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Items: 27

1.

Discovery, Characterization, and Effects on Renal Fluid and Electrolyte Excretion of the Kir4.1 Potassium Channel Pore Blocker, VU0134992.

Kharade SV, Kurata H, Bender AM, Blobaum AL, Figueroa EE, Duran A, Kramer M, Days E, Vinson P, Flores D, Satlin LM, Meiler J, Weaver CD, Lindsley CW, Hopkins CR, Denton JS.

Mol Pharmacol. 2018 Aug;94(2):926-937. doi: 10.1124/mol.118.112359. Epub 2018 Jun 12.

2.

Screening for AMPA receptor auxiliary subunit specific modulators.

Azumaya CM, Days EL, Vinson PN, Stauffer S, Sulikowski G, Weaver CD, Nakagawa T.

PLoS One. 2017 Mar 30;12(3):e0174742. doi: 10.1371/journal.pone.0174742. eCollection 2017.

3.

Discovery of a Novel Series of Orally Bioavailable and CNS Penetrant Glucagon-like Peptide-1 Receptor (GLP-1R) Noncompetitive Antagonists Based on a 1,3-Disubstituted-7-aryl-5,5-bis(trifluoromethyl)-5,8-dihydropyrimido[4,5-d]pyrimidine-2,4(1H,3H)-dione Core.

Nance KD, Days EL, Weaver CD, Coldren A, Farmer TD, Cho HP, Niswender CM, Blobaum AL, Niswender KD, Lindsley CW.

J Med Chem. 2017 Feb 23;60(4):1611-1616. doi: 10.1021/acs.jmedchem.6b01706. Epub 2017 Feb 3.

PMID:
28103022
4.

An insecticide resistance-breaking mosquitocide targeting inward rectifier potassium channels in vectors of Zika virus and malaria.

Swale DR, Engers DW, Bollinger SR, Gross A, Inocente EA, Days E, Kanga F, Johnson RM, Yang L, Bloomquist JR, Hopkins CR, Piermarini PM, Denton JS.

Sci Rep. 2016 Nov 16;6:36954. doi: 10.1038/srep36954.

5.

Selective Small Molecule Activators of TREK-2 Channels Stimulate Dorsal Root Ganglion c-Fiber Nociceptor Two-Pore-Domain Potassium Channel Currents and Limit Calcium Influx.

Dadi PK, Vierra NC, Days E, Dickerson MT, Vinson PN, Weaver CD, Jacobson DA.

ACS Chem Neurosci. 2017 Mar 15;8(3):558-568. doi: 10.1021/acschemneuro.6b00301. Epub 2016 Nov 23.

6.

Development and validation of a thallium flux-based functional assay for the sodium channel NaV1.7 and its utility for lead discovery and compound profiling.

Du Y, Days E, Romaine I, Abney KK, Kaufmann K, Sulikowski G, Stauffer S, Lindsley CW, Weaver CD.

ACS Chem Neurosci. 2015 Jun 17;6(6):871-8. doi: 10.1021/acschemneuro.5b00004. Epub 2015 Apr 30.

PMID:
25879403
7.

The discovery and characterization of a centrally penetrant (ML396) and a peripherally restricted (ML397) pan-Group III mGlu positive allosteric modulators.

Jalan-Sakrikar N, Roper-Field J, Klar R, Mattman M, Walker AG, Zamorano R, Xiang Z, Byers CF, Blobaum AL, Engers D, Weaver CD, Days E, Utley TJ, Melancon B, Daniels JS, Wood MR, Lindsley CW, Conn PJ, Hopkins CR, Niswender CM.

Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2010-.
2014 Apr 15 [updated 2015 Jan 16].

8.

Discovery of (S)-2-cyclopentyl-N-((1-isopropylpyrrolidin2-yl)-9-methyl-1-oxo-2,9-dihydro-1H-pyrrido[3,4-b]indole-4-carboxamide (VU0453379): a novel, CNS penetrant glucagon-like peptide 1 receptor (GLP-1R) positive allosteric modulator (PAM).

Morris LC, Nance KD, Gentry PR, Days EL, Weaver CD, Niswender CM, Thompson AD, Jones CK, Locuson CW, Morrison RD, Daniels JS, Niswender KD, Lindsley CW.

J Med Chem. 2014 Dec 11;57(23):10192-7. doi: 10.1021/jm501375c. Epub 2014 Dec 2.

9.

Discovery and characterization of a potent and selective inhibitor of Aedes aegypti inward rectifier potassium channels.

Raphemot R, Rouhier MF, Swale DR, Days E, Weaver CD, Lovell KM, Konkel LC, Engers DW, Bollinger SR, Hopkins C, Piermarini PM, Denton JS.

