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ImQuest Team Presentation
  1. Development of Highly Potent Pyrimidinedione Inhibitors as Topical Microbicides

  2. Comparative Evaluation of Twelve Pyrimidinedione Inhibitors of HIV-1 for Further Preclinical Development

  3. Advanced Preclinical Development of Cyanovirin-N as an Anti-HIV Vaginal Microbicide

  4. Oral Presentation: Comparative Evaluation of Twelve Pyrimidinedione Inhibitors of HIV-1 for Further Preclinical and Clinical Development

  5. Inhibition of Late Stage Events in HIV Replication: Therapeutic Compounds with Effects on Viral RNA Synthesis

  6. In Vitro Strategies for the Inhibition of Sexually Transmitted Diseases: Preclinical Development of Topical Mono- and Combination Microbicide Therapies

  7. Mono- and Combination Therapy Efficacy of Unique Antiviral Agents that Target the HIV-1 Nucleocapsid Protein (NCp7)

  8. Efficacy, Resistance, Fitness and Replication capacity Profiles of Novel Pyrimidinedione Nonnucleoside Inhibitors of HIV-1 and HIV-2
Recently Published Manuscripts by ImQuest BioSciences Staff
  1. Chen, X., Yang, L., Zhang, N., Turpin, J.A., Buckheit, R.W., Osterling, C., Oppenheim, J.J. and Howard, O.M.Z. Shikonin, a component of Chinese herbal medicine, inhibits chemokine receptor function and suppresses human immunodeficiency virus type-1. Antimicrob. Agents Chemother. 47: 2810-2816. 2003.

  2. Novikov, M.S., Ozerov, A.A., Sim, O.G. and Buckheit, R.W., Jr. Synthesis and anti-HIV-1 activity of 2-[[2-(3,5-dimethylphenoxy)ethyl]thio]pyrimidin-4(3H)-ones. Chemistry of Heterocyclic Compounds. 40:37-42. 2004.

  3. Buckheit, R.W., Jr. Understanding HIV resistance, fitness, replication capacity and compensation: targeting viral fitness as a therapeutic strategy. In press. Expert Opin. Investig. Drugs 13: 933-958. 2004.

  4. .Ozerov A.A., Novikov M.S., Gnatjuk V.P., Lobachev A.A., Buckheit R.W. Synthesis and anti-HIV-1 activity of 1-(benzyloxymethyl)-5-(arylamino)uracil derivatives methylated in side chain. Bulletin of Volgograd Scientific Centre of Russian Academy of Medical Sciences.1:26-28. 2004.

  5. Novikov M.S., Sim O.G., Ozerov A.A., Buckheit R.W. Synthesis and antiviral activity of 2-(alkylthio)-5-[2-(aryloxy)ethyl]-6-methylpyrimidine-4(3H)-ones. Bulletin of Volgograd Scientific Centre of Russian Academy of Medical Sciences. 2:30-31. 2004.

  6. Colleluori, D.M., Tien, D., Kang, F., Pagliei, T., Kuss, R., McCormick, T., Watson, K., McFadden, K., Chaiken, I., Buckheit, R.W., Jr. and Romano, J.W. Expression, purification, and characterization of recombinant cyanovirin-N for vaginal anti-HIV microbicide development. Protein Expression and Purification. 39:229-236. 2004.

  7. Mori, T., O’Keefe, B.R., Sowder III, R.C., Bringans, S., Gardella, R., Berg, S., Cochran, P., Turpin, J.A., Buckheit, R.W., Jr., McMahon, J.B. and Boyd, M.R. Isolation and characterization of griffithsin, a novel HIV-inactivating protein from the red algae Griffithsia sp. J. Biol. Chemistry. 280:9345-9353. 2005.

  8. Horvath, A., Tokes, S., Hartman, T., Watson, K., Turpin, J.A., Buckheit, R.W., Jr., Sebesteyen, Z., Szollosi, J., Benko, I., Bardos, T.J., Dunn, J.A., Toth, F.D., Fesus, L. and Aradi, J. Suligovir [(s4dU)35] inhibits HIV-1 entry by targeting CD4 and cell surface thioredoxin. Virology. 334:214-223. 2005.

