Development of 99mTc-labeled trivalent isonitrile radiotracer for folate receptor imaging.
Bioorg Med Chem
; 27(10): 1925-1931, 2019 05 15.
Article
en En
| MEDLINE
| ID: mdl-30992201
ABSTRACT
Folate receptors (FR) are frequently overexpressed in a wide variety of human cancers. The aim of this study was to develop a trivalent 99mTc(CO)3-labeled folate radiotracer containing isonitrile (CN-R) as the coordinating ligand for FR target imaging. [99mTc]Tc-10 was HPLC purified (>98% chemical purity) and evaluated in vitro and in vivo as a potential agent for targeting FR-positive KB cells. [99mTc]Tc-10 is a hydrophilic compound with partition coefficient of -2.90⯱â¯0.13 that showed high binding affinity (0.04⯱â¯0.002â¯nM) in vitro. High accumulation and retention of [99mTc]Tc-10 (5.32⯱â¯2.99% ID/g) was observed in mice with KB tumors at 4â¯h after injection through the tail vein, which was significantly inhibited by co-injection of free folic acid (FA). SPECT (single photon emission tomography)/CT results were in accordance with biodistribution data at all time points.
Palabras clave
Texto completo:
1
Colección:
01-internacional
Banco de datos:
MEDLINE
Asunto principal:
Radiofármacos
/
Receptores de Folato Anclados a GPI
/
Nitrilos
Límite:
Animals
/
Humans
Idioma:
En
Revista:
Bioorg Med Chem
Asunto de la revista:
BIOQUIMICA
/
QUIMICA
Año:
2019
Tipo del documento:
Article
País de afiliación:
Pakistán