Publications
Novel preclinical models of topical PrEP and pharmacodynamics provide rationale for sutained intravaginal ring delivery of microbicide combinations.
Mesquita, P.M., Srinivasan, P., Johnson, T.J., Rastogi, R., Evans-Strickfaden, T., Kay, M.S., Buckheit, K.W., Buckheit, R.W., Jr., Smith, J.M., Kiser, P.F. and Herold, B.C., 2013
In vitro and ex vivo evaluations of transdermal delivery of the HIV inhibitor IQP-0410.
Ham, A.S., Lustig, W., Yang, L., Boczar, A., Buckheit, K.W., and Buckheit, R.W., Jr., 2013.
The Continuing Evolution of HIV Therapy: Identification and Development of Novel Antiretroviral Agents Targeting Viral and Cellular Targets
T.L. Hartman and R.W. Buckheit Jr., Molecular Biology International, 2012.
Selection and characterization of viruses resistant to the dual-acting pyrimidinedione entry and nonnucleoside reverse transcriptase inhibitor IQP-0410.
Buckheit, R.W., Jr., Buckheit, K.W., Sturdevant-Buckheit, C., and Buckheit, R.W., III., 2013.
Development of a combination microbicide gel formulation containing IQP-0528 and tenofovir for the prevention of HIV infection.
Ham, A.S., Ugaonkar, S.R., Shi, D., Buckheit, K.W., Lakougna, H., Nagaraja, U., Gwozdz, G., Goldman, L., Kiser, P.F. and Buckheit, R.W., Jr., 2012.
Safe and sustained vaginal delivery of pyrimidinedione HIV-1 inhibitors from polyurethane rings.
Johnson, T., Srinivasan, P., Albright, T., Buckheit, K.W., Rabe, L., Martin, A., Otten, R., McNicholl, J., Buckheit, R.W., Jr., Smith, J. and Kiser, P. 56:1291-1299. 2012.
Safety and efficacy of tenofovir / IQP-0528 combination gels - a dual compartment microbicide for HIV-1 prevention.
Dezzutti, C.S., Shetler, C., Mahalingham, A., Ugaonkar, S.R., Gwozdz, G., Buckheit, K.W. and Buckheit, R.W., Jr., 2012.
Synthesis and anti-HIV activities of symmetrical dicarboxylate esters of dinucleotide reverse transcriptase inhibitors.
Agarwal, H.K., Buckheit, K.W., Buckheit, R.W., Jr. and Parang, K., 22: 5451-5454. 2012.
Vaginal film drug delivery of the pyrimidinedione IQP-0528 for the prevention of HIV infection.
Ham AS, Rohan LC, Boczar A, Yang L, W Buckheit K, Buckheit RW Jr. Pharm Res. 2012 Jul;29(7):1897-907.
The Continuing Evolution of HIV-1 Therapy: Identification and Development of Novel Antiretroviral Agents Targeting Viral and Cellular Targets.
Hartman, T.L. and Buckheit, R.W., Jr., doi:10.1155/2012/401965, Molecular Biology International, vol. 2012, Article ID 401965., 17 pages, 2012.
Factors Important to the Prioritization and Development of Successful Topical Microbicides for HIV-1
Buckheit, K.W. and Buckheit, R.W., Jr., doi:10.1155/2012/781305, Molecular Biology International, vol. 2012, Article ID 781305, 12 pages, 2012.
Development of a combination microbicide gel formulation containing IQP-0528 and tenefovir for the prevention of HIV infection.
Ham AS, Ugaonkar SR, Shi L, Buckheit KW, Lakougna H, Nagaraja U, Gwozdz G, Goldman L, Kiser PF, Buckheit RW Jr. J Pharm Sci. 2012 Apr;101(4):1423-35.
De novo design of antiviral and antibacterial peptides with varying loop structures.
Wang, G., Buckheit, K.W., Mishra, B., Lushnikova, T. and Buckheit, R.W., Jr., J. AIDS Clinic Res. S2:003. Doi: 10.4172/2156-6113. 2011.
