Beuck, Simon, Schaenzer, Wilhelm and Thevis, Mario (2012). Hypoxia-inducible factor stabilizers and other small-molecule erythropoiesis-stimulating agents in current and preventive doping analysis. Drug Test. Anal., 4 (11). S. 830 - 846. HOBOKEN: WILEY-BLACKWELL. ISSN 1942-7603
Full text not available from this repository.Abstract
Increasing the blood's capacity for oxygen transport by erythropoiesis-stimulating agents (ESAs) constitutes a prohibited procedure of performance enhancement according to the World Anti-Doping Agency (WADA). The advent of orally bio-available small-molecule ESAs such as hypoxia-inducible factor (HIF) stabilizers in the development of novel anti-anaemia therapies expands the list of potential ESA doping techniques. Here, the erythropoiesis-stimulating properties and doping relevance of experimental HIF-stabilizers, such as cobaltous chloride, 3,4-dihydroxybenzoic acid or GSK360A, amongst others, are discussed. The stage of clinical trials is reviewed for the anti-anaemia drug candidates FG-2216, FG-4592, GSK1278863, AKB-6548, and BAY85-3934. Currently available methods and strategies for the determination of selected HIF stabilizers in sports drug testing are based on liquid chromatography-electrospray ionization-tandem mass spectrometry (LC-ESI-MS/MS). For the support of further analytical assay development, patents claiming distinct compounds for the use in HIF-mediated therapies are evaluated and exemplary molecular structures of HIF stabilizers presented. Moreover, data concerning the erythropoiesis-enhancing effects of the GATA inhibitors K7174 and K11706 as well as the lipidic small-molecule ESA PBI-1402 are elucidated the context of doping analysis. Copyright (C) 2012 John Wiley & Sons, Ltd.
Item Type: | Journal Article | ||||||||||||||||
Creators: |
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URN: | urn:nbn:de:hbz:38-479502 | ||||||||||||||||
DOI: | 10.1002/dta.390 | ||||||||||||||||
Journal or Publication Title: | Drug Test. Anal. | ||||||||||||||||
Volume: | 4 | ||||||||||||||||
Number: | 11 | ||||||||||||||||
Page Range: | S. 830 - 846 | ||||||||||||||||
Date: | 2012 | ||||||||||||||||
Publisher: | WILEY-BLACKWELL | ||||||||||||||||
Place of Publication: | HOBOKEN | ||||||||||||||||
ISSN: | 1942-7603 | ||||||||||||||||
Language: | English | ||||||||||||||||
Faculty: | Unspecified | ||||||||||||||||
Divisions: | Unspecified | ||||||||||||||||
Subjects: | no entry | ||||||||||||||||
Uncontrolled Keywords: |
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URI: | http://kups.ub.uni-koeln.de/id/eprint/47950 |
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