***Any published research which received funding from the University of Wisconsin Carbone Cancer Center (UWCCC) Support Grant (CCSG), including the use of UWCCC Shared Resources to generate or analyze data or conduct clinical trials, must reference the UWCCC. See Acknowledging UWCCC in Publications, Posters, and Presentations. Please acknowledge “UWCCC Small Molecule Screening Facility” for any work supported by the SMSF. Thank you!***
Sample Acknowledgment “The author(s) thank the University of Wisconsin Carbone Cancer Center Small Molecule Screening Facility, supported by P30 CA014520, for use of its facilities and services.”
Research reported in the following publications utilized HTS, assay, chemistry or modeling services of the Small Molecule Screening Facility.
| Alnammi M, Shengchao L, Ericksen SS, Ananiev GE, Voter AF, Guo S, Keck JL, Hoffmann FM, Wildman SA, Gitter A. Evaluating Scalable Supervised Learning for Synthesize-on-Demand Chemical Libraries. J. Chem. Inf. Model. 2023 Aug 25;63(17):5513-5528. doi: 10.1021/acs.jcim.3c00912. |
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| Polaske TJ, Gahan CG, Nyffeler KE, Lynn DM, Blackwell HE. Identification of Small Molecules That Strongly Inhibit Bacterial Quorum Sensing Using a High-Throughput Lipid Vesicle Lysis Assay. Cell Chem. Biol. 2022 Apr 21;29(4):605-614.e4. doi: 10.1016/j.chembiol.2021.12.005. |
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| Liu WH, Miner III RE, Albaugh BN, Ananiev GE, Wildman SA, Denu JM. Discovery and Mechanism of Small Molecule Inhibitors Selective for the Chromatin-Binding Domains of Oncogenic UHRF1. Biochemistry. 2022 Feb 10;61(5):354-366. doi: 10.1021/acs.biochem.1c00698. |
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| Bates PD, Rakhmilevich AL, Cho MM, Bouchlaka MN, Rao SL, Hales JM, Orentas RJ, Fry TJ, Gilles SD, Sondel PM, Capitini CM. Combining Immunocytokine and Ex Vivo Activated NK Cells as a Platform for Enhancing Graft-Versus-Tumor Effects Against GD2+ Murine Neuroblastoma. Front. Immunol. 2021 Aug 19;12:668307. doi: 10.3389/fimmu.2021.668307. |
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| Zhang F, Zhao M, Braun DR, Ericksen SS, Piotrowski JS, Nelson J, Peng J, Ananiev GE, Chanana S, Barns K, Fossen J, Sanchez H, Chevrette MG, Guzei IA, Zhao C, Guo L, Tang W, Currie CR, Rajski SR, Audhya A, Andes DR, Bugni TS. A Marine Microbiome Antifungal Targets Urgent-Threat Drug-Resistant Fungi. Science. 2020 Nov 20;370(6519):974-978. doi: 10.1126/science.abd6919. |
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| Zhang H, Ericksen SS, Lee CP, Ananiev GE, Wlodarchak N, Yu P, Mitchell JC, Gitter A, Wright SJ, Hoffmann FM, Wildman SA, Newton MA. Predicting Kinase Inhibitors Using Bioactivity Matrix Derived Informer Sets. PLoS Comput Biol. 2019 Aug 5;15(8):e1006813. doi: 10.1371/journal.pcbi.1006813. |
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| Chevrette MG, Carlson CM, Ortega HE, Thomas C, Ananiev GE, Barns KJ, Book AJ, Cagnazzo J, Carlos C, Flanigan W, Grubbs KJ, Horn HA, Hoffmann FM, Klassen JL, Knack JJ, Lewin GR, McDonald BR, Muller L, Melo WGP, Pinto-Tomás AA, Schmitz A, Wendt-Pienkowski E, Wildman S, Zhao M, Zhang F, Bugni TS, Andes DR, Pupo MT, Currie CR. The Antimicrobial Potential of Streptomyces from Insect Microbiomes. Nat Commun. 2019 Jan 31;10(1):516. doi: 10.1038/s41467-019-08438-0. |
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| Liu S, Alnammi M, Ericksen SS, Voter AF, Ananiev GE, Keck JL, Hoffmann FM, Wildman SA, Gitter A. Practical Model Selection for Prospective Virtual Screening. J Chem Inf Model. 2019:59(1):282-293. doi: 10.1021/acs.jcim.8b00363. |
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| Zhang F, Braun DR, Ananiev GE, Hoffmann FM, Tsai IW, Rajski SR, Bugni TS. Biemamides A-E, Inhibitors of the TGF-β Pathway That Block the Epithelial to Mesenchymal Transition. Org Lett. 2018;20(18):5529-5532. |
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| Zhang F, Barns K, Hoffmann FM, Braun DR, Andes DR, Bugni TS. Thalassosamide, a Siderophore Discovered from the Marine-Derived Bacterium Thalassospira profundimaris. J Nat Prod. 2017;80(9):2551-2555. |
