uu.seUppsala University Publications
Change search
CiteExportLink to record
Permanent link

Direct link
Cite
Citation style
  • apa
  • ieee
  • modern-language-association
  • vancouver
  • Other style
More styles
Language
  • de-DE
  • en-GB
  • en-US
  • fi-FI
  • nn-NO
  • nn-NB
  • sv-SE
  • Other locale
More languages
Output format
  • html
  • text
  • asciidoc
  • rtf
Preparation and evaluation of a Ga-68-labeled RGD-containing octapeptide for noninvasive imaging of angiogenesis: biodistribution in non-human primate
Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Medicine, Department of Surgical Sciences, Radiology.
GE Healthcare, Uppsala Imanet, SE-75109 Uppsala, Sweden..
2018 (English)In: American Journal of Nuclear Medicine and Molecular Imaging, ISSN 2160-8407, Vol. 8, no 1, p. 15-31Article in journal (Refereed) Published
Abstract [en]

Monitoring general disease marker such as angiogenesis may contribute to the development of personalized medicine and improve therapy outcome. Readily availability of positron emitter based imaging agents providing quantification would expand clinical positron emission tomography (PET) applications. Generator produced Ga-68 provides PET images of high resolution and the half-life time frame is compatible with the pharmacokinetics of small peptides comprising arginine-glycine-aspartic acid (RGD) sequence specific to alpha(v)beta(3) integrin receptors. The main objective of this study was to develop a method for Ga-68-labeling of RGD containing bicyclic octapeptide ([Ga-68]Ga-DOTA-RGD) with high specific radioactivity and preclinically assess its imaging potential. DOTA-RGD was labeled using generator eluate preconcentration technique and microwave heating. The binding and organ distribution properties of [Ga-68]Ga-DOTA-RGD were tested in vitro by autoradiography of frozen tumor sections, and in vivo in mice carrying a Lewis Lung carcinoma graft (LL2), and in non-human primate (NHP). Another peptide with aspartic acid-glycine-phenylalanine sequence was used as a negative control. The full Ga-68 radioactivity eluted from two generators was quantitatively incorporated into 3-8 nanomoles of the peptide conjugates. The target binding specificity was confirmed by blocking experiments. The specific uptake in the LL2 mice model was observed in vivo and confirmed in the corresponding ex vivo biodistribution experiments. Increased accumulation of the radioactivity was detected in the wall of the uterus of the female NHP probably indicating neovascularization. [Ga-68]Ga-DOTA-RGD demonstrated potential for the imaging of angiogenesis.

Place, publisher, year, edition, pages
2018. Vol. 8, no 1, p. 15-31
Keywords [en]
Ga-68, RGD, PET, animal PET, angiogenesis, cancer, endometriosis, Lewis lung carcinoma, organ distribution, frozen section autoradiography, whole body autoradiography
National Category
Radiology, Nuclear Medicine and Medical Imaging
Identifiers
URN: urn:nbn:se:uu:diva-350549ISI: 000426585200002PubMedID: 29531858OAI: oai:DiVA.org:uu-350549DiVA, id: diva2:1209068
Available from: 2018-05-21 Created: 2018-05-21 Last updated: 2018-05-21Bibliographically approved

Open Access in DiVA

No full text in DiVA

Other links

PubMedhttps://www.ncbi.nlm.nih.gov/pmc/articles/PMC5840320/

Authority records BETA

Velikyan, Irina

Search in DiVA

By author/editor
Velikyan, Irina
By organisation
Radiology
In the same journal
American Journal of Nuclear Medicine and Molecular Imaging
Radiology, Nuclear Medicine and Medical Imaging

Search outside of DiVA

GoogleGoogle Scholar

pubmed
urn-nbn

Altmetric score

pubmed
urn-nbn
Total: 18 hits
CiteExportLink to record
Permanent link

Direct link
Cite
Citation style
  • apa
  • ieee
  • modern-language-association
  • vancouver
  • Other style
More styles
Language
  • de-DE
  • en-GB
  • en-US
  • fi-FI
  • nn-NO
  • nn-NB
  • sv-SE
  • Other locale
More languages
Output format
  • html
  • text
  • asciidoc
  • rtf