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Items: 1 to 50 of 60

1.

Targeting CDK9 Reactivates Epigenetically Silenced Genes in Cancer.

Zhang H, Pandey S, Travers M, Sun H, Morton G, Madzo J, Chung W, Khowsathit J, Perez-Leal O, Barrero CA, Merali C, Okamoto Y, Sato T, Pan J, Garriga J, Bhanu NV, Simithy J, Patel B, Huang J, Raynal NJ, Garcia BA, Jacobson MA, Kadoch C, Merali S, Zhang Y, Childers W, Abou-Gharbia M, Karanicolas J, Baylin SB, Zahnow CA, Jelinek J, Graña X, Issa JJ.

Cell. 2018 Nov 15;175(5):1244-1258.e26. doi: 10.1016/j.cell.2018.09.051. Epub 2018 Oct 25.

PMID:
30454645
2.

Design and synthesis of functionalized piperazin-1yl-(E)-stilbenes as inhibitors of 17α-hydroxylase-C17,20-lyase (Cyp17).

Blass BE, Iyer P, Abou-Gharbia M, Childers WE, Gordon JC, Ramanjulu M, Morton G, Arumugam P, Boruwa J, Ellingboe J, Mitra S, Reddy Nimmareddy R, Paliwal S, Rajasekhar J, Shivakumar S, Srivastava P, Tangirala RS, Venkataramanaiah K, Bobbala R, Yanamandra M, Krishnakanth Reddy L.

Bioorg Med Chem Lett. 2018 Jul 15;28(13):2270-2274. doi: 10.1016/j.bmcl.2018.05.040. Epub 2018 May 22.

PMID:
29803730
3.

Novel inhibitors of Staphylococcus aureus RnpA that synergize with mupirocin.

Lounsbury N, Eidem T, Colquhoun J, Mateo G, Abou-Gharbia M, Dunman PM, Childers WE.

Bioorg Med Chem Lett. 2018 Apr 1;28(6):1127-1131. doi: 10.1016/j.bmcl.2018.01.022. Epub 2018 Jan 31.

PMID:
29463447
4.

A Mitochondrial-targeted purine-based HSP90 antagonist for leukemia therapy.

Bryant KG, Chae YC, Martinez RL, Gordon JC, Elokely KM, Kossenkov AV, Grant S, Childers WE, Abou-Gharbia M, Altieri DC.

Oncotarget. 2017 Dec 11;8(68):112184-112198. doi: 10.18632/oncotarget.23097. eCollection 2017 Dec 22.

5.

Design, synthesis and SAR of new-di-substituted pyridopyrimidines as ATP-competitive dual PI3Kα/mTOR inhibitors.

Al-Ashmawy AAK, Ragab FA, Elokely KM, Anwar MM, Perez-Leal O, Rico MC, Gordon J, Bichenkov E, Mateo G, Kassem EMM, Hegazy GH, Abou-Gharbia M, Childers W.

Bioorg Med Chem Lett. 2017 Jul 15;27(14):3117-3122. doi: 10.1016/j.bmcl.2017.05.044. Epub 2017 May 15.

PMID:
28571824
6.

Nuclear Magnetic Resonance Structure of the Human Polyoma JC Virus Agnoprotein.

Coric P, Saribas AS, Abou-Gharbia M, Childers W, Condra JH, White MK, Safak M, Bouaziz S.

J Cell Biochem. 2017 Oct;118(10):3268-3280. doi: 10.1002/jcb.25977. Epub 2017 May 3.

7.

Design, synthesis, and evaluation of (2S,4R)-Ketoconazole sulfonamide analogs as potential treatments for Metabolic Syndrome.

Blass BE, Iyer P, Abou-Gharbia M, Childers WE, Gordon JC, Ramanjulu M, Morton G, Arumugam P, Boruwa J, Ellingboe J, Mitra S, Nimmareddy RR, Paliwal S, Rajasekhar J, Shivakumar S, Srivastava P, Tangirala RS, Venkataramanaiah K, Yanamandra M.

Bioorg Med Chem Lett. 2016 Dec 1;26(23):5825-5829. doi: 10.1016/j.bmcl.2016.10.016. Epub 2016 Oct 10.

