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Items: 45


Bayesian model of disease progression in GNE myopathy.

Quintana M, Shrader J, Slota C, Joe G, McKew JC, Fitzgerald M, Gahl WA, Berry S, Carrillo N.

Stat Med. 2019 Apr 15;38(8):1459-1474. doi: 10.1002/sim.8050. Epub 2018 Dec 3.


Efficient Synthesis of 1,9-Substituted Benzo[h][1,6]naphthyridin-2(1H)-ones and Evaluation of their Plasmodium falciparum Gametocytocidal Activities.

Li H, Sun W, Huang X, Lu X, Patel PR, Kim M, Orr MJ, Fisher RM, Tanaka TQ, McKew JC, Simeonov A, Sanderson PE, Zheng W, Williamson KC, Huang W.

ACS Comb Sci. 2017 Dec 11;19(12):748-754. doi: 10.1021/acscombsci.7b00119. Epub 2017 Oct 27.


Intrathecal 2-hydroxypropyl-β-cyclodextrin decreases neurological disease progression in Niemann-Pick disease, type C1: a non-randomised, open-label, phase 1-2 trial.

Ory DS, Ottinger EA, Farhat NY, King KA, Jiang X, Weissfeld L, Berry-Kravis E, Davidson CD, Bianconi S, Keener LA, Rao R, Soldatos A, Sidhu R, Walters KA, Xu X, Thurm A, Solomon B, Pavan WJ, Machielse BN, Kao M, Silber SA, McKew JC, Brewer CC, Vite CH, Walkley SU, Austin CP, Porter FD.

Lancet. 2017 Oct 14;390(10104):1758-1768. doi: 10.1016/S0140-6736(17)31465-4. Epub 2017 Aug 10.


Safety, pharmacokinetics and sialic acid production after oral administration of N-acetylmannosamine (ManNAc) to subjects with GNE myopathy.

Xu X, Wang AQ, Latham LL, Celeste F, Ciccone C, Malicdan MC, Goldspiel B, Terse P, Cradock J, Yang N, Yorke S, McKew JC, Gahl WA, Huizing M, Carrillo N.

Mol Genet Metab. 2017 Sep;122(1-2):126-134. doi: 10.1016/j.ymgme.2017.04.010. Epub 2017 Apr 26.


High throughput cell-based assay for identification of glycolate oxidase inhibitors as a potential treatment for Primary Hyperoxaluria Type 1.

Wang M, Xu M, Long Y, Fargue S, Southall N, Hu X, McKew JC, Danpure CJ, Zheng W.

Sci Rep. 2016 Sep 27;6:34060. doi: 10.1038/srep34060.


In vitro evaluation of imidazo[4,5-c]quinolin-2-ones as gametocytocidal antimalarial agents.

Patel PR, Sun W, Kim M, Huang X, Sanderson PE, Tanaka TQ, McKew JC, Simeonov A, Williamson KC, Zheng W, Huang W.

Bioorg Med Chem Lett. 2016 Jun 15;26(12):2907-2911. doi: 10.1016/j.bmcl.2016.04.045. Epub 2016 Apr 19.


High-Throughput Phenotypic Screening of Human Astrocytes to Identify Compounds That Protect Against Oxidative Stress.

Thorne N, Malik N, Shah S, Zhao J, Class B, Aguisanda F, Southall N, Xia M, McKew JC, Rao M, Zheng W.

Stem Cells Transl Med. 2016 May;5(5):613-27. doi: 10.5966/sctm.2015-0170. Epub 2016 Mar 31.


Quantitative hydrophilic interaction chromatography-mass spectrometry analysis of N-acetylneuraminic acid and N-acetylmannosamine in human plasma.

Shi Y, Xu X, Fang M, Zhang M, Li Y, Gillespie B, Yorke S, Yang N, McKew JC, Gahl WA, Huizing M, Carrillo-Carrasco N, Wang AQ.

