Bierbach, Ulrich - Wake Forest University

个人简介

Diploma (Chemistry), 1989, University of Oldenburg, Germany Ph.D., 1992, University of Oldenburg, Germany (S. Pohl) Postdoctoral Fellow (German Research Council, DFG), 1992–1993, Leiden University, The Netherlands (J. Reedijk) DFG Research Fellow, 1994–1996, Virginia Commonwealth University (N. Farrell) Research Associate, 1996–1998, Virginia Commonwealth University (N. Farrell) Postdoctoral Research Associate, 1998–1999, University of Minnesota (L. Que, Jr.)

研究领域

Research in our laboratory is concerned with the design of small-molecule agents for the cure and management of life-threatening diseases and for probing and modulating gene regulation. Structurally novel drugs and drug conjugates are prepared using organic and inorganic synthetic methodologies. The interactions of these agents with potential biomolecular targets (DNA, DNA-processing enzymes, metalloenzymes) are studied using bioanalytical (LC-MS) and high-resolution structural (NMR, X-ray) methods, as well as biophysical and molecular biology techniques. Biological activity studies are carried out in vitro and in vivo by collaborators at WFU School of Medicine. Our research is funded through the National Institutes of Health.

近期论文

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A. J. Pickard, F. Liu, T. F. Bartenstein, L. G. Haines, K. E. Levine, G. L. Kucera, U. Bierbach: Redesigning the DNA-Targeted Chromophore in Platinum–Acridine Anticancer Agents: A Structure–Activity Relationship Study. Chemistry - A European Journal, 20, 16174-16187. (2014) DOI: 10.1002/chem.201404845 S. Ding, A. J. Pickard, G. L. Kucera, U. Bierbach: Design of Enzymatically Cleavable Prodrugs of a Potent Platinum-Containing Anticancer Agent.Chemistry - A European Journal, 20, 16164-16173. (2014) DOI: 10.1002/chem.201404675 X. Qiao, S. Ding, F. Liu, G. L. Kucera, U. Bierbach: Investigating the cellular fate of a DNA-targeted platinum-based anticancer agent by orthogonal double-click chemistry. Journal of Biological Inorganic Chemistry, 19, 415-426. (2014) DOI: 10.1007/s00775-013-1086-1 A. J. Pickard, U. Bierbach: The Cell’s Nucleolus: an Emerging Target for Chemotherapeutic Intervention. ChemMedChem, 8, 1441-1449. (2013) DOI: 10.1002/cmdc.201300262 S. Dutta, M. J. Snyder, D. Rosile, K. L. Binz, E. H. Roll, J. Suryadi, U. Bierbach, M. Guthold: PT-ACRAMTU, A Platinum–Acridine Anticancer Agent, Lengthens and Aggregates, but does not Stiffen or Soften DNA. Cell Biochemistry and Biophysics, 67, 1103-1113. (2013) DOI: 10.1007/s12013-013-9614-8 S. Ding, X. Qiao, J. Suryadi, G. S. Marrs, G. L. Kucera, U. Bierbach: Using Fluorescent Post-Labeling To Probe the Subcellular Localization of DNA-Targeted Platinum Anticancer Agents. Angewandte Chemie, 52, 3350-3354. (2013) DOI: 10.1002/anie.201210079 S. Ding, X. Qiao, G. L. Kucera, U. Bierbach: Design of a platinum–acridine–endoxifen conjugate targeted at hormone-dependent breast cancer. Chemical Communications, 49, 2415-2417. (2013) DOI: 10.1039/C3CC38957J S. Ding, X. Qiao, G. L. Kucera, U. Bierbach: Using a Build-and-Click Approach for Producing Structural and Functional Diversity in DNA-Targeted Hybrid Anticancer Agents. Journal