Wagner Group: Publications

1. Dirice E, Walpita D, Vetere A, Meier BC, Kahraman S, Hu J, Dancik V, Burns SM, Gilbert TJ, Olson DE, Clemons PA, Kulkarni RN*, Wagner BK*. Inhibition of DYRK1A stimulates human beta-cell proliferation. Diabetes 2016; accepted.

2. Wagner BK, Schreiber SL. The power of sophisticated phenotypic screening and modern mechanism-of-action methods. Cell Chem BIol 2016; 23:3-9.

3. Rees MG, Seashore-Ludlow B, Cheah JH, Adams DJ, Price EV, Gill S, Javaid S, Coletti ME, Jones VL, Bodycombe NE, Soule CK, Alexander B, Li A, Montgomery P, Kotz JD, Hon CS, Munoz B, Liefeld T, Dančík V, Haber DA, Clish CB, Bittker JA, Palmer M, Wagner BK, Clemons PA, Shamji AF, Schreiber SL. Correlating chemical sensitivity and basal gene expression reveals mechanism of action. Nat Chem Biol 2016; 12:109-116.

4. de Waal L, Lewis TA, Rees MG, Tsherniak A, Wu X, Choi PS, Gechijian L, Hartigan C, Faloon PW, Hickey MJ, Tolliday N, Carr SA, Clemons PA, Munoz B, Wagner BK, Shamji AF, Koehler AN, Schenone M, Burgin AB, Schreiber SL, Greulich H, Meyerson M. Identification of cancer-cytotoxic modulators of PDE3A by predictive chemogenomics. Nat Chem Biol 2016; 12:102-108.

5. Wagner FF, Lundh M, Kaya T, McCarren P, Zhang YL, Chattopadhyay S, Gale JP, Galbo T, Fisher SL, Meier BC, Vetere A, Richardson S, Morgan NG, Christensen DP, Gilbert TJ, Hooker JM, Leroy M, Walpita D, Mandrup-Poulsen T, Wagner BK, Holson EB. An Isochemogenic Set of Inhibitors To Define the Therapeutic Potential of Histone Deacetylases in β-Cell Protection. ACS Chem Biol 2016; 11:363-374.

6. Wagner BK. The resurgence of phenotypic screening in drug discovery and development. Expert Opin Drug Discov 2016; 11:121-125.

7. Bhatt S, Gupta MK, Khamaisi M, Martinez R, Gritsenko MA, Wagner BK, Guye P, Busskamp V, Shirakawa J, Wu G, Liew CW, Clauss TR, Valdez I, El Ouaamari A, Dirice E, Takatani T, Keenan HA, Smith RD, Church G, Weiss R, Wagers AJ, Qian WJ, King GL, Kulkarni RN. Preserved DNA damage checkpoint pathway protects against complications in long-standing type 1 diabetes. Cell Metab 2015; 22:239-252.

8. Chou DH-C, Vetere A, Choudhary A, Scully SS, Schenone M, Tang A, Gomez R, Burns SM, Lundh M, Vital T, Comer E, Faloon PW, Dančík V, Ciarlo C, Paulk J, Dai M, Reddy C, Sun H, Young M, Donato N, Jaffe, JD, Clemons PA, Palmer MA, Carr SA, Schreiber SL, Wagner BK. Kinase-independent small-molecule inhibition of JAK-STAT signaling. JACS 2015; 137:7929-7934.

9. Scully SS, Zheng S, Wagner BK, Schreiber SL. Synthesis of oxazocenones via gold(I)-catalyzed 8-endo-dig hydroalkoxylation of alkynamides. Org Lett 2015; 17:418-421.

10. Burns SM, Vetere A, Walpita D, Dančík V, Khodier C, Perez JR, Clemons PA, Wagner BK, Altshuler D. High-throughput luminescent reporter of pancreatic beta-cell function enables discovery of small-molecule regulators of insulin secretion. Cell Metabolism 2015; 21:126-137.

11. Johannessen CM, Clemons PA, Wagner BK. Integrating phenotypic small-molecule profiling and human genetics: the next phase in drug discovery. Trends Genet 2015; 31:16-23.

12. Dahllöf MS, Christensen DP, Harving M, Wagner BK, Mandrup-Poulsen T, Lundh M. HDAC inhibitor-mediated beta-cell protection against cytokine-induced toxicity is STAT1 Tyr701 phosphorylation independent. J Interferon Cytokine Res 2015; 35:63-70.

