Publications

Older Publications

  1. Jiang X, Williams N, De Brabander JK. Synthesis of psymberin analogues: probing a functional correlation with the pederin/mycalamide family of natural products. Org Lett. 2007 Jan 18;9(2):227-30. PubMed PMID: 17217271; PubMed Central PMCID: PMC2631385
  2. Williams NS, Burgett AW, Atkins AS, Wang X, Harran PG, McKnight SL. Therapeutic anticancer efficacy of a synthetic diazonamide analog in the absence of overt toxicity. Proc Natl Acad Sci U S A. 2007 Feb 13;104(7):2074-9. Epub 2007 Feb 7. PubMed PMID: 17287337; PubMed Central PMCID: PMC1794345.
  3. Rasko DA, Moreira CG, Li de R, Reading NC, Ritchie JM, Waldor MK, Williams N, Taussig R, Wei S, Roth M, Hughes DT, Huntley JF, Fina MW, Falck JR, Sperandio V. Targeting QseC signaling and virulence for antibiotic development. 2008 Aug 22;321(5892):1078-80. doi: 10.1126/science.1160354. PubMed PMID: 18719281; PubMed Central PMCID: PMC2605406
  4. Chen B, Dodge ME, Tang W, Lu J, Ma Z, Fan CW, Wei S, Hao W, Kilgore J, Williams NS, Roth MG, Amatruda JF, Chen C, Lum L. Small molecule-mediated disruption of Wnt-dependent signaling in tissue regeneration and cancer. Nat Chem Biol. 2009 Feb;5(2):100-7. doi: 10.1038/nchembio.137. Epub 2009 Jan 4. PubMed PMID: 19125156; PubMed Central PMCID: PMC2628455.
  5. Lu J, Ma Z, Hsieh JC, Fan CW, Chen B, Longgood JC, Williams NS, Amatruda JF, Lum L, Chen C. Structure-activity relationship studies of small-molecule inhibitors of Wnt response. Bioorg Med Chem Lett. 2009 Jul 15;19(14):3825-7. doi: 10.1016/j.bmcl.2009.04.040. Epub 2009 Apr 18. PubMed PMID: 19410457; PubMed Central PMCID: PMC2709695.
  6. Dineen SP, Roland CL, Greer R, Carbon JG, Toombs JE, Gupta P, Bardeesy N, Sun H, Williams N, Minna JD, Brekken RA. Smac mimetic increases chemotherapy response and improves survival in mice with pancreatic cancer. Cancer Res. 2010 Apr 1;70(7):2852-61. doi: 10.1158/0008-5472.CAN-09-3892. Epub 2010 Mar 23. PubMed PMID: 20332237; PubMed Central PMCID: PMC2848888.
  7. Pieper AA, Xie S, Capota E, Estill SJ, Zhong J, Long JM, Becker GL, Huntington P, Goldman SE, Shen CH, Capota M, Britt JK, Kotti T, Ure K, Brat DJ, Williams NS, MacMillan KS, Naidoo J, Melito L, Hsieh J, De Brabander J, Ready JM, McKnight SL. Discovery of a proneurogenic, neuroprotective chemical. 2010 Jul 9;142(1):39-51. doi: 10.1016/j.cell.2010.06.018. PubMed PMID: 20603013; PubMed Central PMCID: PMC2930815.
  8. MacMillan KS, Naidoo J, Liang J, Melito L, Williams NS, Morlock L, Huntington PJ, Estill SJ, Longgood J, Becker GL, McKnight SL, Pieper AA, De Brabander JK, Ready JM. Development of proneurogenic, neuroprotective small molecules. J Am Chem Soc. 2011 Feb 9;133(5):1428-37. doi: 10.1021/ja108211m. Epub 2011 Jan 6. PubMed PMID: 21210688; PubMed Central PMCID: PMC3033481.
