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Magid Abou-Gharbia, Ph.D., FRSC

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Magid Abou-Gharbia, Ph.D., FRSC Abou-Gharbia PUBLICATIONS: 1. “Pharmacology of COR-003 (Levoketoconazole), an Investigational Treatment for Endogenous Cushing’s Syndrome, Ruth Thieroff-Ekerdt, Philip Lavin, Magid Abou-Gharbia, Fredric Cohen, Clinical Pharmacology in Drug Development, in press 2. “Design, Synthesis and Evaluation of (2S,4R)-ketoconazole-Sulfon-amid- Analogs as Potential Treatment for metabolic syndrome”, Benjamin E Blass, Pravin Iyer, Magid Abou-Gharbia, Wayne W Childers, John C Gordon, Mercy Ramanjulu, George Morton, Premkumar Arumugam, Joshodeep Boruwa, John Ellingboe, Sayan Mitra, Rajashekar Reddy Nimmareddy, Shalini Paliwal, Jamallamudi Rajasekhar, Savithiri Shivakumar, Pratima Srivastava, Raghuram S. Tangirala, Konda Venkataramanaiah, and Mahesh Yanamandra, Bioorg.MedChem Let., in press 3. “12/15-lipoxygenase Inhibition Reverses Cognitive Impairment, Brain Amyloidosis, and Tau Pathology by Stimulating Autophagy in Aged triple- transgenic mice, Antonio Di Meco, Jian-Guo Li; Benjamin E. Blass.; Magid Abou-Gharbia, Elizabeth Lauretti and Domenico Pratico, Biological Psychiatry, 2016, 1-9. 4. “Emerging from the unknown: Structural and functional features of agnoprotein of polyomaviruses”, A. S. Saribas, P. Coric, A. Hamazaspyan, W. Davis, R. Axman, M. K. White, M. Abou-Gharbia, W. Childers, J. H. condra, S. Bouaziz and M. Safak, J. Cell Physiol. 2016, 231, 2115-2127. 5. “Targeting calcium signaling to induce epigenetic reactivation of tumor suppressor genes in cancer, Noël J.-M. Raynal, Justin Lee, Youjun Wang, Judith Garriga, Gabriel Malouf, Sarah Dumont, Elisha J Dettman, Vazganush Gharibyan, Saira Ahmed, Woonbok Chung, Wayne E. Childers, Magid Abou-Gharbia, Ryan A. Henry, Andrew J. Andrews5, Jaroslav Jelinek, Stephen B. Baylin6, Don Gill2, and Jean-Pierre J. Issa, Cancer Research. 2015, 76, 1494-1505. 6. “Novel inhibitors of Staphylococcus aureus RnpA that synergize with mupirocin”, N. Lounsbury, T. Eidem, G. Mateo, M. Abou-Gharbia, P. M. Dunman and W. E. Childers, Bioorganic and Medicinal Chemistry Letters, 2015, 59, 2016-2028 7. “Heterocyclic chalcone activators of nuclear factor (erythroid-derived 2)-like 2 (Nrf2) with improved in vivo efficacy”, N. Lounsbury, G. Mateo, B. Jones, S. Papaiahgari, R. K. Thimmulappa, C. Teijaro, J. Gordon, K. Korzekwa, M. Ye, G, Allaway, M. Abou-Gharbia, S. Biswal and W. E. Childers, Jr. Bioorg. Med. 08/19/2016 Page 1 Magid Abou-Gharbia, Ph.D., FRSC Chem. 2015, 23 (17): 3552-9. (Impact Factor: 2.793). 8. Pharmacologic blockade of 12/15-lipoxygenase ameliorates memory deficits, Aβ and tau neuropathology in the triple-transgenic mice, Chu, J.; Li, J.-G.; Giannopoulos, P. F.; Blass, B. E.; Childers, W.; Abou-Gharbia, M.; Pratico, D. Molecular Psychiatry, 2015, 1-10. 9. Small-Molecule inhibitors of Staphylococcus aureus RnpA-Mediated RNA Turnover and rRNA Processing, T.E. Eidem, N. Lounsbury, J. F., Emery, J. Bulger, A. Smith, M. Abou-Gharbia, W. Childers and P. M. Dunmann , Antimicrob. Agents Chemother., 59:4, 2015, 2016-2028. 