13. Walpita D, Wagner BK. Evaluation of compounds in primary human islet cell culture. Curr Prot Chem Biol 2014; 6:157-168.

14. Wawer MJ, Jaramillo DE, Dancik V, Fass DM, Haggarty SJ, Shamji AF, Wagner BK, Schreiber SL, Clemons PA. Automated structure-activity relationship mining: connecting chemical structure to biological profiles. J Biomol Screen 2014; 19:738-748.

15. Meier BC, Wagner BK. Inhibition of HDAC3 as a strategy for developing novel diabetes therapeutics. Epigenomics 2014; 6:209-214.

16. Vetere A, Choudhary A, Burns SM, Wagner BK. Targeting the pancreatic beta cell to treat diabetes. Nat Rev Drug Disc 2014; 13:278-289.

17. Dančík V, Carrel H, Bodycombe NE, Seiler KP, Fomina-Yadlin D, Kubicek ST, Hartwell K, Shamji AF, Wagner BK, Clemons PA. Connecting small molecules with similar assay performance profiles leads to new biological hypotheses. J Biomol Screen 2014; 19:771-781.

18. Choudhary A, Hu He KH, Mertins P, Udeshi ND, Dančík V, Fomina-Yadlin D, Kubicek S, Clemons PA, Schreiber SL, Carr SA, Wagner BK. Quantitative-proteomic comparison of alpha and beta cells to uncover novel targets for lineage reprogramming. PLoS ONE 2014; 9:e95194. PMCID: PMC3997365

19. Yuan Y, Hartland K, Boskovic Z, Wang Y, Walpita D, Lysy PA, Zhong C, Young DW, Kim YK, Tolliday NJ, Sokal EM, Schreiber SL, Wagner BK. A small-molecule inducer of PDX1 expression identified by high-throughput screening. Chem Biol 2013; 20:1513-1522. PMCID: PMC3927138

20. Lundh M, Scully SS, Mandrup-Poulsen T, Wagner BK. Small-molecule inhibition of inflammatory beta-cell death. Diab Obes Metab 2013; 15(Suppl. 3):176-184. PMCID: PMC3777666

21. Yuan Y, Tang AJ, Castoreno AB, Kuo S-Y, Wang Q, Kuballa P, Xavier R, Shamji AF, Schreiber SL, Wagner BK. Gossypol and an HMT G9a inhibitor act in synergy to induce cell death in pancreatic cancer cells. Cell Death & Dis 2013; 4:e690. PMCID: PMC3702302

22. Scully SS, Tang AJ, Lundh M, Mosher CM, Perkins KM, Wagner BK. Small-molecule inhibitors of cytokine-mediated STAT1 signal transduction in ß-cells with improved aqueous solubility. J Med Chem 2013; 56:4125-4129. PMCID: PMC3690275

23. Schenone M, Dančík V, Wagner BK, Clemons PA. Target identification and mechanism of action in chemical biology and drug discovery. Nat Chem Biol 2013; 9:232-240.

24. Adams DJ, Boskovic ZV, Theriault JR, Wang AJ, Stern AM, Wagner BK, Shamji AF, Schreiber SL. High-Throughput Screening Identifies Small-Molecule Enhancers of Reactive Oxygen Species that are Nontoxic or Cause Genotype-Selective Cell Death. ACS Chem Biol 2013; 8:923-929. PMCID: PMC3658551

25. Hu He KH, Gilbert TJ, Fomina-Yadlin D, and Wagner BK. Small molecule-induced beta-cell regeneration from alternate cell sources. Curr Tissue Eng 2012; 1:83-90.

26. Adams DJ, Dai M, Pellegrino G, Wagner BK, Stern AM, Shamji AF, and Schreiber SL. Synthesis, cellular evaluation and mechanism-of-action of piperlongumine analogs. Proc Natl Acad Sci USA 2012; 109:15115-15120. PMCID: PMC3458345

27. Vetere A, and Wagner BK. Chemical methods to induce beta-cell proliferation. Intl J Endocrinol 2012; 2012:925143. PMCID: PMC3395230

28. Chou DH-C, Holson EB, Wagner FF, Tang AJ, Maglathlin RL, Lewis TA, Schreiber SL, and Wagner BK. Inhibition of histone deacetylase 3 protects beta cells from cytokine-induced apoptosis. Chem Biol 2012; 19:669-673. PMCID: PMC3383610

