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Items: 1 to 50 of 85

1.

Identification, design and synthesis of novel pyrazolopyridine influenza virus nonstructural protein 1 antagonists.

Patnaik S, Basu D, Southall N, Dehdashti S, Wan KK, Zheng W, Ferrer M, Taylor M, Engel DA, Marugan JJ.

Bioorg Med Chem Lett. 2019 May 1;29(9):1113-1119. doi: 10.1016/j.bmcl.2019.02.027. Epub 2019 Feb 26.

PMID:
30852083
2.

Proteolytic cleavage of host proteins by the Group IV viral proteases of Venezuelan equine encephalitis virus and Zika virus.

Morazzani EM, Compton JR, Leary DH, Berry AV, Hu X, Marugan JJ, Glass PJ, Legler PM.

Antiviral Res. 2019 Apr;164:106-122. doi: 10.1016/j.antiviral.2019.02.001. Epub 2019 Feb 10.

3.

Neural stem cells for disease modeling and evaluation of therapeutics for Tay-Sachs disease.

Vu M, Li R, Baskfield A, Lu B, Farkhondeh A, Gorshkov K, Motabar O, Beers J, Chen G, Zou J, Espejo-Mojica AJ, Rodríguez-López A, Alméciga-Díaz CJ, Barrera LA, Jiang X, Ory DS, Marugan JJ, Zheng W.

Orphanet J Rare Dis. 2018 Sep 17;13(1):152. doi: 10.1186/s13023-018-0886-3.

4.

Optimization of the first small-molecule relaxin/insulin-like family peptide receptor (RXFP1) agonists: Activation results in an antifibrotic gene expression profile.

Wilson KJ, Xiao J, Chen CZ, Huang Z, Agoulnik IU, Ferrer M, Southall N, Hu X, Zheng W, Xu X, Wang A, Myhr C, Barnaeva E, George ER, Agoulnik AI, Marugan JJ.

Eur J Med Chem. 2018 Aug 5;156:79-92. doi: 10.1016/j.ejmech.2018.06.008. Epub 2018 Jun 7.

PMID:
30006176
5.

A widely-applicable high-throughput cellular thermal shift assay (CETSA) using split Nano Luciferase.

Martinez NJ, Asawa RR, Cyr MG, Zakharov A, Urban DJ, Roth JS, Wallgren E, Klumpp-Thomas C, Coussens NP, Rai G, Yang SM, Hall MD, Marugan JJ, Simeonov A, Henderson MJ.

Sci Rep. 2018 Jun 21;8(1):9472. doi: 10.1038/s41598-018-27834-y.

6.

Metarrestin, a perinucleolar compartment inhibitor, effectively suppresses metastasis.

Frankowski KJ, Wang C, Patnaik S, Schoenen FJ, Southall N, Li D, Teper Y, Sun W, Kandela I, Hu D, Dextras C, Knotts Z, Bian Y, Norton J, Titus S, Lewandowska MA, Wen Y, Farley KI, Griner LM, Sultan J, Meng Z, Zhou M, Vilimas T, Powers AS, Kozlov S, Nagashima K, Quadri HS, Fang M, Long C, Khanolkar O, Chen W, Kang J, Huang H, Chow E, Goldberg E, Feldman C, Xi R, Kim HR, Sahagian G, Baserga SJ, Mazar A, Ferrer M, Zheng W, Shilatifard A, Aubé J, Rudloff U, Marugan JJ, Huang S.

Sci Transl Med. 2018 May 16;10(441). pii: eaap8307. doi: 10.1126/scitranslmed.aap8307.

7.

Neural stem cells for disease modeling and evaluation of therapeutics for infantile (CLN1/PPT1) and late infantile (CLN2/TPP1) neuronal ceroid lipofuscinoses.

Sima N, Li R, Huang W, Xu M, Beers J, Zou J, Titus S, Ottinger EA, Marugan JJ, Xie X, Zheng W.

Orphanet J Rare Dis. 2018 Apr 10;13(1):54. doi: 10.1186/s13023-018-0798-2.

8.

Preclinical Pharmacological Development of Chlorcyclizine Derivatives for the Treatment of Hepatitis C Virus Infection.

Rolt A, Le D, Hu Z, Wang AQ, Shah P, Singleton M, Hughes E, Dulcey AE, He S, Imamura M, Uchida T, Chayama K, Xu X, Marugan JJ, Liang TJ.

J Infect Dis. 2018 May 5;217(11):1761-1769. doi: 10.1093/infdis/jiy039.

