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Daniel S. Pilch, PhD

Selected Publications

  1. Kaul, M., Zheng, Y., Parhi, A. K., LaVoie, E. J. & Pilch, D. S. (2014) “Inhibition of RND-Type Efflux Pumps Confers the FtsZ-Directed Prodrug TXY436 with Activity against Gram-Negative Bacteria” Biochem. Pharmacol. 89, 321-328.
  2. Kaul, M., Mark, L., Zheng, Y., Parhi, A. K., LaVoie, E. J. & Pilch, D. S. (2013) “Pharmacokinetics and in Vivo Antistaphylococcal Efficacy of TXY541, a 1-Methylpiperidine-4-Carboxamide Prodrug of PC190723” Biochem. Pharmacol. 86, 1699-1707.
  3. Kaul, M., Mark, L., Zheng, Y., Parhi, A. K., LaVoie, E. J. & Pilch, D. S. (2013) “An FtsZ-Targeting Prodrug with Oral Antistaphylococcal Efficacy in VivoAntimicrob. Agents Chemother. 57, 5860-5869.
  4. Kaul, M., Zhang, Y., Parhi, A. K., LaVoie, E. J., Tuske, S., Arnold, E., Kerrigan, J. E. & Pilch, D. S. (2013) “Enterococcal and Streptococcal Resistance to PC190723 and Related Compounds: Molecular Insights from a FtsZ Mutational Analysis” Biochimie 95, 1880-1887.
  5. Parhi, A. K., Zhang, Y., Saionz, K. W., Pradhan, P., Kaul, M., Pilch, D. S. & LaVoie, E. J. (2013) “Antibacterial Activity of Quinoxalines, Quinazolines, and 1,5-Naphthyridines” Bioorg. Med. Chem. Lett. 23, 4968-4974.
  6. Kelley, C., Lu, S., Parhi, A., Kaul, M., Pilch, D. S. & LaVoie, E. J. (2013) “Antimicrobial Activity of Various 4- and 5-Substituted 1-Phenylnaphthalenes” Eur. J. Med. Chem. 60, 395-409.
  7. Zhang, Y., Giurelo, D., Parhi, A., Kaul, M., Pilch, D. S. & LaVoie, E. J. (2013) “Substituted 1,6-Diphenylnaphthalenes as FtsZ-Targeting Antibacterial Agents” Bioorg. Med. Chem. Lett. 23, 2001-2006.
  8. Kaul, M., Parhi, A. K., Zhang, Y., LaVoie, E. J., Tuske, S., Arnold, E., Kerrigan, J. E. & Pilch, D. S. (2012) “A Bactericidal Guanidinomethyl Biaryl That Alters the Dynamics of Bacterial FtsZ Polymerization” J. Med. Chem. 55, 10160-10176.
  9. Parhi, A., Lu, S., Kelley, C., Kaul, M., Pilch, D. S., & LaVoie, E. J. (2012) “Antibacterial Activity of Substituted Dibenzo[a,g]quinolizin-7-ium Derivatives” Bioorg. Med. Chem. Lett. 22, 6962-6966.
  10. Parhi, A., Kelley, C., Kaul, M., Pilch, D. S., & LaVoie, E. J. (2012) “Antibacterial Activity of Substituted 5-Methylbenzo[c]phenanthridinium Derivatives” Bioorg. Med. Chem. Lett. 22, 7080-7083.
  11. Kelley, C., Zhang, Y., Parhi, A., Kaul, M., Pilch, D. S. & LaVoie, E. J. (2012) “3-Phenyl-Substituted 6,7-Dimethoxyisoquinoline Derivatives as FtsZ-Targeting Antibacterial Agents” Bioorg. Med. Chem. 20, 7012-7029.
  12. Kaul, M., Barbieri, C. M., Srinivasan, A. R. & Pilch, D. S. (2007) “Molecular Determinants of Antibiotic Recognition and Resistance by Aminoglycoside Phosphotransferase (3?)-IIIa: A Calorimetric and Mutational Analysis” J. Mol. Biol. 369, 142-156.