PMID:
27789139
8.

12/15-Lipoxygenase Inhibition Reverses Cognitive Impairment, Brain Amyloidosis, and Tau Pathology by Stimulating Autophagy in Aged Triple Transgenic Mice.

Di Meco A, Li JG, Blass BE, Abou-Gharbia M, Lauretti E, Praticò D.

Biol Psychiatry. 2017 Jan 15;81(2):92-100. doi: 10.1016/j.biopsych.2016.05.023. Epub 2016 Jun 4.

PMID:
27499089
9.

Resistance to BET Bromodomain Inhibitors Is Mediated by Kinome Reprogramming in Ovarian Cancer.

Kurimchak AM, Shelton C, Duncan KE, Johnson KJ, Brown J, O'Brien S, Gabbasov R, Fink LS, Li Y, Lounsbury N, Abou-Gharbia M, Childers WE, Connolly DC, Chernoff J, Peterson JR, Duncan JS.

Cell Rep. 2016 Aug 2;16(5):1273-1286. doi: 10.1016/j.celrep.2016.06.091. Epub 2016 Jul 21.

10.

Emerging From the Unknown: Structural and Functional Features of Agnoprotein of Polyomaviruses.

Saribas AS, Coric P, Hamazaspyan A, Davis W, Axman R, White MK, Abou-Gharbia M, Childers W, Condra JH, Bouaziz S, Safak M.

J Cell Physiol. 2016 Oct;231(10):2115-27. doi: 10.1002/jcp.25329. Epub 2016 Feb 24. Review. Erratum in: J Cell Physiol. 2016 Dec;231(12):2789.

11.

Targeting Calcium Signaling Induces Epigenetic Reactivation of Tumor Suppressor Genes in Cancer.

Raynal NJ, Lee JT, Wang Y, Beaudry A, Madireddi P, Garriga J, Malouf GG, Dumont S, Dettman EJ, Gharibyan V, Ahmed S, Chung W, Childers WE, Abou-Gharbia M, Henry RA, Andrews AJ, Jelinek J, Cui Y, Baylin SB, Gill DL, Issa JP.

Cancer Res. 2016 Mar 15;76(6):1494-505. doi: 10.1158/0008-5472.CAN-14-2391. Epub 2015 Dec 30.

12.

Heterocyclic chalcone activators of nuclear factor (erythroid-derived 2)-like 2 (Nrf2) with improved in vivo efficacy.

Lounsbury N, Mateo G, Jones B, Papaiahgari S, Thimmulappa RK, Teijaro C, Gordon J, Korzekwa K, Ye M, Allaway G, Abou-Gharbia M, Biswal S, Childers W Jr.

Bioorg Med Chem. 2015 Sep 1;23(17):5352-9. doi: 10.1016/j.bmc.2015.07.056. Epub 2015 Jul 29.

PMID:
26278028
13.

Small-molecule inhibitors of Staphylococcus aureus RnpA-mediated RNA turnover and tRNA processing.

Eidem TM, Lounsbury N, Emery JF, Bulger J, Smith A, Abou-Gharbia M, Childers W, Dunman PM.

Antimicrob Agents Chemother. 2015 Apr;59(4):2016-28. doi: 10.1128/AAC.04352-14. Epub 2015 Jan 20.

14.

Pharmacologic blockade of 12/15-lipoxygenase ameliorates memory deficits, Aβ and tau neuropathology in the triple-transgenic mice.

Chu J, Li JG, Giannopoulos PF, Blass BE, Childers W, Abou-Gharbia M, Praticò D.

Mol Psychiatry. 2015 Nov;20(11):1329-38. doi: 10.1038/mp.2014.170. Epub 2015 Jan 6.

PMID:
25560760
15.

Nuclear magnetic resonance structure revealed that the human polyomavirus JC virus agnoprotein contains an α-helix encompassing the Leu/Ile/Phe-rich domain.

Coric P, Saribas AS, Abou-Gharbia M, Childers W, White MK, Bouaziz S, Safak M.