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| Ericksen SS, Wu H, Zhang H, Michael LA, Newton MA, Hoffmann FM, Wildman SA. Machine Learning Consensus Scoring Improves Performance Across Targets in Structure-Based Virtual Screening. J Chem Inf Model. 2017;57(7):1579-1590. |
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| Zhang X, Jiang S, Mitok KA, Li L, Attie AD, Martin TFJ. BAIAP3, a C2 domain-containing Munc13 protein, controls the fate of dense-core vesicles in neuroendocrine cells. J Cell Biol. 2017;216(7):2151-2166. |
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| Voter AF, Killoran MP, Ananiev GE, Wildman SA, Hoffmann FM, Keck JL. A High-Throughput Screening Strategy to Identify Inhibitors of SSB Protein-Protein Interactions in an Academic Screening Facility. SLAS Discov. 2017:2472555217712001. |
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| Li M, Zhao H, Ananiev GE, Musser MT, Ness KH, Maglaque DL, Saha K, Bhattacharyya A, Zhao X. Establishment of Reporter Lines for Detecting Fragile X Mental Retardation (FMR1) Gene Reactivation in Human Neural Cells. Stem Cells. 2017;35(1):158-169. |
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| Chamcheu JC, Adhami VM, Esnault S, Sechi M, Siddiqui IA, Satyshur KA, Syed DN, Dodwad SM, Chaves-Rodriquez MI, Longley BJ, Wood GS, Mukhtar H. Dual Inhibition of PI3K/Akt and mTOR by the Dietary Antioxidant, Delphinidin, Ameliorates Psoriatic Features In Vitro and in an Imiquimod-Induced Psoriasis-Like Disease in Mice. Antioxid Redox Signal. 2017;26(2):49-69. |
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| Voter AF, Manthei KA, Keck JL. A High-Throughput Screening Strategy to Identify Protein-Protein Interaction Inhibitors That Block the Fanconi Anemia DNA Repair Pathway. J Biomol Screen. 2016;21(6):626-33. |
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| Zhao Z, Wang L, James T, Jung Y, Kim I, Tan R, Hoffmann FM, Xu W. Reciprocal Regulation of ERα and ERβ Stability and Activity by Diptoindonesin G. Chem Biol. 2015;22(12):1608-21. |
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| Goel SA, Guo LW, Wang B, Guo S, Roenneburg D, Ananiev GE, Hoffmann FM, Kent KC. High-Throughput Screening Identifies Idarubicin as a Preferential Inhibitor of Smooth Muscle versus Endothelial Cell Proliferation. PLoS One. 2014;9(2). |
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| Mehraein-Ghomi F, Kegel SJ, Church DR, Schmidt JS, Reuter QR, Saphner EL, Basu HS, Wilding G. Targeting androgen receptor and JunD interaction for prevention of prostate cancer progression. Prostate, 2014; 74: 792–803. doi: 10.1002/pros.22800 |
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| Guo F, Wan L, Zheng A, Stanevich V, Wei Y, Satyshur KA, Shen M, Lee W, Kang Y, Xing Y. Structural insights into the tumor-promoting function of the MTDH-SND1 complex. Cell Rep. 2014 Sep 25;8(6):1704-13. doi: 10.1016/j.celrep.2014.08.033. Epub 2014 Sep 18. |
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| Chu UB, Vorperian SK, Satyshur K, Eickstaedt K, Cozzi NV, Mavlyutov T, Hajipour AR, Ruoho AE. Noncompetitive inhibition of indolethylamine-N-methyltransferase by N,N-dimethyltryptamine and N,N-dimethylaminopropyltryptamine. Biochemistry. 2014 May 13;53(18):2956-65. doi: 10.1021/bi500175p. Epub 2014 Apr 28. |
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| Brandhorst TT, Roy R, Wüthrich M, Nanjappa S, Filutowicz H, Galles K, Tonelli M, McCaslin DR, Satyshur K, Klein B. Structure and function of a fungal adhesin that binds heparin and mimics thrombospondin-1 by blocking T cell activation and effector function. PLoS Pathog. 2013;9(7):e1003464. |
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| Zeng H, Wu J, Bedford MT, Sbardella G, Hoffmann FM, Bi K, Xu W. A TR-FRET-based functional assay for screening activators of CARM1. Chembiochem. 2013 May 10;14(7):827-35. |
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| Pusztai E, Toulokhonova S, Temple N, Albright H, Zakai U, Guo G, Guzei I, Hu R, West, R. Synthesis and Photophysical Properties of Asymmetric Substituted Silafluorenes. Organometallics. 2013;32(9):2529-2535. |
