Improved synthesis on solid phase of dithiocarbamic cRGD‐derivative and ^99mTc‐radiolabelling

Abstract

In the field of angiogenesis, small cyclic pentapeptides containing the RGD motif are playing a relevant role for their high affinity and specificity for integrin receptors and for the possibility to act at both therapeutic and diagnostic level by inhibiting pathological angiogenesis and by serving as shuttles to deliver imaging-probe including SPECT/PET radionuclides to specific tissues.In the last decade, several new protocols were reported in literature for the direct synthesis of cyclic RDG either in solution or by SPPS. Here, we have elaborated and tested some alternative approaches using different resins and different protective groups. The introduction of the dithiocarbamate function, useful to complex radiometals suitable for nuclear medicine applications, has also been considered and achieved.

Microfluidic Generation of Amino-Functionalized Hydrogel Microbeads Capable of On-Bead Bioassay

“…We found that the non-functionalized PEG microbeads were more compatible with various solvents due to the increase in amphiphilicity [22]. Compared with commercially available PEG-based microbeads, such as PEGA resin [23,24], TentaGel XV resin [25,26], and ChemMatrix resin [27,28], PEG-amine hydrogel microbeads did not swell relatively with various solvents because of the high degree of crosslink [4,5]. However, our PEG-amine microbeads did not need a high swelling ratio because most of the active functional groups were exposed at the shell region [22,29].…”

Recent Applications of Retro-Inverso Peptides

“…They are highly correlated with angiogenesis, tumorigenesis, metastasis, and drug resistance [84][85][86]. In particular, integrin α v β 3 isoform represents an interesting molecular target for many diagnostic and therapeutic applications [87][88][89][90]. α v β 3 specifically recognizes the consensus tripeptide Arg-Gly-Asp (RGD), derived from extracellular matrix proteins, which has been largely exploited as radiolabeled carrier for the early diagnosis of malignant tumors [91].…”

Nitrido Technetium-99 m Core in Radiopharmaceutical Applications: Four Decades of Research

“…Besides, [ 99m Tc][TcN(S 2 CNR 2 ) 2 ] complexes containing the 4-(cyclohexylpiperazine) scaffold were used for the imaging of sigma receptors overexpressed in a variety of cancers [124]; likewise, the 2-methoxyphenylpiperazine moiety was tested for 5-HT1A receptor binding for imaging of brain disorders [125] and the RGDfK motif for non-invasive imaging of α v β 3 expression in malignant tumors [126,127].…”