J Virol. 2014 Jun;88(12):6556-75. doi: 10.1128/JVI.00146-14. Epub 2014 Mar 26. Erratum in: J Virol. 2014 Sep;88(18):11000.

16.

Estrogen receptor antagonists are anti-cryptococcal agents that directly bind EF hand proteins and synergize with fluconazole in vivo.

Butts A, Koselny K, Chabrier-Roselló Y, Semighini CP, Brown JC, Wang X, Annadurai S, DiDone L, Tabroff J, Childers WE Jr, Abou-Gharbia M, Wellington M, Cardenas ME, Madhani HD, Heitman J, Krysan DJ.

MBio. 2014 Feb 11;5(1):e00765-13. doi: 10.1128/mBio.00765-13.

17.

Discovery of innovative therapeutics: today's realities and tomorrow's vision. 2. Pharma's challenges and their commitment to innovation.

Abou-Gharbia M, Childers WE.

J Med Chem. 2014 Jul 10;57(13):5525-53. doi: 10.1021/jm401564r. Epub 2014 Feb 7.

PMID:
24428137
18.

Synthesis and evaluation of Strychnos alkaloids as MDR reversal agents for cancer cell eradication.

Munagala S, Sirasani G, Kokkonda P, Phadke M, Krynetskaia N, Lu P, Sharom FJ, Chaudhury S, Abdulhameed MD, Tawa G, Wallqvist A, Martinez R, Childers W, Abou-Gharbia M, Krynetskiy E, Andrade RB.

Bioorg Med Chem. 2014 Feb 1;22(3):1148-55. doi: 10.1016/j.bmc.2013.12.022. Epub 2013 Dec 21.

PMID:
24405813
19.

Essential roles of Leu/Ile/Phe-rich domain of JC virus agnoprotein in dimer/oligomer formation, protein stability and splicing of viral transcripts.

Sami Saribas A, Abou-Gharbia M, Childers W, Sariyer IK, White MK, Safak M.

Virology. 2013 Aug 15;443(1):161-76. doi: 10.1016/j.virol.2013.05.003. Epub 2013 Jun 6.

20.

A novel assay platform for the detection of translation modulators of spermidine/spermine acetyltransferase.

Perez-Leal O, Abou-Gharbia M, Gordon J, Childers WE, Merali S.

Curr Pharm Des. 2014;20(2):245-52.

21.

Discovery of innovative therapeutics: today's realities and tomorrow's vision. 1. Criticisms faced by the pharmaceutical industry.

Abou-Gharbia M, Childers WE.

J Med Chem. 2013 Jul 25;56(14):5659-72. doi: 10.1021/jm400330j. Epub 2013 Apr 29.

PMID:
23557017
22.

Design and synthesis of 2-aminothiazole based antimicrobials targeting MRSA.

Annadurai S, Martinez R, Canney DJ, Eidem T, Dunman PM, Abou-Gharbia M.

Bioorg Med Chem Lett. 2012 Dec 15;22(24):7719-25. doi: 10.1016/j.bmcl.2012.09.095. Epub 2012 Oct 3.

PMID:
23116888
23.

A new and efficient synthetic route for the anxiolytic agent CL285032.

Ghidu VP, Ilies MA, Cullen T, Pollet R, Abou-Gharbia M.

Bioorg Med Chem Lett. 2011 Jan 1;21(1):259-61. doi: 10.1016/j.bmcl.2010.11.017. Epub 2010 Nov 5.

PMID:
21095124
24.

β-lactamase inhibitors display anti-seizure properties in an invertebrate assay.

Rawls SM, Karaca F, Madhani I, Bhojani V, Martinez RL, Abou-Gharbia M, Raffa RB.

Neuroscience. 2010 Sep 15;169(4):1800-4. doi: 10.1016/j.neuroscience.2010.06.041. Epub 2010 Jun 23.

25.

The synthesis and biological evaluation of quinolyl-piperazinyl piperidines as potent serotonin 5-HT1A antagonists.

