Radiohybridization PET imaging of KRAS G12D mRNA expression in human pancreas cancer xenografts with [64Cu]DO3A-peptide nucleic acid-peptide nanoparticles

Preparation, 99mTc-labeling and biodistribution studies of a PNA oligomer containing a new ligand derivative of 2,2′-dipicolylamine

“…This behavior is comparable to plain radiolabeled PNAs [23,24]. Conjugation of targeting peptide moieties to PNA significantly increases the kidney accumulation of PNA constructs [14,[17][18][19]29,30,44,87,88]. A preliminary SPECT study in a NMRI, nu/nu mouse was also performed with [ 99m Tc(CO) 3 (Dpa-PNA)].…”

“…In such constructs, the role of the PNA is to direct the bioconjugate to a specific mRNA -a unique or a uniquely over-expressed mRNA in a diseased cell -while the function of the radioactive probe is to allow imaging to possibly provide information on cellular gene expression pattern and detect molecular changes at relatively early stages [13,42]. Hence, a number of in vivo biodistribution/hybridization studies of radiolabeled PNAs were undertaken [14,[17][18][19][20]22,[24][25][26][27][28][29][30][31][32][33]36,39,41,[43][44][45][46]. The majority of these reports involved the use of 99m Tc, probably due its ideal nuclear properties and the convenient availability from a commercial generator [47][48][49][50].…”

Non-Hybridization Saturable Mechanisms Play a Role in the Uptake of68Ga-Labeled LNA–DNA Mixmer Antisense Oligonucleotides in Rats

“…In contrast, proving of specifi c hybridization in an imaging experiment seems to be a more diffi cult task, especially in vivo, where the concentration of the probe is sub-therapeutic and hence may not affect the magnitude of mRNA or protein production. So far, to the best of our knowledge, only a few research groups have reported indirect evidences of antisense mechanisms in cell culture experiments and in xenograft models Nakamura et al, , 2005Liu et al, 2006;Chakrabarti et al, 2007;Tian et al, 2007;Jia et al, 2008).…”

Radioisotopes and Nanomedicine

“…Authors designed a series of radiohybridization probes linked with copper-64 to target various single nucleotide polymorphisms in KRAS mRNA. The probe had good selectivity for KRAS-mutated in mice engrafted with AsPC1, a pancreatic cancer cell line (Chakrabarti et al 2007). Similarly, Petersen et al designed copper-64 labeled liposomes for PET imaging in a mouse model (Petersen et al 2011).…”