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Items: 42

1.

Dexpramipexole depletes blood and tissue eosinophils in nasal polyps with no change in polyp size.

Laidlaw TM, Prussin C, Panettieri RA, Lee S, Ferguson BJ, Adappa ND, Lane AP, Palumbo ML, Sullivan M, Archibald D, Dworetzky SI, Hebrank GT, Bozik ME.

Laryngoscope. 2019 Feb;129(2):E61-E66. doi: 10.1002/lary.27564. Epub 2018 Oct 4.

PMID:
30284267
2.

Dexpramipexole as an oral steroid-sparing agent in hypereosinophilic syndromes.

Panch SR, Bozik ME, Brown T, Makiya M, Prussin C, Archibald DG, Hebrank GT, Sullivan M, Sun X, Wetzler L, Ware J, Fay MP, Dunbar CE, Dworetzky SI, Khoury P, Maric I, Klion AD.

Blood. 2018 Aug 2;132(5):501-509. doi: 10.1182/blood-2018-02-835330. Epub 2018 May 8. Erratum in: Blood. 2018 Sep 27;132(13):1461.

3.

The targeted eosinophil-lowering effects of dexpramipexole in clinical studies.

Dworetzky SI, Hebrank GT, Archibald DG, Reynolds IJ, Farwell W, Bozik ME.

Blood Cells Mol Dis. 2017 Mar;63:62-65. doi: 10.1016/j.bcmd.2017.01.008. Epub 2017 Jan 16.

PMID:
28178599
4.

JBS Special Issue: Innovative Screening Methodologies to Identify New Compounds for the Treatment of Central Nervous System Disorders.

Burris KD, Dworetzky SI.

J Biomol Screen. 2016 Jun;21(5):425-6. doi: 10.1177/1087057116644231. No abstract available. Erratum in: J Biomol Screen. 2016 Aug;21(7):766.

PMID:
27206854
5.

The mitochondrial complex V-associated large-conductance inner membrane current is regulated by cyclosporine and dexpramipexole.

Alavian KN, Dworetzky SI, Bonanni L, Zhang P, Sacchetti S, Li H, Signore AP, Smith PJ, Gribkoff VK, Jonas EA.

Mol Pharmacol. 2015 Jan;87(1):1-8. doi: 10.1124/mol.114.095661. Epub 2014 Oct 20.

6.

Discovery of (S,E)-3-(2-fluorophenyl)-N-(1-(3-(pyridin-3-yloxy)phenyl)ethyl)-acrylamide as a potent and efficacious KCNQ2 (Kv7.2) opener for the treatment of neuropathic pain.

Wu YJ, Conway CM, Sun LQ, Machet F, Chen J, Chen P, He H, Bourin C, Calandra V, Polino JL, Davis CD, Heman K, Gribkoff VK, Boissard CG, Knox RJ, Thompson MW, Fitzpatrick W, Weaver D, Harden DG, Natale J, Dworetzky SI, Starrett JE Jr.

Bioorg Med Chem Lett. 2013 Nov 15;23(22):6188-91. doi: 10.1016/j.bmcl.2013.08.092. Epub 2013 Sep 8.

PMID:
24070783
7.

Discovery of a novel series of quinolone α7 nicotinic acetylcholine receptor agonists.

McDonald IM, Mate RA, Zusi FC, Huang H, Post-Munson DJ, Ferrante MA, Gallagher L, Bertekap RL Jr, Knox RJ, Robertson BJ, Harden DG, Morgan DG, Lodge NJ, Dworetzky SI, Olson RE, Macor JE.

Bioorg Med Chem Lett. 2013 Mar 15;23(6):1684-8. doi: 10.1016/j.bmcl.2013.01.070. Epub 2013 Jan 29.

PMID:
23414838
8.

Effects of dexpramipexole on brain mitochondrial conductances and cellular bioenergetic efficiency.

Alavian KN, Dworetzky SI, Bonanni L, Zhang P, Sacchetti S, Mariggio MA, Onofrj M, Thomas A, Li H, Mangold JE, Signore AP, Demarco U, Demady DR, Nabili P, Lazrove E, Smith PJ, Gribkoff VK, Jonas EA.

Brain Res. 2012 Mar 29;1446:1-11. doi: 10.1016/j.brainres.2012.01.046. Epub 2012 Jan 28.

9.

