Journal
ACS MEDICINAL CHEMISTRY LETTERS
Volume 2, Issue 5, Pages 363-367Publisher
AMER CHEMICAL SOC
DOI: 10.1021/ml100296z
Keywords
Targeted delivery; riboflavin antagonist; isothermal titration calorimetry; surface plasmon resonance spectroscopy
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Funding
- NIH [1F33CA138031-01A1]
- NSF [CHE-0959681]
- HHMI
- NCI, NIH [1 R01 CA119409]
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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 nonriboflavin-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 values 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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