10. “Discovery of first-in- class therapeutics-Venlafaxine(Effexor), desvenlafaxine(pristiq), temsirolimus(Torisel), ILS-920 and gemtuzumab ozogamicin(Mylotarg), Magid Abou-Gharbia, HMJ 2014; 4:317-332. 11. “Unleashing the power of Semi-Synthesis: The Discovery of Toresil”, J.S. Skotnicki and M. Abou-Gharbia, in Orphan Drugs and Rare Diseases, Editors: David C Pryde, Michael J Palmer, RSC Publisher, 2014, 347-366. 12. “ 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 15;88(12):6556-75. doi: 10.1128/JVI.00146-14. Epub 2014 Mar 26. 13. “Estrogen receptor antagonists are anti-cryptococcal agents that directly bind EF-hand proteins and synergize with fluconazole in vivo”, Arielle Butts, Kristy Koselny, Yeissa Chabrier-Rosello, Camille P. Semighini, Jessica C.S. Brown, Xuying Wang, Sivakumar Annadurai, Louis DiDone, Julie Tabroff, Wayne E. Childers, Jr., Magid Abou-Gharbia, Melanie Wellington, Maria E. Cardenas, Hiten D. Madhani, Joseph Heitman and Damian J. Krysan, m Bio , February 2014,Volume 5(1),e 00765-13. 14. “Discovery of Innovative Therapeutics: Today’s Realities and Tomorrow’s Vision. 2. Pharma Challenges and their Commitment to Innovation,” M. Abou- Gharbia, W. Childerss, J.Med.Chem, 2014, 57, 5525-5553 15. “Synthesis and Evaluation of Strychnos Alkaloids as MDR Reersal Agents for Cancer Cell Eradication”, Gopal Sirasani, Surendrachary Munagala, Manali Phadke, Natalkia Krynetskaia, Frances Sharom, Disshartha Chaudhury, Gregory Tawa, Wayne Childers, Magid Abou-Gharbia, Evgeny Krynetskiy, and Rodrigo B. Andrade, Bioorganic & Med Chem. , 2014, 22, 1148-1155. 16. “A Novel Assay Platform for the Detection of Translation Modulators of Spirmidine/Spermine Acetyl transferase”, Oscar Perez-Leal, Magid Abou- Gharbia, John Gordon, Wayne Childers and Salim Merali, Current Pharmaceutical Design, 2014, 20: 245-255. 08/19/2016 Page 2 Magid Abou-Gharbia, Ph.D., FRSC 17. “Synthesis of rapamycin glycoconjugates via a CuAAC-based approach”, Lisa Moni , Alberto Marra, Jerauld S. Skotnicki, Frank E. Koehn , Magid Abou-Gharbia Alessandro Dondoni, Tetrahedron.Lett., 54 (2013)6999-7003 18. “Discovery of Innovative Therapeutics: Today’s Realities and Tomorrow’s Vision. 1. Criticisms Faced by the Pharmaceutical industry,” M. Abou- Gharbia, W. Childerss, J.Med.Chem, 2013, 56(14), 5659-5672. 19. “Essential roles of Leu/Ile/Phe-rich domain of JC virus agnoprotein in dimer/oligomer formation protein stability and splicing of viral transcripts”, A. Sami Saribas, Magid Abou Gharbia, Wayne Childers, Ilker K. Sariyer, Martyn K. White and Mahmut Safak , Virology, 2013, 443(1), 161-76. 20. “Targeting Neurodegenerative Diseases: Drug Discovery in a Challenging Arena”, M. Abou-Gharbia and W. Childers, Pure and Applied Chemistry, 2012, 84, 1543-1556 21. “Design and synthesis of 2-aminothiazole based antimicrobials targeting MRSA”, Annadurai, S., Martinez, R., Canney, DJ, Eidem, T,, Dunman, PM., Abou-Gharbia, M, Biorg Med Chem Lett, 2012 Dec 15;22(24):7719-25. PMID: 23116888 22. “A new and efficient synthetic route for the anxiolytic agent CL285032,” V.P. Ghidu, M.A. Ilies, T. Cullen, R.Pollet and M. Abou-Gharbia, Bioorg. Med. Chem. Lett,(1): 259-61(2011). 