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Plantinga A, Witte A, Li MH, et al. Bioanalytical Screening of Riboflavin Antagonists for Targeted Drug Delivery - A Thermodynamic and Kinetic Study. ACS Med Chem Lett. 2011;2(5):363-367doi: 10.1021/ml100296z.
Plantinga, A., Witte, A., Li, M. H., Harmon, A., Choi, S. K., Banaszak Holl, M. M., Orr, B. G., Baker, J. R., & Sinniah, K. (2011). Bioanalytical Screening of Riboflavin Antagonists for Targeted Drug Delivery - A Thermodynamic and Kinetic Study. ACS medicinal chemistry letters, 2(5), 363-367. https://doi.org/10.1021/ml100296z
Plantinga, Anna, et al. "Bioanalytical Screening of Riboflavin Antagonists for Targeted Drug Delivery - A Thermodynamic and Kinetic Study." ACS medicinal chemistry letters vol. 2,5 (2011): 363-367. doi: https://doi.org/10.1021/ml100296z
Plantinga A, Witte A, Li MH, Harmon A, Choi SK, Banaszak Holl MM, Orr BG, Baker JR, Sinniah K. Bioanalytical Screening of Riboflavin Antagonists for Targeted Drug Delivery - A Thermodynamic and Kinetic Study. ACS Med Chem Lett. 2011 May 12;2(5):363-367. doi: 10.1021/ml100296z. PMID: 21686082; PMCID: PMC3114641.
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ACS Med Chem Lett. 2011 May 12;2(5):363-367. doi: 10.1021/ml100296z.

Bioanalytical Screening of Riboflavin Antagonists for Targeted Drug Delivery - A Thermodynamic and Kinetic Study.

ACS medicinal chemistry letters

Anna Plantinga, Amanda Witte, Ming-Hsin Li, Andrew Harmon, Seok Ki Choi, Mark M Banaszak Holl, Bradford G Orr, James R Baker, Kumar Sinniah

Affiliations

  1. Calvin College, Department of Chemistry & Biochemistry, 3201 Burton St. SE Grand Rapids, MI 49546.

PMID: 21686082 PMCID: PMC3114641 DOI: 10.1021/ml100296z

Abstract

The present study screened riboflavin mimicking small molecules to determine their binding activity for the riboflavin binding protein. We performed thermodynamic and kinetic binding studies of these molecules using a combination of two analytical approaches; isothermal titration calorimetry and surface plasmon resonance spectroscopy. Screening of a biased set of non-riboflavin based small molecules by microcalorimetry led to the discovery of two known drug molecules, quinacrine and chloroquine, as favorable ligands for the riboflavin receptor with K(D) value of 264, and 2100 nM, respectively. We further demonstrated that quinacrine is a competitive ligand for the receptor as measured by surface plasmon resonance. Thus this study describes the identification of a novel class of dual acting riboflavin antagonists that target riboflavin receptor for cellular uptake and display multifunctional activities upon cellular entry.

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