J Chromatogr B Analyt Technol Biomed Life Sci. 2015 Sep 1;1000:105-11. doi: 10.1016/j.jchromb.2015.07.018. Epub 2015 Jul 17.


Identification of 53 compounds that block Ebola virus-like particle entry via a repurposing screen of approved drugs.

Kouznetsova J, Sun W, Martínez-Romero C, Tawa G, Shinn P, Chen CZ, Schimmer A, Sanderson P, McKew JC, Zheng W, García-Sastre A.

Emerg Microbes Infect. 2014 Dec;3(12):e84. doi: 10.1038/emi.2014.88. Epub 2014 Dec 17.


Small molecule inhibition of group I p21-activated kinases in breast cancer induces apoptosis and potentiates the activity of microtubule stabilizing agents.

Ong CC, Gierke S, Pitt C, Sagolla M, Cheng CK, Zhou W, Jubb AM, Strickland L, Schmidt M, Duron SG, Campbell DA, Zheng W, Dehdashti S, Shen M, Yang N, Behnke ML, Huang W, McKew JC, Chernoff J, Forrest WF, Haverty PM, Chin SF, Rakha EA, Green AR, Ellis IO, Caldas C, O'Brien T, Friedman LS, Koeppen H, Rudolph J, Hoeflich KP.

Breast Cancer Res. 2015 Apr 23;17:59. doi: 10.1186/s13058-015-0564-5.


Financing translation: analysis of the NCATS rare-diseases portfolio.

Fagnan DE, Yang NN, McKew JC, Lo AW.

Sci Transl Med. 2015 Feb 25;7(276):276ps3. doi: 10.1126/scitranslmed.aaa2360. Review.


High-throughput viability assay using an autonomously bioluminescent cell line with a bacterial Lux reporter.

Class B, Thorne N, Aguisanda F, Southall N, McKew JC, Zheng W.

J Lab Autom. 2015 Apr;20(2):164-74. doi: 10.1177/2211068214560608. Epub 2014 Dec 1.


ERK and β-arrestin interaction: a converging point of signaling pathways for multiple types of cell surface receptors.

Eishingdrelo H, Sun W, Li H, Wang L, Eishingdrelo A, Dai S, McKew JC, Zheng W.

J Biomol Screen. 2015 Mar;20(3):341-9. doi: 10.1177/1087057114557233. Epub 2014 Oct 31.


Atypical presentation of GNE myopathy with asymmetric hand weakness.

de Dios JK, Shrader JA, Joe GO, McClean JC, Williams K, Evers R, Malicdan MC, Ciccone C, Mankodi A, Huizing M, McKew JC, Bluemke DA, Gahl WA, Carrillo-Carrasco N.

Neuromuscul Disord. 2014 Dec;24(12):1063-7. doi: 10.1016/j.nmd.2014.07.006. Epub 2014 Aug 7.


Niemann-Pick Disease Type C: Induced Pluripotent Stem Cell-Derived Neuronal Cells for Modeling Neural Disease and Evaluating Drug Efficacy.

Yu D, Swaroop M, Wang M, Baxa U, Yang R, Yan Y, Coksaygan T, DeTolla L, Marugan JJ, Austin CP, McKew JC, Gong DW, Zheng W.

J Biomol Screen. 2014 Sep;19(8):1164-73. doi: 10.1177/1087057114537378. Epub 2014 Jun 6.


Mutation update for GNE gene variants associated with GNE myopathy.

Celeste FV, Vilboux T, Ciccone C, de Dios JK, Malicdan MC, Leoyklang P, McKew JC, Gahl WA, Carrillo-Carrasco N, Huizing M.

Hum Mutat. 2014 Aug;35(8):915-26. doi: 10.1002/humu.22583. Review.


Chemical signatures and new drug targets for gametocytocidal drug development.

Sun W, Tanaka TQ, Magle CT, Huang W, Southall N, Huang R, Dehdashti SJ, McKew JC, Williamson KC, Zheng W.

Sci Rep. 2014 Jan 17;4:3743. doi: 10.1038/srep03743.