9.

Inhibition of PIP4Kγ ameliorates the pathological effects of mutant huntingtin protein.

Al-Ramahi I, Giridharan SSP, Chen YC, Patnaik S, Safren N, Hasegawa J, de Haro M, Wagner Gee AK, Titus SA, Jeong H, Clarke J, Krainc D, Zheng W, Irvine RF, Barmada S, Ferrer M, Southall N, Weisman LS, Botas J, Marugan JJ.

Elife. 2017 Dec 26;6. pii: e29123. doi: 10.7554/eLife.29123.

10.

Discovery of a Positive Allosteric Modulator of the Thyrotropin Receptor: Potentiation of Thyrotropin-Mediated Preosteoblast Differentiation In Vitro.

Neumann S, Eliseeva E, Boutin A, Barnaeva E, Ferrer M, Southall N, Kim D, Hu X, Morgan SJ, Marugan JJ, Gershengorn MC.

J Pharmacol Exp Ther. 2018 Jan;364(1):38-45. doi: 10.1124/jpet.117.244095. Epub 2017 Oct 31.

11.

Mutation of Asn-475 in the Venezuelan Equine Encephalitis Virus nsP2 Cysteine Protease Leads to a Self-Inhibited State.

Compton JR, Mickey MJ, Hu X, Marugan JJ, Legler PM.

Biochemistry. 2017 Nov 28;56(47):6221-6230. doi: 10.1021/acs.biochem.7b00746. Epub 2017 Nov 9.

PMID:
29064679
12.

Development of an Aryloxazole Class of Hepatitis C Virus Inhibitors Targeting the Entry Stage of the Viral Replication Cycle.

He S, Li K, Lin B, Hu Z, Xiao J, Hu X, Wang AQ, Xu X, Ferrer M, Southall N, Zheng W, Aubé J, Schoenen FJ, Marugan JJ, Liang TJ, Frankowski KJ.

J Med Chem. 2017 Jul 27;60(14):6364-6383. doi: 10.1021/acs.jmedchem.7b00561. Epub 2017 Jul 13.

13.

Analytical Characterization of Methyl-β-Cyclodextrin for Pharmacological Activity to Reduce Lysosomal Cholesterol Accumulation in Niemann-Pick Disease Type C1 Cells.

Li R, Hao J, Fujiwara H, Xu M, Yang S, Dai S, Long Y, Swaroop M, Li C, Vu M, Marugan JJ, Ory DS, Zheng W.

Assay Drug Dev Technol. 2017 May/Jun;15(4):154-166. doi: 10.1089/adt.2017.774.

14.

ML290 is a biased allosteric agonist at the relaxin receptor RXFP1.

Kocan M, Sarwar M, Ang SY, Xiao J, Marugan JJ, Hossain MA, Wang C, Hutchinson DS, Samuel CS, Agoulnik AI, Bathgate RAD, Summers RJ.

Sci Rep. 2017 Jun 7;7(1):2968. doi: 10.1038/s41598-017-02916-5.

15.

ML372 blocks SMN ubiquitination and improves spinal muscular atrophy pathology in mice.

Abera MB, Xiao J, Nofziger J, Titus S, Southall N, Zheng W, Moritz KE, Ferrer M, Cherry JJ, Androphy EJ, Wang A, Xu X, Austin C, Fischbeck KH, Marugan JJ, Burnett BG.

JCI Insight. 2016 Nov 17;1(19):e88427. doi: 10.1172/jci.insight.88427.

16.

Induced Pluripotent Stem Cells for Disease Modeling and Evaluation of Therapeutics for Niemann-Pick Disease Type A.

Long Y, Xu M, Li R, Dai S, Beers J, Chen G, Soheilian F, Baxa U, Wang M, Marugan JJ, Muro S, Li Z, Brady R, Zheng W.

Stem Cells Transl Med. 2016 Dec;5(12):1644-1655. Epub 2016 Aug 2.

17.

Activation of β-Glucocerebrosidase Reduces Pathological α-Synuclein and Restores Lysosomal Function in Parkinson's Patient Midbrain Neurons.

Mazzulli JR, Zunke F, Tsunemi T, Toker NJ, Jeon S, Burbulla LF, Patnaik S, Sidransky E, Marugan JJ, Sue CM, Krainc D.

J Neurosci. 2016 Jul 20;36(29):7693-706. doi: 10.1523/JNEUROSCI.0628-16.2016.

18.

