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The binding of flavopiridol to blood serum albumin

DOI: 10.1002/chir.20925 DOI Help
PMID: 21038395 PMID Help

Authors: Daniel Myatt (Diamond Light Source) , Louise Johnson (Diamond Light Source) , Sonja Baumli (Department of Biochemistry, University of Oxford) , Guiliano Siligardi (Diamond Light Source)
Co-authored by industrial partner: No

Type: Journal Paper
Journal: Chirality , VOL 22 (1E) , PAGES E40-E43

State: Published (Approved)
Published: October 2010

Abstract: Flavopiridol is a potent cyclin-dependant kinase (CDK) inhibitor and is in clinical trials for anticancer treatment. A limiting factor in its drug development has been the high dosage required in human clinical trials. The high dosage is suggested to be necessary because of significant flavopiridol binding to human blood serum. Albumin is the major protein component of blood serum and has been suggested as a likely high affinity binding target. We characterized the binding of human serum albumin to flavopiridol using circular dichroism (hereafter CD). Flavopiridol bound to human serum albumin has a diagnostic CD binding peak at 284 nm. The diagnostic CD binding peak was unobservable for flavopiridol with bovine serum albumin, using the same experimental conditions. However, under higher albumin concentrations a small CD signal is observed confirming, flavopiridol binds to bovine serum albumin as well.

Journal Keywords: Flavopiridol; Circular Dichroism; Albumin; Cancer; Drug Transport

Subject Areas: Medicine, Biology and Bio-materials

Instruments: B23-Circular Dichroism

Added On: 23/03/2010 22:33

Discipline Tags:

Non-Communicable Diseases Health & Wellbeing Cancer Life Sciences & Biotech

Technical Tags:

Spectroscopy Circular Dichroism (CD)