  13. Barbieri, C. M., Kaul, M., Bozza-Hingos, M., Zhao, F., Tor, Y., Hermann, T. & Pilch, D. S. (2007) “Defining the Molecular Forces That Determine the Impact of Neomycin on Bacterial Protein Synthesis: Importance of the 2?-Amino Functionality” Antimicrob. Agents Chemother. 51, 1760-1769.
  14. Barbieri, C. M., Kaul, M. & Pilch, D. S. (2007) “Use of 2-Aminopurine As a Fluorescent Tool for Characterizing Antibiotic Recognition of the Bacterial rRNA A-Site” Tetrahedron 63, 3567-3574.
  15. Barbieri, C. M. & Pilch, D. S. (2006) “Complete Thermodynamic Characterization of the Multiple Protonation Equilibria of the Aminoglycoside Antibiotic Paromomycin: A Calorimetric and Natural Abundance 15N NMR Study” Biophys. J. 90, 1338-1349.
  16. Kaul, M., Barbieri, C. M. & Pilch, D. S. (2006) “Aminoglycoside-Induced Reduction in Nucleotide Mobility at the Ribosomal RNA A-Site As a Potentially Key Determinant of Antibacterial Activity” J. Am. Chem. Soc. 128, 1261-1271.
  17. Pilch, D. S., Kaul, M. & Barbieri, C. M. (2005) “Ribosomal RNA Recognition by Aminoglycoside Antibiotics” In Topics in Current Chemistry, Vol. 253: DNA Binders and Related Subjects (Waring, M. J. & Chaires, J. B., Eds.) pp. 179-204, Springer-Verlag, Berlin-Heidelberg, Germany.
  18. Kaul, M., Barbieri, C. M. & Pilch, D. S. (2005) “Defining the Basis for the Specificity of Aminoglycoside-rRNA Recognition: A Comparative Study of Drug Binding to the A Sites of Escherichia coli and Human rRNA” J. Mol. Biol. 346, 119-134.
  19. Barbieri, C. M., Srinivasan, A. R. & Pilch, D. S. (2004) “Deciphering the Origins of Observed Heat Capacity Changes for Aminoglycoside Binding to Prokaryotic and Eukaryotic Ribosomal RNA A-Sites: A Calorimetric, Computational, and Osmotic Stress Study” J. Am. Chem. Soc., 126, 14380-14388.
  20. Kaul, M., Barbieri, C. M. & Pilch, D. S. (2004) “Fluorescence-Based Approach for Detecting and Characterizing Antibiotic-Induced Conformational Changes in Ribosomal RNA: Comparing Aminoglycoside Binding to Prokaryotic and Eukaryotic Ribosomal RNA Sequences” J. Am. Chem. Soc., 126, 3447-3453.
  21. Pilch, D. S., Kaul, M., Barbieri, C. M. & Kerrigan, J. E. (2003) “Thermodynamics of Aminoglycoside-rRNA Recognition” Biopolymers 70, 58-79.
  22. Barbieri, C. M., Li, T.-K., Guo, S., Wang, G., Shallop, A. J., Pan, W., Yang, G., Gaffney, B. L., Jones, R. A. & Pilch, D. S. (2003) “Aminoglycoside Complexation with a DNA•RNA Hybrid Duplex: The Thermodynamics of Recognition and Inhibition of RNA Processing Enzymes” J. Am. Chem. Soc., 125, 6469-6477.
  23. Kaul, M., Barbieri, C. M., Kerrigan, J. E. & Pilch, D. S. (2003) “Coupling of Drug Protonation to the Specific Binding of Aminoglycosides to the A site of 16 S rRNA: Elucidation of the Number of Amino Groups Involved and their Identities” J. Mol. Biol., 326, 1373-1387.
  24. Kaul, M. & Pilch, D. S. (2002) "Thermodynamics of Aminoglycoside-rRNA Recognition: The Binding of Neomycin-Class Aminoglycosides to the A-Site of 16S rRNA" Biochemistry 41, 7695-7706.