Dr David Shackleford - Researcher Profile

Biography

Position

Biopharmaceutics section leader
Centre for Drug Candidate Optimisation
Monash Institute of Pharmaceutical Sciences

Qualifications

DOCTOR OF PHILOSOPHY

Institution: University of South Australia

Year awarded: 2001

Publications

Book Chapters

Shackleford, D., Porter, C.J., Charman, W.N., 2007, Lymphatic absorption of orally administered prodrugs, in Prodrugs: Challenges and Rewards, eds V.J. Stella, R.T. Borchardt, M.J. Hageman, R. Oliyai, H. Magg and J.W. Tilley, Springer and AAPS Press, New York, USA, pp. 653-682.

Journal Articles

Younis, Y., Douelle, F., Feng, T., Cabrera, D.G., Le Manach, C., Nchinda, A.T., Duffy, S., White, K.L., Shackleford, D., Morizzi, J., Mannila, J.M., Katneni, K., Bhamidipati, R., Zabiulla, M.K., Joseph, J.T., Bashyam, S., Waterson, D., Witty, M.J., Hardick, D., Wittlin, S., Avery, V.M., Charman, S.A., Chibale, K., 2012, 3,5-Diaryl-2-aminopyridines as a novel class of orally active antimalarials demonstrating single dose cure in mice and clinical candidate potential, Journal of Medicinal Chemistry [P], vol 55, issue 7, American Chemical Society, Washington DC USA, pp. 3479-3487.

Davis, R.A., Buchanan, M.S., Duffy, S., Avery, V.M., Charman, S.A., Charman, W.N., White, K.L., Shackleford, D., Edstein, M.D., Andrews, K., Camp, D.G., Quinn, R.J., 2012, Antimalarial activity of pyrroloiminoquinones from the Australian marine sponge Zyzzya sp., Journal of Medicinal Chemistry [P], vol 55, issue 12, American Chemical Society, Washington DC USA, pp. 5851-5858.

Buckner, F.S., Bahia, M.T., Suryadevara, P.K., White, K.L., Shackleford, D., Chennamaneni, N.K., Hulverson, M.A., Laydbak, J.U., Chatelain, E., Scandale, I., Verlinde, C.L.M., Charman, S.A., Lepesheva, G.I., Gelb, M.H., 2012, Pharmacological characterization, structural studies, and in vivo activities of anti-chagas disease lead compounds derived from tipifarnib, Antimicrobial Agents And Chemotherapy [P], vol 56, issue 9, American Society for Microbiology, Washington DC, USA, pp. 4914-4921.

Mannila, A.H., Morizzi, J., Nguyen, T.T., Charman, S.A., McIntosh, M.P., Shackleford, D., 2012, Probing a potential in vivo drug-excipient interaction: Temporal effects of a modified beta-cyclodextrin on the intravenous pharmacokinetics of a model high-affinity drug ligand, Journal of Pharmaceutical Sciences [P], vol 101, issue 9, Wiley-Blackwell, Malden, Massachusetts USA, pp. 3381-3389.

Hung, L., Villemagne, V., Cheng, L., Sherratt, N., Ayton, S., White, A., Crouch, P., Lim, S., Leong, S., Wilkins, S., George, J., Roberts, B., Pham, C., Liu, X., Chiu, F., Shackleford, D., Powell, A., Masters, C., Bush, A., O'Keefe, G., Culvenor, J., Cappai, R., Cherny, R., Donnelly, P., Hill, A., Finkelstein, D., Barnham, K., 2012, The hypoxia imaging agent CU(atsm) is neuroprotective and improves motor and cognitive functions in multiple animal models of Parkinson's disease, Journal of Experimental Medicine [P], vol 209, issue 4, Rockefeller University Press, New York, pp. 837-854.

Ndakala, A., Gessner, R., Gitari, P., October, N., White, K., Hudson, A., Fakorede, F., Shackleford, D., Kaiser, M., Yates, C., Charman, S., Chibale, K., 2011, Antimalarial Pyrido[1,2-a]benzimidazoles, Journal of Medicinal Chemistry [P], vol 54, ACS Publications, USA, pp. 4581-4589.

