title: Radiopeptide internalisation and externalization assays: cell viability and radioligand integrity.
abstract: Various aspects of radiopeptide receptor-mediated cell internalisation and externalization assays were assessed, including the integrity of externalized peptides and the effect of varying the pH and incubation time of the acid wash step (to remove surface receptor-bound ligand) on efficacy and cell viability. The observed intact proportion of externalized peptide was 5-10%, and acid wash buffers with pH 2.8 or below were found to be detrimental to cell viability and integrity, particularly following prolonged incubation times.
authors.affiliation: Centre for Molecular Oncology and Imaging, Institute of Cancer, Barts and the London School of Medicine and Dentistry, Queen Mary University of London, Charterhouse Square, London EC1M 6BQ, United Kingdom.
authors.forename: Syed Ali Raza
authors.initials: SA
authors.lastname: Naqvi
authors.forename: Jane K
authors.initials: JK
authors.lastname: Sosabowski
authors.forename: Saeed Ahamad
authors.initials: SA
authors.lastname: Nagra
authors.forename: Malik M
authors.initials: MM
authors.lastname: Ishfaq
authors.forename: Stephen J
authors.initials: SJ
authors.lastname: Mather
authors.forename: Torkjel
authors.initials: T
authors.lastname: Matzow
mesh_terms: D000818:Animals; D045744:Cell Line, Tumor; D002470:Cell Survival / Q000187:drug effects; D004705:Endocytosis / Q000502:physiology; D005089:Exocytosis / Q000502:physiology; D005755:Gastrins / Q000737:chemistry / Q000493:pharmacokinetics* / Q000494:pharmacology; D007205:Indium Radioisotopes / Q000737:chemistry / Q000493:pharmacokinetics* / Q000494:pharmacology; D009942:Organometallic Compounds / Q000138:chemical synthesis / Q000493:pharmacokinetics* / Q000494:pharmacology; D010190:Pancreatic Neoplasms / Q000378:metabolism / Q000473:pathology / Q000532:radiotherapy*; D019275:Radiopharmaceuticals / Q000138:chemical synthesis / Q000493:pharmacokinetics* / Q000494:pharmacology; D051381:Rats
chemical_list: C522059:APH070; D005755:Gastrins; D007205:Indium Radioisotopes; D009942:Organometallic Compounds; D019275:Radiopharmaceuticals