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Items: 43

1.

Identification of Antimalarial Inhibitors Using Late-Stage Gametocytes in a Phenotypic Live/Dead Assay.

Spicer TP, Gardiner DL, Schoenen FJ, Roy S, Griffin PR, Chase P, Scampavia L, Hodder P, Trenholme KR.

SLAS Discov. 2018 Aug 24:2472555218796410. doi: 10.1177/2472555218796410. [Epub ahead of print]

PMID:
30142014
2.

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.

3.

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.

4.
5.

Targeting p97 to Disrupt Protein Homeostasis in Cancer.

Vekaria PH, Home T, Weir S, Schoenen FJ, Rao R.

Front Oncol. 2016 Aug 3;6:181. doi: 10.3389/fonc.2016.00181. eCollection 2016. Review.

6.

A New Glucocerebrosidase Chaperone Reduces α-Synuclein and Glycolipid Levels in iPSC-Derived Dopaminergic Neurons from Patients with Gaucher Disease and Parkinsonism.

Aflaki E, Borger DK, Moaven N, Stubblefield BK, Rogers SA, Patnaik S, Schoenen FJ, Westbroek W, Zheng W, Sullivan P, Fujiwara H, Sidhu R, Khaliq ZM, Lopez GJ, Goldstein DS, Ory DS, Marugan J, Sidransky E.

J Neurosci. 2016 Jul 13;36(28):7441-52. doi: 10.1523/JNEUROSCI.0636-16.2016.

7.

Autophagy activation by novel inducers prevents BECN2-mediated drug tolerance to cannabinoids.

Kuramoto K, Wang N, Fan Y, Zhang W, Schoenen FJ, Frankowski KJ, Marugan J, Zhou Y, Huang S, He C.

Autophagy. 2016 Sep;12(9):1460-71. doi: 10.1080/15548627.2016.1187367. Epub 2016 Jun 15.

8.

Novel Cephalosporins Selectively Active on Nonreplicating Mycobacterium tuberculosis.

Gold B, Smith R, Nguyen Q, Roberts J, Ling Y, Lopez Quezada L, Somersan S, Warrier T, Little D, Pingle M, Zhang D, Ballinger E, Zimmerman M, Dartois V, Hanson P, Mitscher LA, Porubsky P, Rogers S, Schoenen FJ, Nathan C, Aubé J.

J Med Chem. 2016 Jul 14;59(13):6027-44. doi: 10.1021/acs.jmedchem.5b01833. Epub 2016 Jun 17.

9.

Evaluating p97 Inhibitor Analogues for Potency against p97-p37 and p97-Npl4-Ufd1 Complexes.

Gui L, Zhang X, Li K, Frankowski KJ, Li S, Wong DE, Moen DR, Porubsky PR, Lin HJ, Schoenen FJ, Chou TF.

ChemMedChem. 2016 May 6;11(9):953-7. doi: 10.1002/cmdc.201600036. Epub 2016 Apr 4.

PMID:
27043824
10.

N-Phenylbenzamides as Potent Inhibitors of the Mitochondrial Permeability Transition Pore.

Roy S, Šileikytė J, Neuenswander B, Hedrick MP, Chung TD, Aubé J, Schoenen FJ, Forte MA, Bernardi P.

ChemMedChem. 2016 Feb 4;11(3):283-8. doi: 10.1002/cmdc.201500545. Epub 2015 Dec 23.

11.

Threading the Needle: Small-Molecule Targeting of a Xenobiotic Receptor to Ablate Escherichia coli Polysaccharide Capsule Expression Without Altering Antibiotic Resistance.

Arshad M, Goller CC, Pilla D, Schoenen FJ, Seed PC.

J Infect Dis. 2016 Apr 15;213(8):1330-9. doi: 10.1093/infdis/jiv584. Epub 2015 Dec 15.

12.

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.

13.

Discovery, Synthesis, and Optimization of Diarylisoxazole-3-carboxamides as Potent Inhibitors of the Mitochondrial Permeability Transition Pore.

Roy S, Šileikytė J, Schiavone M, Neuenswander B, Argenton F, Aubé J, Hedrick MP, Chung TD, Forte MA, Bernardi P, Schoenen FJ.

ChemMedChem. 2015 Oct;10(10):1655-71. doi: 10.1002/cmdc.201500284. Epub 2015 Aug 18.

14.

Advancing Biological Understanding and Therapeutics Discovery with Small-Molecule Probes.