PLoS One. 2014 Nov 6;9(11):e110772. doi: 10.1371/journal.pone.0110772. eCollection 2014. Erratum in: PLoS One. 2015;10(3):e0119883. Bollinger, Sean F [corrected to Bollinger, Sean R].

10.

Identification of positive allosteric modulators VU0155094 (ML397) and VU0422288 (ML396) reveals new insights into the biology of metabotropic glutamate receptor 7.

Jalan-Sakrikar N, Field JR, Klar R, Mattmann ME, Gregory KJ, Zamorano R, Engers DW, Bollinger SR, Weaver CD, Days EL, Lewis LM, Utley TJ, Hurtado M, Rigault D, Acher F, Walker AG, Melancon BJ, Wood MR, Lindsley CW, Conn PJ, Xiang Z, Hopkins CR, Niswender CM.

ACS Chem Neurosci. 2014 Dec 17;5(12):1221-37. doi: 10.1021/cn500153z. Epub 2014 Oct 9.

11.

A Duplexed High-Throughput Screen to Identify Allosteric Modulators of the Glucagon-Like Peptide 1 and Glucagon Receptors.

Morris LC, Days EL, Turney M, Mi D, Lindsley CW, Weaver CD, Niswender KD.

J Biomol Screen. 2014 Jul;19(6):847-58. doi: 10.1177/1087057114520971. Epub 2014 Feb 13.

12.

Development and validation of fluorescence-based and automated patch clamp-based functional assays for the inward rectifier potassium channel Kir4.1.

Raphemot R, Kadakia RJ, Olsen ML, Banerjee S, Days E, Smith SS, Weaver CD, Denton JS.

Assay Drug Dev Technol. 2013 Nov-Dec;11(9-10):532-43. doi: 10.1089/adt.2013.544. Epub 2013 Nov 22.

13.

Dihydrothiazolopyridone derivatives as a novel family of positive allosteric modulators of the metabotropic glutamate 5 (mGlu5) receptor.

Bartolomé-Nebreda JM, Conde-Ceide S, Delgado F, Iturrino L, Pastor J, Pena MÁ, Trabanco AA, Tresadern G, Wassvik CM, Stauffer SR, Jadhav S, Gogi K, Vinson PN, Noetzel MJ, Days E, Weaver CD, Lindsley CW, Niswender CM, Jones CK, Conn PJ, Rombouts F, Lavreysen H, Macdonald GJ, Mackie C, Steckler T.

J Med Chem. 2013 Sep 26;56(18):7243-59. doi: 10.1021/jm400650w. Epub 2013 Sep 4.

14.

Discovery and Characterization of a Selective Activator of the G-Protein Activated Inward-Rectifying Potassium (GIRK) Channel.

Days E, Kaufmann K, Romaine I, Niswender C, Lewis M, Utley T, Du Y, Sliwoski G, Morrison R, Dawson ES, Engers JL, Denton J, Daniels JS, Sulikowski GA, Lindsley CW, Weaver CD.

Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2010-.
2012 Apr 6 [updated 2013 Mar 14].

15.

ML297 (VU0456810), the first potent and selective activator of the GIRK potassium channel, displays antiepileptic properties in mice.

Kaufmann K, Romaine I, Days E, Pascual C, Malik A, Yang L, Zou B, Du Y, Sliwoski G, Morrison RD, Denton J, Niswender CM, Daniels JS, Sulikowski GA, Xie XS, Lindsley CW, Weaver CD.

ACS Chem Neurosci. 2013 Sep 18;4(9):1278-86. doi: 10.1021/cn400062a. Epub 2013 Jun 13.

16.

Identification and characterization of a compound that protects cardiac tissue from human Ether-à-go-go-related gene (hERG)-related drug-induced arrhythmias.

Potet F, Lorinc AN, Chaigne S, Hopkins CR, Venkataraman R, Stepanovic SZ, Lewis LM, Days E, Sidorov VY, Engers DW, Zou B, Afshartous D, George AL Jr, Campbell CM, Balser JR, Li M, Baudenbacher FJ, Lindsley CW, Weaver CD, Kupershmidt S.

J Biol Chem. 2012 Nov 16;287(47):39613-25. doi: 10.1074/jbc.M112.380162. Epub 2012 Oct 2.

17.

Optimization of an ether series of mGlu5 positive allosteric modulators: molecular determinants of MPEP-site interaction crossover.

Manka JT, Vinson PN, Gregory KJ, Zhou Y, Williams R, Gogi K, Days E, Jadhav S, Herman EJ, Lavreysen H, Mackie C, Bartolomé JM, Macdonald GJ, Steckler T, Daniels JS, Weaver CD, Niswender CM, Jones CK, Conn PJ, Lindsley CW, Stauffer SR.

