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.)
Research in our laboratory is concerned with the design, preclinical development, and
commercialization of mixed organic–inorganic pharmaceuticals for treating life-
threatening diseases. At the top of our extensive portfolio are platinum–acridine hybrid
agents (PAHAs, or simply, PAs), which have evolved as one of the most potent types of
platinum-containing anticancer drugs with a unique spectrum of activity. We design,
optimize, and test these compounds using unique modular-synthetic and screening
methodology. Other techniques employed in this challenging interdisciplinary and
collaborative effort include mechanistic studies in cell-free systems and assays in
cancer cells, computational and bioinformatics tools, and a host of spectroscopic
techniques, all of which help us to shed light on the compounds’ mechanism of action
(MoA). Formulations and bioconjugate platforms are now being developed to turn PAs
into safer, tumor-targeted precision medicines for personalized oncology applications.
Selected Recent Publications and Patents
Zhang S, Wu, H, Day CS, Bierbach U: Platinum–Acridine Agents with High Activity in
Cancers Expressing the Solute Carrier MATE1 (SLC47A1). ACS Med. Chem. Lett.
Ulrich Bierbach, Xiyuan Yao, Hanwen Wang: Payload and Linker Designs for Platinum-
Acridine Anticancer Agents and Methods Thereof. US patent 11,591,357 (issued
Wu H, Bierbach U: Chemosensitivity-Gene Expression Correlations and Functional
Enrichment Analysis Provide Insight into the Mechanism of Action of a Platinum-
Acridine Anticancer Agent. ChemMedChem 17:e202200331 (2022).
Yao X, Bierbach U: DNA Adduct Detection after Post-Labeling Technique with PCR
Amplification (DNA-ADAPT-qPCR) Identifies the Pre-ribosomal RNA Gene as a Direct
Target of Platinum-Acridine Anticancer Agents. Chem. Eur. J. 27:14681-14689 (2021).
Ulrich Bierbach, Song Ding, Christopher L. Hackett: Liposomal Formulations of
Platinum-Acridine Anticancer Agents and Methods Thereof. US patent 10,925,2021
Zhang S, Yao X, Watkins NH, Rose PK, Caruso SR, Day CS, Bierbach U: Discovery of
a Chiral DNA-Targeted Platinum-Acridine Agent with Potent Enantioselective Anticancer
Activity. Angew. Chem. Int. Ed. 59:21965-21970 (2020).
Yao X, Watkins NH, Brown-Harding H, Bierbach U: A membrane Transporter
Determines the Spectrum of Activity of a Potent Platinum-Acridine Hybrid Anticancer
Agent. Sci. Rep.10:15201 (2020).
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Awards and Accomplishments
Wake Forest University Award for Excellence in Research (WFU, 2005)
Levison Family Faculty Fellowship (WFU, 2016-2019)
URECA Award for Excellence in Mentored Scholarship in the Sciences and Social
Sciences (WFU, 2023)