Childers WE Jr, Havran LM, Asselin M, Bicksler JJ, Chong DC, Grosu GT, Shen Z, Abou-Gharbia MA, Bach AC 3rd, Harrison BL, Kagan N, Kleintop T, Magolda R, Marathias V, Robichaud AJ, Sabb AL, Zhang MY, Andree TH, Aschmies SH, Beyer C, Comery TA, Day M, Grauer SM, Hughes ZA, Rosenzweig-Lipson S, Platt B, Pulicicchio C, Smith DE, Sukoff-Rizzo SJ, Sullivan KM, Adedoyin A, Huselton C, Hirst WD.

J Med Chem. 2010 May 27;53(10):4066-84. doi: 10.1021/jm1000908.

PMID:
20443629
26.

Begacestat (GSI-953): a novel, selective thiophene sulfonamide inhibitor of amyloid precursor protein gamma-secretase for the treatment of Alzheimer's disease.

Martone RL, Zhou H, Atchison K, Comery T, Xu JZ, Huang X, Gong X, Jin M, Kreft A, Harrison B, Mayer SC, Aschmies S, Gonzales C, Zaleska MM, Riddell DR, Wagner E, Lu P, Sun SC, Sonnenberg-Reines J, Oganesian A, Adkins K, Leach MW, Clarke DW, Huryn D, Abou-Gharbia M, Magolda R, Bard J, Frick G, Raje S, Forlow SB, Balliet C, Burczynski ME, Reinhart PH, Wan HI, Pangalos MN, Jacobsen JS.

J Pharmacol Exp Ther. 2009 Nov;331(2):598-608. doi: 10.1124/jpet.109.152975. Epub 2009 Aug 11.

PMID:
19671883
27.

Comparison of human and rat uterine leiomyomata: identification of a dysregulated mammalian target of rapamycin pathway.

Crabtree JS, Jelinsky SA, Harris HA, Choe SE, Cotreau MM, Kimberland ML, Wilson E, Saraf KA, Liu W, McCampbell AS, Dave B, Broaddus RR, Brown EL, Kao W, Skotnicki JS, Abou-Gharbia M, Winneker RC, Walker CL.

Cancer Res. 2009 Aug 1;69(15):6171-8. doi: 10.1158/0008-5472.CAN-08-4471. Epub 2009 Jul 21.

28.

Prodrugs of perzinfotel with improved oral bioavailability.

Baudy RB, Butera JA, Abou-Gharbia MA, Chen H, Harrison B, Jain U, Magolda R, Sze JY, Brandt MR, Cummons TA, Kowal D, Pangalos MN, Zupan B, Hoffmann M, May M, Mugford C, Kennedy J, Childers WE Jr.

J Med Chem. 2009 Feb 12;52(3):771-8. doi: 10.1021/jm8011799.

PMID:
19146418
29.

Discovery of innovative small molecule therapeutics.

Abou-Gharbia M.

J Med Chem. 2009 Jan 8;52(1):2-9. doi: 10.1021/jm8012823. No abstract available.

PMID:
19072120
30.

Discovery of begacestat, a Notch-1-sparing gamma-secretase inhibitor for the treatment of Alzheimer's disease.

Mayer SC, Kreft AF, Harrison B, Abou-Gharbia M, Antane M, Aschmies S, Atchison K, Chlenov M, Cole DC, Comery T, Diamantidis G, Ellingboe J, Fan K, Galante R, Gonzales C, Ho DM, Hoke ME, Hu Y, Huryn D, Jain U, Jin M, Kremer K, Kubrak D, Lin M, Lu P, Magolda R, Martone R, Moore W, Oganesian A, Pangalos MN, Porte A, Reinhart P, Resnick L, Riddell DR, Sonnenberg-Reines J, Stock JR, Sun SC, Wagner E, Wang T, Woller K, Xu Z, Zaleska MM, Zeldis J, Zhang M, Zhou H, Jacobsen JS.

J Med Chem. 2008 Dec 11;51(23):7348-51. doi: 10.1021/jm801252w.

PMID:
19012391
31.

Enhanced clearance of Abeta in brain by sustaining the plasmin proteolysis cascade.

