Publications for Preclinical Pharmacology Core

(core staff in bold)

Xin, J., N. Williams, and J. De Brabander (2007). Synthesis of psymberin analogs: probing a functional correlation with the pederin/mycalamide family of natural products Organic Letters 9:227-230. PMCID: PMC2631385.

Williams, N.S., A.W.G. Burgett, A.S. Atkins, X. Wang, P.G. Harran, and S.L. McKnight (2007). Therapeutic anti-cancer efficacy of a synthetic diazonamide analog in the absence of overt toxicity. Proceedings of the National Academy of Sciences USA 104:2074-2079.  PMCID: PMC1794345.

Rasko, D.A., C.G. Moreira, D.R. Li, N.C. Reading, J.M. Ritchie, M.K. Waldor, N. Williams, R. Taussig, S. Wei, M. Roth, D.T. Hughes, J.F. Huntley, M.W. Fina, J.R. Falck, and V. Sperandio (2008). Targeting QseC signaling and virulence for antibiotic development. Science 321:1078-1080. PMCID: PMC2605406.

Chen, B., M.E. Dodge, W. Tang, J. Lu, Z. Ma, C.-W. Fan, S. Wei, W. Hao, J. Kilgore, N.S. Williams, M.G. Roth, J.F. Amatruda, C. Chen, and L. Lum (2009) Small molecule-mediated disruption of Wnt-dependent signaling in tissue regeneration and cancer. Nature Chemical Biology 5:100-107.  PMCID: PMC2628455.

Lu, J., Z. Ma, J.-C. Hsieh, C.-W. Fan, B. Chen, J.C. Longgood, N.S. Williams, J.F. Amatruda, L. Lum, and C. Chen  (2009) Structure-activity relationship studies of small-molecule inhibitors of Wnt response.  Bioorganic & Medicinal Chemistry Letters, 19:3825-3827.  PMCID: PMC2709695.

Dineen, S.P., C.L. Roland, R. Greer, J.G. Carbon, J.E. Toombs, P. Gupta, N. Bardeesy, H. Sun, N. Williams, J.D. Minna, and R.A. Brekken (2010) Smac mimetic increases chemotherapy response and improves survival in mice with pancreatic cancer.  Cancer Research 70:2852-2861.  PMCID: PMC2848888.

Pieper, A.A., S. Xie, E. Capota, S.J. Estill, J. Zhong, J.M. Long, G.L. Becker, P. Huntington, S.E. Goldman, C.H. Shen, M. Capota, J.K. Britt, T. Kotti, K. Ure, D.J. Brat, N.S. Williams, K.S. MacMillan, J. Naidoo, L. Melito, J. Hsieh, J. De Brabander, J.M. Ready, S.L. McKnight (2010) Discovery of a proneurogenic, neuroprotective chemical.  Cell 9:39-51. PMCID: PMC2930815.

Macmillan K.S., J Naidoo,  J. Liang, L. Melito, N.S. Williams, L. Morlock, P.J. Huntington, S.J. Estill, J. Longgood G.L. Becker, S.L. McKnight, A.A. Pieper, J.K. De Brabander, and J.M. Ready. (2011) Development of proneurogenic, neuroprotective small molecules.  Journal of the American Chemical Society. 133:1428-37. PMCID: PMC3033481.

Mata, M.A., N. Satterly, G.A. Versteeg, D. Frantz, S. Wei, N. Williams, M. Schmolke, S. Pena-Llopis, J. Brugarolas, C. Forst, M.A. White, A. Garcia-Sastre, M.G. Roth, and B.M.A. Fontoura. (2011) Chemical inhibition of RNA viruses Reveals REDD1 as host defense factor.  Nature Chemical Biology, 7:712-719. PMCID: PMC3329801.

Wang Y., Q.S. Zang, Z. Liu, Q. Wu, D. Maass, G. Dulan, P.W. Shaul, L. Melito, D.E. Frantz, J.A. Kilgore, N.S. Williams, L.S. Terada, F.E. Nwariaku. (2011) Regulation of VEGF induced endothelial cell migration by mitochondrial reactive oxygen species.  American Journal of Physiology, Cell Physiology 301:C695-C704.   PMCID: PMC3174570.

Zang, Q.S., H. Sadek, D.L. Maass, B. Martinez, J.A. Kilgore, N.S. Williams, D.E. Frantz, J.G. Wigginton, F.E. Nwariaku, S.E. Wolf, and J.P. Minei (2012) Specific Inhibition of mitochondrial oxidative stress suppresses inflammation and improves cardiac function in a rat pneumonia-related sepsis model.  American Journal of Physiology, Heart and Circulatory Physiology, 302:H1847-H1859.  PMID: 22408027.