Schreiber SL, Kotz JD, Li M, Aubé J, Austin CP, Reed JC, Rosen H, White EL, Sklar LA, Lindsley CW, Alexander BR, Bittker JA, Clemons PA, de Souza A, Foley MA, Palmer M, Shamji AF, Wawer MJ, McManus O, Wu M, Zou B, Yu H, Golden JE, Schoenen FJ, Simeonov A, Jadhav A, Jackson MR, Pinkerton AB, Chung TD, Griffin PR, Cravatt BF, Hodder PS, Roush WR, Roberts E, Chung DH, Jonsson CB, Noah JW, Severson WE, Ananthan S, Edwards B, Oprea TI, Conn PJ, Hopkins CR, Wood MR, Stauffer SR, Emmitte KA; NIH Molecular Libraries Project Team.

Cell. 2015 Jun 4;161(6):1252-65. doi: 10.1016/j.cell.2015.05.023. Review.

15.

Benzothiazole and Pyrrolone Flavivirus Inhibitors Targeting the Viral Helicase.

Sweeney NL, Hanson AM, Mukherjee S, Ndjomou J, Geiss BJ, Steel JJ, Frankowski KJ, Li K, Schoenen FJ, Frick DN.

ACS Infect Dis. 2015 Mar 13;1(3):140-148.

16.

Simultaneously Targeting the NS3 Protease and Helicase Activities for More Effective Hepatitis C Virus Therapy.

Ndjomou J, Corby MJ, Sweeney NL, Hanson AM, Aydin C, Ali A, Schiffer CA, Li K, Frankowski KJ, Schoenen FJ, Frick DN.

ACS Chem Biol. 2015 Aug 21;10(8):1887-96. doi: 10.1021/acschembio.5b00101. Epub 2015 May 22.

17.

Small Molecules Targeting the Mitochondrial Permeability Transition.

Sileikyte J, Roy S, Porubsky P, Neuenswander B, Wang J, Hedrick M, Pinkerton AB, Salaniwal S, Kung P, Mangravita-Novo A, Smith LH, Bourdette DN, Jackson MR, Aubé J, Chung TDY, Schoenen FJ, Forte MA, Bernardi P.

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].

18.

Design of high-throughput screening assays and identification of a SUMO1-specific small molecule chemotype targeting the SUMO-interacting motif-binding surface.

Alontaga AY, Li Y, Chen CH, Ma CT, Malany S, Key DE, Sergienko E, Sun Q, Whipple DA, Matharu DS, Li B, Vega R, Li YJ, Schoenen FJ, Blagg BS, Chung TD, Chen Y.

ACS Comb Sci. 2015 Apr 13;17(4):239-46. doi: 10.1021/co500181b. Epub 2015 Mar 23.

19.

Potency enhancement of the κ-opioid receptor antagonist probe ML140 through sulfonamide constraint utilizing a tetrahydroisoquinoline motif.

Frankowski KJ, Slauson SR, Lovell KM, Phillips AM, Streicher JM, Zhou L, Whipple DA, Schoenen FJ, Prisinzano TE, Bohn LM, Aubé J.

Bioorg Med Chem. 2015 Jul 15;23(14):3948-56. doi: 10.1016/j.bmc.2014.12.033. Epub 2014 Dec 23.

20.

Inhibitors of the Plasmodium falciparum M17 Leucine Aminopeptidase.

Schoenen FJ, Whipple D, Baillargeon P, Brown CL, Chase P, Ferguson J, Fernandez-Vega V, Hodder P, Mathew R, Neuenswander B, Porubsky P, Rogers S, Skinner-Adams T, Sosa M, Spicer T, To J, Tower NA, Trenholme KR, Wang J, Weiner WS, Aubé J, Rosen H, White EL, Gardiner DL, Dalton JP.

Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2010-.
2013 Dec 12 [updated 2014 Sep 18].

21.

Evaluating p97 inhibitor analogues for their domain selectivity and potency against the p97-p47 complex.

Fang CJ, Gui L, Zhang X, Moen DR, Li K, Frankowski KJ, Lin HJ, Schoenen FJ, Chou TF.

ChemMedChem. 2015 Jan;10(1):52-6. doi: 10.1002/cmdc.201402420. Epub 2014 Nov 6.

22.

Discovery of ML370, an inhibitor of Vibrio cholerae Quorum Sensing Acting via the LuxO response regulator.

Faloon P, Weiner WS, Matharu DS, Neuenswander B, Porubsky P, Youngsaye W, Bennion M, Ng WL, Hurley A, Mosher CM, Johnston S, Dandapani S, Schoenen FJ, Aubé J, Munoz B, Palmer M, Bassler BL, Schreiber SL.

Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2010-.
2013 Apr 12 [updated 2014 Sep 18].

23.

Inhibitors of the Plasmodium falciparum M18 Aspartyl Aminopeptidase.