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| Ozawa M, Shimojima M, Goto H, Watanabe S, Hatta Y, Kiso M, Furuta Y, Horimoto T, Peters N, Hoffmann FM, Kawaoka Y. A cell-based screening system for influenza A viral RNA transcription/replication inhibitors. Scientific Reports. 2013;3. |
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| Moser LA1, Pollard AM, Knoll LJ. A genome-wide siRNA screen to identify host factors necessary for growth of the parasite Toxoplasma gondii. PLoS One. 2013 Jun 28;8(6):e68129. doi: 10.1371/journal.pone.0068129. Print 2013. |
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| Wagner EK, Nath N, Flemming R, Feltenberger JB, Denu JM. Identification and Characterization of Small Molecule Inhibitors of a Plant Homeodomain Finger. Biochemistry. 2012;51(41):8293-306. |
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| Tomasini-Johansson BR, Johnson IA, Hoffmann FM, Mosher DF. Quantitative microtiter fibronectin fibrillogenesis assay: use in high throughput screening for identification of inhibitor compounds. Matrix Biol. 2012;31(6):360-7. |
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| Tebbets B, Stewart D, Lawry S, Nett J, Nantel A, Andes D, Klein BS. Identification and characterization of antifungal compounds using a Saccharomyces cerevisiae reporter bioassay. PLoS One. 2012;7(5). |
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| Khan N, Afaq F, Khusro FH, Adhami VM, Suh Y, Mukhtar H. Dual inhibition of phosphatidylinositol 3-kinase/Akt and mammalian target of rapamycin signaling in human nonsmall cell lung cancer cells by a dietary flavonoid fisetin. Int J Cancer. 2012;130(7):1695-705. |
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| Parrish JD, Ischay MA, Lu Z, Guo S, Peters NR, Yoon TP. Endoperoxide synthesis by photocatalytic aerobic [2 + 2 + 2] cycloadditions. Org Lett. 2012;14(6):1640-3. |
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| Ding Y, Ko MH, Pehar M, Kotch F, Peters NR, Luo Y, Salamat SM, Puglielli L. Biochemical inhibition of the acetyltransferases ATase1 and ATase2 reduces β-secretase (BACE1) levels and Aβ generation. J Biol Chem. 2012;287(11):8424-33. |
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| Powell E, Shanle E, Brinkman A, Li J, Kales S, Wisinski K, and Xu W. Identification of estrogen receptor dimer selective ligands reveals growth-inhibitory effects on cells that co-express ERα and ERβ. PLoS One. 2012;7(2). |
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| Wagner EK, Albaugh BN, Denu JM. High-throughput strategy to identify inhibitors of histone-binding domains. Methods Enzymol. 2012;512:161-85. |
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| Huang HS, Pyeon D, Pearce SM, Lank SM, Griffin LM, Ahlquist P, Lambert PF. Novel antivirals inhibit early steps in HPV infection. Antiviral Res. 2012;93(2):280-7. |
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| Shanle, EK, Hawse JR, Xu W. Generation of stable reporter breast cancer cell lines for the identification of ER subtype selective ligands. Biochem Pharmacol. 2011;82(12):1940-9. |
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| Wiemer AJ, Hegde S, Gumperz JE, Huttenlocher A. A live imaging cell motility screen identifies prostaglandin E2 as a T cell stop signal antagonist. J Immunol. 2011;187(7):3663-70. |
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| Phan T, Yu X, Kunnimalaiyaan M, Chen H. Antiproliferative effect of chrysin on anaplastic thyroid cancer. J Surg Res. 2011;170(1):84-8. |
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| Truong M, Cook MR, Pinchot SN, Kunnimalaiyaan M, Chen H. Resveratrol induces Notch2-mediated apoptosis and suppression of neuroendocrine markers in medullary thyroid cancer. Ann Surg Oncol. 2011;18(5):1506-11. |
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| Chen G, Gulbranson DR, Hou Z, Bolin JM, Ruotti V, Probasco MD, Smuga-Otto K, Howden SE, Diol NR, Propson NE, Wagner R, Lee GO, Antosiewicz-Bourget J, Teng JM, Thomson JA. Chemically defined conditions for human iPSC derivation and culture. Nat Methods. 2011;8(5):424-9. |
