| Title |
Synthesis and evaluation of ortho-[18F]fluorocelecoxib for COX-2 cholangiocarcinoma imaging
|
|---|---|
| Published in |
Drug Design, Development and Therapy, May 2018
|
| DOI | 10.2147/dddt.s161718 |
| Pubmed ID | |
| Authors |
Chi-Wei Chang, Chun-Nan Yeh, Yi-Hsiu Chung, Yong-Ren Chen, Shi-Wei Tien, Tsung-Wen Chen, Shiou-Shiow Farn, Ying-Cheng Huang, Chung-Shan Yu |
| Abstract |
An 18F-tagged NSAID analog was prepared for use as a probe for COX-2 expression, which is associated with tumor development. The in vivo uptake of celecoxib was monitored with ortho-[18F]fluorocelecoxib using positron emission tomography (PET). The binding affinity of ortho-[18F]fluorocelecoxib to COX-1 and COX-2 enzymes were assessed using the competitor celecoxib. The IC50 values were 0.039 μM and 0.024 μM, respectively. A selectivity index of 1.63 was obtained (COX-2 vs COX-1). COX-2 overexpressed cholangiocarcinoma (CCA) murine cells took up more ortho-[18F]fluorocelecoxib than that by usual CCA cells from 10 to 60 minutes post incubation. Competitive inhibition (blocking) of the tracer uptake of ortho-[18F]fluorocelecoxib in the presence of celecoxib by the COX-2 overexpressed CCA cells and the usual CCA cells gave the IC50 values of 0.5 μM and 46.5 μM, respectively. Based on the in vitro accumulation data and in vivo metabolism half-life (30 min), PET scanning was performed 30-60 min after the administration of ortho-[18F]fluorocelecoxib through the tail vein. Study of ortho-[18F]F-celecoxib in the CCA rats showed a tumor to normal ratio (T/N) of 1.38±0.23 and uptake dose of 1.14±0.25 (%ID/g). The inferior in vivo blocking results of 1.48±0.20 (T/N) and 1.18±0.22 (%ID/g) suggests that the nonspecificity is associated with the complex role of peroxidase or the binding to carbonic anhydrase. |
X Demographics
The data shown below were collected from the profile of 1 X user who shared this research output. Click here to find out more about how the information was compiled.
Geographical breakdown
| Country | Count | As % |
|---|---|---|
| Taiwan | 1 | 100% |
Demographic breakdown
| Type | Count | As % |
|---|---|---|
| Members of the public | 1 | 100% |
Mendeley readers
The data shown below were compiled from readership statistics for 18 Mendeley readers of this research output. Click here to see the associated Mendeley record.
Geographical breakdown
| Country | Count | As % |
|---|---|---|
| Unknown | 18 | 100% |
Demographic breakdown
| Readers by professional status | Count | As % |
|---|---|---|
| Researcher | 4 | 22% |
| Student > Ph. D. Student | 3 | 17% |
| Student > Postgraduate | 3 | 17% |
| Student > Bachelor | 1 | 6% |
| Student > Master | 1 | 6% |
| Other | 3 | 17% |
| Unknown | 3 | 17% |
| Readers by discipline | Count | As % |
|---|---|---|
| Medicine and Dentistry | 4 | 22% |
| Chemistry | 4 | 22% |
| Social Sciences | 1 | 6% |
| Biochemistry, Genetics and Molecular Biology | 1 | 6% |
| Neuroscience | 1 | 6% |
| Other | 1 | 6% |
| Unknown | 6 | 33% |
Attention Score in Context
This research output has an Altmetric Attention Score of 1. This is our high-level measure of the quality and quantity of online attention that it has received. This Attention Score, as well as the ranking and number of research outputs shown below, was calculated when the research output was last mentioned on 24 May 2018.
All research outputs
#17,649,940
of 25,870,940 outputs
Outputs from Drug Design, Development and Therapy
#1,131
of 2,287 outputs
Outputs of similar age
#221,369
of 341,380 outputs
Outputs of similar age from Drug Design, Development and Therapy
#26
of 60 outputs
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