Brian S. J. Blagg

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Publications from The University of Kansas

43. Wang, Mingwen; Blagg,* B. S. J. Synthesis of a versatile metacyclophane macrolactam. Tetrahedron Letters. 2008, 49, 141-144.
42. Hadden, M. K.; Blagg,* B. S. J. Dimeric Approaches to Anticancer Chemotherapeutics. Invited review Anti-cancer Agents Med. Chem. 2008 in press.
41. Burlison, J. A.; Avila, C.; Vielhauer, G.; Lubbers, D. J.; Holzbeierlein, J.; Blagg,* B. S. J. Development of Novobiocin Analogues That Manifest Anti-proliferative Activity against Several Cancer Cell Lines. J. Org. Chem. 2008, 73, 2130-2137.
40. Hastings, Jedidiah M.; Blagg,* Brian S.J. Synthesis and Evaluation of Derrubone and Select Analogues. J. Org. Chem. 2008, 73, 369-373.
39. Hadden, M. K.; Galam, L.; Matts, R. A.; Blagg,* B. S. J. Derrubone, an Inhibitor of the Hsp90 Protein Folding Machinery. J. Nat. Prod. 2007, 70, 2014-2018.
38. Hadden, M. Kyle; Blagg,* Brian S.J. Cytotoxic small molecule dimmers and their activity against human breast cancer cells. Bioorg. Med. Chem. Lett. 2007, 17, 5063–5067.
37. Bishop, S.; Burlison, J.; Blagg,* B. S. J. Hsp90: A Novel Target for the Disruption of Multiple Signaling Cascades. Invited Review for Current Cancer Drug Targets. 2007, 7, 369–388.
36. Huang, Y–T.; Blagg,* B. S. J. A Library of Noviosylated Coumarin Analogues. J. Org. Chem. 2007, 72, 3609–3613.
35. Imormino, R.M.; Blagg, B. S. J.; Gewirth,* D.T. Inhibitory Ligands Adopt Different Conformations When Boundto Hsp90 or GRP94: Implications for Paralog-specific Drug Design. Submitted to J. Med. Chem.
34. Blagg,* B. S. J.; Hong, K. H.; Galam, L.; Avila, C.; Kalyanaraman, P.; Hartson, S. D.; Matts, R. L. The Role of Curcumin: An Unfolding Story. Submitted to ACS Chem. Biol.
33. Holzbeierlein, J. M.; Cronk, B.; Yu, X. M.; Goetzol, M. A.; Hoestje, S. M.; Neckers, L.; Blagg,* B. S. J. Novobiocin Analogues Downregulate Oncogenic Proteins in Prostate Cancer Cells. Submitted to Cancer Res.
32. Joseph S. Tash, Ramappa Chakrasali, Sudhakar R. Jakkaraj, Jennifer Hughes, S. Kendall Smith, Kaori Hornbaker, Leslie L. Heckert, Sedide B. Ozturk, M. Kyle Hadden, Terri Goss Kinzy, Brian S.J. Blagg, and Gunda I. Georg. Gamendazole, an Orally Active Indazole Carboxylic Acid Male Contraceptive Agent, Targets HSP90AB1 (HSP90BETA) and EEF1A1 (eEF1A), and Stimulates Il1a Transcription in Rat Sertoli Cells. Biol Reprod. 2008, 78, 1139 - 1152.
31. Galam, L.; Hadden, M. K.; Ma, Z.; Ye, Q–Z.; Yun, B–G.; Blagg, B. S. J.; Matts,* R. L. High-throughput Assay for the Identification of Hsp90-inhibitors based on Hsp90-dependence of the Refolding of Firefly Luciferase. Bioorg. Med. Chem. 2007, 15, 1939-1946.
30. Michaelis, M. L.; Burlison, J. A.; Hadden, M. K.; Neckers, L. M.; Blagg,* B. S. J. A Non-toxic Hsp90 Inhibitor Protects Neurons from Ab-induced Toxicity. Bioorg. Med. Chem. Lett. 2007, 17, 1984-1990.