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| Siddiqui IA, Asim M, Hafeez BB, Adhami VM, Tarapore RS, Mukhtar H. Green tea polyphenol EGCG blunts androgen receptor function in prostate cancer. FASEB J. 2011;25(4):1198-207. |
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| Bhatia N, Yang B, Xiao TZ, Peters N, Hoffmann FM, Longley BJ. Identification of novel small molecules that inhibit protein-protein interactions between MAGE and KAP-1. Arch Biochem Biophys. 2011;508(2):217-21. |
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| Pinchot SN, Jaskula-Sztul R, Ning L, Peters NR, Cook MR, Kunnimalaiyaan M, Chen H. Identification and validation of Notch pathway activating compounds through a novel high-throughput screening method. Cancer. 2011;117(7):1386-98. |
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| Zarebczan B, Pinchot SN, Kunnimalaiyaan M, Chen H. Hesperetin, a potential therapy for carcinoid cancer. Am J Surg. 2011;201(3):329-32; discussion 333. |
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| Schiro MM, Stauber SE, Peterson TL, Krueger C, Darnell SJ, Satyshur KA, Drinkwater NR, Newton MA, Hoffmann FM. Mutations in protein-binding hot-spots on the hub protein Smad3 differentially affect its protein interactions and Smad3-regulated gene expression. PLoS One. 2011;6(9). |
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| Yu Z, Zhao LX, Jiang CL, Duan Y, Wong L, Carver KC, Schuler LA, Shen B. Bafilomycins produced by an endophytic actinomycete Streptomyces sp. YIM56209. J Antibiot (Tokyo). 2011;64(1):159-62. |
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| Maurer LM, Tomasini-Johansson BR, Ma W, Annis DS, Eickstaedt NL, Ensenberger MG, Satyshur KA, Mosher DF. Extended binding site on fibronectin for the functional upstream domain of protein F1 of Streptococcus pyogenes. J Biol Chem. 2010;285(52):41087-99. Erratum in: J Biol Chem. 2011;286(33). |
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| Lipinski RJ, Bushman W. Identification of Hedgehog signaling inhibitors with relevant human exposure by small molecule screening Toxicol In Vitro. 2010 Aug;24(5):1404-9. doi: 10.1016/j.tiv.2010.04.011.010.04.011 |
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| Kolonko EM, Albaugh BN, Lindner SE, Chen Y, Satyshur KA, Arnold KM, Kaufman PD, Keck JL, Denu JM. Catalytic activation of histone acetyltransferase Rtt109 by a histone chaperone. Proc Natl Acad Sci U S A. 2010;107(47):20275-80. |
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| Powell E, Huang SX, Xu Y, Rajski SR, Wang Y, Peters N, Guo S, Xu HE, Hoffmann FM, Shen B, Xu W. Identification and characterization of a novel estrogenic ligand actinopolymorphol A. Biochem Pharmacol. 2010;80(8):1221-9. |
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| Chen G, Hou Z, Gulbranson DR, Thomson JA. Actin-myosin contractility is responsible for the reduced viability of dissociated human embryonic stem cells. Cell Stem Cell. 2010;7(2):240-8. |
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| Jasenosky, LD, Neumann, G, Kawaoka, Y. Minigenome-Based Reporter System Suitable for High-Throughput Screening of Compounds Able To Inhibit EbolavirusReplication and/or Transcription. Antimicrobial Agents amd Chemotherapy. 2010;54(7):3007–3010. |
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| Mehraein-Ghomi F, Basu HS, Church DR, Hoffmann FM, Wilding G. Androgen receptor requires JunD as a coactivator to switch on an oxidative stress generation pathway in prostate cancer cells. Cancer Research. 2010;70(11):4560-8. |
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| Basu HS, Mahlum A, Mehraein-Ghomi F, Kegel SJ, Guo S, Peters NR, Wilding G. Pretreatment with anti-oxidants sensitizes oxidatively stressed human cancer cells to growth inhibitory effect of suberoylanilide hydroxamic acid (SAHA). Cancer Chemotherapy Pharmacology. 2010 May 30. |
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| Luo Y, Li W, Ju J, Yuan Q, Peters N, Hoffmann FM, Huang Sheng-Xiong, Bugni TS, Rajski S, Osada H, Shen B. Functional characterization of TtnD and TtnF, unveiling new insights into tautomycetin biosynthesis. Journal of the American Chemical Society 2010;132(19):6663-71. |
