Abstract:
:Aiming to develop a new (99m)Tc-labeled folate derivative for FR-positive tumor imaging, a simpler method has been established to synthesize the folate-drug conjugates with free α-carboxyl group. In this study, the conjugate pteroyl-lys-HYNIC was synthesized and labeled with (99m)Tc using tricine and TPPTS as co-ligands. The radiochemical purity of the final complex (99m)Tc(HYNIC-lys-pteroyl)(tricine/TPPTS), 5 was high (>98%), and it remained stable in saline and plasma over 6h after preparation. The biologic evaluation results showed that the (99m)Tc labeled pteroyl-lys conjugate was able to specifically target the FR-positive tumor cells and tissues both in vitro and in vivo, highlighting its potential as an effective folate receptor targeted agent for tumor imaging.
journal_name
Bioorg Med Chem Lettjournal_title
Bioorganic & medicinal chemistry lettersauthors
Guo H,Xie F,Zhu M,Li Y,Yang Z,Wang X,Lu Jdoi
10.1016/j.bmcl.2011.02.014subject
Has Abstractpub_date
2011-04-01 00:00:00pages
2025-9issue
7eissn
0960-894Xissn
1464-3405pii
S0960-894X(11)00188-0journal_volume
21pub_type
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