Atropisomeric 3-(beta-hydroxyethyl)-4-arylquinolin-2-ones as Maxi-K potassium channel openers.

Vrudhula VM, Dasgupta B, Qian-Cutrone J, Kozlowski ES, Boissard CG, Dworetzky SI, Wu D, Gao Q, Kimura R, Gribkoff VK, Starrett JE Jr.

J Med Chem. 2007 Mar 8;50(5):1050-7. Epub 2007 Feb 3.

PMID:
17274609
10.

3-[(5-Chloro-2-hydroxyphenyl)methyl]-5-[4-(trifluoromethyl)phenyl ]-1,3,4-oxadiazol-2(3H)-one, BMS-191011: opener of large-conductance Ca(2+)-activated potassium (maxi-K) channels, identification, solubility, and SAR.

Romine JL, Martin SW, Meanwell NA, Gribkoff VK, Boissard CG, Dworetzky SI, Natale J, Moon S, Ortiz A, Yeleswaram S, Pajor L, Gao Q, Starrett JE Jr.

J Med Chem. 2007 Feb 8;50(3):528-42.

PMID:
17266205
11.

Pharmacological activation and inhibition of Slack (Slo2.2) channels.

Yang B, Gribkoff VK, Pan J, Damagnez V, Dworetzky SI, Boissard CG, Bhattacharjee A, Yan Y, Sigworth FJ, Kaczmarek LK.

Neuropharmacology. 2006 Sep;51(4):896-906. Epub 2006 Jul 28.

PMID:
16876206
12.

Recent developments on KCNQ potassium channel openers.

Wua YJ, Dworetzky SI.

Curr Med Chem. 2005;12(4):453-60. Review.

PMID:
15720253
13.

A thallium-sensitive, fluorescence-based assay for detecting and characterizing potassium channel modulators in mammalian cells.

Weaver CD, Harden D, Dworetzky SI, Robertson B, Knox RJ.

J Biomol Screen. 2004 Dec;9(8):671-7.

PMID:
15634793
14.

(S,E)-N-[1-(3-heteroarylphenyl)ethyl]-3-(2-fluorophenyl)acrylamides: synthesis and KCNQ2 potassium channel opener activity.

L'Heureux A, Martel A, He H, Chen J, Sun LQ, Starrett JE, Natale J, Dworetzky SI, Knox RJ, Harden DG, Weaver D, Thompson MW, Wu YJ.

Bioorg Med Chem Lett. 2005 Jan 17;15(2):363-6.

PMID:
15603955
15.

3-Thio-quinolinone maxi-K openers for the treatment of erectile dysfunction.

Boy KM, Guernon JM, Sit SY, Xie K, Hewawasam P, Boissard CG, Dworetzky SI, Natale J, Gribkoff VK, Lodge N, Starrett JE Jr.

Bioorg Med Chem Lett. 2004 Oct 18;14(20):5089-93.

PMID:
15380205
16.

Synthesis and KCNQ2 opener activity of N-(1-benzo[1,3]dioxol-5-yl-ethyl, N-[1-(2,3-dihydro-benzofuran-5-yl)-ethyl, and N-[1-(2,3-dihydro-1H-indol-5-yl)-ethyl acrylamides.

Wu YJ, Sun LQ, He H, Chen J, Starrett JE Jr, Dextraze P, Daris JP, Boissard CG, Pieschl RL, Gribkoff VK, Natale J, Knox RJ, Harden DG, Thompson MW, Fitzpatrick W, Weaver D, Wu D, Gao Q, Dworetzky SI.

Bioorg Med Chem Lett. 2004 Sep 6;14(17):4533-7.

PMID:
15357987
17.

Synthesis and structure-activity relationship of acrylamides as KCNQ2 potassium channel openers.

Wu YJ, He H, Sun LQ, L'Heureux A, Chen J, Dextraze P, Starrett JE Jr, Boissard CG, Gribkoff VK, Natale J, Dworetzky SI.

J Med Chem. 2004 May 20;47(11):2887-96.

PMID:
15139767
18.

(S)-N-[1-(4-cyclopropylmethyl-3,4-dihydro-2H-benzo[1,4]oxazin-6-yl)-ethyl]-3-(2-fluoro-phenyl)-acrylamide is a potent and efficacious KCNQ2 opener which inhibits induced hyperexcitability of rat hippocampal neurons.