Identification of novel human immunodeficiency virus type 1 inhibitory peptides based on the antimicrobial peptide database.
Wang, G., Watson, K.M., Peterkofsky, A. and Buckheit, R.W., Jr., 54: 1343-1346. 2010.
Antiviral interactions of highly potent 2,4 (1H, 3H)-pyrimidinedione congeners and other anti-HIV agents.
Hartman, T.L., Yang, L., and Buckheit, R.W., Jr., 92: 505-508. 2011.
Antiviral Interactions of Combinations of Highly Potent 2,4 (1H, 3H)-Pyrimidinedione Congeners and Other Anti-HIV Agents
T.L. Hartman, L. Yang and R.W. Buckheit, Jr., Antiviral Research, 2011. 92: p.505-8.
Development of dual-acting pyrimidinediones as novel and highly potent topical anti-HIV microbicides.
Buckheit, K.W., Yang, L. and Buckheit, R.W., Jr., 55: 5243-5254. 2011.
Enzymatic triggered release of the HIV-1 entry inhibitor from prostate specific antigen degradable microparticles.
Enzymatic triggered release of the HIV-1 entry inhibitor from prostate specific antigen degradable microparticles.
Vaginal microbicide gel for delivery of IQP-0528, a pyrimidinedione analog with a dual mechanism of action against HIV-1.
Mahalingham, A., Simmons, A.P., Ugaonkar, S.R., Watson, K.M., Dezzutti, C.S., Rohan, L.C., Buckheit, R.W., Jr. and Kiser, P.F., 55: 1650-1660. 2011.
An Investigation of Phenylthiazole Antiflaviviral Agents.
Mayhoub A.S., Khaliq M., Botting C, Li Z., Kuhn RJ., and Cushman M. 2011. Biorganic & Medicinal Chemistry. 2011 Jun 15; 19(12): 3845-54
Design, Synthesis, and Biological Evaluation of Thiazoles Targeting Flavivirus Envelope Protein.
Mayhoub A.S., Khaliq M., Kuhn RJ., and Cushman M. Journal of Medicinal Chemistry. 2011 Mar 24; 54(6): 1704-14
Binaphthyl-based dicationic peptoids with therapeutic potential.
Bremner, J.B., Keller, P.A., Pyne, S.G., Boyle, T.P., Brkic, Z., David, D.M., Garas, A., Morgan, J., Rbertson, M., Somphol, K., Miller, M.H., Howe, A.S., Ambrose, P., Bhavnani, S., Fritsche, T.R., Biedenbach, D.J., Jones, R.N., Buckheit, R.W., Jr., Watson, K.M., Baylis, D., Coates, J.A., Deadman, J., Jeevarajah, D., McCracken, A. and Rhodes, D.I., 49: 537-540. 2010.
Development of hexadecyloxypropyl tenofovir (CMX 157) for the treatment of infection caused by wild type and nucleoside/nucleotide-resistant HIV.
Lanier, E.R., Ptak, R.G., Lampert, B.M., Keilholz, L., Hartman, T., Buckheit, R.W., Jr., Mankowski, M.K., Osterling, M.C., Almond, M.R., Painter, G.R., Antimicrob Agents Chemother, 54:2901-2909. 2010.
Inhibition of human immunodeficiency virus type 1 by triciribine involves the accessory protein Nef.
Ptak, R.G., Gentry, B.G., Hartman, T.L., Watson, K.M., Osterling, M.C., Buckheit, R.W., Jr., Townsend, L.B. and Drach, J.C., 54: 1512-1519. 2010.
Development of gfstopical microbicides to prevent the sexual transmission of HIV.
Buckheit, R.W., Jr., Watson, K.M, Morrow, K. and Ham, A., Antiviral Res. 85: 142-158. 2010.
Multivalent binding oligomers inhibit HIV Tat-Tar interaction critical for viral replication.