Jacobsen JS, Comery TA, Martone RL, Elokdah H, Crandall DL, Oganesian A, Aschmies S, Kirksey Y, Gonzales C, Xu J, Zhou H, Atchison K, Wagner E, Zaleska MM, Das I, Arias RL, Bard J, Riddell D, Gardell SJ, Abou-Gharbia M, Robichaud A, Magolda R, Vlasuk GP, Bjornsson T, Reinhart PH, Pangalos MN.

Proc Natl Acad Sci U S A. 2008 Jun 24;105(25):8754-9. doi: 10.1073/pnas.0710823105. Epub 2008 Jun 16.

32.

Binding of rapamycin analogs to calcium channels and FKBP52 contributes to their neuroprotective activities.

Ruan B, Pong K, Jow F, Bowlby M, Crozier RA, Liu D, Liang S, Chen Y, Mercado ML, Feng X, Bennett F, von Schack D, McDonald L, Zaleska MM, Wood A, Reinhart PH, Magolda RL, Skotnicki J, Pangalos MN, Koehn FE, Carter GT, Abou-Gharbia M, Graziani EI.

Proc Natl Acad Sci U S A. 2008 Jan 8;105(1):33-8. Epub 2007 Dec 27.

33.

Desvenlafaxine succinate: A new serotonin and norepinephrine reuptake inhibitor.

Deecher DC, Beyer CE, Johnston G, Bray J, Shah S, Abou-Gharbia M, Andree TH.

J Pharmacol Exp Ther. 2006 Aug;318(2):657-65. Epub 2006 May 4.

PMID:
16675639
34.

Lecozotan (SRA-333): a selective serotonin 1A receptor antagonist that enhances the stimulated release of glutamate and acetylcholine in the hippocampus and possesses cognitive-enhancing properties.

Schechter LE, Smith DL, Rosenzweig-Lipson S, Sukoff SJ, Dawson LA, Marquis K, Jones D, Piesla M, Andree T, Nawoschik S, Harder JA, Womack MD, Buccafusco J, Terry AV, Hoebel B, Rada P, Kelly M, Abou-Gharbia M, Barrett JE, Childers W.

J Pharmacol Exp Ther. 2005 Sep;314(3):1274-89. Epub 2005 Jun 10.

PMID:
15951399
35.

Synthesis and biological evaluation of benzodioxanylpiperazine derivatives as potent serotonin 5-HT(1A) antagonists: the discovery of Lecozotan.

Childers WE Jr, Abou-Gharbia MA, Kelly MG, Andree TH, Harrison BL, Ho DM, Hornby G, Huryn DM, Potestio L, Rosenzweig-Lipson SJ, Schmid J, Smith DL, Sukoff SJ, Zhang G, Schechter LE.

J Med Chem. 2005 May 19;48(10):3467-70.

PMID:
15887953
36.

Tiplaxtinin, a novel, orally efficacious inhibitor of plasminogen activator inhibitor-1: design, synthesis, and preclinical characterization.

Elokdah H, Abou-Gharbia M, Hennan JK, McFarlane G, Mugford CP, Krishnamurthy G, Crandall DL.

J Med Chem. 2004 Jul 1;47(14):3491-4.

PMID:
15214776
37.

Design, synthesis, and biological evaluation of thio-containing compounds with serum HDL-cholesterol-elevating properties.

Elokdah H, Sulkowski TS, Abou-Gharbia M, Butera JA, Chai SY, McFarlane GR, McKean ML, Babiak JL, Adelman SJ, Quinet EM.

J Med Chem. 2004 Jan 29;47(3):681-95.

PMID:
14736248
38.

Design, synthesis, and preclinical characterization of novel, highly selective indole estrogens.

Miller CP, Collini MD, Tran BD, Harris HA, Kharode YP, Marzolf JT, Moran RA, Henderson RA, Bender RH, Unwalla RJ, Greenberger LM, Yardley JP, Abou-Gharbia MA, Lyttle CR, Komm BS.

J Med Chem. 2001 May 24;44(11):1654-7. No abstract available.

PMID:
11356100
39.

Design, synthesis, SAR, and biological evaluation of highly potent benzimidazole-spaced phosphono-alpha-amino acid competitive NMDA antagonists of the AP-6 type.