29. Burlison, J. A.; Neckers, L. M.; Smith, A.; Maxwell, A.; Blagg,* B. S. J. Novobiocin. Redesigning DNA Gyrase Inhibitors for Selective Inhibition of Hsp90. J. Am. Chem. Soc. 2006, 128, 15529–15536.
28. Burlison, J. A.; Blagg,* B. S. J. Coumermycin A1 Analogues that Inhibit the Hsp90 Protein Folding Machinery. Org. Lett. 2006, 8, 4855–4858.
27. Wang, M.; Shen, G.; Welch, T. R.; Blagg,* B. S. J. Design, Synthesis and Structure – Activity Relationships for Chimeric Inhibitors of Hsp90. J. Org. Chem. 2006, 71, 7618–7631.
26. Hadden, M. K.; Lubbers, D.; Blagg,* B. S. J. Geldanamycin, Radicicol, and Chimeric Inhibitors of the Hsp90 N-terminal ATP Binding Site. Curr. Topics Med. Chem. 2006, 6, 1173–1182.
25. Chaudhury, S.; Welch, Timothy R.; Blagg,* B. S. J. Hsp90 as a Target for Drug Development. ChemMedChem. 2006, 1, 1331–1340.
24. Duvvuri, M.; Konkar, S.; Hong, K. H.; Blagg, B. S. J.; Krise,* J. P. Increasing Differential Selectivity of Drugs to Cancer Cells: A Case Study with Hsp90 Inhibitors. ACS Chem. Biol. 2006, 1, 309–315.
23. Avila, C.; Hadden, M. K.; Ma, Z.; Kornilayev, B. A.; Ye, Q–Z.; Blagg,* B. S. J. High-throughput Screening for Hsp90 ATPase Inhibitors. Bioorg. Med. Chem. Lett. 2006, 16, 3005–3008.
22. Wang, M.; Shen, G.; Blagg,* B. S. J. Radanamycin, A Macrocyclic Chimera of Radicicol and Geldanamycin. Bioorg. Med. Chem. Lett. 2006, 16, 2459–2462.
21. Peng, W.; Blagg,* B. S. J. A Versatile Approach Toward the Ansamycin Antibiotics. Org. Lett. 2006, 8, 975–978.
20. Avila, C.; Kornilaev, B.; Blagg,* B. S. J. Development and Optimization of a Useful Assay for Determining Hsp90’s Inherent ATPase Activity. Bioorg. Med. Chem. 2006, 14, 1134–1142.
19. Blagg,* B. S. J.; Kerr, T. D. Hsp90 Inhibitors: Small Molecules that Transform the Hsp90 Protein Folding Machinery into a Catalyst for Protein Degradation. Med. Res. Rev. 2006, 26, 310–338.
18. Yu, X–M.; Shen, G.; Cronk, B.; Marcu, M.; Holzberlein, J.; Neckers, L. M.; Blagg,* B. S. J. Hsp90 Inhibitors Identified from a Library of Novobiocin Analogues. J. Am. Chem. Soc. 2005, 127, 12778–12779.
17. Yu, X–M.; Han, H.; Blagg,* B. S. J. Synthesis of Mono- and Dihydroxylated Furanoses, Pyranoses, and an Oxepanose for the Preparation of Natural Product Analogue Libraries. J. Org. Chem. 2005, 70, 5599–5605.
16. Shen, G.; Blagg,* B. S. J. Radester, A Novel Inhibitor of the Hsp90 Protein Folding Machinery. Org. Lett. 2005, 7, 2157–2160.
15. Clevenger, R. C.; Blagg,* B. S. J. Design, Synthesis, and Evaluation of a Radicicol and Geldanamycin Chimera, Radamide. Org. Lett. 2004, 6, 4459–4462.
14. Shen, G.; Yu, X. M.; Blagg,* B. S. J. Synthesis of Photolabile Novobiocin Analogues. Bioorg. Med. Chem. Lett. 2004, 14, 5903–5906.
13. Yu, X. M.; Shen, G.; Blagg,* B. S. J. Synthesis of (–)-Noviose from 2,3-O-Isopropylidene-D-erythronolactol. J. Org. Chem. 2004, 7375–7378.
12. Clevenger, R. C.; Raible, J. M.; Peck, A. M.; Blagg,* B. S. J. B. Biotinylated Geldanamycin. J. Org. Chem. 2004, 69, 4375–4380.

