Recent Publications

Recent Publications:




Shoemaker, R.H., Halliday, S. Fletcher, T., Buckheit, R. and Sausville, E.A. Characterization of a quantitative PCR-based assay for agents active against human herpesvirus 8. In preparation.


Huang, M., Buckheit, R.W.,Jr., Turpin, J.A., and Rice, W.G., Identification of a benzoylmethylindolepyridinium derivative as a broadly antiretroviral nonnucleoside reverse transcriptase inhibitor. In preparation.




Kodihalli, S. D. Kobasa and R.G. Webster: Strategies for inducing protection against avian influenza A subtypes with DNA vaccines. (In press Vaccine)


Garcia, A.C., De Clerq, E., Pannecouque, C., Witvrouw, M., Stup, T.L.,Turpin, J.A., Buckheit, R.W., Jr. and Cushman, M. Synthesis and anti-HIV activity of cosalane analogs incorporating nitrogen in the linker chain. Submitted. 1999.


Stoddart, C.A., Moreno, M.E., Linquist-Stepps, V.D., Bare, C., Bogan, M.R., Gobbi, A., Buckheit, R.W., Jr., Bedard, J., Rando, R.F., and McCune, J.M. Antiviral activity of dOTC (BCH-10652) against 3TC-resistant human immunodeficieny virus type 1 in SCID-hu thy/liv mice. Submitted. 1999.


Quan, Y., Motakis, D., Buckheit, R.W., Jr., Xu, Z.Q.,. Flavin, M.T., Parniak, M.A. and Wainberg, M.A. Sensitivity and resistance to (+)-calanolide A of wild type and mutated forms of HIV-1 reverse transcriptase. Antiviral Therapy. In press. 1999.


Halliday, S.M., Russell, J.D., Osterling, M.C. and Buckheit, R.W., Jr. Therapeutic Potential of the phosphorothioate oligonucleotide ISIS 5320: Topical and combination anti-HIV use. Submitted. 1999.


Morningstar, M.L., Roth, T., Kroeger Smith, M., Zajac, M., Watson, K.,Buckheit, R.W., Jr. and Michejda, C.J. Synthesis and biological activity of potent non-nucleoside inhibitors of HIV-1 reverse transcriptase that retain activity against mutant forms of the enzyme. Submitted. 1999.


Huang, M., Buckheit, R.W., Jr., Turpin, J.A. and Rice, W.G. Identification of a benzoylmethylindolepyridinium (BMIP) derivative as a broadly antiretroviral nonnucleoside reverse transcriptase inhibitor. Submitted. 1999.


Xu, Ze-Qi, Buckheit, R.W., Jr., Stup, T.L., Flavin, M.T., Khilevich, A., Lin, L. and Zembower, D.E. In vitro anti-human immunodeficiency virus (HIV) activity of the chromanone derivative, 12-oxocalanolide A, a novel NNRTI. In press. 1999


Rice, W.G., Schaeffer, C.A., Summers, M.F., Turpin, J.A., Huang, M.and Buckheit, R.W., Jr. Identification of an inhibitor of the human immunodeficiency virus nucleocapsid protein zinc finger as a candidate for usage as a topical microbicide to prevent sexual transmission. Submitted. 1999.


Lewis, MG, Yalley-Ogunro, J, Greenhouse, JJ, Brennan, TP, Bo Jiang, J, Vancott, TC, Lu, YC, Eddy, GA and Birx, BL. Limited Protection from a Pathogenic Chimeric Simian-Human Immunodeficiency Virus Challenge Following Immunization with Attenuated Simian Immunodeficiency Virus. J. Virol. 73:1262-1270, 1999


Mascola, JR, Lewis, MG, Stiegler, G, Harris, D, VanCott, TC, Louder, M, J, Brown, CR, Sapan, CV, Frankel, S, Robb, M, Lu, YC, Katinger, H and Birx, D. Protection of macaques against SHIV-89.6p by passive transfer of neutralizing antibodies. J. Virol. 73:4009-4018, 1999


Buckheit, R.W., Jr., White, E.L., Fliakas-Boltz, V., Russell, J., Stup, T.L., Kinjerski, T.L., Osterling, M.C., Weigand, A. and Bader, J.P. Unique anti-human immunodeficiency virus activity of the nonnucleoside reverse transcriptase inhibitors calanolide A, costatolide and dihydrocostatolide. Antimicrobial Agents Chemoth. 43:1827-1834. 1999.