  9. Wang Y, Zang QS, Liu Z, Wu Q, Maass D, Dulan G, Shaul PW, Melito L, Frantz DE, Kilgore JA, Williams NS, Terada LS, Nwariaku FE. Regulation of VEGF-induced endothelial cell migration by mitochondrial reactive oxygen species. Am J Physiol Cell Physiol. 2011 Sep;301(3):C695-704. doi: 10.1152/ajpcell.00322.2010. Epub 2011 Jun 8. PubMed PMID: 21653897; PubMed Central PMCID: PMC3174570.
  10. Mata MA, Satterly N, Versteeg GA, Frantz D, Wei S, Williams N, Schmolke M, Peña-Llopis S, Brugarolas J, Forst CV, White MA, García-Sastre A, Roth MG, Fontoura BM. Chemical inhibition of RNA viruses reveals REDD1 as a host defense factor. Nat Chem Biol. 2011 Sep 11;7(10):712-9. doi: 10.1038/nchembio.645. PubMed PMID: 21909097; PubMed Central PMCID: PMC3329801.
  11. Zang QS, Sadek H, Maass DL, Martinez B, Ma L, Kilgore JA, Williams NS, Frantz DE, Wigginton JG, Nwariaku FE, Wolf SE, Minei JP. Specific inhibition of mitochondrial oxidative stress suppresses inflammation and improves cardiac function in a rat pneumonia-related sepsis model. Am J Physiol Heart Circ Physiol. 2012 May 1;302(9):H1847-59. doi: 10.1152/ajpheart.00203.2011. Epub 2012 Mar 9. PubMed PMID: 22408027.
  12. Sivanand S, Peña-Llopis S, Zhao H, Kucejova B, Spence P, Pavia-Jimenez A, Yamasaki T, McBride DJ, Gillen J, Wolff NC, Morlock L, Lotan Y, Raj GV, Sagalowsky A, Margulis V, Cadeddu JA, Ross MT, Bentley DR, Kabbani W, Xie XJ, Kapur P, Williams NS, Brugarolas J. A validated tumorgraft model reveals activity of dovitinib against renal cell carcinoma. Sci Transl Med. 2012 Jun 6;4(137):137ra75. doi: 10.1126/scitranslmed.3003643. PubMed PMID: 22674553; PubMed Central PMCID: PMC3570965.
  13. Huang X, Dong Y, Bey EA, Kilgore JA, Bair JS, Li LS, Patel M, Parkinson EI, Wang Y, Williams NS, Gao J, Hergenrother PJ, Boothman DA. An NQO1 substrate with potent antitumor activity that selectively kills by PARP1-induced programmed necrosis. Cancer Res. 2012 Jun 15;72(12):3038-47. doi: 10.1158/0008-5472.CAN-11-3135. Epub 2012 Apr 24. PubMed PMID: 22532167.
  14. De Jesús-Cortés H, Xu P, Drawbridge J, Estill SJ, Huntington P, Tran S, Britt J, Tesla R, Morlock L, Naidoo J, Melito LM, Wang G, Williams NS, Ready JM, McKnight SL, Pieper AA. Neuroprotective efficacy of aminopropyl carbazoles in a mouse model of Parkinson disease. Proc Natl Acad Sci U S A. 2012 Oct 16;109(42):17010-5. doi: 10.1073/pnas.1213956109. Epub 2012 Oct 1. PubMed PMID: 23027934; PubMed Central PMCID: PMC3479520.
  15. Tesla R, Wolf HP, Xu P, Drawbridge J, Estill SJ, Huntington P, McDaniel L, Knobbe W, Burket A, Tran S, Starwalt R, Morlock L, Naidoo J, Williams NS, Ready JM, McKnight SL, Pieper AA. Neuroprotective efficacy of aminopropyl carbazoles in a mouse model of amyotrophic lateral sclerosis.Proc Natl Acad Sci U S A. 2012 Oct 16;109(42):17016-21. doi: 10.1073/pnas.1213960109. Epub 2012 Oct 1. PubMed PMID: 23027932; PubMed Central PMCID: PMC3479516.