Efficacy and Mechanism of Action of Low Dose Emetine against Human Cytomegalovirus.

Mukhopadhyay R, Roy S, Venkatadri R, Su YP, Ye W, Barnaeva E, Mathews Griner L, Southall N, Hu X, Wang AQ, Xu X, Dulcey AE, Marugan JJ, Ferrer M, Arav-Boger R.

PLoS Pathog. 2016 Jun 23;12(6):e1005717. doi: 10.1371/journal.ppat.1005717. eCollection 2016 Jun.

19.

Disease models for the development of therapies for lysosomal storage diseases.

Xu M, Motabar O, Ferrer M, Marugan JJ, Zheng W, Ottinger EA.

Ann N Y Acad Sci. 2016 May;1371(1):15-29. doi: 10.1111/nyas.13052. Epub 2016 May 4. Review.

20.

Structural Insights into the Activation of Human Relaxin Family Peptide Receptor 1 by Small-Molecule Agonists.

Hu X, Myhr C, Huang Z, Xiao J, Barnaeva E, Ho BA, Agoulnik IU, Ferrer M, Marugan JJ, Southall N, Agoulnik AI.

Biochemistry. 2016 Mar 29;55(12):1772-83. doi: 10.1021/acs.biochem.5b01195. Epub 2016 Mar 4.

21.

Discovery, Optimization, and Characterization of Novel Chlorcyclizine Derivatives for the Treatment of Hepatitis C Virus Infection.

He S, Xiao J, Dulcey AE, Lin B, Rolt A, Hu Z, Hu X, Wang AQ, Xu X, Southall N, Ferrer M, Zheng W, Liang TJ, Marugan JJ.

J Med Chem. 2016 Feb 11;59(3):841-53. doi: 10.1021/acs.jmedchem.5b00752. Epub 2016 Feb 1.

22.

Activation of Relaxin Family Receptor 1 from Different Mammalian Species by Relaxin Peptide and Small-Molecule Agonist ML290.

Huang Z, Myhr C, Bathgate RA, Ho BA, Bueno A, Hu X, Xiao J, Southall N, Barnaeva E, Agoulnik IU, Marugan JJ, Ferrer M, Agoulnik AI.

Front Endocrinol (Lausanne). 2015 Aug 17;6:128. doi: 10.3389/fendo.2015.00128. eCollection 2015.

23.

High-Throughput Screening, Discovery, and Optimization To Develop a Benzofuran Class of Hepatitis C Virus Inhibitors.

He S, Jain P, Lin B, Ferrer M, Hu Z, Southall N, Hu X, Zheng W, Neuenswander B, Cho CH, Chen Y, Worlikar SA, Aubé J, Larock RC, Schoenen FJ, Marugan JJ, Liang TJ, Frankowski KJ.

ACS Comb Sci. 2015 Oct 12;17(10):641-52. doi: 10.1021/acscombsci.5b00101. Epub 2015 Sep 17.

24.

Repurposing of the antihistamine chlorcyclizine and related compounds for treatment of hepatitis C virus infection.

He S, Lin B, Chu V, Hu Z, Hu X, Xiao J, Wang AQ, Schweitzer CJ, Li Q, Imamura M, Hiraga N, Southall N, Ferrer M, Zheng W, Chayama K, Marugan JJ, Liang TJ.

Sci Transl Med. 2015 Apr 8;7(282):282ra49. doi: 10.1126/scitranslmed.3010286.

25.

SMN Modulator ML372 Increases SMN Protein Abundance, Body Weight, Lifespan, and Rescues Motor Function in SMNΔ7 SMA Mice.

Burnett BG, Xiao J, Southall N, Zheng W, Ferrer M, Cherry JJ, Androphy EJ, Fischbeck K, Marugan JJ.

Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2010-.
2013 Dec 15 [updated 2015 Feb 11].

26.

Targeting ATM ameliorates mutant Huntingtin toxicity in cell and animal models of Huntington's disease.

Lu XH, Mattis VB, Wang N, Al-Ramahi I, van den Berg N, Fratantoni SA, Waldvogel H, Greiner E, Osmand A, Elzein K, Xiao J, Dijkstra S, de Pril R, Vinters HV, Faull R, Signer E, Kwak S, Marugan JJ, Botas J, Fischer DF, Svendsen CN, Munoz-Sanjuan I, Yang XW.

Sci Transl Med. 2014 Dec 24;6(268):268ra178. doi: 10.1126/scitranslmed.3010523.

PMID:
25540325
27.