Buckheit, R.W., Jr., Russell, J.D., Pallansch, L.A. and Driscoll, J.S. Anti-HIV-1 Activity of 2’-fluoro-2’,3’-dideoxyarabinosyladenine (F-ddA) used in combination with other mechanistically diverse inhibitors of HIV-1 replication. Antiviral Chem.Chemotherapy. 10:115-119. 1999.


Ruell, J.A., De Clerq, E., Pannecouque, C., Witvrouw, M., Stup, T.L.,Turpin, J.A., Buckheit, R.W., Jr. and Cushman, M. Synthesis and anti-HIV activity of cosalane analogs with substituted benzoic acid rings attached to the pharmacophore through methylene and amide linkers. J.Org. Chem. 64: 5858-5866. 1999.


Zaharevitz, D.W., Gussio, R., Jalluri, R., Patabiraman, P., Pallansch, L.A., Weigand, A. and Buckheit, R.W., Jr. Combination of 3D database searching and 3D QSAR in the discovery of novel inhibitors of HIV-1 reverse transcriptase. Manuscript in preparation. 1999.


Yang, S., Buckheit, R.W., Jr., Cragg, G.M., Bader, J.P., McCloud, T., Clanton, D., Boyd, M.R., Newman, D. and Sauseville, E.A. Natural product based anti-HIV drug discovery. Manuscript in preparation. 1999.


Casimiro-Garcia, A., Micklatcher, M., Turpin, J.A., Stup, T.L., Watson, K., Buckheit, R.W., Jr. and Cushman, M. Novel modifications in the alkenyldiarylmethane (ADAM) series of nonnucleoside reverse transcriptase inhibitors. Submitted. 1999.


Turpin, J. A., Song, Y., Inman, J. K., Huang, M., Wallqvist, A., Maynard, A., Covell, D.G., Rice, W.G., and Appella, E. Synthesis and biological properties of novel pyridinioalkanoyl thiolesters (PATE) as anti-HIV-1 agents that target the viral nucleocapsid protein zinc fingers. J. Med. Chem.42: 67. 1999.


Cushman, M., S. Insaf, G. Paul, E. De Clercq, D. Schols, C. Pannccouque, M. Witrouw, C. A. Schaeffer, J. A. Turpin and W. G. Rice. Extension of the polyanionic cosalane pharmacophore as a strategy for increasing anti-HIV potency. J. Med. Chem. 42: 1767. 1999.


Lin, Z., N. Neamati, N, Kiryu, Y., J. A. Turpin, C. Aberham, K. Strebel, K. Kohn, W. G. Rice, Y. Pommier and T. R. Burke, Jr. Chicoric acid analogues as HIV-1 integrase inhibitors. J. Med. Chem. 42:1401, 1999.


Howard, O. M. Z., A.-K. Shirakawa, Turpin, J.A., A. Maynard, G. J. Tobin, M. Carrington, J. J. Oppenheim and M. Dean. Naturally occurring CCR5 Extracellular and transmembrane domain variants affect HIV-1 co-receptor and ligand binding function. J. Biol. Chem. 274:16228. 1999.


Garcia, A. C., E. de Clerq, C. Pannecouque, M. Witvrouw, T. L. Stup, J. A. Turpin, R. W. Buckheit, Jr. and M. Cushman. Synthesis and anti-HIV activity of cosalane analogs with substitute benzoic acid rings attached to. 1999.


Turpin, J. A., S. J. Terpening, C. Schaeffer, K. Williamson, C. Palamone, L. Graham and W. G. Rice. Prolonged loss of HIV-1 infectivity after treatment of productively infected monocyte/macrophages (Mo/M) with a retroviral zinc finger inhibitor. J. Virol. Submitted. 1999.


Neamati, N., Lin, Z., H. E. Winslow, H. Zhao, J. A. Turpin, C. Aberham, A. Orr, K. Strebel, W. G. Rice, T. R. Burke, Jr., and Y. Pommier. Design and synthesis of novel HIV-1 integrase inhibitors with antiviral activity: a remarkable metal-dependent inhibition of HIV-1 integrase by salicylhydrazides. J. Med. Chem. Submitted. 1999.


Neamati, N., J. A. Turpin, H. E. Winslow, J. L. Christensen, K. Williamson, A. Orr, W. G. Rice, and Y. Pommier. Thiazolothiazepine inhibitors of HIV-1 integrase. J. Med. Chem. Submitted. 1999.


Govorkova, E.A., S. Kodihalli, I.V. Alymova, B. Fanget and R.G. Webster: Growth and immunogenicity of influenza viruses cultivated in Vero, MDCK cells and embryonated chicken eggs. Brown, F. Robertson, J.S. and J.M. Woods. (eds) Inactivated Influenza Vaccine prepared in Cell Culture. Dev. Biol. Stand Basel, Karger, Vol 98, pp 39-51, 1999.


