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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. 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.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. Science. 2008 Aug 22;321(5892):1078-80. 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. 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. 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. 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. Cell. 2010 Jul 9;142(1):39-51. 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. 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. 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. 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. 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. 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. PMCID: PMC4795165.
  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. 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. 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. 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. 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. 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. 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. 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. 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. Carcinogenesis. 2013 Oct;34(10):2361-9. 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. Cell. 2013 Oct 24;155(3):552-66. 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. 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. 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. 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. 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. 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. 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. PMCID: PMC5102342.
  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. Erratum in: Chem Biol. 2015 Apr 23;22(4):559. 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. 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. 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. 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. PMCID: PMC4803448
  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. 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. Science. 2015 Jun 12;348(6240):aaa2340. 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. Oncotarget. 2015 Jul 10;6(19):16951-62. PMCID: PMC4627284.
  39. Chen B, Trang V, Lee A, Williams NS, Wilson AN, Epstein EH Jr, Tang JY, Kim J. Posaconazole, a second-generation triazole antifungal drug, inhibits the Hedgehog signaling pathway and progression of basal cell carcinoma. Mol Cancer Ther. 2016 May;15(5):866-76. PMCID: PMC4873341.
  40. Theodoropoulos PC, Gonzales SS, Winterton SE, Rodriguez-Navas C, McKnight JS, Morlock LK, Hanson JM, Cross B, Owen AE, Duan Y, Moreno JR, Lemoff A, Mirzaei H, Posner BA, Williams NS, Ready JM, Nijhawan D. Discovery of tumor-specific irreversible inhibitors of stearoyl CoA desaturase. Nat Chem Biol. 2016 Apr;12(4):218-25. PMCID: PMC4798879.
  41. Sun H, Olson KC, Gao C, Prosdocimo DA, Zhou M, Wang Z, Jeyaraj D, Youn JY, Ren S, Liu Y, Rau CD, Shah S, Ilkayeva O, Gui WJ, Williams NS, Wynn RM, Newgard CB, Cai H, Xiao X, Chuang DT, Schulze PC, Lynch C, Jain MK, Wang Y. Catabolic Defect of Branched-Chain Amino Acids Promotes Heart Failure. Circulation. 2016 May 24;133(21):2038-49. PMCID: PMC4879058.
  42. Zhang L, Theodoropoulos PC, Eskiocak U, Wang W, Moon YA, Posner B, Williams NS, Wright WE, Kim SB, Nijhawan D, De Brabander JK, Shay JW. Selective targeting of mutant adenomatous polyposis coli (APC) in colorectal cancer. Sci Transl Med. 2016 Oct 19;8(361). PubMed PMID: 27798265.
  43. Huang X, Motea EA, Moore ZR, Yao J, Dong Y, Chakrabarti G, Kilgore JA, Silvers MA, Patidar PL, Cholka A, Fattah F, Cha Y, Anderson GG, Kusko R, Peyton M, Yan J, Xie XJ, Sarode V, Williams NS, Minna JD, Beg M, Gerber DE, Bey EA, Boothman DA. Leveraging an NQO1 Bioactivatable Drug for Tumor-Selective Use of Poly(ADP-ribose) Polymerase Inhibitors. Cancer Cell. 2016 Dec 12;30(6):940-952. PMCID: PMC5161231.
  44. You L, Zhang C, Yarravarapu N, Morlock L, Wang X, Zhang L, Williams NS, Lum L, Chen C. Development of a triazole class of highly potent Porcn inhibitors. Bioorg Med Chem Lett. 2016 Dec 15;26(24):5891-5895. PMCID: PMC5142825.
  45. Tso SC, Lou M, Wu CY, Gui WJ, Chuang JL, Morlock LK, Williams NS, Wynn RM, Qi X, Chuang DT. Development of Dihydroxyphenyl Sulfonylisoindoline Derivatives as Liver-Targeting Pyruvate Dehydrogenase Kinase Inhibitors. J Med Chem. 2017 Feb 9;60(3):1142-1150. PMCID: PMC5996997
  46. Han T, Goralski M, Gaskill N, Capota E, Kim J, Ting TC, Xie Y, Williams NS, Nijhawan D. Anticancer sulfonamides target splicing by inducing RBM39 degradation via recruitment to DCAF15. Science. 2017 Apr 28;356(6336). PMID: 28302793
  47. McCarthy JS, Lotharius J, Rückle T, Chalon S, Phillips MA, Elliott S, Sekuloski S, Griffin P, Ng CL, Fidock DA, Marquart L, Williams NS, Gobeau N, Bebrevska L, Rosario M, Marsh K, Möhrle JJ. Safety, tolerability, pharmacokinetics, and activity of the novel long-acting antimalarial DSM265: a two-part first-in-human phase 1a/1b randomised study. Lancet Infect Dis. 2017 Jun;17(6):626-635. PMCID: PMC5446412.