Collaborative development of 2-hydroxypropyl-β-cyclodextrin for the treatment of Niemann-Pick type C1 disease.

Ottinger EA, Kao ML, Carrillo-Carrasco N, Yanjanin N, Shankar RK, Janssen M, Brewster M, Scott I, Xu X, Cradock J, Terse P, Dehdashti SJ, Marugan J, Zheng W, Portilla L, Hubbs A, Pavan WJ, Heiss J, Vite CH, Walkley SU, Ory DS, Silber SA, Porter FD, Austin CP, McKew JC.

Curr Top Med Chem. 2014;14(3):330-9. Review.


Rapid identification of antifungal compounds against Exserohilum rostratum using high throughput drug repurposing screens.

Sun W, Park YD, Sugui JA, Fothergill A, Southall N, Shinn P, McKew JC, Kwon-Chung KJ, Zheng W, Williamson PR.

PLoS One. 2013 Aug 21;8(8):e70506. doi: 10.1371/journal.pone.0070506. eCollection 2013. Erratum in: PLoS One. 2013;8(9). doi:10.1371/annotation/df5a5a46-cf30-4842-bf11-b6cee36c1f9b.


A phenotypic compound screening assay for lysosomal storage diseases.

Xu M, Liu K, Swaroop M, Sun W, Dehdashti SJ, McKew JC, Zheng W.

J Biomol Screen. 2014 Jan;19(1):168-75. doi: 10.1177/1087057113501197. Epub 2013 Aug 27.


A high-throughput screening assay for determining cellular levels of total tau protein.

Dehdashti SJ, Zheng W, Gever JR, Wilhelm R, Nguyen DT, Sittampalam G, McKew JC, Austin CP, Prusiner SB.

Curr Alzheimer Res. 2013 Sep;10(7):679-87.


Phenotypic screens as a renewed approach for drug discovery.

Zheng W, Thorne N, McKew JC.

Drug Discov Today. 2013 Nov;18(21-22):1067-73. doi: 10.1016/j.drudis.2013.07.001. Epub 2013 Jul 9. Review.


A high-throughput screening assay for assessing the viability of Cryptococcus neoformans under nutrient starvation conditions.

Dehdashti SJ, Abbott J, Nguyen DT, McKew JC, Williamson PR, Zheng W.

Anal Bioanal Chem. 2013 Aug;405(21):6823-9. doi: 10.1007/s00216-013-7134-4. Epub 2013 Jun 30.


An alternative direct compound dispensing method using the HP D300 digital dispenser.

Jones RE, Zheng W, McKew JC, Chen CZ.

J Lab Autom. 2013 Oct;18(5):367-74. doi: 10.1177/2211068213491094. Epub 2013 May 24.


A quantitative high throughput assay for identifying gametocytocidal compounds.

Tanaka TQ, Dehdashti SJ, Nguyen DT, McKew JC, Zheng W, Williamson KC.

Mol Biochem Parasitol. 2013 Mar;188(1):20-5. doi: 10.1016/j.molbiopara.2013.02.005. Epub 2013 Feb 27.


NIH TRND program: successes in preclinical therapeutic development.

McKew JC, Pilon AM.

Trends Pharmacol Sci. 2013 Feb;34(2):87-9. doi: 10.1016/ Epub 2012 Nov 19. No abstract available.


δ-Tocopherol reduces lipid accumulation in Niemann-Pick type C1 and Wolman cholesterol storage disorders.

Xu M, Liu K, Swaroop M, Porter FD, Sidhu R, Firnkes S, Ory DS, Marugan JJ, Xiao J, Southall N, Pavan WJ, Davidson C, Walkley SU, Remaley AT, Baxa U, Sun W, McKew JC, Austin CP, Zheng W.

J Biol Chem. 2012 Nov 16;287(47):39349-60. doi: 10.1074/jbc.M112.357707. Epub 2012 Oct 3. Erratum in: J Biol Chem. 2013 Jan 4;288(1):296. Finkes, Sally [corrected to Firnkes, Sally].


