| RRC ID |
57826
|
| 著者 |
Kawatani M, Yamamoto K, Yamada D, Kamiya M, Miyakawa J, Miyama Y, Kojima R, Morikawa T, Kume H, Urano Y.
|
| タイトル |
Fluorescence Detection of Prostate Cancer by an Activatable Fluorescence Probe for PSMA Carboxypeptidase Activity.
|
| ジャーナル |
J Am Chem Soc
|
| Abstract |
Prostate cancer (PCa) is a common malignant tumor among adult males, and convenient intraoperative detection of PCa would reduce the risk of leaving positive surgical margins, especially during nerve-sparing procedures. To achieve rapid, fluorescence-based visualization of PCa, we focused on the glutamate carboxypeptidase (CP) activity of prostate-specific membrane antigen (PSMA), a type II transmembrane glycoprotein that is attracting attention as a PCa biomarker. Based on our finding that aryl glutamate conjugates with an azoformyl linker are recognized by PSMA and have a sufficiently low LUMO (lowest unoccupied molecular orbital) energy level to quench the fluorophore through photoinduced electron transfer, we designed and synthesized a first-in-class activatable fluorescence probe for CP activity of PSMA. The developed probe allowed us to visualize the CP activity of PSMA in living cells and in clinical specimens from PCa patients and is expected to be useful for rapid intraoperative detection and diagnosis of PCa.
|
| 巻・号 |
141(26)
|
| ページ |
10409-10416
|
| 公開日 |
2019-7-3
|
| DOI |
10.1021/jacs.9b04412
|
| PMID |
31244179
|
| MeSH |
Antigens, Surface / analysis
Antigens, Surface / metabolism*
Cell Line, Tumor
Fluorescence*
Fluorescent Dyes / chemistry*
Glutamate Carboxypeptidase II / analysis
Glutamate Carboxypeptidase II / metabolism*
Humans
Male
Molecular Structure
Optical Imaging
PC-3 Cells
Prostatic Neoplasms / diagnostic imaging*
Prostatic Neoplasms / metabolism
Recombinant Proteins / analysis
Recombinant Proteins / metabolism
Spectrometry, Fluorescence
Substrate Specificity
|
| IF |
14.695
|
| 引用数 |
7
|
| リソース情報 |
| ヒト・動物細胞 |
LNCap.FGC(RCB2144) |
