Differences in protein binding and excretion of Triapine and its Fe(III) complex
- Author(s)
- Karla Pelivan, Walter Miklos, Sushilla Van Schoonhoven, Gunda Köllensperger, Lars Gille, Walter Berger, Petra Heffeter, Christian Kowol, Bernhard Keppler
- Abstract
Triapine has been investigated as anticancer drug in multiple clinical phase I/II trials. Although promising anti leukemic activity was observed, Triapine was ineffective against solid tumors. The reasons are currently widely unknown. The biological activity of Triapine is strongly connected to its iron complex (Fe-Triapine) which is pharmacologically not investigated. Here, novel analytical tools for Triapine and Fe-Triapine were developed and applied for cell extracts and body fluids of treated mice. Triapine and its iron complex showed a completely different behavior: for Triapine, low protein binding was observed in contrast to fast protein adduct formation of Fe-Triapine. Notably, both drugs were rapidly cleared from the body (serum half-life time
- Organisation(s)
- Department of Inorganic Chemistry, Department of Analytical Chemistry
- External organisation(s)
- Medizinische Universität Wien, Veterinärmedizinische Universität Wien
- Journal
- Journal of Inorganic Biochemistry
- Volume
- 160
- Pages
- 61-69
- No. of pages
- 9
- ISSN
- 0162-0134
- DOI
- https://doi.org/10.1016/j.jinorgbio.2015.10.006
- Publication date
- 07-2016
- Peer reviewed
- Yes
- Austrian Fields of Science 2012
- 104003 Inorganic chemistry, 106002 Biochemistry
- Keywords
- ASJC Scopus subject areas
- Biochemistry, Inorganic Chemistry
- Sustainable Development Goals
- SDG 3 - Good Health and Well-being
- Portal url
- https://ucrisportal.univie.ac.at/en/publications/929c834a-6ef3-4977-b6c2-9790d41342fe