Schoenen FJ, Weiner WS, Baillargeon P, Brown CL, Chase P, Ferguson J, Fernandez-Vega V, Ghosh P, Hodder P, Krise JP, Matharu DS, Neuenswander B, Porubsky P, Rogers S, Skinner-Adams T, Sosa M, Spicer T, To J, Tower NA, Trenholme KR, Wang J, Whipple D, Aubé J, Rosen H, White EL, Dalton JP, Gardiner DL.

Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2010-.
2013 Apr 12 [updated 2014 Sep 18].

24.

A Small Molecule Inhibitor of the MITF Molecular Pathway.

Faloon PW, Bennion M, Weiner WS, Smith RA, Wurst J, Weiwer M, Hartland C, Mosher CM, Johnston S, Porubsky P, Neuenswander B, Dandapani S, Munoz B, Schoenen FJ, Metkar S, Haq R, Fisher DE, Aubé J, Palmer M, Schreiber SL.

Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2010-.
2012 Dec 13 [updated 2014 Sep 18].

25.

Ebselen inhibits hepatitis C virus NS3 helicase binding to nucleic acid and prevents viral replication.

Mukherjee S, Weiner WS, Schroeder CE, Simpson DS, Hanson AM, Sweeney NL, Marvin RK, Ndjomou J, Kolli R, Isailovic D, Schoenen FJ, Frick DN.

ACS Chem Biol. 2014 Oct 17;9(10):2393-403. doi: 10.1021/cb500512z. Epub 2014 Aug 15.

26.

Specific inhibition of p97/VCP ATPase and kinetic analysis demonstrate interaction between D1 and D2 ATPase domains.

Chou TF, Bulfer SL, Weihl CC, Li K, Lis LG, Walters MA, Schoenen FJ, Lin HJ, Deshaies RJ, Arkin MR.

J Mol Biol. 2014 Jul 29;426(15):2886-99. doi: 10.1016/j.jmb.2014.05.022. Epub 2014 May 27.

27.

Identification of Potent and Selective Inhibitors of the Plasmodium falciparum M18 Aspartyl Aminopeptidase (PfM18AAP) of Human Malaria via High-Throughput Screening.

Spicer T, Fernandez-Vega V, Chase P, Scampavia L, To J, Dalton JP, Da Silva FL, Skinner-Adams TS, Gardiner DL, Trenholme KR, Brown CL, Ghosh P, Porubsky P, Wang JL, Whipple DA, Schoenen FJ, Hodder P.

J Biomol Screen. 2014 Aug;19(7):1107-15. doi: 10.1177/1087057114525852. Epub 2014 Mar 11.

28.

Hepatitis C Virus NS3 Helicase Inhibitor Discovery.

Li K, Frankowski KJ, Hanson AM, Ndjomou J, Shanahan MA, Mukherjee S, Kolli R, Shadrick WR, Sweeney NL, Belon CA, Neuenswander B, Ferguson J, Aubé J, Schoenen FJ, Blagg BSJ, Frick DN.

Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2010-.
2011 Dec 16 [updated 2013 Mar 14].

29.

Benzylmorpholine analogs as selective inhibitors of lung cytochrome P450 2A13 for the chemoprevention of lung cancer in tobacco users.

Blake LC, Roy A, Neul D, Schoenen FJ, Aubé J, Scott EE.

Pharm Res. 2013 Sep;30(9):2290-302. doi: 10.1007/s11095-013-1054-z. Epub 2013 Jun 12.

30.

Primuline derivatives that mimic RNA to stimulate hepatitis C virus NS3 helicase-catalyzed ATP hydrolysis.

Sweeney NL, Shadrick WR, Mukherjee S, Li K, Frankowski KJ, Schoenen FJ, Frick DN.

J Biol Chem. 2013 Jul 5;288(27):19949-57. doi: 10.1074/jbc.M113.463166. Epub 2013 May 23.

31.

Selective, reversible inhibitors of the AAA ATPase p97.

Chou TF, Li K, Nordin BE, Porubsky P, Frankowski K, Patricelli MP, Aubé J, Schoenen FJ, Deshaies R.

Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2010-.
2011 Apr 14 [updated 2013 May 1].

32.

Small-molecule pyrimidine inhibitors of the cdc2-like (Clk) and dual specificity tyrosine phosphorylation-regulated (Dyrk) kinases: development of chemical probe ML315.

Coombs TC, Tanega C, Shen M, Wang JL, Auld DS, Gerritz SW, Schoenen FJ, Thomas CJ, Aubé J.

Bioorg Med Chem Lett. 2013 Jun 15;23(12):3654-61. doi: 10.1016/j.bmcl.2013.02.096. Epub 2013 Mar 30.

33.

Skeletal diversification via heteroatom linkage control: preparation of bicyclic and spirocyclic scaffolds from N-substituted homopropargyl alcohols.

Painter TO, Bunn JR, Schoenen FJ, Douglas JT, Day VW, Santini C.