Evaluation of cholesterol reduction activity of methyl-β-cyclodextrin using differentiated human neurons and astrocytes.

Swaroop M, Thorne N, Rao MS, Austin CP, McKew JC, Zheng W.

J Biomol Screen. 2012 Oct;17(9):1243-51. Epub 2012 Aug 24.


Plasma and tissue concentrations of α-tocopherol and δ-tocopherol following high dose dietary supplementation in mice.

Baxter LL, Marugan JJ, Xiao J, Incao A, McKew JC, Zheng W, Pavan WJ.

Nutrients. 2012 Jun;4(6):467-90. doi: 10.3390/nu4060467. Epub 2012 Jun 6.


Osteogenic effects of a potent Src-over-Abl-selective kinase inhibitor in the mouse.

Murrills RJ, Fukayama S, Boschelli F, Matteo JJ, Owens J, Golas JM, Patel D, Lane G, Liu YB, Carter L, Jussif J, Spaulding V, Wang YD, Boschelli DH, McKew JC, Li XJ, Lockhead S, Milligan C, Kharode YP, Diesl V, Bai Y, Follettie M, Bex FJ, Komm B, Bodine PV.

J Pharmacol Exp Ther. 2012 Mar;340(3):676-87. doi: 10.1124/jpet.111.185793. Epub 2011 Dec 9.


Cytosolic phospholipase A2α blockade abrogates disease during the tissue-damage effector phase of experimental autoimmune encephalomyelitis by its action on APCs.

Thakker P, Marusic S, Stedman NL, Lee KL, McKew JC, Wood A, Goldman SJ, Leach MW, Collins M, Kuchroo VK, Wolf SF, Clark JD, Hassan-Zahraee M.

J Immunol. 2011 Aug 15;187(4):1986-97. doi: 10.4049/jimmunol.1002789. Epub 2011 Jul 11.


The cPLA2α inhibitor efipladib decreases nociceptive responses without affecting PGE2 levels in the cerebral spinal fluid.

Nickerson-Nutter CL, Goodwin D, Shen MW, Damphousse C, Duan W, Samad TA, McKew JC, Lee KL, Zaleska MM, Mollova N, Clark JD.

Neuropharmacology. 2011 Mar;60(4):633-41. doi: 10.1016/j.neuropharm.2010.11.025. Epub 2010 Dec 10.


Benzhydrylquinazolinediones: novel cytosolic phospholipase A2alpha inhibitors with improved physicochemical properties.

Kirincich SJ, Xiang J, Green N, Tam S, Yang HY, Shim J, Shen MW, Clark JD, McKew JC.

Bioorg Med Chem. 2009 Jul 1;17(13):4383-405. doi: 10.1016/j.bmc.2009.05.027. Epub 2009 May 18.


Reactions of functionalized sulfonamides: application to lowering the lipophilicity of cytosolic phospholipase A2alpha inhibitors.

Chen L, Wang W, Lee KL, Shen MW, Murphy EA, Zhang W, Xu X, Tam S, Nickerson-Nutter C, Goodwin DG, Clark JD, McKew JC.

J Med Chem. 2009 Feb 26;52(4):1156-71. doi: 10.1021/jm8009876.


Blockade of cytosolic phospholipase A2 alpha prevents experimental autoimmune encephalomyelitis and diminishes development of Th1 and Th17 responses.

Marusic S, Thakker P, Pelker JW, Stedman NL, Lee KL, McKew JC, Han L, Xu X, Wolf SF, Borey AJ, Cui J, Shen MW, Donahue F, Hassan-Zahraee M, Leach MW, Shimizu T, Clark JD.

J Neuroimmunol. 2008 Nov 15;204(1-2):29-37. doi: 10.1016/j.jneuroim.2008.08.012.


Piperazine sulfonamides as potent, selective, and orally available 11beta-hydroxysteroid dehydrogenase type 1 inhibitors with efficacy in the rat cortisone-induced hyperinsulinemia model.