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| Cook MR, Pinchot SN, Jaskula-Sztul R, Luo J, Kunnimalaiyaan M, Chen H. Identification of a novel Raf-1 pathway activator that inhibits gastrointestinal carcinoid cell growth. Mol Cancer Ther. 2010;9(2):429-37. |
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| Lu D, Bernstein DA, Satyshur KA, Keck JL. Small-molecule tools for dissecting the roles of SSB/protein interactions in genome maintenance. Proc Natl Acad Sci U S A. 2010;107(2):633-8. |
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| Ewald JA, Peters N, Desotelle JA, Hoffmann FM, Jarrard DF. A high-throughput method to identify novel senescence-inducing compounds. J Biomol Screen. 2009;14(7): 853-8. |
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| Ju J, Rajski SR, Lim Si-Kyu, Seo Jeong-Woo, Peters NR, Hoffmann FM, Shen B. Lactimidomycin, iso-migrastatin and related glutarimide-containing 12-membered macrolides are extremely potent inhibitors of cell migration. Journal of the American Chemical Society. 2009;131(4):1370-1. |
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| Peterson KJ, Sadowsky JD, Scheef EA, Pal S, Kourentzi KD, Willson RC, Bresnick EH, Sheibani N, Gellman SH. A Fluorescence Polarization Assay for Identifying Ligands that Bind to Vascular Endothelial Growth Factor. Anal. Biochem. 2008;378(1):8-14. |
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| Ju J, Rajski SR, Lim Si-Kyu, Seo Jeong-Woo, Peters NR, Hoffmann FM, Shen B. Evaluation of new migrastatin and dorrigocin congeners unveils cell migration inhibitors with dramatically improved potency. Bioorganic & Medicinal Chemistry Letters, 2008;18(22):5951-4. |
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| Trubetskoy OV, Finel M, Kurkela M, Fitzgerald M, Peters NR, Hoffmann FM, Trubetskoy VS. High throughput screening assay for UDP-glucuronosyltransferase 1A1 glucuronidation profiling. Assay and Drug Development Technologies. 2007;5(3):343-54. |
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| Ahmed, A, Peters, NR, Fitzgerald MK, Watson JA, Hoffmann, FM, Thorson JS. Colchicine Glycorandomization Influences Cytotoxicity and Mechanism of Action. Journal of the American Chemical Society. 2006;10.1021 /ja064686s. |
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| Carlson EE, May JF, Kiessling LL. Chemical probes of UDP-galactopyranose mutase. Chemistry and Biology. 2006;13(8):825-37. |
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| Zhang C, Albermann C, Fu X, Peters NR, Chisholm JD, Zhang G, Gilbert EJ, Wang PG, Van Vranken DL, Thorson JS. RebG- and RebM-Catalyzed Indolocarbazole Diversification. Chembiochem. 2006;7(5):795-804. |
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| Rutkoski TJ, Kurten EL, Mitchell JC, Raines RT. Disruption of Shape-Complementarity Markers to Create Cytotoxic Variants of Ribonuclease A. Journal of Molecular Biology. 2005;354 (1):41-54. |
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| Langenhan JM, Peters NR, Guzei IA, Hoffmann FM, Thorson JS. Enhancing the Anti-Cancer Properties of Cardiac Glycosides via Neoglycorandomization. Proc Natl Acad Sci USA. 2005;102(35):12305-10. |
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| Kozlov M, Bergendahl V, Burgess R, Goldfarb A, Mustaev A. Homogenous fluorescent assay for RNA polymerase. Analytical Biochemistry. 2005;342(2):206-13. |
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| Ason B, Knauss DJ, Balke AM, Merkel G, Skalka AM, Reznikoff WS. Targeting Tn5 transposase identifies human immunodeficiency virus type 1 inhibitors. Antimicrobial Agents and Chemotherapy. 2005;49(5):2035-43. |
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| Kim, M, Wessely, V, Lan, Q. Identification of Mosquito Sterol Carrier Protein-2 Inhibitors. Journal of Lipid Research. 2005;46(4):650-7. |
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| Soltero-Higgin M, Carlson EE, Phillips JH, Kiessling LL. Identification of inhibitors for UDP-galactopyranose mutase. J Am Chem Soc. 2004;126(34):10532-3. |
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| Ason B, Reznikoff WS. A high-throughput assay for Tn5 Tnp-induced DNA cleavage. Nucleic Acids Res. 2004;32(10):e83. |