29. Yuan Y, Wang Q, Paulk J, Kubicek S, Kemp M, Adams DJ, Shamji AF, Wagner BK, and Schreiber SL. A small-molecule probe of the histone methyltransferase G9a induces cellular senescence in pancreatic adenocarcinoma. ACS Chem Biol 2012; 7:1152-1157. PMCID: PMC3401036

30. Kubicek S, Gilbert JC, Fomina-Yadlin D, Gitlin AD, Yuan Y, Wagner FF, Holson EB, Luo T, Lewis TA, Taylor B, Gupta S, Shamji AF, Wagner BK, Clemons PA, and Schreiber SL. Chromatin-targeting small molecules cause class-specific transcriptional changes in pancreatic endocrine cells. Proc Natl Acad Sci USA 2012; 109:5364-5369. PMCID: PMC3325696

31. Fomina-Yadlin D, Kubicek S, Vetere A, Hu He K, Schreiber SL, and Wagner BK. GW8510 increases insulin expression in pancreatic alpha cells through activation of p53 transcriptional activity. PLoS ONE 2012; 7:e28808. PMCID: PMC3252286

32. Walpita D, Hasaka T, Spoonamore J, Vetere A, Takane KK, Fomina-Yadlin D, Fiaschi-Taesch N, Shamji A, Clemons PA, Stewart AF, Schreiber SL, and Wagner BK. A human islet cell-culture system for high-throughput screening. J Biomol Screen 2012; 17:509-518. Featured image on issue cover.

33. Wagner BK, Gilbert TJ, Hanai JI, Imamura S, Bodycombe NE, Bon R, Waldmann H, Clemons PA, Sukhatme VP, and Mootha VK. A small-molecule screening strategy to identify suppressors of statin myopathy. ACS Chem Biol 2011; 6:900-904. PMCID: PMC3176973

34. Chou DH-C, Duvall JR, Gerard B, Liu H, Pandya BA, Suh BC, Forbeck EM, Faloon P, Wagner BK, and Marcaurelle LA. Synthesis of a novel suppressor of ß-cell apoptosis via diversity-oriented synthesis. ACS Med Chem Lett 2011; 2:698-702. PMCID: PMC2924935

35. Faloon PW, Chou DHC, Forbeck EM, Walpita D, Morgan B, Buhrlage S, Ting A, Perez J, MacPherson LJ, Duvall JR, Dandapani S, Marcaurelle LA, Munoz B, Palmer M, Foley M, Wagner B, and Schreiber SL. Identification of small molecule inhibitors that suppress cytokine-induced apoptosis in human pancreatic islet cells. Probe Reports from the NIH Molecular Libraries Program (Internet). Bethesda (MD): National Center for Biotechnology Information, May 26, 2011.

36. Clemons PA, Wilson JA, Dančík V, Muller S, Carrinski HA, Wagner BK, Koehler AN, and Schreiber SL. Quantifying structure and performance diversity for sets of small molecules comprising small-molecule screening collections. Proc Natl Acad Sci USA 2011; 108:6817. PMCID: PMC3084049

37. Bochner BB, Siri M, Huang RH, Noble S, Lei X-H, Clemons PA, and Wagner BK. Assay of the multiple energy-producing pathways of mammalian cells. PLoS ONE 2011; 6:e18147. PMCID: PMC3063803

38. Wagner BK. Screening: Low-fat worms on drugs. Nat Chem Biol 2011; 7:194-195.

39. Kim YK, Lee J-S, Bi X, Ha H-H, Ng SH, Ahn Y, Wagner BK, Clemons PA, and Chang YT. The binding of fluorophores to proteins depends on the cellular environment. Angew Chemie 2011; 50:2761-2763.

40. Wagner BK. Grand Challenge Commentary: Chemical transdifferentiation and regenerative medicine. Nat Chem Biol 2010; 6:877-879.