Wu YJ, Boissard CG, Chen J, Fitzpatrick W, Gao Q, Gribkoff VK, Harden DG, He H, Knox RJ, Natale J, Pieschl RL, Starrett JE Jr, Sun LQ, Thompson M, Weaver D, Wu D, Dworetzky SI.

Bioorg Med Chem Lett. 2004 Apr 19;14(8):1991-5.

PMID:
15050644
19.

The synthesis and structure-activity relationships of 3-amino-4-benzylquinolin-2-ones; discovery of novel KCNQ2 channel openers.

Hewawasam P, Chen N, Ding M, Natale JT, Boissard CG, Yeola S, Gribkoff VK, Starrett J, Dworetzky SI.

Bioorg Med Chem Lett. 2004 Apr 5;14(7):1615-8.

PMID:
15026035
20.

(S)-N-[1-(3-morpholin-4-ylphenyl)ethyl]- 3-phenylacrylamide: an orally bioavailable KCNQ2 opener with significant activity in a cortical spreading depression model of migraine.

Wu YJ, Boissard CG, Greco C, Gribkoff VK, Harden DG, He H, L'Heureux A, Kang SH, Kinney GG, Knox RJ, Natale J, Newton AE, Lehtinen-Oboma S, Sinz MW, Sivarao DV, Starrett JE Jr, Sun LQ, Tertyshnikova S, Thompson MW, Weaver D, Wong HS, Zhang L, Dworetzky SI.

J Med Chem. 2003 Jul 17;46(15):3197-200.

PMID:
12852750
21.

4-Aryl-3-(hydroxyalkyl)quinolin-2-ones: novel maxi-K channel opening relaxants of corporal smooth muscle targeted for erectile dysfunction.

Hewawasam P, Fan W, Ding M, Flint K, Cook D, Goggins GD, Myers RA, Gribkoff VK, Boissard CG, Dworetzky SI, Starrett JE Jr, Lodge NJ.

J Med Chem. 2003 Jul 3;46(14):2819-22.

PMID:
12825925
22.

Novel openers of Ca2+-dependent large-conductance potassium channels: symmetrical pharmacophore and electrophysiological evaluation of bisphenols.

Li Y, Johnson G, Romine JL, Meanwell NA, Martin SW, Dworetzky SI, Boissard CG, Gribkoff VK, Starrett JE Jr.

Bioorg Med Chem Lett. 2003 Apr 17;13(8):1437-9.

PMID:
12668007
23.

4,5-diphenyltriazol-3-ones: openers of large-conductance Ca(2+)-activated potassium (maxi-K) channels.

Romine JL, Martin SW, Gribkoff VK, Boissard CG, Dworetzky SI, Natale J, Li Y, Gao Q, Meanwell NA, Starrett JE Jr.

J Med Chem. 2002 Jul 4;45(14):2942-52.

PMID:
12086481
24.

The synthesis and characterization of BMS-204352 (MaxiPost) and related 3-fluorooxindoles as openers of maxi-K potassium channels.

Hewawasam P, Gribkoff VK, Pendri Y, Dworetzky SI, Meanwell NA, Martinez E, Boissard CG, Post-Munson DJ, Trojnacki JT, Yeleswaram K, Pajor LM, Knipe J, Gao Q, Perrone R, Starrett JE Jr.

Bioorg Med Chem Lett. 2002 Apr 8;12(7):1023-6.

PMID:
11909708
25.

Maxi-K potassium channels: form, function, and modulation of a class of endogenous regulators of intracellular calcium.

Gribkoff VK, Starrett JE Jr, Dworetzky SI.

Neuroscientist. 2001 Apr;7(2):166-77. Review.

PMID:
11496927
26.

Targeting acute ischemic stroke with a calcium-sensitive opener of maxi-K potassium channels.

Gribkoff VK, Starrett JE Jr, Dworetzky SI, Hewawasam P, Boissard CG, Cook DA, Frantz SW, Heman K, Hibbard JR, Huston K, Johnson G, Krishnan BS, Kinney GG, Lombardo LA, Meanwell NA, Molinoff PB, Myers RA, Moon SL, Ortiz A, Pajor L, Pieschl RL, Post-Munson DJ, Signor LJ, Srinivas N, Taber MT, Thalody G, Trojnacki JT, Wiener H, Yeleswaram K, Yeola SW.

Nat Med. 2001 Apr;7(4):471-7.