Huang X., Y. Dong, E.A. Bey, J.A. Kilgore, J.S. Bair, L.S. Li, M. Patel, E.l. Parkinson, Y. Wang, N.S. Williams, J. Gao, P.J. Hergenrother, and D.A. Boothman (2012) An NQO1 substrate with potent anti-tumor activity that selectively kills by PARP1-induced programmed necrosis. Cancer Research. 72:3038-3047.  PMID:22532167.

Sivanand, S., S. Pena-Llopis, H. Zhao, B. Kucejova, P. Spence, A. Pavia-Jimenex, T. Yamasaki, D.J. McBride, J. Gillen, N.C. Wolff, L. Morlock, Y. Lotan, G.V. Raj, A. Sagalowsky, V. Margulis, J.A. Cadeddu, M.T. Ross, D.R. Bentley, W. Kabbani, X.-J. Xie, P. Kapur, N.S. Williams, J. Brugarolas (2012). A validated tumorgraft model reveals activity of dovitinib against renal cell carcinoma. Science Translational Medicine, 4:137ra75.  PMCID: PMC3570965.

De Jesús-Cortés H., S.J. Estill, P. Huntington, S. Tran, J. Britt, R. Tesla, L. Morlock, J. Naidoo, L.M. Melito, G. Wang, N.S. Williams, J. M. Ready, S.L. McKnight, A.A. Pieper (2012). Neuroprotective efficacy of aminopropyl carbazoles in a mouse model of Parkinson disease. Proceedings of the National Academy of Sciences, USA.  109:17010-17015. PMCID: PMC3479520.

Tesla R., H.P. Wolf, P. Xu, J. Drawbridge, S.J. Estill, P. Huntington, L. McDaniel, W. Knobbe, A. Burket, S. Tran, R. Starwalt, L. Morlock, J. Naidoo, N.S. Williams, J.M. Ready, S.L. McKnight, A.A. Pieper (2012). Neuroprotective efficacy of aminopropyl carbazoles in a mouse model of amyotrophic lateral sclerosis. Proceedings of the National Academy of Sciences, USA.  109:17016-17021. PMCID: PMC3479516.

Wu, C., Y. Feng, E.R. Cardenas, N. Williams, P.E. Floreancig, J.K. De Brabander, and M.G. Roth (2012) Studies toward the Unique Pederin Family Member Psymberin:  Structure−activity relationships, biochemical studies, and genetics identify the mode-of-action of psymberin.  Journal of the American Chemical Society. 134: 18998-19003. PMCID: PMC3504174.

Wang, C. and N.S .Williams (2013) A mass balance approach for calculation of recovery and binding enables the use of ultrafiltration as a rapid method for measurement of plasma protein binding for even highly lipophilic compounds.  Journal of Pharmaceutical and Biomedical Analysis. 75: 112-117. PMCID: PMC3545278

Wang, G,. X. Wang, H. Yu, S. Wei, N.S. Williams, D.L. Holmes, R. Halfmann, J. Naidoo, L. Wang, L. Li, S. Chen, P. Harran, X. Lei, and X. Wang (2013) Small-molecule activation of the TRAIL receptor DR5 in human cancer cells. Nature Chemical Biology. 9:84-89. PMID:  23292651.

Wang, X., J. Moon, M.E. Dodge, X. Pan, L. Zhang, J.M. Hanson, R. Tuladhar, Z. Ma, H. Shi, N.S. Williams, J.F. Amatruda, T.J. Carroll, L. Lum, C. Chen (2013).  The development of highly potent inhibitors for porcupine. Journal of Medicinal Chemistry. 56:2700-2704. PMCID: PMC3631274.

Tso, S.-C., Z. Qi, W.-J. Gui, J.L. Chuang, L.K. Morlock, A.L. Wallace, K. Ahmed, S. Laxman, P.M. Campeau, B.H. Lee, S.M. Hutson, B.P. Tu, N.S. Williams U.K. Tambar, R.M. Wynn, and D.T. Chuang (2013) Structure-based design and mechanism of allosteric inhibitors for mitochondrial branched-chain -ketoacid dehydrogenase kinase.  Proceedings of the National Academy of Sciences, USA. 110:9728-9733. PMCID: PMC3683707.