Multivalent binding oligomers inhibit HIV Tat-Tar interaction critical for viral replication.
Inhibition of Human Immunodeficiency Virus Type 1 by Triciribine Involves the Accessory Protein Nef.
R.G. Ptak, B.G. Gentry, T.L. Hartman, K.M. Watson, M.C. Osterling, R.W. Buckheit, Jr., L.B. Townsend, and J.C. Drach, Antimicrobical Agents and Chemotherapy, 2010. 54(4): p.1512-9.
Development of topical microbicides to prevent the sexual transmission of HIV
Buckheit RW, Watson KM, Morrow KM, Ham AS. Antiviral Research 2010 85(1):142-58.
Crystallographic study of a novel sub-nanomolar inhibitor provides insight on the binding interactions of alkenylydiarylmethanes with human immunodeficiency virus-1 (HIV-1) reverse transcriptase.
Cullen, M.D., Ho, W.C., Bauman, J.D., Das, K., Arnold, E., Hartman, T., Watson, K., Buckheit, R.W., Jr., Pannecouque, C., DeClerq, E. and Cushman, M., J. Med. Chem. 52: 6467-6473. 2009.
1-Benzoyl Derivatives of 5-(Arylamino)uracils as anti-HIV-1 and Anti-EBV agents.
Novikov, M.S., Buckheit, R.W., Jr., Temburnikar, K., Khandazhinskaya, A.L., Ivanov, A.V., Seley-Radtke, K.L., Bioorg Med Chem 18: 8310-8314. 2010.
Synthesis of alkenyldiarylmethanes (ADAMs) containing the benzo[d]isoxazole and oxazolidin-2-one rings, a new series of potent non-nucleoside HIV-1 reverse transcriptase inhibitors.
Deng, B-L., Zhao, Y., Hartman, T.L., Watson, K., Buckheit, R.W., Jr., Pannecouque, C., De Clercq, E. and Cushman, M. - Eur. J. Med. Chem. 44: 1210-1214. 2009
Review: Novel targets of HIV therapy.
Greene, W.C., Debyser, Z., Ikeda, Y., Freed, E.O., Stephens, E., Yonemoto, W., Buckheit, R.W., Jr., Este, J.A., and Cihlar, T. - Antiviral Research. 80: 251-265. 2008.
Anti-HIV-1 activity of antimicrobial peptides derived from human and bovine cathelicidins.
Wang, G., Watson, K.M., and Buckheit, R.W., Jr. - Antimicrob. Agents Chemother. 52:3438-3440. 2008.
Comparative evaluation of virus tansmission inhibition by dual-acting pyrimidinedione microbicides using the microbicide transmission and sterilization assay (MTSA). Electronic publication ahead of print.
Watson, K.M., Buckheit, C.E. and Buckheit, R.W., Jr. - Antimicrob. Agents Chemother. 2008.
Investigation of the alkenyldiarylmethane non-nucleoside reverse transcriptase inhibitors as potential cAMP phosphodiesterase-4B2 inhibitors.
Cullen, M.D., York-Fong, C., Houslay, M., Hartman, T.L., Watson, K.M., Buckheit, R.W., Jr., Pannecouque, C., DeClercq, E. and Cushman, M. - Bioorg. Med. Chemistry Letters. 18: 1530-1533. 2008.
Development of a comprehensive human immunodeficiency virus type-1 screening algorithm for discovery and preclinical testing of topical microbicides.
Lackman-Smith, C., Osterling, C., Luckenbaugh, K., Mankowski, M., Snyder, B., Lewis, G., Paull, J., Profy, A., Ptak, R., Buckheit, R.W., Jr., Watson, K.M., Cummins, J.E. and Sanders-Beer, B.E. - Antimicrob. Agents Chemother. 52: 1768-1781. 2008.
Inhibition of tubulin polymerization by select alkenyldiarylmethanes.
Cullen, M.D., Hamel, E., Hartman, T.L., Watson, K.M., Buckheit, R.W., Jr., Pannecouque, C., De Clercq, E. and Cushman, M. - Bioorg. Med. Chemistry 18:469-473. 2008.