Kodihalli, S. H. Goto, D. Kobasa, S. Krauss, Y. Kawaoka, and R.G. Webster: DNA vaccine encoding hemagglutinin provides protective immunity in mice against H5N1 influenza virus. J.Virol. 73:2094-2098, 1999.


Kobasa, D., S. Kodihalli, M. Luo, M. R. Castrucci, I. Donatelli, Y. Suzuki, T. Suzuki and Y. Kawaoka: Amino acid residues contributing to the substrate specificity of the influenza A virus neuraminidase. J. Virol. 73: 6743-51, 1999.


Buckheit, R.W., Jr., Lackman-Smith, C., Snow, M.J., Halliday, S.M., Agrawal, V.K. and Broom, A.D. PMTI, a broadly active unusual single stranded polyribonucleotide, inhibits HIV replication by two distinct mechanisms. Antiviral Chem.Chemotherapy. In press. 1999.


Turpin, J.A., Young, S., Inman, J., Huang, M., Whalqvist, A., Maynard, A., Covell, D.G., Rice, W.G., and Appella, E., Synthesis and biological properties of novel pyridinioalkanoyl thiolesters (PATE) as anti-HIV-1 agents that target the viral nucleocapsid protein zinc fingers. J. Med Chem 42: 67-86. 1999




White, E.L., Rose, L.M., Allan, P.W., Buckheit, R.W., Jr., Shannon, W.M. and Secrist, J.A., III. Polyamine pools in human immunodeficiency virus infected cells. J. Acq. Immunodef. Syndromes and Human Retrov. 17:101-103. 1998.


Cushman, M., Casimiro-Garcia, A., Hejchman, E., Ruell, J.A., Huang, M., Schaeffer, C.A., Willimson, K., Rice, W.G. and Buckheit, R.W., Jr. New alkenyldiarylmethanes with enhanced potencies as anti-HIV agents which act as non-nucleoside reverse transcriptase inhibitors. J. Med. Chem. 41:2076-2089. 1998.


Turpin, J.A., Buckheit, R.W., Jr., Derse, D., Hollingshead, M., Williamson, K., Palamone, C., Osterling, M.C., Hill, S.A., Graham, L., Schaeffer, C.A., Bu, M., Huang, M., Cholody, W.M., Michejda, C.J., and Rice, W.G. Inhibition of acute, latent and chronic phase HIV-1 replication by a bistriazoloacridone analog that selectively inhibits HIV-1 transcription. Antimicrob. Agents Chemother. 42:487-494. 1998.


Rininger, J.A., Miller, S.B., Ma, X., Chigurpati, P., Calabreses, C., Standish, L., Wells, K., Steadle-Foster, L., Buckheit, R.W., Jr. and Babish, J.G. Preliminary, open-label, safety and efficacy study of the novel kinase inhibitor andrographolide in asymptomatic human immunodeficiency virus-infected individuals. Submitted. 1998.


Tutonda, M.G., Buckheit, R.W., Jr., Agrawal, V.K. and Broom, A.D. Antiviral oligo and polyribonucleotides containing selected triazol[2,3-a] purines. J. Med. Chem. 41:4958-4964. 1998.


O’Keefe, B.R., Erim, T., Beutler, J.A., Cardellina, J.H. III, Gulakowski, R.J., Krepps, B.L., McMahon, J.B., Sowder, R.C. II, Johnson, D.G.,Buckheit, R.W., Jr., Stup, T.L. and Boyd, M.R. Isolation and characterization of adociavirin, a novel HIV-inhibitory protein from the sponge Adocia sp. FEBS Letter. 431:85-90. 1998.


Howard, O.M.Z., Oppenheim, J.J., Hollingshead, M.G., Covey, J.M., Bigelow, J., McCormack, J.J., Buckheit, R.W., Jr., Clanton, D.J.,Turpin, J.A. and Rice, W.G. Inhibition of in vitro and in vivo HIV replication by a distamycin analog that interferes with chemokine receptor function: A candidate for chemotherapeutic and microbicidal application. J. Med. Chem. 41:2184. 1998.


Langlois, AJ, Desrosiers, RC, Lewis, MG, KewalRamani, VN, Littman, DR, Zhou, JY, Manson, K, Wyand, MS, Bolognesi, DP and Montefori, DC. Neutralizing antibodies in sera form macaques immunized with attenuated simian immunodeficiency virus. J. Virol. 72:6950-6955, 1998.