PMID:
11283675
27.

Formation of intermediate-conductance calcium-activated potassium channels by interaction of Slack and Slo subunits.

Joiner WJ, Tang MD, Wang LY, Dworetzky SI, Boissard CG, Gan L, Gribkoff VK, Kaczmarek LK.

Nat Neurosci. 1998 Oct;1(6):462-9.

PMID:
10196543
28.
29.

The pharmacology and molecular biology of large-conductance calcium-activated (BK) potassium channels.

Gribkoff VK, Starrett JE Jr, Dworetzky SI.

Adv Pharmacol. 1997;37:319-48. Review. No abstract available.

PMID:
8891106
30.

Synthesis and biological evaluation of an iodinated iberiotoxin analogue, [mono-iodo-Tyr5, Phe36]-iberiotoxin.

Kozlowski ES, Johnson G, Dischino DD, Dworetzky SI, Boissard CG, Gribkoff VK.

Int J Pept Protein Res. 1996 Aug;48(2):194-9.

PMID:
8872538
31.

Phenotypic alteration of a human BK (hSlo) channel by hSlobeta subunit coexpression: changes in blocker sensitivity, activation/relaxation and inactivation kinetics, and protein kinase A modulation.

Dworetzky SI, Boissard CG, Lum-Ragan JT, McKay MC, Post-Munson DJ, Trojnacki JT, Chang CP, Gribkoff VK.

J Neurosci. 1996 Aug 1;16(15):4543-50.

32.

Effects of channel modulators on cloned large-conductance calcium-activated potassium channels.

Gribkoff VK, Lum-Ragan JT, Boissard CG, Post-Munson DJ, Meanwell NA, Starrett JE Jr, Kozlowski ES, Romine JL, Trojnacki JT, Mckay MC, Zhong J, Dworetzky SI.

Mol Pharmacol. 1996 Jul;50(1):206-17.

PMID:
8700114
33.

Cloning and expression of a human large-conductance calcium-activated potassium channel.

Dworetzky SI, Trojnacki JT, Gribkoff VK.

Brain Res Mol Brain Res. 1994 Nov;27(1):189-93.

PMID:
7877450
34.

Opening of large-conductance calcium-activated potassium channels by the substituted benzimidazolone NS004.

McKay MC, Dworetzky SI, Meanwell NA, Olesen SP, Reinhart PH, Levitan IB, Adelman JP, Gribkoff VK.

J Neurophysiol. 1994 May;71(5):1873-82.

PMID:
8064354
35.

The substituted benzimidazolone NS004 is an opener of the cystic fibrosis chloride channel.

Gribkoff VK, Champigny G, Barbry P, Dworetzky SI, Meanwell NA, Lazdunski M.

J Biol Chem. 1994 Apr 15;269(15):10983-6.

37.

Sequence-specific DNA-binding proteins are components of a nuclear matrix-attachment site.

Dworetzky SI, Wright KL, Fey EG, Penman S, Lian JB, Stein JL, Stein GS.

Proc Natl Acad Sci U S A. 1992 May 1;89(9):4178-82.

38.

Regulation of transcription-factor activity during growth and differentiation: involvement of the nuclear matrix in concentration and localization of promoter binding proteins.

Stein GS, Lian JB, Dworetzky SI, Owen TA, Bortell R, Bidwell JP, van Wijnen AJ.

J Cell Biochem. 1991 Dec;47(4):300-5. Review.

PMID:
1795014
39.

Progressive changes in the protein composition of the nuclear matrix during rat osteoblast differentiation.

Dworetzky SI, Fey EG, Penman S, Lian JB, Stein JL, Stein GS.

Proc Natl Acad Sci U S A. 1990 Jun;87(12):4605-9.

40.

The effects of variations in the number and sequence of targeting signals on nuclear uptake.

Dworetzky SI, Lanford RE, Feldherr CM.

J Cell Biol. 1988 Oct;107(4):1279-87.

41.

The pore complex in nucleocytoplasmic exchange.

Feldherr CM, Dworetzky SI.

Cell Biol Int Rep. 1988 Sep;12(9):791-808. Review. No abstract available.

PMID:
2461807
42.

Translocation of RNA-coated gold particles through the nuclear pores of oocytes.

Dworetzky SI, Feldherr CM.

J Cell Biol. 1988 Mar;106(3):575-84.

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