Kilgore, J.A., X. Du, L. Melito, S. Wei, C. Wang, H.G. Chin, B. Posner, S. Pradhan, J.M. Ready, and N.S. Williams (2013) Identification of DNMT1 selective antagonists using a novel scintillation proximity assay.  Journal of Biological Chemistry. 288:19673-19684. PMCID: PMC3707673..

Awasthi, N., C. Zhang, A.M. Schwarz, S.Hinz, C. Wang, N.S. Williams, M.A. Schwarz, and R.E. Schwarz (2013) Comparative benefits of Nab-paclitaxel over gemcitabine or polysorbate-based docetaxel in experimental pancreatic cancer.  Carcinogenesis 34(10):2361-2369.  PMCID: PMC4023322.

Kim, H.S., S. Mendiratta, J. Kim, C. V. Pecot, J.E. Larsen, I. Zubovych, B. Y. Seo, J. Kim, B. Eskiocak, H. Chung, E. McMillan, S. Wu, J. De Brabander, K. Komurov, J.E. Toombs, S. Wei, M. Peyton, N. Williams, A.F. Gazdar, B. A. Posner, R. A. Brekken, A.K. Sood, R.J.. Deberadinis, M.G. Roth, J. D. Minna, M.A. White (2013) Systematic identification of molecular subtype-selective vulnerabilities in non-small-cell lung cancer.  Cell 155(3):552-566. PMCID: PMC3836195.

Tso, S-C, X. Qi, W.-J. Gui, C.-Y. Wu, J.L. Chuang, I. Wernstedt-Asterholm, L.K. Morlock, K.R. Owens, P.E. Scherer, N.S. Williams, U.K. Tambar, R.M. Wynn, and D.T. Chuang (2014) Structure-guided development of specific pyruvate dehydrogenase kinase inhibitors targeting the ATP-binding pocket.  Journal of Biological Chemistry, 289(7):4432-4443. PMID 24356970.

 Chau, V., S.K Lim, W. Mo, C. Liu, A.J. Patel, R.M. McKay, S. Wei, B.A. Posner, J.K. De Brabander, N.S. Williams, L.F. Parada, and L.Q. Le (2014) Preclinical therapeutic efficacy of a novel pharmacologic inducer of apoptosis in malignant peripheral nerve sheath tumors.  Cancer Research 74 (2):586-597.  PMCID: PMC3924305.

Naidoo J., H. De Jesus-Cortes, P. Huntington, S. Estill, L.K. Morlock, R. Starwalt, T.J. Mangano, N.S. Williams, A.A. Pieper, and J.M. Ready (2014) Discovery of a neuroprotective chemical, (S)-N-(3-(3,6-Dibromo-9H-carbazol-9-yl)-2-fluoropropyl)-6-methoxypyridin-2-amine [(-)-P7C3-S243], with improved druglike properties.  Journal of Medicinal Chemistry 57(9):3746-3754.  PMID 24697290.

Walker A.K., P.D. Rivera, Q. Wang, J.C. Chuang, S. Tran, S. Osborne-Lawrence, S.J. Estill, R. Starwalt, P. Huntington, L. Morlock, J. Naidoo, N.S. Williams, J. M. Ready, A.J. Eisch, A.A. Pieper, and J.M. Zigman (2014) The P7C3 class of neuroprotective compounds exerts antidepressant efficacy in mice by increasing hippocampal neurogenesis.  Molecular Psychiatry.  2014 Apr 22. doi: 10.1038/mp.2014.34 [Epub ahead of print]. PMID 24751964.

Tso S.C, W.J. Gui, C.Y. Wu, J.L. Chuang, X. Qi, K.J. Skvorak, K. Dorko, A.L. Wallace, L.K. Morlock, B.H. Lee, S.M. Hutson, S.C. Strom, N.S. Williams, U.K. Tambar, R.M. Wynn, and D.T. Chuang (2014) Benzothiophene Carboxylate Derivatives as Novel Allosteric Inhibitors of Branched-chain α-Ketoacid Dehydrogenase Kinase.  Journal of Biological Chemistry. 2014 289(7):4432-4443. PMCID:PMC3924305.

Derebe, M.G., C.M. Zlatkov, S. Gattu, K.A. Ruhn, S. Vaishnava, G.E. Diehl, J.B. MacMillan, N.S. Williams, L.V. Hooper (2014) Serum amyloid A is a retinol binding protein that transports retinol during bacterial infection.  eLife 2014;10.7554/eLife.03206. PMID:25073702.