Dow, G., Milner, E., Bathurst, I., Bhonsle, J., Caridha, D., Gardner, S., Gerena, L., Kozar, M., Lanteri, C., Mannila, A., McCalmont, W., Moon, J., Read, K., Norval, S., Roncal, N., Shackleford, D., Sousa, J., Steuten, J., White, K., Zeng, Q., Charman, S., 2011, Central nervous system exposure of next generation quinoline methanols is reduced relative to mefloquine after intravenous dosing in mice, Malaria Journal [P], vol 10, issue 150, BioMed Central, United Kingdom, pp. e1-e11.

Flynn, B., Gurmit, G., Grobelny, D., Chaplin, J., Paul, D., Leske, A., Lavranos, T., Chalmers, D., Charman, S., Kostewicz, E., Shackleford, D., Morizzi, J., Hamel, E., Jung, K., Kremmidiotis, G., 2011, Discovery of 7-hydroxy-6-methoxy-2-methyl-3-(3,4,5-trimethoxybenzoyl)benzo[b]furan (BNC105), a tubulin polymerization inhibitor with potent antiproliferative and tumor vascular disrupting properties, Journal of Medicinal Chemistry [P], vol 54, issue 17, AMER CHEMICAL SOC, USA, pp. 6014-6027.

Gujjar, R., El Mazouni, F., White, K., White, J., Creason, S., Shackleford, D., Deng, X., Charman, W., Bathurst, I., Burrows, J., Floyd, D., Matthews, D., Buckner, F., Charman, S., Phillips, M., Rathod, P., 2011, Lead optimization of aryl and aralkyl amine-based triazolopyrimidine inhibitors of plasmodium falciparum dihydroorotate dehydrogenase with antimalarial activity in mice, Journal of Medicinal Chemistry [P], vol 54, American Chemical Society, USA, pp. 3935-3949.

Coteron, J., Marco, M., Esquivias, J., Deng, X., White, K., White, J., Koltun, M., El Mazouni, F., Kokkonda, S., Katneni, K., Bhamidipati, R., Shackleford, D., Angulo-Barturen, I., Ferrer, S., Jimenez-Diaz, M., Gamo, F., Goldsmith, E., Charman, W., Bathurst, I., Floyd, D., Matthews, D., Burrows, J., Rathod, P., Charman, S., Phillips, M., 2011, Structure-guided lead optimization of triazolopyrimidine-ring substituents identifies potent Plasmodium falciparum dihydroorotate dehydrogenase inhibitors with clinical candidate potential, Journal of Medicinal Chemistry [P], vol 54, issue 15, American Chemical Society, USA, pp. 5540-5561.

Charman, S., Arbe-Barnes, S., Bathurst, I., Brun, R., Campbell, M., Charman, W., Chiu, F., Chollet, J., Craft, C., Creek, D., Dong, Y., Matile, H., Maurer, M., Morizzi, J., Nguyen, T., Papastogiannidis, P., Scheurer, C., Shackleford, D., Sriraghavan, K., Stingelin, L., Tang, Y., Urwyler, H., Wang, X., White, K., Wittlin, S., Zhou, L., Vennerstrom, J., 2011, Synthetic ozonide drug candidate OZ439 offers new hope for a single-dose cure of uncomplicated malaria, Proceedings Of The National Academy Of Sciences Of The United States Of America [P], vol 108, issue 11, National Academy of Sciences, Washington D.C., USA, pp. 4400-4405.

McIntosh, M.P., Leong, N., Katneni, K., Morizzi, J., Shackleford, D.M., Prankerd, R.J., 2010, Impact of chlorpromazine self-association on its apparent binding constants with cyclodextrins: Effect of SBE7-beta-CD on the disposition of chlorpromazine in the rat, Journal of Pharmaceutical Sciences [P], vol 99, issue 7, John Wiley & Sons, Inc., USA, pp. 2999-3008.