Bioorg Med Chem Lett. 2012 Oct 15;22(20):6481-5. doi: 10.1016/j.bmcl.2012.08.043. Epub 2012 Aug 24.

18.

Functional impact of allosteric agonist activity of selective positive allosteric modulators of metabotropic glutamate receptor subtype 5 in regulating central nervous system function.

Noetzel MJ, Rook JM, Vinson PN, Cho HP, Days E, Zhou Y, Rodriguez AL, Lavreysen H, Stauffer SR, Niswender CM, Xiang Z, Daniels JS, Jones CK, Lindsley CW, Weaver CD, Conn PJ.

Mol Pharmacol. 2012 Feb;81(2):120-33. doi: 10.1124/mol.111.075184. Epub 2011 Oct 21.

19.

Identification and optimization of small molecules that restore E-cadherin expression and reduce invasion in colorectal carcinoma cells.

Stoops SL, Pearson AS, Weaver C, Waterson AG, Days E, Farmer C, Brady S, Weaver CD, Beauchamp RD, Lindsley CW.

ACS Chem Biol. 2011 May 20;6(5):452-65. doi: 10.1021/cb100305h. Epub 2011 Feb 9.

20.

Discovery and optimization of a novel, selective and brain penetrant M1 positive allosteric modulator (PAM): the development of ML169, an MLPCN probe.

Reid PR, Bridges TM, Sheffler DJ, Cho HP, Lewis LM, Days E, Daniels JS, Jones CK, Niswender CM, Weaver CD, Conn PJ, Lindsley CW, Wood MR.

Bioorg Med Chem Lett. 2011 May 1;21(9):2697-701. doi: 10.1016/j.bmcl.2010.12.015. Epub 2010 Dec 9.

21.

Discovery of N-Aryl Piperazines as Selective mGlu(5) Potentiators with Efficacy in a Rodent Model Predictive of Anti-Psychotic Activity.

Zhou Y, Manka JT, Rodriguez AL, Weaver CD, Days EL, Vinson PN, Jadhav S, Hermann EJ, Jones CK, Conn PJ, Lindsley CW, Stauffer SR.

ACS Med Chem Lett. 2010 Nov 11;1(8):433-438. Epub 2010 Aug 13.

22.

Discovery of novel allosteric modulators of metabotropic glutamate receptor subtype 5 reveals chemical and functional diversity and in vivo activity in rat behavioral models of anxiolytic and antipsychotic activity.

Rodriguez AL, Grier MD, Jones CK, Herman EJ, Kane AS, Smith RL, Williams R, Zhou Y, Marlo JE, Days EL, Blatt TN, Jadhav S, Menon UN, Vinson PN, Rook JM, Stauffer SR, Niswender CM, Lindsley CW, Weaver CD, Conn PJ.

Mol Pharmacol. 2010 Dec;78(6):1105-23. doi: 10.1124/mol.110.067207. Epub 2010 Oct 5.

23.

Small-molecule screen identifies inhibitors of the neuronal K-Cl cotransporter KCC2.

Delpire E, Days E, Lewis LM, Mi D, Kim K, Lindsley CW, Weaver CD.

Proc Natl Acad Sci U S A. 2009 Mar 31;106(13):5383-8. doi: 10.1073/pnas.0812756106. Epub 2009 Mar 11.

24.

Discovery and characterization of novel allosteric potentiators of M1 muscarinic receptors reveals multiple modes of activity.

Marlo JE, Niswender CM, Days EL, Bridges TM, Xiang Y, Rodriguez AL, Shirey JK, Brady AE, Nalywajko T, Luo Q, Austin CA, Williams MB, Kim K, Williams R, Orton D, Brown HA, Lindsley CW, Weaver CD, Conn PJ.

Mol Pharmacol. 2009 Mar;75(3):577-88. doi: 10.1124/mol.108.052886. Epub 2008 Dec 1.

25.

Discovery, characterization, and antiparkinsonian effect of novel positive allosteric modulators of metabotropic glutamate receptor 4.

Niswender CM, Johnson KA, Weaver CD, Jones CK, Xiang Z, Luo Q, Rodriguez AL, Marlo JE, de Paulis T, Thompson AD, Days EL, Nalywajko T, Austin CA, Williams MB, Ayala JE, Williams R, Lindsley CW, Conn PJ.

Mol Pharmacol. 2008 Nov;74(5):1345-58. doi: 10.1124/mol.108.049551. Epub 2008 Jul 29.

26.

Pro-inflammatory cytokines modify neuronal nicotinic acetylcholine receptor assembly.

Gahring LC, Days EL, Kaasch T, González de Mendoza M, Owen L, Persiyanov K, Rogers SW.

J Neuroimmunol. 2005 Sep;166(1-2):88-101.

PMID:
16024094

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