Format

Send to

Choose Destination
Bioorg Med Chem. 2019 May 15;27(10):1925-1931. doi: 10.1016/j.bmc.2019.04.013. Epub 2019 Apr 10.

Development of 99mTc-labeled trivalent isonitrile radiotracer for folate receptor imaging.

Author information

1
Department of Nuclear Medicine, Seoul National University College of Medicine, Seoul, Republic of Korea; Isotope Production Division, Pakistan Institute of Nuclear Science & Technology (PINSTECH), P. O, Nilore, Islamabad, Pakistan.
2
Department of Nuclear Medicine, Seoul National University College of Medicine, Seoul, Republic of Korea; Department of Biomedical Sciences, Seoul National University Graduate School, Seoul, Republic of Korea; Cancer Research Institute, Seoul National University College of Medicine, Seoul, Republic of Korea.
3
Department of Nuclear Medicine, Seoul National University College of Medicine, Seoul, Republic of Korea; Cancer Research Institute, Seoul National University College of Medicine, Seoul, Republic of Korea.
4
Department of Nuclear Medicine, Seoul National University College of Medicine, Seoul, Republic of Korea.
5
Department of Nuclear Medicine, Seoul National University College of Medicine, Seoul, Republic of Korea; Department of Biomedical Sciences, Seoul National University Graduate School, Seoul, Republic of Korea; Cancer Research Institute, Seoul National University College of Medicine, Seoul, Republic of Korea. Electronic address: jmjng@snu.ac.kr.

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 ± 0.13 that showed high binding affinity (0.04 ± 0.002 nM) in vitro. High accumulation and retention of [99mTc]Tc-10 (5.32 ± 2.99% ID/g) was observed in mice with KB tumors at 4 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.

KEYWORDS:

Folic acid; Isocyanide; Technetium-99m; Tricarbonyl; Trivalent probe

PMID:
30992201
DOI:
10.1016/j.bmc.2019.04.013

Supplemental Content

Full text links

Icon for Elsevier Science
Loading ...
Support Center