41. Clemons PA, Bodycombe NE, Carrinski HA, Wilson JA, Shamji AF, Wagner BK, Koehler AN, and Schreiber SL. Small molecules of different synthetic and natural origins have distinct distributions of structural complexity that correlate with protein-binding profiles. Proc Natl Acad Sci USA 2010; 107:18787-18792. PMCID: PMC2973913

42. Cancer Target Discovery and Development Network, Schreiber SL, Shamji AF, Clemons PA, Hon C, Koehler AN, Munoz B, Palmer M, Stern AM, Wagner BK, Powers S, Lowe SW, Guo X, Krasnitz A, Sawey ET, Sordella R, Stein L, Trotman LC, Califano A, Dalla-Favera R, Ferrando A, Iavarone A, Pasqualucci L, Silva J, Stockwell BR, Hahn WC, Chin L, DePinho RA, Boehm JS, Gopal S, Huang A, Root DE, Weir BA, Gerhard DS, Zenklusen JC, Roth MG, White MA, Minna JD, MacMillan JB, and Posner BA. Towards patient-based cancer therapeutics. Nat Biotechnol 2010; 28:904-906. PMCID: PMC2939009

43. Fomina-Yadlin D, Kubicek S, Walpita D, Dančík V, Hecksher-Sørensen J, Bittker JA, Sharifnia T, Shamji A, Clemons PA, Wagner BK, and Schreiber SL. Small-molecule inducers of insulin expression in pancreatic alpha cells. Proc Natl Acad Sci USA 2010; 107:15099-15104. PMCID: PMC2930573

44. Chou DH-C, Bodycombe NE, Carrinski HA, Lewis TA, Clemons PA, Schreiber SL, and Wagner BK. Small-molecule suppressors of cytokine-induced beta-cell apoptosis. ACS Chem Biol 2010; 5:729-734. PMCID: PMC2924935

45. Wagner BK and Clemons PA. Connecting synthetic chemistry decisions to cell and genome biology using small-molecule phenotypic profiling. Curr Opin Chem Biol 2009; 13:539-548. PMCID: PMC2787914

46. Wagner BK, Tolliday NJ, and Clemons PA, Eds. Cell-based assays for high-throughput screening. Methods Mol Biol 2009; vol. 486. Humana Press, Totowa, N.J.

47. Wagner BK and Arany Z. High-throughput real-time PCR for detection of gene expression levels. (Book Chapter) Methods Mol Biol 2009; 486:167-175.

48. Tanikawa T, Fridman M, Zhu W, Faulk B, Joseph IC, Kahne D, Wagner BK, and Clemons PA. Using biological performance similarity to inform disaccharide library design. J Am Chem Soc 2009; 131:5075-5083. PMCID: PMC2730776

49. Arany Z, Wagner BK, Ma Y, Chinsomboon J, Laznik D, and Spiegelman BM. Gene expression-based screening identifies microtubule inhibitors as inducers of PGC-1a and oxidative phosphorylation. Proc Natl Acad Sci USA 2008; 105:4721-4726. PMCID: PMC2290788

50. Wagner BK, Carrinski HA, Ahn YH, Kim YK, Gilbert TJ, Fomina DA, Schreiber SL, Chang YT, and Clemons PA. Small-molecule fluorophores to detect cell-state switching in the context of high-throughput screening. J Am Chem Soc 2008; 130:4208-4209.

51. Wagner BK*, Kitami T*, Gilbert TJ, Peck D, Ramanathan A, Schreiber SL, Golub TR, and Mootha VK. Large-scale chemical dissection of mitochondrial function. Nat Biotechnol 2008; 26:343-351 * Equal contributors. (News and Views report in same issue, 26:294-296). PMCID: PMC2715872

52. Wagner BK, Haggarty SJ, and Clemons PA. Chemical genomics: probing protein function using small molecules. Am J Pharmacogenomics 2004; 4:313-320.

53. Wagner BK and Clemons PA. Dual-purpose drug discovery. Trends Biotech 2002; 20:492-493.

54. Wagner BK and Clemons PA. An even-handed approach. Trends Biotech 2001; 20:53.

55. Clemons PA and Wagner BK. Hay in a needlestack? Trends Biotech 2001; 19:435-436.

56. Wagner BK and Clemons PA. Better signaling through chemistry. Trends Biotech 2001; 19:127.

57. Clemons PA, Koehler AN, Wagner BK, Sprigings TG, Spring DR, King RW, Schreiber, SL, and Foley MA. one-bead, one-stock solution approach to chemical genetics, part two. Chem Biol 2001; 8:1183-1195.

58. Andreadis A, Wagner BK, Broderick JA, and Kosik KS. A tau promoter region without neuronal specificity. J Neurochem 1996; 66:2257-2263.