Influence of biological assay conditions on stability assessment of radiometal-labelled peptides exemplified using a 177Lu-DOTA-minigastrin derivative


Ocak M., Helbok A., von Guggenberg E., Ozsoy Y., Kabasakal L., Kremser L., ...More

Nuclear Medicine and Biology, vol.38, no.2, pp.171-179, 2011 (SCI-Expanded, Scopus)

  • Publication Type: Article / Article
  • Volume: 38 Issue: 2
  • Publication Date: 2011
  • Doi Number: 10.1016/j.nucmedbio.2010.07.009
  • Journal Name: Nuclear Medicine and Biology
  • Journal Indexes: Science Citation Index Expanded (SCI-EXPANDED), Scopus
  • Page Numbers: pp.171-179
  • Keywords: Radiopeptides, In vitro stability, In vivo stability, Radiometabolites, IN-VIVO EVALUATION, INITIAL CLINICAL-EVALUATION, RADIOLABELED PEPTIDES, POSITIVE TUMORS, RECEPTOR, VITRO, ANALOGS, MINIGASTRIN, SCINTIGRAPHY, STRATEGIES
  • Istanbul University Affiliated: Yes

Abstract

Introduction: Lack of correlation between in vitro and in vivo stability is a general problem for the development of radiopeptides especially in the case of minigastrin derivatives for therapeutic applications. In this study, we compared the influence of experimental conditions on radiopeptide stability results in vitro using a model Minigastrin (MG) analogue labelled with Lu-177. Additionally, we attempted to characterize the main serum enzymatic cleavage sites by matrix-assisted laser desorption/ionization (MALDI) time-of-flight (TOF) mass spectrometry (MS) analysis.