Koltun, M., Morizzi, J., Katneni, K., Charman, S.A., Shackleford, D., McIntosh, M.P., 2010, Preclinical comparison of intravenous melphalan pharmacokinetics administered in formulations containing either (SBE)7m-beta-cyclodextrin or a co-solvent system, Biopharmaceutics and Drug Disposition [E], vol 31, issue 8-9, John Wiley & Sons, Ltd, online, pp. 450-454.

Johnstone, K.D., Karoli, T., Liu, L., Dredge, K., Copeman, E., Li, C.P., Davis, K., Hammond, E., Bytheway, I., Kostewicz, E.S., Chiu, F.C.K., Shackleford, D., Charman, S.A., Charman, W.N., Harenberg, J., Gonda, T., Ferro, V., 2010, Synthesis and Biological Evaluation of Polysulfated Oligosaccharide Glycosides as Inhibitors of Angiogenesis and Tumor Growth, Journal of Medicinal Chemistry [P], vol 53, issue 4, American Chemical Society, USA, pp. 1686-1699.

Burns, C., Fantino, E., Phillips, I.D., Su, S., Harte, M., Bukczynska, P.E., Frazzetto, M., Joffe, M., Kruszelnicki, I., Wang, B., Wang, Y., Wilson, N., Dilley, R.J., Wan, S.S., Charman, S.A., Shackleford, D., Fida, R., Malcontenti-Wilson, C., Wilks, A.F., 2009, CYT997: a novel orally active tubulin polymerization inhibitor with potent cytotoxic and vascular disrupting activity in vitro and in vivo, Molecular Cancer Therapeutics [P], vol 8, issue 11, American Association for Cancer Research, USA, pp. 3036-3045.

Burns, C., Harte, M., Bu, X., Fantino, E., Joffe, M., Sikanyika, H., Su, S., Tranberg, C., Wilson, N., Charman, S.A., Shackleford, D., Wilks, A.F., 2009, Discovery of CYT997: a structurally novel orally active microtubule targeting agent, Bioorganic & Medicinal Chemistry Letters [P], vol 19, issue 16, Pergamon, UK, pp. 4639-4642.

Gujjar, R., Marwaha, A., El Mazouni, F., White, J., White, K.L., Creason, S., Shackleford, D., Baldwin, J., Charman, W.N., Buckner, F.S., Charman, S.A., Rathod, P., Phillips, M., 2009, Identification of a metabolically stable triazolopyrimidine-based dihydroorotate dehydrogenase inhibitor with antimalarial activity in mice, Journal of Medicinal Chemistry [P], vol 52, issue 7, American Chemical Society, USA, pp. 1864-1872.

Trevaskis, N., Shackleford, D., Charman, W.N., Edwards, G.A., Gardin, A., Appel-Dingemanse, S., Kretz, O., Galli, B., Porter, C.J., 2009, Intestinal lymphatic transport enhances the post-prandial oral bioavailability of a novel cannabinoid receptor agonist via avoidance of first-pass metabolism, Pharmaceutical Research [P], vol 26, issue 6, Springer New York LLC, USA, pp. 1486-1495.

Burns, C., Bourke, D.G., Andrau, L., Bu, X., Charman, S.A., Donohue, A.C., Fantino, E., Farrugia, M., Feutrill, J.T., Joffe, M., Kling, R.M., Kurek M., Nero, T.L., Nguyen, T., Palmer, J.T., Phillips, I.D., Shackleford, D., Sikanyika, H., Styles, M., Su, S., Treutlein, H., Zeng, J., Wilks, A.F., 2009, Phenylaminopyrimidines as inhibitors of Janus kinases (JAKs), Bioorganic & Medicinal Chemistry Letters [P], vol 19, issue 20, Pergamon, UK, pp. 5887-5892.

