TY  - JOUR
AU  - Möller, Ines
A2  - Möller, Ines
A2  - Thomas, Andreas
A2  - Geyer, Hans
A2  - Schänzer, Wilhelm
A2  - Thevis, Mario
DB  - BISp
DP  - BISp
KW  - Biochemie
KW  - Blut
KW  - Blutplasma
KW  - Doping
KW  - Dopinganalyse
KW  - Dopingbekämpfung
KW  - Dopingkontrolle
KW  - Dopingnachweis
KW  - Entwicklung
KW  - Erythropoetin
KW  - Flüssigkeitschromatographie
KW  - Leistungssteigerung
KW  - Massenspektrometrie
KW  - Peptid
KW  - Untersuchung, empirische
LA  - eng
TI  - Synthesis, characterisation, and mass spectrometric detection of a pegylated EPO-mimetic peptide for sports drug testing purposes
TT  - Synthese, Charakterisierung und massenspektrometrischer Nachweis eines pegylierten EPO-mimetischen Peptids zu Doping-Testzwecken
PY  - 2011
N2  - Erythropoietin (EPO) and other erythropoiesis-stimulating agents possess a high misuse potential in elite sport due to their ability to increase the oxygen transport capacity, which plays a vital role in enhancing endurance performance. Currently, a new generation of EPO-mimetic peptides is under development from which peginesatide (also referred to as Hematide™), a pegylated homodimeric peptide of approximately 45 kDa with no structural relationship to erythropoietin, is the most advanced drug candidate undergoing phase-III clinical trials. Since preventive doping research aims at the development of detection methods before a drug receives clinical approval, a selective and sensitive assay has to be established knowing that conventional doping control assays for EPO will not succeed in detecting peginesatide. Thus, a pegylated EPO-mimetic peptide simulating the structure and properties of the lead drug candidate peginesatide was synthesised as a model compound for this new class of emerging drugs and characterised by means of gel electrophoresis, matrix-assisted laser desorption/ionisation (MALDI) mass spectrometry, as well as liquid chromatography/electrospray ionisation tandem mass spectrometry (LC/ESI-MS/MS) after proteolytic digestion. Based on these results, a mass spectrometric detection method of the product in plasma was developed targeting a pentapeptide fragment after protein precipitation and subtilisin digestion. Its fitness for purpose was evaluated by the determination of selected method characteristics focusing particularly on specificity, recovery (ca. 60%), and limit of detection (1 ng/mL).   Verf.-Referat
L2  - https://dx.doi.org/10.1002/rcm.5109
L2  - https://onlinelibrary.wiley.com/doi/abs/10.1002/rcm.5109
DO  - 10.1002/rcm.5109
SP  - S. 2115-2123
SN  - 0951-4198
JO  - Rapid communications in mass spectrometry
IS  - 15
VL  - 25
M3  - Elektronische Ressource (online)
M3  - Gedruckte Ressource
ID  - PU201410009726
ER  -