Huang, M., Zensen, R., Cho, M., and Martin, M. Construction and characterization of a temperature sensitive human immunodeficiency virus type 1 reverse transcriptase mutant. J. Virol. 72:2047-54. 1998


Huang, M., Turpin, J.A., Graham, L. , Janini, G.M., Covell, D.G., Maynard, A., and Rice, W.G. Selectivity of anti-HIV agents for the nucleocapsid zinc finger protein and not other zinc finger proteins. J. Med. Chem. 41:1371-1381. 1998


Cushman, M., Casimiro-Garcia, A., Hejchman, E., Ruell, J.A., Huang,M., Williamson, K., Rice, W.G., Buckheit, R.W.,Jr. New Alkenyldiarylmethanes (ADAMS) with enhanced potencies as anti- HIV agents which act as non-nucleoside reverse transcriptase inhibitors. J Med Chem 41:2076-89. 1998.


Maynard, A., Huang, M., Rice, W.G., and Covell, D.G. Reactivity of the HIV-1 NCp7 zinc finger domains from the perspective of density-functional theory. PNAS, 95:11578-11583. 1998


Palmer, S., Alaeus, A., Albert, J. and Cox, S. Drug Susceptibility of Subtypes A, B, C, D, and E Human Immunodeficiency Virus Type 1 Primary Isolates. AIDS Res. Hum. Retroviruses 14(2): 157-162. 1998.


Shafer, R. W., Winters, M. A., Palmer, S., and Merigan, T. C. Multiple concurrent reverse transcriptase and protease mutations and multidrug resistance in HIV-1 isolates from heavily treated HIV-1 infected patients. Ann. Intern. Med. 128(11) 1998.


Palmer, S. Rationalizing salvage therapy. GMHC Treatment Issues 12(6) 1998.


Palmer, S., Shafer, R. and Merigan, T. C. Highly drug-resistant human immunodeficiency virus type 1 clinical isolates are cross-resistant to many antiretroviral compounds in current clinical development. AIDS “submitted” 1998.


Palmer, S., Shafer, R. and Merigan, T. C. Both nucleoside and nucleotide analogs are potentiated by hydroxyurea against drug-susceptible and drug-resistant HIV isolates. Antimicrob. Agents Chemother. “submitted” 1998.


Palmer, S., Shafer, R. and Merigan, T. C. New drug combinations against highly drug resistant HIV isolates in Vitro. Manuscript in progress. 1998.


Gong, W., O. M. Z. Howard, J. A. Turpin, M. C. Grimm, H. Ureda, P. Gray, C. J. Raport, J. J. Oppenheimer, and J. M. Wang. Monocyte chemotactic protein (MCP)-2 activates CCR5 and blocks CD4/CCR5-mediated HIV-1 entry/replication. J. Biol. Chem. 273:4289. 1998.


Huang, M., J. A. Turpin, A. Maynard, L. Graham, G. M. Janini, D. G. Covell and W. G. Rice. Anti-HIV agents that selectively target retroviral nucleocapsid protein zinc fingers without affecting cellular zinc finger proteins. J. Med Chem. 41:1371.1998


Howard, O. M. Z., T. Korte, N. Tarasova, M. Grimm, J. A. Turpin, W. G. Rice, C. J. Michejda, R. Blumenthal and J. J. Oppenheim. Small molecule inhibitor of HIV-1 cell fusion blocks chemokine receptor mediated function. J. Leukocyte Biol. 64:6. 1998.


Montefiori, DC, Reimann, KA, Wyand, MS, Manson, K, Lewis, MG, Collman, RG, Sodroski, JA, Bolognesi, DP and Letvin, NL. Neutralizing antibody responses in macaques infected with chimeric simian-human immunodeficiency virus (SHIV) containing the envelope glycoprotein of either a laboratory-adapted variant or primary isolate of human immunideficiency virus type 1. J. Virol.72:3427-3431, 1998


Alymova, I.V., S. Kodihalli, E.A Govorkova, B. Fanget, C. Gerdil, and R.G. Webster: Immunogenicity and Protective efficacy in mice of influenza B vaccines grown in mammalian cells or embryonated chicken eggs. J.Virol. 72:4472-4477, 1998.


Shortridge, K.F. N.N. Zhou, P. Gao, T. Ito, Y. Kawaoka, S. Kodihalli, S. Krauss, D. Markwell, K. G. Murti, M. Morwood, D. Senne, L. Sims, A. Takada, Yi. Guan and Robert G. Webster. Characterization of avian H5N1 influenza viruses from poultry in Hong Kong. Virology. 331-342. 1998.