  48. Luthra P, Aguirre S, Yen BC, Pietzsch CA, Sanchez-Aparicio MT, Tigabu B, Morlock LK, García-Sastre A, Leung DW, Williams NS, Fernandez-Sesma A, Bukreyev A, Basler CF. Topoisomerase II Inhibitors Induce DNA Damage-Dependent Interferon Responses Circumventing Ebola Virus Immune Evasion. MBio. 2017 Apr 4;8(2). pii: e00368-17. PMCID: PMC5380843.
  49. Eskiocak B, McMillan E, Mendiratta S, Kollipara R, Zhang H, Humphries C, Wang C, Garcia-Rodriguez J, Ding M, Zaman A, Rosales T, Eskiocak U, Smith MP, Sudderth J, Komurov K, DeBerardinis RJ, Wellbrock C, Davies MA, Wargo JA, Yu Y, De Brabander JK, Williams NS, Chin L, Rizos H, Long GV, Kittler R, White M. Biomarker Accessible and Chemically Addressable Mechanistic Subtypes of BRAF Melanoma. Cancer Discov. 2017 Aug;7(8):832-851. PMCID: PMC5540806.
  50. Antczak MI, Zhang Y, Wang C, Doran J, Naidoo J, Voruganti S, Williams NS, Markowitz SD, Ready JM. Inhibitors of 15-Prostaglandin Dehydrogenase To Potentiate Tissue Repair. J Med Chem. 2017 May 11;60(9):3979-4001. PMCID: PMC5580352.
  51. Moon J, Zhou H, Zhang LS, Tan W, Liu Y, Zhang S, Morlock LK, Bao X, Palecek SP, Feng JQ, Williams NS, Amatruda JF, Olson EN, Bassel-Duby R, Lum L. Blockade to pathological remodeling of infarcted heart tissue using a porcupine antagonist. Proc Natl Acad Sci U S A. 2017 Feb 14;114(7):1649-1654. PMCID: PMC5320972.
  52. Nanayakkara AK, Follit CA, Chen G, Williams NS, Vogel PD, Wise JG. Targeted inhibitors of P-glycoprotein increase chemotherapeutic-induced mortality of multidrug resistant tumor cells. Sci Rep. 2018 Jan 17;8(1):967. doi: 10.1038/s41598-018-19325-x. PubMed PMID: 29343829; PubMed Central PMCID: PMC5772368.
  53. Qi C, Wang X, Shen Z, Chen S, Yu H, Williams N, Wang G. Anti-mitotic chemotherapeutics promote apoptosis through TL1A-activated death receptor 3 in cancer cells. Cell Res. 2018 May;28(5):544-555. doi: 10.1038/s41422-018-0018-6. Epub 2018 Mar 1. PubMed PMID: 29497138; PubMed Central PMCID: PMC5951888.
  54. McMillan EA, Ryu MJ, Diep CH, Mendiratta S, Clemenceau JR, Vaden RM, Kim JH, Motoyaji T, Covington KR, Peyton M, Huffman K, Wu X, Girard L, Sung Y, Chen PH, Mallipeddi PL, Lee JY, Hanson J, Voruganti S, Yu Y, Park S, Sudderth J, DeSevo C, Muzny DM, Doddapaneni H, Gazdar A, Gibbs RA, Hwang TH, Heymach JV, Wistuba I, Coombes KR, Williams NS, Wheeler DA, MacMillan JB, Deberardinis RJ, Roth MG, Posner BA, Minna JD, Kim HS, White MA. Chemistry-First Approach for Nomination of Personalized Treatment in Lung Cancer. Cell. 2018 https://doi.org/10.1016/j.cell.2018.03.02 PubMed PMID: 29681454.
  55. Winterton SE, Capota E, Wang X, Chen H, Mallipeddi PL, Williams NS, Posner BA, Nijhawan D, Ready JM. Discovery of Cytochrome P450 4F11 Activated Inhibitors of Stearoyl Coenzyme A Desaturase. J Med Chem. 2018 Jun 28;61(12):5199-5221. PubMed PMID: 29869888.
  56. Voorhees JR, Remy MT, Cintrón-Pérez CJ, El Rassi E, Khan MZ, Dutca LM, Yin TC, McDaniel LN, Williams NS, Brat DJ, Pieper AA. (-)-P7C3-S243 Protects a Rat Model of Alzheimer's Disease From Neuropsychiatric Deficits and Neurodegeneration Without Altering Amyloid Deposition or Reactive Glia. Biol Psychiatry. 2018 Oct 1;84(7):488-498. PMID: 29246437.
  57. Bauman MD, Schumann CM, Carlson EL, Taylor SL, Vázquez-Rosa E, Cintrón-Pérez CJ, Shin MK, Williams NS, Pieper AA. Neuroprotective efficacy of P7C3 compounds in primate hippocampus. Transl Psychiatry. 2018 Sep 26;8(1):202. PMCID: PMC6158178.
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