  16. Wu CY, Feng Y, Cardenas ER, Williams N, Floreancig PE, De Brabander JK, Roth MG. Studies toward the unique pederin family member psymberin: structure-activity relationships, biochemical studies, and genetics identify the mode-of-action of psymberin. J Am Chem Soc. 2012 Nov 21;134(46):18998-9003. doi: 10.1021/ja3057002. Epub 2012 Nov 13. PubMed PMID: 23088155; PubMed Central PMCID: PMC3504174
  17. Wang G, Wang X, Yu H, Wei S, Williams N, Holmes DL, Halfmann R, Naidoo J, Wang L, Li L, Chen S, Harran P, Lei X, Wang X. Small-molecule activation of the TRAIL receptor DR5 in human cancer cells. Nat Chem Biol. 2013 Feb;9(2):84-9. doi: 10.1038/nchembio.1153. Epub 2012 Dec 23. PubMed PMID: 23292651.
  18. Wang C, Williams NS. 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. J Pharm Biomed Anal. 2013 Mar 5;75:112-7. doi: 10.1016/j.jpba.2012.11.018. Epub 2012 Nov 21. PubMed PMID: 23312388; PubMed Central PMCID: PMC3545278.
  19. Wang X, Moon J, Dodge ME, Pan X, Zhang L, Hanson JM, Tuladhar R, Ma Z, Shi H, Williams NS, Amatruda JF, Carroll TJ, Lum L, Chen C. The development of highly potent inhibitors for porcupine. J Med Chem. 2013 Mar 28;56(6):2700-4. doi: 10.1021/jm400159c. Epub 2013 Mar 19. PubMed PMID: 23477365; PubMed Central PMCID: PMC3631274.
  20. Tso SC, Qi X, Gui WJ, Chuang JL, Morlock LK, Wallace AL, Ahmed K, Laxman S, Campeau PM, Lee BH, Hutson SM, Tu BP, Williams NS, Tambar UK, Wynn RM, Chuang DT. Structure-based design and mechanisms of allosteric inhibitors for mitochondrial branched-chain α-ketoacid dehydrogenase kinase. Proc Natl Acad Sci U S A. 2013 Jun 11;110(24):9728-33. doi: 10.1073/pnas.1303220110. Epub 2013 May 28. PubMed PMID: 23716694; PubMed Central PMCID: PMC3683707
  21. Kilgore JA, Du X, Melito L, Wei S, Wang C, Chin HG, Posner B, Pradhan S, Ready JM, Williams NS. Identification of DNMT1 selective antagonists using a novel scintillation proximity assay. J Biol Chem. 2013 Jul 5;288(27):19673-84. doi: 10.1074/jbc.M112.443895. Epub 2013 May 13. PubMed PMID: 23671287; PubMed Central PMCID: PMC3707673.
  22. Awasthi N, Zhang C, Schwarz AM, Hinz S, Wang C, Williams NS, Schwarz MA, Schwarz RE. Comparative benefits of Nab-paclitaxel over gemcitabine or polysorbate-based docetaxel in experimental pancreatic cancer. 2013 Oct;34(10):2361-9. doi: 10.1093/carcin/bgt227. Epub 2013 Jun 26. PubMed PMID: 23803690; PubMed Central PMCID: PMC4023322
  23. Kim HS, Mendiratta S, Kim J, Pecot CV, Larsen JE, Zubovych I, Seo BY, Kim J, Eskiocak B, Chung H, McMillan E, Wu S, De Brabander J, Komurov K, Toombs JE, Wei S, Peyton M, Williams N, Gazdar AF, Posner BA, Brekken RA, Sood AK, Deberardinis RJ, Roth MG, Minna JD, White MA. Systematic identification of molecular subtype-selective vulnerabilities in non-small-cell lung cancer. 2013 Oct 24;155(3):552-66. doi: 10.1016/j.cell.2013.09.041. Epub 2013 Oct 24. PubMed PMID: 24243015; PubMed Central PMCID: PMC3836195.
