Folate Receptor-Specific Positron Emission Tomography Imaging with Folic Acid-Conjugated Tissue Inhibitor of Metalloproteinase-2 


Vol. 34,  No. 11, pp. 3243-3248, Nov.  2013
10.5012/bkcs.2013.34.11.3243


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  Abstract

The tissue inhibitor of metalloproteinase-2 (TIMP-2) inhibits matrix metalloproteinases activity and modulates cellular proliferation and apoptosis. The human serum albumin-TIMP-2 with folic acid conjugate (termed HT2-folate) was synthesized to promote uptake through folate receptors (FRs), and a corresponding radiolabeled compound was prepared for tumor diagnosis by positron emission tomography (PET). 68Ga-NOTAHT2- folate was synthesized from 68Ga and the NOTA chelator with HT2-folate. The fusion protein was identified using MALDI-TOF mass spectrometry. The radioligand was prepared with a high radiochemical yield. Cell-surface association of 68Ga-NOTA-HT2-folate significantly increased over time in FR-positive tumor cells. In animal PET and biodistribution studies, tumor uptake was very high as early as 1 h after radioligand injection. Folate conjugation enhanced the selective receptor-targeting efficacy of HT2 in FRexpressing tumors, and its radioligand will be useful as an in vitro tool and for in vivo tumor diagnosis by PET imaging.

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  Cite this article

[IEEE Style]

S. Kim, N. Choi, S. Hwang, M. S. Yim, J. Lee, S. Lee, G. Cho, E. K. Ryu, "Folate Receptor-Specific Positron Emission Tomography Imaging with Folic Acid-Conjugated Tissue Inhibitor of Metalloproteinase-2," Bulletin of the Korean Chemical Society, vol. 34, no. 11, pp. 3243-3248, 2013. DOI: 10.5012/bkcs.2013.34.11.3243.

[ACM Style]

Sung-Min Kim, Naeun Choi, Seungkyun Hwang, Min Su Yim, Jung-Sik Lee, Sang-Mok Lee, Gyunggoo Cho, and Eun Kyoung Ryu. 2013. Folate Receptor-Specific Positron Emission Tomography Imaging with Folic Acid-Conjugated Tissue Inhibitor of Metalloproteinase-2. Bulletin of the Korean Chemical Society, 34, 11, (2013), 3243-3248. DOI: 10.5012/bkcs.2013.34.11.3243.

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ISSN(Print) 0253-2964
ISSN(Online) 1229-5949