Synthesis and Biological Evaluation of Low Molecular Weight Fluorescent Imaging Agents for the Prostate-Specific Membrane Antigen
- Authors
- Chen, Ying; Pullambhatla, Mrudula; Banerjee, Sangeeta R.; Byun, Youngjoo; Stathis, Marigo; Rojas, Camilo; Slusher, Barbara S.; Mease, Ronnie C.; Pomper, Martin G.
- Issue Date
- 12월-2012
- Publisher
- AMER CHEMICAL SOC
- Citation
- BIOCONJUGATE CHEMISTRY, v.23, no.12, pp.2377 - 2385
- Indexed
- SCIE
SCOPUS
- Journal Title
- BIOCONJUGATE CHEMISTRY
- Volume
- 23
- Number
- 12
- Start Page
- 2377
- End Page
- 2385
- URI
- https://scholar.korea.ac.kr/handle/2021.sw.korea/106769
- DOI
- 10.1021/bc3003919
- ISSN
- 1043-1802
- Abstract
- Targeted near-infrared (MR) optical imaging can be used in vivo to detect specific tissues, including malignant cells. A series of NIR fluorescent ligands targeting the prostate-specific membrane antigen (PSMA) was synthesized and each compound was tested for its ability to image PSMA+ tissues in experimental models of prostate cancer. The agents were prepared by conjugating commercially available active esters of NIR dyes, including IRDye800CW, IRDye800RS, Cy5.5, Cy7, or a derivative of indocyanine green (ICG) to the terminal amine group of (S)-2-(3-((S)-5-amino-1-carboxypentyl)ureido)pentanedioic acid 1, (14S,18S)-1-amino-8,16-dioxo-3,6-dioxa-9,15,17-triazaicosane-14,18,20-tricarboxylic acid 2 and (3S,7S)-26-amino-5,13,20-trioxo-4,6,12,21-tetraaza-hexacosane-1,3,7,22-tetracarboxylic acid 3. The K-i values for the dye-inhibitor conjugates ranged from 1 to 700 pM. All compounds proved capable of imaging PSMA+ tumors selectively to varying degrees depending on the choice of fluorophore and linker. The highest tumor uptake was observed with IRDye800CW employing a poly(ethylene glycol) or lysine suberate linker, as in 800CW-2 and 800CW-3, while the highest tumor to nontarget tissue ratios were obtained for Cy7 with these same linkers, as in Cy7-2 and Cy7-3. Compounds 2 and 3 provide useful scaffolds for targeting of PSMA+ tissues in vivo and should be useful for preparing NIR dye conjugates designed specifically for clinical intraoperative optical imaging devices.
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Collections - College of Pharmacy > Department of Pharmaceutical Science > 1. Journal Articles
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