| RRC ID |
41860
|
| 著者 |
Nishii R, Kawai K, Garcia Flores L 2nd, Kataoka H, Jinnouchi S, Nagamachi S, Arano Y, Tamura S.
|
| タイトル |
A novel radiopharmaceutical for detection of malignant melanoma, based on melanin formation: 3-iodo-4-hydroxyphenyl-L-cysteine.
|
| ジャーナル |
Nucl Med Commun
|
| Abstract |
The aim of this study was to develop a new artificial amino acid radiopharmaceutical labelled with radioiodine for detection of malignant melanoma, based on melanin formation. By considering the affinity for tyrosinase, a starting enzyme on the branching point to melanin biosynthesis, 3-[125I]iodo-4-hydroxyphenyl-L-cysteine (125I-L-PC) was synthesized and evaluated biologically. Labelling of 125I-L-PC using the chloramine-T method was carried out conveniently and efficiently in a short period of time, with high specific activity. In a biodistribution study, 125I-L-PC showed a low accumulation in normal tissue and relative retention in B16 melanoma. A high contrast image of peripheral tumour was obtained during autoradiography. During an in vitro accumulation study, inhibition of 125I-L-PC with a tyrosinase inhibitor suggested interaction of this tracer with tyrosinase. It indicates that the uptake mechanism of 125I-L-PC to melanoma tissue was dependent on high tyrosinase activity in melanoma cells. Thus, 125I-L-PC appears to be a promising radioiodinated amino acid radiopharmaceutical for imaging malignant melanoma in relation to melanin formation, namely specific metabolism with high tyrosinase activity.
|
| 巻・号 |
24(5)
|
| ページ |
575-82
|
| 公開日 |
2003-5-1
|
| DOI |
10.1097/00006231-200305000-00015
|
| PMID |
12717077
|
| MeSH |
Animals
Cysteine / analogs & derivatives
Cysteine / chemical synthesis
Cysteine / pharmacokinetics*
Isotope Labeling / methods
Melanins / biosynthesis*
Melanoma / diagnostic imaging*
Melanoma / metabolism*
Mice
Mice, Inbred C57BL
Organ Specificity
Predictive Value of Tests
Radiopharmaceuticals / chemical synthesis
Radiopharmaceuticals / pharmacokinetics
Skin Neoplasms / diagnostic imaging
Skin Neoplasms / metabolism
Tissue Distribution
Tomography, Emission-Computed, Single-Photon / methods
Whole-Body Counting
|
| IF |
1.334
|
| 引用数 |
5
|
|
WOS 分野
|
RADIOLOGY, NUCLEAR MEDICINE & MEDICAL IMAGING
|
| リソース情報 |
| ヒト・動物細胞 |
B16 melanoma |