Comparative evaluation of the inhibitory activity of a series of pyrimidinedione congeners which inhibit both HIV-1 and HIV-2.
Buckheit, R.W., Jr., Hartman, T.L., Watson, K.M., Chung, S-G. and Cho, E-H. - Antimicrobial Agents Chemother. 52: 225-236. 2008.
Synthesis and biological evaluation of alkenyldiarylmethane HIV-1 non-nucleoside reverse transcriptase inhibitors that possess increased hydrolytic stability.
Cullen, M., Deng, B.L., Hartman, T., Watson, K. Buckheit, R.W., Jr., Pannecouque, C., DeClercq, E. and Cushman, M. - J. Med. Chem. 50:4854-4867. 2007.
Synthesis and Anti-HIV Activity of New Metabolically Stable Alkenyldiarylmethane Non-Nucleoside Reverse Transcriptase Inhibitors (NNRTIs) Incorporating N-Methoxy Imidoyl Halide and 1,2,4-Oxadiazole Systems.
Sakamoto, T., Cullen, MD, Hartman, TL, Watson, KM, Buckheit, RW, Jr., Pannecouque, C. and De Clercq, E. and Cushman, M. - J. Med. Chem. 50: 3314-3321. 2007.
The structure-activity relationships of 2,4 (1H, 3H)-pyrimidinedione derivatives as potent human immunodeficiency virus type-1 and type-2 inhibitors.
Buckheit, R.W., Jr., Hartman, T.L., Watson, K., Kwon, H-S., Lee, S-H., Lee, J-W., Kang, D-W., Chung, S-G., Cho, E-H. - Antiviral Chemistry and Chemotherapy, 18: 259-275. 2007.
Synthesis, biological activity, and crystal structure of potent nonnucleoside inhibitors of HIV-1 reverse transcriptase that retain activity against mutant forms of the enzyme.
Morningstar, M.L., Roth, T., Farnsworth, D.W., Kroeger-Smith, M., Watson, K., Buckheit, R.W., Jr., Das, K., Zhang, W., Arnold, E., Julias, J.G., Hughes, S.H. and Michejda, C.J. - J. Med. Chem. 50: 4003-4015. 2007.
Carrageenan/MIV-150 (PC-815), a combination microbicide.
Fernández-Romero, JA, Thorn, M, Turville, SG, Titchen, K, Sudol, K., Li, J., Maguire, RM, Buckheit R.W., Jr, Hartman, T.L., and Phillips, D.M. - Sex Transm. Dis. 34: 9-14. 2007.
Total synthesis of Anibamine, a novel natural product as a chemokine receptor CCR5 antagonist.
Li, G., Watson, K., Buckheit, R.W. and Zhang, Y. - Organic Letters. 9: 2043-2046. 2007.
Replacement of the metabolically labile methyl esters in the alkenyldiarylmethane series of non-nucleoside reverse transcriptase inhibitors with isoxazolone, oxazolone, or cyano substituents.
Deng, B.L., Hartman, T.L., Buckheit, R.W., Jr., Pannecouque, C., DeClercq, E. and Cushman, M. - J. Med.Chem. 49: 5316-5323. 2006.
Synthesis and anti-HIV-1 activity of 1-[2-(2-benzyl-4-methylphenoxy)ethyl]uracil derivatives.
Novikov M.S., Orlova Yu.A., Ozerov A.A., Hartman T., Buckheit R.W. - Bulletin of Volgograd Scientific Centre of Russian Academy of Medical Science. 2006. - No. 4. - P. 11-15.
Synthesis of novel non-symmetrical 1,3-disubstituted uracil derivatives and investigation of their anti-HIV-1 activity in vitro.
Novikov M.S., Orlova Yu.A., Solodunova A.A., Ozerov A.A., Hartman T., Buckheit R.W. - Bulletin of Volgograd Scientific Centre of Russian Academy of Medical Science. 2006. - No. 4. - P. 6-8.
