM, Sanchez M, Wagner M, Raphaelli K, Banerjee P, Ahaghotu C, Wunderler D, Priest BT, Mehl JT, Garcia ML, McManus OB, Kaczorowski GJ, Slaughter RS.

Diabetes. 2006 Apr;55(4):1034-42. Erratum in: Diabetes. 2006 Jun;55(6):1904.

41.

A cell-sparing electric field stimulation technique for high-throughput screening of voltage-gated ion channels.

Bugianesi RM, Augustine PR, Azer K, Dufresne C, Herrington J, Kath GS, McManus OB, Napolitano CS, Rush A, Sachs J, Simpson N, Wismer MK, Kaczorowski GJ, Slaughter RS.

Assay Drug Dev Technol. 2006 Feb;4(1):21-35.

PMID:
16506886
42.

Block of peripheral nerve sodium channels selectively inhibits features of neuropathic pain in rats.

Brochu RM, Dick IE, Tarpley JW, McGowan E, Gunner D, Herrington J, Shao PP, Ok D, Li C, Parsons WH, Stump GL, Regan CP, Lynch JJ Jr, Lyons KA, McManus OB, Clark S, Ali Z, Kaczorowski GJ, Martin WJ, Priest BT.

Mol Pharmacol. 2006 Mar;69(3):823-32. Epub 2005 Nov 21.

PMID:
16301337
43.

Role of the C-terminus of the high-conductance calcium-activated potassium channel in channel structure and function.

Schmalhofer WA, Sanchez M, Dai G, Dewan A, Secades L, Hanner M, Knaus HG, McManus OB, Kohler M, Kaczorowski GJ, Garcia ML.

Biochemistry. 2005 Aug 2;44(30):10135-44.

PMID:
16042390
44.

Biophysical and pharmacological properties of the voltage-gated potassium current of human pancreatic beta-cells.

Herrington J, Sanchez M, Wunderler D, Yan L, Bugianesi RM, Dick IE, Clark SA, Brochu RM, Priest BT, Kohler MG, McManus OB.

J Physiol. 2005 Aug 15;567(Pt 1):159-75. Epub 2005 Jun 2.

45.

Substitution of a single residue in Stichodactyla helianthus peptide, ShK-Dap22, reveals a novel pharmacological profile.

Middleton RE, Sanchez M, Linde AR, Bugianesi RM, Dai G, Felix JP, Koprak SL, Staruch MJ, Bruguera M, Cox R, Ghosh A, Hwang J, Jones S, Kohler M, Slaughter RS, McManus OB, Kaczorowski GJ, Garcia ML.

Biochemistry. 2003 Nov 25;42(46):13698-707.

PMID:
14622016
46.

Molecular analysis of two cytochrome P450 monooxygenase genes required for paxilline biosynthesis in Penicillium paxilli, and effects of paxilline intermediates on mammalian maxi-K ion channels.

McMillan LK, Carr RL, Young CA, Astin JW, Lowe RG, Parker EJ, Jameson GB, Finch SC, Miles CO, McManus OB, Schmalhofer WA, Garcia ML, Kaczorowski GJ, Goetz M, Tkacz JS, Scott B.

Mol Genet Genomics. 2003 Oct;270(1):9-23. Epub 2003 Jul 18.

PMID:
12884010
47.

Identification of a new class of inhibitors of the voltage-gated potassium channel, Kv1.3, with immunosuppressant properties.

Schmalhofer WA, Bao J, McManus OB, Green B, Matyskiela M, Wunderler D, Bugianesi RM, Felix JP, Hanner M, Linde-Arias AR, Ponte CG, Velasco L, Koo G, Staruch MJ, Miao S, Parsons WH, Rupprecht K, Slaughter RS, Kaczorowski GJ, Garcia ML.

Biochemistry. 2002 Jun 18;41(24):7781-94.

PMID:
12056910
48.

Oxidative regulation of large conductance calcium-activated potassium channels.

Tang XD, Daggett H, Hanner M, Garcia ML, McManus OB, Brot N, Weissbach H, Heinemann SH, Hoshi T.

J Gen Physiol. 2001 Mar;117(3):253-74.

49.

Potassium channels: from scorpion venoms to high-resolution structure.

Garcia ML, Gao Y, McManus OB, Kaczorowski GJ.

Toxicon. 2001 Jun;39(6):739-48. Review. No abstract available.

PMID:
11137531
50.

Correolide and derivatives are novel immunosuppressants blocking the lymphocyte Kv1.3 potassium channels.

Koo GC, Blake JT, Shah K, Staruch MJ, Dumont F, Wunderler D, Sanchez M, McManus OB, Sirotina-Meisher A, Fischer P, Boltz RC, Goetz MA, Baker R, Bao J, Kayser F, Rupprecht KM, Parsons WH, Tong XC, Ita IE, Pivnichny J, Vincent S, Cunningham P, Hora D Jr, Feeney W, Kaczorowski G, et al.

Cell Immunol. 1999 Nov 1;197(2):99-107.

PMID:
10607427

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