Sökning: L773:0362 4803 > Synthesis and chara...
Fältnamn | Indikatorer | Metadata |
---|---|---|
000 | 04067naa a2200505 4500 | |
001 | oai:DiVA.org:uu-108589 | |
003 | SwePub | |
008 | 090923s2011 | |||||||||||000 ||eng| | |
024 | 7 | a https://urn.kb.se/resolve?urn=urn:nbn:se:uu:diva-1085892 URI |
024 | 7 | a https://doi.org/10.1002/jlcr.19092 DOI |
040 | a (SwePub)uu | |
041 | a engb eng | |
042 | 9 SwePub | |
072 | 7 | a ref2 swepub-contenttype |
072 | 7 | a art2 swepub-publicationtype |
100 | 1 | a Blom, Elisabethu Uppsala universitet,Institutionen för biokemi och organisk kemi,Bengt Långström4 aut0 (Swepub:uu)elblo622 |
245 | 1 0 | a Synthesis and characterization of scVEGF-PEG-[68Ga]NOTA and scVEGF-PEG-[68Ga]DOTA PET tracers |
264 | c 2011-08-08 | |
264 | 1 | b Wiley,c 2011 |
338 | a print2 rdacarrier | |
520 | a Vascular endothelial growth factor (VEGF) signaling via vascular endothelial growth factor receptor 2 (VEGFR-2) on tumor endothelial cells is a critical driver of tumor angiogenesis. Novel anti-angiogenic drugs target VEGF/VEGFR-2 signaling and induce changes in VEGFR-2 prevalence. To monitor VEGFR-2 prevalence in the course of treatment, we are evaluating (68)Ga positron emission tomography imaging agents based on macrocyclic chelators, site-specifically conjugated via polyethylene glycol (PEG) linkers to engineered VEGFR-2 ligand, single-chain (sc) VEGF. The (68)Ga-labeling was performed at room temperature with NOTA (2,2', 2 ''-(1,4,7-triazonane-1,4,7-triyl) triacetic acid) conjugates or at 90 degrees C by using either conventional or microwave heating with NOTA and DOTA (2,2', 2 '', 2'''-(1,4,7,10-tetraazacyclododecane-1,4,7,10-tetrayl) tetraacetic acid) conjugates. The fastest (similar to 2min) and the highest incorporation (>90%) of (68)Ga into conjugate that resulted in the highest specific radioactivity (similar to 400MBq/nmol) was obtained with microwave heating of the conjugates. The bioactivity of the NOTA-and DOTA-containing tracers was validated in 3-D tissue culture model of 293/KDR cells engineered to express high levels of VEGFR-2. The NOTA-containing tracer also displayed a rapid accumulation (similar to 20s after intravenous injection) to steady-state level in xenograft tumor models. A combination of high specific radioactivity and maintenance of functional activity suggests that scVEGF-PEG-[(68)Ga] NOTA and scVEGF-PEG-[(68)Ga] DOTA might be promising tracers for monitoring VEGFR-2 prevalence and should be further explored. | |
650 | 7 | a NATURVETENSKAPx Kemix Organisk kemi0 (SwePub)104052 hsv//swe |
650 | 7 | a NATURAL SCIENCESx Chemical Sciencesx Organic Chemistry0 (SwePub)104052 hsv//eng |
650 | 7 | a TEKNIK OCH TEKNOLOGIERx Medicinteknikx Medicinsk bildbehandling0 (SwePub)206032 hsv//swe |
650 | 7 | a ENGINEERING AND TECHNOLOGYx Medical Engineeringx Medical Image Processing0 (SwePub)206032 hsv//eng |
653 | a scVEGF | |
653 | a (68)Ga | |
653 | a radiolabeling | |
653 | a angiogenesis | |
653 | a VEGFR-2 | |
653 | a PET | |
700 | 1 | a Velikyan, Irinau Uppsala universitet,Enheten för biomedicinsk strålningsvetenskap4 aut0 (Swepub:uu)irinveli |
700 | 1 | a Monazzam, Azitau Uppsala universitet,Endokrin tumörbiologi4 aut0 (Swepub:uu)azmon677 |
700 | 1 | a Razifar, Pashau Uppsala universitet,Centrum för bildanalys,Bildanalys och människa-datorinteraktion4 aut0 (Swepub:uu)serra226 |
700 | 1 | a Nair, Manoj4 aut |
700 | 1 | a Razifar, Payam4 aut |
700 | 1 | a Vanderheyden, Jean-Luc4 aut |
700 | 1 | a Krivoshein, Arcadius V.4 aut |
700 | 1 | a Backer, Marina4 aut |
700 | 1 | a Backer, Joseph4 aut |
700 | 1 | a Långström, Bengtu Uppsala universitet,Institutionen för biokemi och organisk kemi4 aut0 (Swepub:uu)benglang |
710 | 2 | a Uppsala universitetb Institutionen för biokemi och organisk kemi4 org |
773 | 0 | t Journal of labelled compounds & radiopharmaceuticalsd : Wileyg 54:11, s. 685-692q 54:11<685-692x 0362-4803x 1099-1344 |
856 | 4 8 | u https://urn.kb.se/resolve?urn=urn:nbn:se:uu:diva-108589 |
856 | 4 8 | u https://doi.org/10.1002/jlcr.1909 |
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