In vitro preclinical testing of nonoxynol-9 as potential anti-human immunodeficiency virus microbicide: a retrospective analysis of results from five laboratories.
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. - Antimicrob. Agents Chemother. 50:713-723. 2006.
In vitro and in vivo characterization of a potential universal placebo designed for use in vaginal microbicide clinical trials.
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. - AIDS Res. Hu. Retrov. 21: 11-19. 2005.
Synthesis and antiviral properties of 1-{[2-(phenoxy)ethoxy]methyl}uracil derivatives.
Novikov, M.S., Ozerov, A.A., Orlova, J.A., Buckheit, R.W., Jr. - Chemistry of Heterocyclic Compounds. 5:726-731. 2005.
Potent inhibition of HIV-1 entry by (s4dU)35.
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. - Virology. 334:214-223. 2005.
Synthesis and anti-HIV activity of new alkenyldiarylmethane (ADAM) non-nucleoside reverse transcriptase inhibitors (NNRTIs) incorporating benzoxazolone and benzisoxazole rings.
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. - J.Med.Chem. 48:6140-6155. 2005.
Isolation and characterization of griffithsin, a novel HIV-inactivating protein from the red algae Griffithsia sp.
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. - J. Biol. Chemistry. 280:9345-9353. 2005.
An unusual “senseless” 2’,5’-oligoribonucleotide with potent anti-HIV activity.
Aboul-Fadi, T., Agrawal, V.K., Buckheit, R.W., Jr. and Broom, A.D. - Nucleosides and Nucleotides 23:545-554. 2004.
Optimization of unique uncharged thioesters as inhibitors of HIV replication.
Srivastava, P., Hara, T., Fattah, R.J., Schito, M., Hartman, T., Buckheit, R.W., Jr., Turpin, J.A., Inman, J.K., and Appella, E. - Bioorg.Med.Chem. 12: 6437-6450. 2004.
Expression, purification, and characterization of recombinant cyanovirin-N for vaginal anti-HIV microbicide development.
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. - Protein Expression and Purification. 39:229-236. 2004.
Synthesis and antiviral activity of 2-(alkylthio)-5-[2-(aryloxy)ethyl]-6-methylpyrimidine-4(3H)-ones.
Novikov M.S., Sim O.G., Ozerov A.A., Buckheit R.W. - Bulletin of Volgograd Scientific Centre of Russian Academy of Medical Sciences. 2:30-31. 2004.
Synthesis and anti-HIV-1 activity of 1-(benzyloxymethyl)-5-(arylamino)uracil derivatives methylated in side chain.
Ozerov A.A., Novikov M.S., Gnatjuk V.P., Lobachev A.A., Buckheit R.W. - Bulletin of Volgograd Scientific Centre of Russian Academy of Medical Sciences.1:26-28. 2004.
Understanding HIV resistance, fitness, replication capacity and compensation: targeting viral fitness as a therapeutic strategy. In press.
Buckheit, R.W., Jr. - Expert Opin. Investig. Drugs 13: 933-958. 2004.
Synthesis and anti-HIV-1 activity of 2-[[2-(3,5-dimethylphenoxy)ethyl]thio]pyrimidin-4(3H)-ones.
Novikov, M.S., Ozerov, A.A., Sim, O.G. and Buckheit, R.W., Jr. - Chemistry of Heterocyclic Compounds. 40:37-42. 2004.
Antiviral activity of hop constituents against a series of DNA and RNA viruses.
Buckwold, V.E., Wilson, R.J.H., Nalca, A., Beer, B., Voss, T.G., Turpin, J.A., Buckheit, R.W., Jr., Wei, J., Wenzel-Mathers, M., Walton, E., Pallansch, M., Ward, P., Wells, J., Chuvala, L., Sloane, S., Paulman, R., Russell, J., Hartman,T. and Ptak, R. - Antiviral Research. 61:57-62. 2004.
