Welcome to Wake Chemistry
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Small-Molecule DNA Interactions, Targeted Chemotherapy
Research in our laboratory is interdisciplinary in nature and spans the fields of organic and inorganic synthesis, medicinal chemistry, (bio)physical chemistry, and molecular and cellular biology. The ultimate goal of our research program is to design structurally unique organic–inorganic hybrid molecules as pharmacophores for tackling chemoresistant disease (in particular non-small cell lung cancer) and as probes of biomolecular structure and function. While the major thrust of our current research efforts is to promote our hybrid agents into clinical trials, we are equally interested in developing this technology into a tool for probing and manipulating nucleic acid secondary structure in live cells. Collaborations exist with the Comprehensive Cancer Center of Wake Forest University Health Sciences and several extramural research centers.
C. L. Smyre, G. Saluta, T. E. Kute, G. L. Kucera and U. Bierbach: Inhibition of DNA Synthesis by a DNA Platinating–Intercalating Hybrid Agent Leads to Potent Cell Kill in Non-Small Cell Lung Cancer. ACS Med. Chem. Lett; online ASAP.
H. Kostrhunova, J. Malina, A. J. Pickard, J. Stepankova, M. Vojtiskova, J. Kasparkova, T. Muchova, M. L. Rohlfing, U. Bierbach and 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. Mol. Pharmaceutics; online ASAP.
L. A. Graham, G. M. Wilson, T. K. West, C. S. Day, G. L. Kucera and U. Bierbach: Unusual Reactivity of a Potent Platinum–Acridine Hybrid Antitumor Agent. ACS Med. Chem. Lett. 2:687 (2011).
J. Roy Choudhury, L. Rao and U. Bierbach: Rates of intercalator-driven platination of DNA determined by a restriction enzyme cleavage inhibition assay: J. Biol. Inorg. Chem. 16:373 (2011).
L. C. Eiter, N. W. Hall, C. S. Day, G. Saluta, G. L. Kucera and 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 (2009).
Z. Ma, J. Roy Choudhury, M. W. Wright, C. S. Day, G. Saluta, G. L. Kucera and U. Bierbach: A non-cross-linking platinum–acridine agent with potent activity in non-small-cell lung cancer. J. Med. Chem. 51:7574 (2008).
Z. Ma, C. S. Day and U. Bierbach: Unexpected reactivity of the 9-aminoacridine chromophore in guanidylation reactions. J. Org. Chem. 72:5387 (2007).
C. G. Barry, C. S. Day and U. Bierbach: Duplex promoted platination of adenine-N3 in the minor groove of DNA: Challenging a longstanding bioinorganic paradigm. J. Am. Chem. Soc., 127:1160 (2005).
S. M. Hess, A. M. Mounce, R. C. Sequeira, T. M. Augustus, M. C. Ackley and U. Bierbach: Platinum-acridinylthiourea conjugates show cell line specific cytotoxic enhancement in H460 lung carcinoma cells compared to cisplatin. Cancer Chemother. Pharmacol. 56:337 (2005).
E. T. Martins, H. Baruah, J. Kramarczyk, G. Saluta, C. S. Day, G. L. Kucera and U. Bierbach: Design, synthesis and biological activity of a novel non-cisplatin-type platinum-acridine pharmacophore. J. Med. Chem., 44:4492 (2001).