of Medicinal Chemistry, 55, 10198-10203. (2012) DOI: 10.1021/jm301278c J. Suryadi, U. Bierbach: DNA Metalating-Intercalating Hybrid Agents for the Treatment of Chemoresistant Cancers. Chemistry - A European Journal, 18, 12926-12934. (2012) DOI: 10.1002/chem.201202050 K. Cheung-Ong, K. T. Song, Z. Ma, D. Shabtai, A. Y. Lee, D. Gallo, L. E. Heisler, G. W. Brown, U. Bierbach, G. Giaever, C. Nislow: Comparative Chemogenomics To Examine the Mechanism of Action of DNA-Targeted Platinum-Acridine Anticancer Agents. ACS Chemical Biology, 7, 1892-1901. (2012) DOI: 10.1021/cb300320d L. A. Graham, J. Suryadi, T. K. West, G. L. Kucera, U. Bierbach: Synthesis, Aqueous Reactivity, and Biological Evalulation of Carboxylic Acid Ester-Functionalized Platinum-Acridine Hybrid Anticancer Agents. Journal of Medicinal Chemistry, 55, 7817-7827. (2012) DOI: 10.1021/jm300879k X. Qiao, A. E. Zeitany, M. W. Wright, A. S. Essader, K. E. Levine, U. Bierbach: Analysis of the DNA damage produced by a platinum–acridine antitumor agent and its effects in NCI-H460 lung cancer cells. Metallomics, 4, 645-652. (2012) DOI: 10.1039/C2MT20031G L. Rao, J. D. Dworkin, W. E. Nell, U. Bierbach: Interactions of Platinum-Modified Perylene Derivative with the Human Telomeric G-Quadruplex. Journal of Physical Chemistry B, 115, 13701-13712. (2011) DOI: 10.1021/jp207265s C. L. Smyre, G. Saluta, T. E. Kute, G. L. Kucera, U. Bierbach: Inhibition of DNA Synthesis by a Platinum–Acridine Hybrid Agent Leads to Potent Cell Kill in Non-Small Cell Lung Cancer. ACS Medicinal Chemistry Letters, 2, 870-874. (2011) DOI: 10.1021/ml2001888 H. Kostrhunova, J. Malina, A. J. Pickard, J. Stepankova, M. Vojtiskova, J. Kasparkova, T. Muchova, M. L. Rohlfing, U. Bierbach, V. Brabec: Replacement of a Thiourea with an Amidine Group in a Monofunctional Platinum–Acridine Antitumor Agent. Effect on DNA Interactions, DNA Adduct Recognition and Repair. Molecular Pharmaceutics, 8, 1941-1954. (2011) DOI: 10.1021/mp200309x L. A. Graham, G. M. Wilson, T. K. West, C. S. Day, G. L. Kucera, U. Bierbach: Unusual Reactivity of a Potent Platinum-Acridine Hybrid Antitumor Agent. ACS Medicinal Chemistry Letters, 2, 687-691. (2011) DOI: 10.1021/ml200104h J. R. Choudhury, L. Rao, U. Bierbach: Rates of intercalator-driven platination of DNA determined by restriction enzyme cleavage inhibition assay. Journal of Biological Inorganic Chemistry, 16, 373-380. (2011). DOI: 10.1007/s00775-010-0733-z L. Rao, T. K. West, G. Saluta, G. L. Kucera, U. Bierbach: Probing Platinum-Adenine-N3 Adduct Formation with DNA Minor-Groove Binding Agents. Chemical Research in Toxicology, 23, 1148-1150. (2010). DOI: 10.1021/tx100170p L. C. Eiter, N. W. Hall, C. S. Day, G. Saluta, G. L. Kucera, U. Bierbach: Gold(I) Analogues of a Platinum-Acridine Antitumor Agent are Only Moderately Cytotoxic but Show Potent Activity against Mycobacterium tuberculosis. J. Med. Chem., 52, 6519-6522. (2009).DOI: 10.1021/jm9012856 A. R. Kheradi, G. Saluta, G. L. Kucera, C. S. Day, U. Bierbach: Synthesis and biological evaluation of platinum-acridine hybrid agents modified with bipyridine non-leaving groups. Bioorg. Med. Chem. Lett., 19, 3423-3425. (2009).DOI: 10.1016/j.bmcl.2009.05.046