J Org Chem. 2013 Apr 19;78(8):3720-30. doi: 10.1021/jo400077m. Epub 2013 Apr 1.

34.

Structure-activity relationship study reveals ML240 and ML241 as potent and selective inhibitors of p97 ATPase.

Chou TF, Li K, Frankowski KJ, Schoenen FJ, Deshaies RJ.

ChemMedChem. 2013 Feb;8(2):297-312. doi: 10.1002/cmdc.201200520. Epub 2013 Jan 11.

35.

Fluorescent primuline derivatives inhibit hepatitis C virus NS3-catalyzed RNA unwinding, peptide hydrolysis and viral replicase formation.

Ndjomou J, Kolli R, Mukherjee S, Shadrick WR, Hanson AM, Sweeney NL, Bartczak D, Li K, Frankowski KJ, Schoenen FJ, Frick DN.

Antiviral Res. 2012 Nov;96(2):245-55. doi: 10.1016/j.antiviral.2012.08.006. Epub 2012 Aug 25.

36.

Identification and analysis of hepatitis C virus NS3 helicase inhibitors using nucleic acid binding assays.

Mukherjee S, Hanson AM, Shadrick WR, Ndjomou J, Sweeney NL, Hernandez JJ, Bartczak D, Li K, Frankowski KJ, Heck JA, Arnold LA, Schoenen FJ, Frick DN.

Nucleic Acids Res. 2012 Sep 1;40(17):8607-21. Epub 2012 Jun 27.

37.

Discovery of Small Molecule Kappa Opioid Receptor Agonist and Antagonist Chemotypes through a HTS and Hit Refinement Strategy.

Frankowski KJ, Hedrick MP, Gosalia P, Li K, Shi S, Whipple D, Ghosh P, Prisinzano TE, Schoenen FJ, Su Y, Vasile S, Sergienko E, Gray W, Hariharan S, Milan L, Heynen-Genel S, Mangravita-Novo A, Vicchiarelli M, Smith LH, Streicher JM, Caron MG, Barak LS, Bohn LM, Chung TD, Aubé J.

ACS Chem Neurosci. 2012 Mar 21;3(3):221-236. Epub 2012 Jan 20.

38.

Optimization of potent hepatitis C virus NS3 helicase inhibitors isolated from the yellow dyes thioflavine S and primuline.

Li K, Frankowski KJ, Belon CA, Neuenswander B, Ndjomou J, Hanson AM, Shanahan MA, Schoenen FJ, Blagg BS, Aubé J, Frick DN.

J Med Chem. 2012 Apr 12;55(7):3319-30. doi: 10.1021/jm300021v. Epub 2012 Mar 22.

39.

Reversible inhibitor of p97, DBeQ, impairs both ubiquitin-dependent and autophagic protein clearance pathways.

Chou TF, Brown SJ, Minond D, Nordin BE, Li K, Jones AC, Chase P, Porubsky PR, Stoltz BM, Schoenen FJ, Patricelli MP, Hodder P, Rosen H, Deshaies RJ.

Proc Natl Acad Sci U S A. 2011 Mar 22;108(12):4834-9. doi: 10.1073/pnas.1015312108. Epub 2011 Mar 7.

40.

Ratio encoding combinatorial libraries with stable isotopes and their utility in pharmaceutical research.

Wagner DS, Markworth CJ, Wagner CD, Schoenen FJ, Rewerts CE, Kay BK, Geysen HM.

Comb Chem High Throughput Screen. 1998 Oct;1(3):143-53.

PMID:
10500773
41.

Isotope or mass encoding of combinatorial libraries.

Geysen HM, Wagner CD, Bodnar WM, Markworth CJ, Parke GJ, Schoenen FJ, Wagner DS, Kinder DS.

Chem Biol. 1996 Aug;3(8):679-88.

42.

Design and synthesis of conformationally constrained analogues of 4-(3-butoxy-4-methoxybenzyl)imidazolidin-2-one (Ro 20-1724) as potent inhibitors of cAMP-specific phosphodiesterase.

Brackeen MF, Cowan DJ, Stafford JA, Schoenen FJ, Veal JM, Domanico PL, Rose D, Strickland AB, Verghese M, Feldman PL.

J Med Chem. 1995 Nov 24;38(24):4848-54.

PMID:
7490734
43.

Phosphodiesterase type IV inhibition. Structure-activity relationships of 1,3-disubstituted pyrrolidines.

Feldman PL, Brackeen MF, Cowan DJ, Marron BE, Schoenen FJ, Stafford JA, Suh EM, Domanico PL, Rose D, Leesnitzer MA, et al.

J Med Chem. 1995 Apr 28;38(9):1505-10.

PMID:
7739009

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