  24. Chau V, Lim SK, Mo W, Liu C, Patel AJ, McKay RM, Wei S, Posner BA, De Brabander JK, Williams NS, Parada LF, Le LQ. Preclinical therapeutic efficacy of a novel pharmacologic inducer of apoptosis in malignant peripheral nerve sheath tumors. Cancer Res. 2014 Jan 15;74(2):586-97. doi: 10.1158/0008-5472.CAN-13-1934. Epub 2013 Nov 27. PubMed PMID: 24285727; PubMed Central PMCID: PMC3947005.
  25. Tso SC, Qi X, Gui WJ, Wu CY, Chuang JL, Wernstedt-Asterholm I, Morlock LK, Owens KR, Scherer PE, Williams NS, Tambar UK, Wynn RM, Chuang DT. Structure-guided development of specific pyruvate dehydrogenase kinase inhibitors targeting the ATP-binding pocket. J Biol Chem. 2014 Feb 14;289(7):4432-43. doi: 10.1074/jbc.M113.533885. Epub 2013 Dec 19. PubMed PMID: 24356970; PubMed Central PMCID: PMC3924305.
  26. Naidoo J, De Jesus-Cortes H, Huntington P, Estill S, Morlock LK, Starwalt R, Mangano TJ, Williams NS, Pieper AA, Ready JM. 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. J Med Chem. 2014 May 8;57(9):3746-54. doi: 10.1021/jm401919s. Epub 2014 Apr 16. PubMed PMID: 24697290; PubMed Central PMCID: PMC4206694.
  27. Tso SC, Gui WJ, Wu CY, Chuang JL, Qi X, Skvora KJ, Dork K, Wallace AL, Morlock LK, Lee BH, Hutson SM, Strom SC, Williams NS, Tambar UK, Wynn RM, Chuang DT. Benzothiophene carboxylate derivatives as novel allosteric inhibitors of branched-chain α-ketoacid dehydrogenase kinase. J Biol Chem. 2014 Jul 25;289(30):20583-93. PubMed PMID: 24895126; PubMed Central PMCID: PMC4110271.
  28. Derebe MG, Zlatkov CM, Gattu S, Ruhn KA, Vaishnava S, Diehl GE, MacMillan JB, Williams NS, Hooper LV. Serum amyloid A is a retinol binding protein that transports retinol during bacterial infection. Elife. 2014 Jul 29;3:e03206. doi: 10.7554/eLife.03206. PubMed PMID: 25073702; PubMed Central PMCID: PMC4129439.
  29. Curtis MM, Russell R, Moreira CG, Adebesin AM, Wang C, Williams NS, Taussig R, Stewart D, Zimmern P, Lu B, Prasad RN, Zhu C, Rasko DA, Huntley JF, Falck JR, Sperandio V. QseC inhibitors as an antivirulence approach for Gram-negative pathogens. MBio. 2014 Nov 11;5(6):e02165. doi: 10.1128/mBio.02165-14. PubMed PMID: 25389178; PubMed Central PMCID: PMC4235214.
  30. Dutca LM, Stasheff SF, Hedberg-Buenz A, Rudd DS, Batra N, Blodi FR, Yorek MS, Yin T, Shankar M, Herlein JA, Naidoo J, Morlock L, Williams N, Kardon RH, Anderson MG, Pieper AA, Harper MM. Early detection of subclinical visual damage after blast-mediated TBI enables prevention of chronic visual deficit by treatment with P7C3-S243. Invest Ophthalmol Vis Sci. 2014 Dec 2;55(12):8330-41. doi: 10.1167/iovs.14-15468. PubMed PMID: 25468886.
  31. Fan CW, Chen B, Franco I, Lu J, Shi H, Wei S, Wang C, Wu X, Tang W, Roth MG, Williams NS, Hirsch E, Chen C, Lum L. The Hedgehog pathway effector smoothened exhibits signaling competency in the absence of ciliary accumulation. Chem Biol. 2014 Dec 18;21(12):1680-9. doi: 10.1016/j.chembiol.2014.10.013. Epub 2014 Dec 4. Erratum in: Chem Biol. 2015 Apr 23;22(4):559. PubMed PMID: 25484239; PubMed Central PMCID: PMC4272670.
