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001-es BibID:	BIBFORM095005
035-os BibID:	(scopus)85107600224 (wos)000666978100001
Első szerző:	Gyuricza Barbara (gyógyszerész)
Cím:	Synthesis of Novel, Dual-Targeting 68Ga-NODAGA-LacN-E[c(RGDfK)]2 Glycopeptide as a PET Imaging Agent for Cancer Diagnosis / Barbara Gyuricza, Judit P. Szabó, Viktória Arató, Dániel Szücs, Adrienn Vágner, Dezső Szikra, Anikó Fekete
Dátum:	2021
ISSN:	1999-4923
Megjegyzések:	Radiolabeled peptides possessing an Arg-Gly-Asp (RGD) motif are widely used radiopharmaceuticals for PET imaging of tumor angiogenesis due to their high affinity and selectivity to ?v?3 integrin. This receptor is overexpressed in tumor and tumor endothelial cells in the case of numerous cancer cell lines, therefore, it is an excellent biomarker for cancer diagnosis. The galectin-3 protein is also highly expressed in tumor cells and N-acetyllactosamine is a well-established ligand of this receptor. We have developed a synthetic method to prepare a lactosamine-containing radiotracer, namely 68Ga-NODAGA-LacN-E[c(RGDfK)]2, for cancer diagnosis. First, a lactosamine derivative with azido-propyl aglycone was synthetized. Then, NODAGA-NHS was attached to the amino group of this lactosamine derivative. The obtained compound was conjugated to an E[c(RGDfK)]2 peptide with a strain-promoted click reaction. We have accomplished the radiolabeling of the synthetized NODAGA-LacN-E[c(RGDfK)]2 precursor with a positron-emitting 68Ga isotope (radiochemical yield of >95%). The purification of the labeled compound with solid-phase extraction resulted in a radiochemical purity of >99%. Subsequently, the octanol?water partition coefficient (log P) of the labeled complex was determined to be ?2.58. In addition, the in vitro stability of 68Ga-NODAGA-LacN-E[c(RGDfK)]2 was investigated and it was found that it was stable under the examined conditions
Tárgyszavak:	Természettudományok Kémiai tudományok idegen nyelvű folyóiratközlemény külföldi lapban folyóiratcikk
Megjelenés:	Pharmaceutics. - 13 : 6 (2021), p. 1-13. -
További szerzők:	Péli-Szabó Judit (1977-) (vegyész) Arató Viktória Zsófia (1989-) (gyógyszerész) Szücs Dániel (1994-) (gyógyszerész) Vágner Adrienn (1990-) (vegyész, kémikus) Szikra Dezső Péter (1983-) (vegyész) Fekete Anikó (1973-) (vegyész)
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