Baudy RB, Fletcher H 3rd, Yardley JP, Zaleska MM, Bramlett DR, Tasse RP, Kowal DM, Katz AH, Moyer JA, Abou-Gharbia M.

J Med Chem. 2001 May 10;44(10):1516-29.

PMID:
11334562
40.

The preclinical pharmacological profile of WAY-132983, a potent M1 preferring agonist.

Bartolomeo AC, Morris H, Buccafusco JJ, Kille N, Rosenzweig-Lipson S, Husbands MG, Sabb AL, Abou-Gharbia M, Moyer JA, Boast CA.

J Pharmacol Exp Ther. 2000 Feb;292(2):584-96.

PMID:
10640295
41.

Synthesis and SAR of adatanserin: novel adamantyl aryl- and heteroarylpiperazines with dual serotonin 5-HT(1A) and 5-HT(2) activity as potential anxiolytic and antidepressant agents.

Abou-Gharbia MA, Childers WE Jr, Fletcher H, McGaughey G, Patel U, Webb MB, Yardley J, Andree T, Boast C, Kucharik RJ Jr, Marquis K, Morris H, Scerni R, Moyer JA.

J Med Chem. 1999 Dec 16;42(25):5077-94.

PMID:
10602693
42.

Discovery of a highly potent, functionally-selective muscarinic M1 agonist, WAY-132983 using rational drug design and receptor modelling.

Sabb AL, Husbands GM, Tokolics J, Stein RP, Tasse RP, Boast CA, Moyer JA, Abou-Gharbia M.

Bioorg Med Chem Lett. 1999 Jul 19;9(14):1895-900.

PMID:
10450949
43.

New generation dopaminergic agents. 2. Discovery of 3-OH-phenoxyethylamine and 3-OH-N1-phenylpiperazine dopaminergic templates.

Mewshaw RE, Husbands M, Gildersleeve ES, Webb MB, Shi X, Mazandarani H, Cockett MI, Ochalski R, Brennan JA, Abou-Gharbia M, Marquis K, McGaughey GB, Coupet J, Andree TH.

Bioorg Med Chem Lett. 1998 Feb 3;8(3):295-300.

PMID:
9871673
44.
45.

New generation dopaminergic agents. 1. Discovery of a novel scaffold which embraces the D2 agonist pharmacophore. Structure-activity relationships of a series of 2-(aminomethyl)chromans.

Mewshaw RE, Kavanagh J, Stack G, Marquis KL, Shi X, Kagan MZ, Webb MB, Katz AH, Park A, Kang YH, Abou-Gharbia M, Scerni R, Wasik T, Cortes-Burgos L, Spangler T, Brennan JA, Piesla M, Mazandarani H, Cockett MI, Ochalski R, Coupet J, Andree TH.

J Med Chem. 1997 Dec 19;40(26):4235-56.

PMID:
9435894
46.

New antihistamines: substituted piperazine and piperidine derivatives as novel H1-antagonists.

Abou-Gharbia M, Moyer JA, Nielsen ST, Webb M, Patel U.

J Med Chem. 1995 Sep 29;38(20):4026-32.

PMID:
7562938
47.

Synthesis and structure-activity relationship of substituted tetrahydro- and hexahydro-1,2-benzisothiazol-3-one 1,1-dioxides and thiadiazinones: potential anxiolytic agents.

Abou-Gharbia M, Moyer JA, Patel U, Webb M, Schiehser G, Andree T, Haskins JT.

J Med Chem. 1989 May;32(5):1024-33.

PMID:
2565399
48.
49.

Antipsychotic activity of substituted gamma-carbolines.

Abou-Gharbia M, Patel UR, Webb MB, Moyer JA, Andree TH, Muth EA.

J Med Chem. 1987 Oct;30(10):1818-23.

PMID:
2888898
50.

Psychotropic agents: synthesis and antipsychotic activity of substituted beta-carbolines.

Abou-Gharbia M, Patel UR, Moyer JA, Muth EA.

J Med Chem. 1987 Jun;30(6):1100-5.

PMID:
2884314

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