  9. Novikov, M.S., Ozerov, A.A., Orlova, J.A., Buckheit, R.W., Jr. Synthesis and antiviral properties of 1-{[2-(phenoxy)ethoxy]methyl}uracil derivatives. Chemistry of Heterocyclic Compounds. 5:726-731. 2005.

  10. Tien, D., Schnaare, R.L., Cohl, G., Moench, T., Doncel, G., Watson, K., Buckheit, R.W., Jr., Lewis, M., Mauck, C., Callahan, M., Douville, K. and Romano, J.W. In vitro and in vivo characterization of a potential universal placebo designed for use in vaginal microbicide clinical trials. AIDS Res. Hu. Retrov. 21: 11-19. 2005..

  11. Beer, B.E., Doncel, G.F., Krebs, F.C., Shattock, R., Fletcher, P., Buckheit, R.W., Jr., Watson, K., Dezzutti, C.S., Cummins, J.E., Bromley, E., Richardson-Harman, N., Pallansch, L., Lackman-Smith, C., Ostreling, C., Mankowski, M., Miller, S.R., Catalone, B.J., Welsh, P.A., Howett, M.K., Wigdahl, B., Turpin, J.A. and Reichelderfer, P. In vitro preclinical testing of nonoxynol-9 as potential anti-human immunodeficiency virus microbicide: a retrospective analysis of results from five laboratories. Antimicrob. Agents Chemother. 50:713-723. 2006.
Works in Progress Involving ImQuest BioSciences Staff

  1. Deng, B.L., Cullen, M.D., Zhou, Z., Hartman, T.L., Buckheit, R.W., Jr., Pannecouque, C., DeClercq, E., Fanwick, P.E. and Cushman, M. Synthesis and anti-HIV activity of new alkenyldiarylmethane (ADAM) non-nucleoside reverse transcriptase inhibitors (NNRTIs) incorporating benzoxazolone and benzisoxazole rings. In press. 2005.

  2. Srivastava, P., Hara, T., Fattah, R.J., Schito, M., Hartman, T., Buckheit, R.W., Jr., Turpin, J.A., Inman, J.K., and Appella, E. Optimization of unique thioesters as antiviral agents that target HIV-1 nucleocapsid protein (NCp7). Submitted. 2005.

  3. Schito, M.L., Hartman, T., Soloff, A.C., Fattah, R.J., Slovitz, D., Trichel, A., Inman, J., Buckheit, R.W., Jr., Appella, E. and Barratt-Boyes, S.M. Zinc finger inhibitor targeting human immunodeficiency virus nucleocapsid is virucidal in the nonhuman primate model. Submitted. 2005.

  4. José A. Fernández-Romero, Mitchell Thorn, Kanani Titchen, Kristin Sudol, Jifan Li, Robin A Maguire, Robert W. Buckheit Jr, Tracy L. Hartman, David M Phillips Carrageenan/MIV-150 (PC-815), a combination microbicide. Submitted. 2005.

  5. Turpin, J.A., Loftus, T.L., Watson, K., Kwon, H-S., Lee, S-H., Lee, J-W., Kang, D-W., Chung, S-G., Cho, E-H., and Buckheit, R.W., Jr. The structure-activity relationships of 2,4 (1H, 3H)-pyrimidinedione derivatives as potent human immunodeficiency virus inhibitors. To be submitted.

  6. Buckheit, R.W., Jr., Palmer, S., Fliakas-Boltz, V., Russell, J., Hartman, T.L., Watson, K., Chung, S-G and Cho, E-H. SJ-3366 rapidly selects for resistant strains of HIV-1 and HIV-2 with reduced sensitivity to virus entry and reverse transcriptase inhibition. To be submitted.

  7. Buckheit, R.W., Jr., Watson, K., Hartman, T.L., Chung, S-G., Cho, E-H, and Turpin, J.A. SJ-3366 inhibits virus entry through interaction with a post-attachment intermediate. To be submitted.

  8. Hartman, T.L., Turpin, J.A. and Buckheit, R.W., Jr. Effect of NNRTI-resistance engendering mutations on viral fitness. To be submitted.

  9. Buckheit, R.W., Jr. Considerations in the Development of Anti-HIV Therapeutics and Microbicides: Preclinical Drug Development Challenges. Commissioned by Expert Opin. Investig. Drugs 2006.
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