Xiang J, Wan ZK, Li HQ, Ipek M, Binnun E, Nunez J, Chen L, McKew JC, Mansour TS, Xu X, Suri V, Tam M, Xing Y, Li X, Hahm S, Tobin J, Saiah E.

J Med Chem. 2008 Jul 24;51(14):4068-71. doi: 10.1021/jm8004948. Epub 2008 Jun 26.


Indole cytosolic phospholipase A2 alpha inhibitors: discovery and in vitro and in vivo characterization of 4-{3-[5-chloro-2-(2-{[(3,4-dichlorobenzyl)sulfonyl]amino}ethyl)-1-(diphenylmethyl)-1H-indol-3-yl]propyl}benzoic acid, efipladib.

McKew JC, Lee KL, Shen MW, Thakker P, Foley MA, Behnke ML, Hu B, Sum FW, Tam S, Hu Y, Chen L, Kirincich SJ, Michalak R, Thomason J, Ipek M, Wu K, Wooder L, Ramarao MK, Murphy EA, Goodwin DG, Albert L, Xu X, Donahue F, Ku MS, Keith J, Nickerson-Nutter CL, Abraham WM, Williams C, Hegen M, Clark JD.

J Med Chem. 2008 Jun 26;51(12):3388-413. doi: 10.1021/jm701467e. Epub 2008 May 23.


Benzenesulfonamide indole inhibitors of cytosolic phospholipase A2alpha: optimization of in vitro potency and rat pharmacokinetics for oral efficacy.

Lee KL, Behnke ML, Foley MA, Chen L, Wang W, Vargas R, Nunez J, Tam S, Mollova N, Xu X, Shen MW, Ramarao MK, Goodwin DG, Nickerson-Nutter CL, Abraham WM, Williams C, Clark JD, McKew JC.

Bioorg Med Chem. 2008 Feb 1;16(3):1345-58. Epub 2007 Oct 22.


Discovery of Ecopladib, an indole inhibitor of cytosolic phospholipase A2alpha.

Lee KL, Foley MA, Chen L, Behnke ML, Lovering FE, Kirincich SJ, Wang W, Shim J, Tam S, Shen MW, Khor S, Xu X, Goodwin DG, Ramarao MK, Nickerson-Nutter C, Donahue F, Ku MS, Clark JD, McKew JC.

J Med Chem. 2007 Mar 22;50(6):1380-400. Epub 2007 Feb 17.


Synthesis of pyrazolo[1,5-alpha]pyrimidinone regioisomers.

Gavrin LK, Lee A, Provencher BA, Massefski WW, Huhn SD, Ciszewski GM, Cole DC, McKew JC.

J Org Chem. 2007 Feb 2;72(3):1043-6.


1,2,4-Oxadiazolidin-3,5-diones and 1,3,5-triazin-2,4,6-triones as cytosolic phospholipase A2alpha inhibitors.

Gopalsamy A, Yang H, Ellingboe JW, McKew JC, Tam S, Joseph-McCarthy D, Zhang W, Shen M, Clark JD.

Bioorg Med Chem Lett. 2006 Jun 1;16(11):2978-81. Epub 2006 Mar 20.


Inhibition of cytosolic phospholipase A2alpha: hit to lead optimization.

McKew JC, Foley MA, Thakker P, Behnke ML, Lovering FE, Sum FW, Tam S, Wu K, Shen MW, Zhang W, Gonzalez M, Liu S, Mahadevan A, Sard H, Khor SP, Clark JD.

J Med Chem. 2006 Jan 12;49(1):135-58.


Structure-activity relationships of indole cytosolic phospholipase A(2)alpha inhibitors: substrate mimetics.

McKew JC, Lovering F, Clark JD, Bemis J, Xiang Y, Shen M, Zhang W, Alvarez JC, Joseph-McCarthy D.

Bioorg Med Chem Lett. 2003 Dec 15;13(24):4501-4.


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