ArticleMolecular imaging and biology2011
Assessing p-glycoprotein (Pgp) activity in vivo utilizing 68Ga-Schiff base complexes.
Article in Molecular imaging and biology, 2011. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 7 papers.
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Who cites it
7 citing papers in PubMed, 13 citations in OpenAlex.
- A brief overview of metal complexes as nuclear imaging agents.Dalton transactions (Cambridge, England : 2003) · 2019Review
- Article
- (67/68)Galmydar: A metalloprobe for monitoring breast cancer resistance protein (BCRP)-mediated functional transport activity.Nuclear medicine and biology · 2016Article
- In vitro and in vivo structure-property relationship of (68)Ga-labeled Schiff base derivatives for functional myocardial pet imaging.Molecular imaging and biology · 2014Article
- A generator-produced gallium-68 radiopharmaceutical for PET imaging of myocardial perfusion.PloS one · 2014Article
- Prospective of ⁶⁸Ga-radiopharmaceutical development.Theranostics · 2013Review
- Activation of P-glycoprotein (Pgp)-mediated drug efflux by extracellular acidosis: in vivo imaging with 68Ga-labelled PET tracer.European journal of nuclear medicine and molecular imaging · 2010Article
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Authors and funding
8 authors at 2 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
purposeThe p-glycoprotein (Pgp) is the most prominent member of active drug transporters leading to a multidrug-resistant phenotype. For identification of tumors functionally overexpressing Pgp in vivo, non-invasive imaging techniques are needed. PROCEDURES: Six Schiff base compounds were synthesized and labeled with (68)Ge/(68)Ga generator-derived (68)Ga. The compounds were studied in vitro in Pgp-positive tumor cells. The property of being a Pgp substrate was tested by comparison of the tracers uptake in R-3327 Dunning prostate carcinoma AT1 cells in presence and absence of the Pgp-inhibitor verapamil. In vivo investigations were performed with tumor-bearing rats imaged with micro-positron emission tomography.
resultsAll ligands were labeled with (68)Ga in yields of >92% beside one (~55%). The tracers showed different accumulation within the cells in vitro (4-60%). In blocking experiments, the ratio (blocked to unblocked) varied from 1.8 to 1.0. For in vivo experiments, (68)Ga-ENBDMPI and (68)Ga-MFL6.MZ were selected. The tumors showed specific uptake of the tracer. Direct intratumoral injection of verapamil increased the tracer concentration by ~25% reflecting the functional Pgp activity.
conclusionsTwo (68)Ga-labeled ligands appear to be valuable for imaging non-invasively the intratumoral Pgp activity. On a long term, patients with multidrug-resistant tumors pre-therapeutically may be identified prior to treatment.
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