Small Molecule, NSC95397, Inhibits the CtBP1-Protein Partner Interaction and CtBP1-Mediated Transcriptional Repression.

Blevins MA, Kouznetsova J, Krueger AB, King R, Griner LM, Hu X, Southall N, Marugan JJ, Zhang Q, Ferrer M, Zhao R.

J Biomol Screen. 2015 Jun;20(5):663-72. doi: 10.1177/1087057114561400. Epub 2014 Dec 4.

28.

Discovery of novel antigiardiasis drug candidates.

Kulakova L, Galkin A, Chen CZ, Southall N, Marugan JJ, Zheng W, Herzberg O.

Antimicrob Agents Chemother. 2014 Dec;58(12):7303-11. doi: 10.1128/AAC.03834-14. Epub 2014 Sep 29.

29.

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.

30.

Lomofungin and dilomofungin: inhibitors of MBNL1-CUG RNA binding with distinct cellular effects.

Hoskins JW, Ofori LO, Chen CZ, Kumar A, Sobczak K, Nakamori M, Southall N, Patnaik S, Marugan JJ, Zheng W, Austin CP, Disney MD, Miller BL, Thornton CA.

Nucleic Acids Res. 2014 Jun;42(10):6591-602. doi: 10.1093/nar/gku275. Epub 2014 May 5.

31.

Discovery and characterization of a G protein-biased agonist that inhibits β-arrestin recruitment to the D2 dopamine receptor.

Free RB, Chun LS, Moritz AE, Miller BN, Doyle TB, Conroy JL, Padron A, Meade JA, Xiao J, Hu X, Dulcey AE, Han Y, Duan L, Titus S, Bryant-Genevier M, Barnaeva E, Ferrer M, Javitch JA, Beuming T, Shi L, Southall NT, Marugan JJ, Sibley DR.

Mol Pharmacol. 2014 Jul;86(1):96-105. doi: 10.1124/mol.113.090563. Epub 2014 Apr 22.

32.

A high throughput screening assay system for the identification of small molecule inhibitors of gsp.

Bhattacharyya N, Hu X, Chen CZ, Mathews Griner LA, Zheng W, Inglese J, Austin CP, Marugan JJ, Southall N, Neumann S, Northup JK, Ferrer M, Collins MT.

PLoS One. 2014 Mar 25;9(3):e90766. doi: 10.1371/journal.pone.0090766. eCollection 2014.

33.

Discovery, optimization, and characterization of novel D2 dopamine receptor selective antagonists.

Xiao J, Free RB, Barnaeva E, Conroy JL, Doyle T, Miller B, Bryant-Genevier M, Taylor MK, Hu X, Dulcey AE, Southall N, Ferrer M, Titus S, Zheng W, Sibley DR, Marugan JJ.

J Med Chem. 2014 Apr 24;57(8):3450-63. doi: 10.1021/jm500126s. Epub 2014 Apr 10.

34.

Discovery of Small Molecule Influenza Virus NS1 Antagonist.

Patnaik S, Basu D, Dehdashti S, Zheng W, Ferrer M, Southall N, Taylor M, Engel DA, Marugan JJ.

Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2010-.
2012 Apr 13 [updated 2013 Sep 3].

35.

Discovery, optimization, and characterization of a novel series of dopamine D2 versus D3 receptor selective antagonists.

Xiao J, Free RB, Barnaeva E, Conroy J, Doyle T, Bryant-Genevier M, Taylor MK, Southall N, Hu X, Ferrer M, Titus S, Zheng W, Sibley DR, Marugan JJ.

Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2010-.
2012 Dec 25 [updated 2013 Sep 3].

36.

Structure-activity relationship of imidazopyridinium analogues as antagonists of neuropeptide s receptor.

Patnaik S, Marugan JJ, Liu K, Zheng W, Southall N, Dehdashti SJ, Thorsell A, Heilig M, Bell L, Zook M, Eskay B, Brimacombe KR, Austin CP.

J Med Chem. 2013 Nov 27;56(22):9045-56. doi: 10.1021/jm400904m. Epub 2013 Nov 11.

37.

Discovery, SAR, and Biological Evaluation of a Non-Inhibitory Chaperone for Acid Alpha Glucosidase.

Marugan JJ, Zheng W, Ferrer M, Motabar O, Southall N, Goldin E, Westbroek W, Sidransky E.

Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2010-.
2011 Dec 16 [updated 2013 May 3].

38.