23. “The Synthesis and Biological Evaluation of Quinolyl-piperazinyl Piperidines as Potent Serotonin 5-HT1A Antagonists”Wayne E. Childers, Jr., Lisa M. Havran, Magda Asselin, James J. Bicksler, Dan C. Chong, George T. Grosu, Zongqi Shen, Magid A. Abou-Gharbia, et al. J. Med. Chem. 53, 4066-4084 (2010); PMID: 20443629 24. “Beta-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; (PMID: 20600649) 25. M. A. Abou-Gharbia and W. E. Childers, The Discovery of Effexor® and Pristiq®, in “Analogue-Based Drug Discovery II, J. Fischer and C. R. Ganellin, eds., Wiley-VCH Verlag GmbH & Co., KgaA, Weinheim, 2010, pp. 507-524. 26. “Begacestat (GSI-953): A Novel, Selective Thiophene Sulfonamide Inhibitor of Amyloid Precursor Protein ɣ-Secretase for the Treatment of Alzheimer’s Disease”, R. L. Martone, H. Zhou, K. Atchison, T. Comery, J. Z. Xu, X. Huang, X. Gong, M. Jin, A. Kreft, B. Harrison, S.C. Mayer, S. Aschmies, C. Gonzales, M.M. Zaleska, D.R. Riddell, E. Wagner, P.Lu, S.C. Sun, 08/19/2016 Page 3 Magid Abou-Gharbia, Ph.D., FRSC J.Sonnenberg-Reines, A. Oganesian, K. Adkins, M. Leach, D.W. Clarke, D. Huryn, M. Abou-Gharbia, R. Magdola, J. Bard, G. Frick, S. Raje, S.B. Forlow, C. Balliet, M.E. Burczynski, J.Pharm.Exp. Ther., 331(2), 598-608 (2009) 27. Comparison of Human and Rat Uterine Leiomyomata: Identification of a Dysregulated mTOR Pathway” J. S. Crabtree, S. A. Jelinsky, H. A. Harris, S. E. Choe, M. M. Cotreau, M.L. Kimberland, E. Wilson2, K. A. Saraf, W. Liu, A. S. McCampbell, B. Dave, R. R. Broaddus, E. L. Brown, W. Kao, J.S. Skotnicki, M. Abou-Gharbia, R. C. Winneker, and C. L. Walker , Cancer Research, 69 (15):6171-8 (2009). 28. “Prodrug of Perzinfotel with improved oral Bioavailability”, R.B. Baudy, J. A. Butera, M. Abou-Gharbia, C. Chen, B. Harrison, U. jain, R. Magolda,J.Y. Sze, M.R. Brandt,T.A. Cummons, D. Kowal, M.N. Pangalos, B. Zupan, M. Hoffmann, M. May, C.Mugford, J. Kennedy and W. Childers, J.Med.Chem., 52(3): 771-8 (2009). 29. “Discovery of Innovative Small Molecule Therapeutics”, M. Abou-Gharbia, J.Med.Chem, 52(1): 2-9 (2009) 30. “Discovery of Begacestat, a notch-1-Sparing gamma Secretase Inhibitor for the treatment of Alzheimer’s Disease”, S.C.Mayer, A.F. Kreft, B.Harrison, M. Abou-Gharbia, M. Antane, S. Aschmies, K. Atchison, M.Chlenov, D.C. Cole, T. Comery, G. Diamantidis, J. Ellingboe, K. Fan, R. Galante, C. Gonzales, D. M. Ho, M.E. Hoke, Y. Hu, D. Huryn, U. Jain, M. Jin, K. Kremer, D. Kubrak, M. Lin, P. Lu, R. Magolda, R. Martone, W.Moore, A. Oganesian, M.N. Pangalos, A. Porte, P. Reinhart, L. Resnick, D.R. Riddell, J. Sonnenberg-Reines, J.R. Stock, S-C Sun, E. Wagner, T. Wang, K. Woller, Z. Xu, M.M. Zaleska, J.Zeldis, M. Zhang, H. Zhou, and J. S. Jacobsen, J. Med. Chem., 2008, 51 (23), pp 7348–7351 31. “Enhanced Clearance of Aβ in Bran by Sustaining the Plasmin Proteolysis Cascade,” J. S. Jacobsen, T.A. Comery, R. L. Martone, H. Elokdah, D. L. Crandall, A. Organesian, S.Aschmies, Y. Kirksey, C. Gonzales, J. Zu, H. Zhou, K. Atchison, E. Wagner, M. M. Zaleska, I. Das, R.L. Arias, J. Bard, D. Riddell, S. J. Gardell, M.A. Abou-Gharbia, A. Robichaud, R. Magolda, G. P. Vlasuk, T. Bjornsson, P. H. Reinhart, and M. N. Pangalos, Proc. Natl. Acad. Sci.105:8754-8759 (2008). 32. “Binding of Rapamycin Analogs to Calcium Channels and FKBP52 contributes to their neuroprotective activities,” B.
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