Bhamidipati, R.K., Morizzi, J., Chiu, F.C.K., Shackleford, D., Charman, S.A., 2009, Simultaneous determination of OZ277, a synthetic 1,2,4-trioxolane antimalarial, and its polar metabolites in rat plasma using hydrophilic interaction chromatography, Journal of Chromatography B: Analytical Technologie..., vol 877, issue 27, Elsevier BV, The Netherlands, pp. 2989-2995.

Shackleford, D.M., Evans, A.M., Milne, R.W., Nation, R.L., 2006, Loading-washout studies of the stereoselective sinusoidal uptake of (R)- and (S)-2-phenylpropionyl acyl glucuronide, Current Drug Metabolism, vol 7, issue 7, Bentham Science Publishers Ltd., Netherlands, pp. 817-826.

Wang, J., Nation, R.L., Evans, A.M., Cox, S., Shackleford, D., 2005, Metabolism and disposition of the antiviral nucleoside analogue AM365 in the isolated perfused rat liver, Current Drug Metabolism, vol 6, issue 5, Bentham Science Publishers Ltd, The Netherlands, pp. 487-493.

Shackleford, D., Nation, R.L., Milne, R., Hayball, P.J., Evans, A.m., 2004, Stereoselective Hepatic Disposition of Model Diastereomeric Acyl Glucuronides, Journal of Pharmacokinetics and Pharmacodynamics, vol 31, issue 1, Springer Netherlands, The Netherlands, pp. 1-27.

Shackleford, D.M., Faassen, W.A.(., Houwing, N., Lass, H., Edwards, G.A., Porter, C.J.H., Charman, W.N., 2003, Contribution of lymphatically transported testosterone undecanoate to the systemic exposure of testosterone after oral administration of two andriol formulations in conscious lymph duct-cannulated dogs, The Journal of Pharmacolgy and Experimental Therapeutics, vol 306, issue 3, American Society for Pharmacology and Experimental Therapeutics, USA, pp. 925-933.

Shackleford, D.M., Porter, C.J.H., Charman, W.N., 2003, Does stereoselective lymphatic absorption contribute to the enantioselective pharmacokinetics of halofantrine in vivo?, Biopharmaceutics & Drug Disposition, vol 24, issue 4, John Wiley & Sons Ltd., UK, pp. 153-157.

Khoo, S., Shackleford, D.M., Porter, C.J.H., Edwards, G.A., Charman, W.N., 2003, Intestinal lymphatic transport of halofantrine occurs after oral administration of a unit-dose lipid-based formulation to fasted dogs, Pharmaceutical Research, vol 20, issue 9, Kluwer Academic/Plenum Publishers, USA, pp. 1460-1465.

Shackleford, D.M., Prankerd, R.J., Scanlon, M.J., Charman, W.N., 2003, Self-micellization of gemfibrozil 1-0- acyl glucuronide in aqueous solution, Pharmaceutical Research, vol 20, issue 3, Kluwer Academic/Plenum Publishers, USA, pp. 465-470.

Lucas, A.N., Brogan, L.R., Nation, R.L., Milne, R.W., Evans, A.M., Shackleford, D.M., 2003, The effects of the phytoestrogenic isoflavone genistein on the hepatic disposition of preformed and hepatically generated gemfibrozil 1-0-acyl glucuronide in the isolated perfused rat liver, Journal of Pharmacy and Pharmacology, vol 55, Pharmaceutical Press, UK, pp. 1433-1439.

Shackleford, D., Hayball, P.J., Reynolds, G.D., Hamon, D., Evans, A., Milne, R., Nation, R.L., 2001, A small-scale synthesis and enantiomeric resolution of (RS)-[1-14C]-2-phenylpropionic acid and biosynthesis of its diastereomeric acyl glucuronides, Journal of Labelled Compounds and Radiopharmaceuticals, vol 44, issue 3, John Wiley & Sons Ltd, UK, pp. 225-234.

Activities

Affiliations with institutes

Centre for Drug Candidate Optimisation
Monash Institute of Pharmaceutical Sciences