  32. Denard B, Pavia-Jimenez A, Chen W, Williams NS, Naina H, Collins R, Brugarolas J, Ye J. Identification of CREB3L1 as a Biomarker Predicting Doxorubicin Treatment Outcome. PLoS One. 2015 Jun 25;10(6):e0129233. doi: 10.1371/journal.pone.0129233. eCollection 2015. PubMed PMID: 26110425; PubMed Central PMCID: PMC4482141.
  33. Ramadori G, Konstantinidou G, Venkateswaran N, Biscotti T, Morlock L, Galié M, Williams NS, Luchetti M, Santinelli A, Scaglioni PP, Coppari R. Diet-induced unresolved ER stress hinders KRAS-driven lung tumorigenesis. Cell Metab. 2015 Jan 6;21(1):117-25. doi: 10.1016/j.cmet.2014.11.020. Epub 2014 Dec 18. PubMed PMID: 25533479; PubMed Central PMCID: PMC4305190
  34. Kemp SW, Szynkaruk M, Stanoulis KN, Wood MD, Liu EH, Willand MP, Morlock L, Naidoo J, Williams NS, Ready JM, Mangano TJ, Beggs S, Salter MW, Gordon T, Pieper AA, Borschel GH. Pharmacologic rescue of motor and sensory function by the neuroprotective compound P7C3 following neonatal nerve injury. Neuroscience. 2015 Jan 22;284:202-16. doi: 10.1016/j.neuroscience.2014.10.005. Epub 2014 Oct 13. PubMed PMID: 25313000.
  35. Ma X, Huang X, Moore Z, Huang G, Kilgore JA, Wang Y, Hammer S, Williams NS, Boothman DA, Gao J. Esterase-activatable β-lapachone prodrug micelles for NQO1-targeted lung cancer therapy. J Control Release. 2015 Feb 28;200:201-11. doi: 10.1016/j.jconrel.2014.12.027. Epub 2014 Dec 24. PubMed PMID: 25542645.
  36. Walker AK, Rivera PD, Wang Q, Chuang JC, Tran S, Osborne-Lawrence S, Estill SJ, Starwalt R, Huntington P, Morlock L, Naidoo J, Williams NS, Ready JM, Eisch AJ, Pieper AA, Zigman JM. The P7C3 class of neuroprotective compounds exerts antidepressant efficacy in mice by increasing hippocampal neurogenesis. Mol Psychiatry. 2015 Apr;20(4):500-8. doi: 10.1038/mp.2014.34. Epub 2014 Apr 22. PubMed PMID: 24751964; PubMed Central PMCID: PMC4206684.
  37. Zhang Y, Desai A, Yang SY, Bae KB, Antczak MI, Fink SP, Tiwari S, Willis JE, Williams NS, Dawson DM, Wald D, Chen WD, Wang Z, Kasturi L, Larusch GA, He L, Cominelli F, Di Martino L, Djuric Z, Milne GL, Chance M, Sanabria J, Dealwis C, Mikkola D, Naidoo J, Wei S, Tai HH, Gerson SL, Ready JM, Posner B, Willson JK, Markowitz SD. TISSUE REGENERATION. Inhibition of the prostaglandin-degrading enzyme 15-PGDH potentiates tissue regeneration. 2015 Jun 12;348(6240):aaa2340. doi: 10.1126/science.aaa2340. PubMed PMID: 26068857; PubMed Central PMCID: PMC4481126.
  38. Wolff NC, Pavía-Jiménez A, Tcheuyap VT, Alexander S, Vishwanath M, Christie A, Xie XJ, Williams NS, Kapur P, Posner B, McKay RM, Brugarolas J. High-throughput simultaneous screen and counterscreen identifies homoharringtonine as synthetic lethal with von Hippel-Lindau loss in renal cell carcinoma. 2015 Jul 10;6(19):16951-62. PubMed PMID: 26219258; PubMed Central PMCID: PMC4627284