5-(4-(4-Acetylphenyl)piperazin-1-ylsulfonyl)indolin-2-one Analogs as Inhibitors of Acid alpha-Glucosidase for Potential Chaperone Treatment of Pompe Disease or Intervention for Diabetes Mellitus Type 2.

Xiao J, Marugan JJ, Zheng W, Motabar O, Southall N, Goldin E, Sidransky E, Liu K, Ferrer M, Austin CP.

Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2010-.
2010 Oct 28 [updated 2013 May 3].

39.

Discovery, optimization, and biological activity of the first potent and selective small-molecule agonist series of human relaxin receptor 1 (RXFP1).

Xiao J, Chen CZ, Huang Z, Agoulnik IU, Ferrer M, Southall N, Hu X, Zheng W, Agoulnik AI, Marugan JJ.

Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2010-.
2012 Mar 10 [updated 2013 May 8].

40.

Induction and reversal of myotonic dystrophy type 1 pre-mRNA splicing defects by small molecules.

Childs-Disney JL, Stepniak-Konieczna E, Tran T, Yildirim I, Park H, Chen CZ, Hoskins J, Southall N, Marugan JJ, Patnaik S, Zheng W, Austin CP, Schatz GC, Sobczak K, Thornton CA, Disney MD.

Nat Commun. 2013;4:2044. doi: 10.1038/ncomms3044.

41.

Identification and optimization of small-molecule agonists of the human relaxin hormone receptor RXFP1.

Xiao J, Huang Z, Chen CZ, Agoulnik IU, Southall N, Hu X, Jones RE, Ferrer M, Zheng W, Agoulnik AI, Marugan JJ.

Nat Commun. 2013;4:1953. doi: 10.1038/ncomms2953.

42.

Discovery and Development of Small Molecules That Reduce PNC Prevalence.

Frankowski K, Patnaik S, Schoenen F, Huang S, Norton J, Wang C, Titus S, Ferrer M, Zheng W, Southall N, Day VW, Aubé J, Marugan JJ.

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

43.

Discovery, SAR, and Biological Evaluation of Non-inhibitory Chaperones of Glucocerebrosidase.

Rogers S, Patnaik S, Schoenen F, Zheng W, Choi J, Motabar O, Southall N, Westbroek W, Goldin E, Sidransky E, Leister W, Marugan JJ, Aubé J.

Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2010-.
2012 Mar 27 [updated 2013 Mar 7].

44.

ML223: A Small Molecule Probe With In Vivo Activity Against Acute Myeloid Leukemia Subtype M4Eo.

Marugan JJ, Xiao J, Zheng W, Southall N, Dehdashti S, Cunningham L, Liu PP.

Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2010-.
2011 Apr 4 [updated 2013 Feb 28].

45.

A homogenous luminescence assay reveals novel inhibitors for giardia lamblia carbamate kinase.

Chen CZ, Southall N, Galkin A, Lim K, Marugan JJ, Kulakova L, Shinn P, van Leer D, Zheng W, Herzberg O.

Curr Chem Genomics. 2012;6:93-102. doi: 10.2174/1875397301206010093. Epub 2012 Dec 31.

46.

Identification of small-molecule agonists of human relaxin family receptor 1 (RXFP1) by using a homogenous cell-based cAMP assay.

Chen CZ, Southall N, Xiao J, Marugan JJ, Ferrer M, Hu X, Jones RE, Feng S, Agoulnik IU, Zheng W, Agoulnik AI.

J Biomol Screen. 2013 Jul;18(6):670-7. doi: 10.1177/1087057112469406. Epub 2012 Dec 4.

47.

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].

48.

Discovery of a novel noniminosugar acid α glucosidase chaperone series.

Xiao J, Westbroek W, Motabar O, Lea WA, Hu X, Velayati A, Zheng W, Southall N, Gustafson AM, Goldin E, Sidransky E, Liu K, Simeonov A, Tamargo RJ, Ribes A, Matalonga L, Ferrer M, Marugan JJ.

J Med Chem. 2012 Sep 13;55(17):7546-59. doi: 10.1021/jm3005543. Epub 2012 Aug 17.

49.

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.

50.

Identification of a selective small-molecule inhibitor series targeting the eyes absent 2 (Eya2) phosphatase activity.

Krueger AB, Dehdashti SJ, Southall N, Marugan JJ, Ferrer M, Li X, Ford HL, Zheng W, Zhao R.

J Biomol Screen. 2013 Jan;18(1):85-96. doi: 10.1177/1087057112453936. Epub 2012 Jul 20.

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