Patent and Patent Applications

11. Blagg, B. S. J.; Neckers, L. M.; Yu, X. M.; Han, H. Novobiocin Analogues for the Treatment of Cancer. US patent filed December 2004.
10. Blagg, B. S. J.; Shen, G.; Clevenger, R. C. Hsp90 Inhibitors. US Patent Application filed in October 2004.

Postdoctoral Studies

9. Elliott, G. I.; Fuchs, J. R.; Blagg, B. S. J.; Ishikawa, H.; Tao, H.; Yuan, Z.-Q.; Boger, D. L. Intramolecular Diels-Alder/1,3-Dipolar Cycloaddition Cascade of 1,3,4-Oxadiazoles. J. Am. Chem. Soc. 2006, 128, 10589–10595.
8. Blagg, B. S. J.; Boger, D. L. Total Synthesis of (+)-Camptothecin. Tetrahedron 2002, 58, 6343-6349.
7. Wilkie, G. D.; Elliott, G. I.; Blagg, B. S. J.; Wolkenberg, S. E.; Soenen, D. R.; Miller, M. M.; Pollack, S.; Boger, D. L. Intramolecular Diels-Alder and Tandem Intramolecular Diels–Alder/1,3-Dipolar Cycloaddition Reactions of 1,3,4-Oxadiazoles. J. Am. Chem. Soc. 2002, 124, 11292-11294.

Graduate Studies

6. Blagg, B. S. J.; Jarstfer, M. B.; Rogers, D. H.; Poulter, C. D. Recombinant Squalene Synthase. A Mechanism for the Rearrangement of Presqualene Diphosphate to Squalene. J. Am. Chem. Soc. 2002, 124, 8846-8853.
5. Koppisch, Andrew T.; Fox, David T.; Blagg, Brian S. J.; Poulter, C. D. E. coli MEP Synthase: Steady-State Kinetic Analysis and Substrate Binding. Biochemistry 2002; 41, 236-243.
4. Hahn, F. M.; Eubanks, L. M.; Blagg, B. S. J.; Poulter, C. D. 1-Deoxy-D-xylulose 5-phosphate Synthase, the Gene Product of Open Reading Frame (ORF) 2816 and ORF 2895 in Rhodobacter Capsulatus. J. Bacteriol. 2001, 183, 1-11.
3. Koppisch, A. T.; Blagg, B. S. J.; Poulter, C. D. Synthesis of 2-C-Methyl-D-erythritol-4-phosphate: The First Pathway-Specific Intermediate in the Methylerythritol Phosphate Route to Isoprenoids. Org. Lett. 2000, 2, 215-217.
2. Blagg, B. S. J.; Poulter, C. D. Synthesis of 1-Deoxy-D-xylulose and 1-Deoxy-D-xylulose-5-phosphate. J. Org. Chem. 1999, 64, 1508-1511.
1. Jarstfer, M. B.; Blagg, B. S. J.; Rogers, D. H.; Poulter, C. D. Biosynthesis of Squalene. Evidence for a Tertiary Cyclopropylcarbinyl Cationic Intermediate in the Rearrangement of Presqualene Diphosphate to Squalene. J. Am. Chem. Soc. 1996, 118, 13089-13090. (Chemical and Engineering News, January 6, 1997, News of the week: "Biosynthesis of Squalene.")

For More Information, Please Contact:

Dr. Brian S. J. Blagg
Department of Medicinal Chemistry
4070 Malott Hall
Tel: 785-864-2288
FAX: 785-864-5326
Email: bblagg@ku.edu