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[(64)Cu]XYIMSR-06: A dual-motif CAIX ligand for PET imaging of clear cell renal cell carcinoma

Carbonic anhydrase IX (CAIX) is a cell surface enzyme that is over-expressed in approximately 95% of cases of clear cell renal cell carcinoma (ccRCC), the most common renal cancer. We synthesized and performed in vitro and in vivo evaluation of a dual-motif ligand, [(64)Cu]XYIMSR-06, for imaging CAI...

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Autores principales: Minn, Il, Koo, Soo Min, Lee, Hye Soo, Brummet, Mary, Rowe, Steven P., Gorin, Michael A., Sysa-Shah, Polina, Lewis, William D., Ahn, Hye-Hyun, Wang, Yuchuan, Banerjee, Sangeeta Ray, Mease, Ronnie C., Nimmagadda, Sridhar, Allaf, Mohamad E., Pomper, Martin G., Yang, Xing
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Impact Journals LLC 2016
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5302928/
https://www.ncbi.nlm.nih.gov/pubmed/27437764
http://dx.doi.org/10.18632/oncotarget.10602
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author Minn, Il
Koo, Soo Min
Lee, Hye Soo
Brummet, Mary
Rowe, Steven P.
Gorin, Michael A.
Sysa-Shah, Polina
Lewis, William D.
Ahn, Hye-Hyun
Wang, Yuchuan
Banerjee, Sangeeta Ray
Mease, Ronnie C.
Nimmagadda, Sridhar
Allaf, Mohamad E.
Pomper, Martin G.
Yang, Xing
author_facet Minn, Il
Koo, Soo Min
Lee, Hye Soo
Brummet, Mary
Rowe, Steven P.
Gorin, Michael A.
Sysa-Shah, Polina
Lewis, William D.
Ahn, Hye-Hyun
Wang, Yuchuan
Banerjee, Sangeeta Ray
Mease, Ronnie C.
Nimmagadda, Sridhar
Allaf, Mohamad E.
Pomper, Martin G.
Yang, Xing
author_sort Minn, Il
collection PubMed
description Carbonic anhydrase IX (CAIX) is a cell surface enzyme that is over-expressed in approximately 95% of cases of clear cell renal cell carcinoma (ccRCC), the most common renal cancer. We synthesized and performed in vitro and in vivo evaluation of a dual-motif ligand, [(64)Cu]XYIMSR-06, for imaging CAIX expression on ccRCC tumors using positron emission tomography (PET). [(64)Cu]XYIMSR-06 was generated in yields of 51.0 ± 4.5% (n=5) and specific activities of 4.1 – 8.9 GBq/μmol (110-240 Ci/mmol). Tumor was visualized on PET images by 1 h post-injection with high tumor-to-background levels (>100 tumor-to-blood and -muscle) achieved within 24 h. Biodistribution studies demonstrated a maximum tumor uptake of 19.3% injected dose per gram of radioactivity at 4 h. Tumor-to-blood, -muscle and -kidney ratios were 129.6 ± 18.8, 84.3 ± 21.0 and 2.1 ± 0.3, respectively, at 8 h post-injection. At 24 h a tumor-to-kidney ratio of 7.1 ± 2.5 was achieved. These results indicate pharmacokinetics superior to those of previously reported imaging agents binding to CAIX. [(64)Cu]XYIMSR-06 is a new low-molecular-weight PET ligand targeting CAIX, which can image localized and metastatic ccRCC.
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spelling pubmed-53029282017-02-13 [(64)Cu]XYIMSR-06: A dual-motif CAIX ligand for PET imaging of clear cell renal cell carcinoma Minn, Il Koo, Soo Min Lee, Hye Soo Brummet, Mary Rowe, Steven P. Gorin, Michael A. Sysa-Shah, Polina Lewis, William D. Ahn, Hye-Hyun Wang, Yuchuan Banerjee, Sangeeta Ray Mease, Ronnie C. Nimmagadda, Sridhar Allaf, Mohamad E. Pomper, Martin G. Yang, Xing Oncotarget Research Paper Carbonic anhydrase IX (CAIX) is a cell surface enzyme that is over-expressed in approximately 95% of cases of clear cell renal cell carcinoma (ccRCC), the most common renal cancer. We synthesized and performed in vitro and in vivo evaluation of a dual-motif ligand, [(64)Cu]XYIMSR-06, for imaging CAIX expression on ccRCC tumors using positron emission tomography (PET). [(64)Cu]XYIMSR-06 was generated in yields of 51.0 ± 4.5% (n=5) and specific activities of 4.1 – 8.9 GBq/μmol (110-240 Ci/mmol). Tumor was visualized on PET images by 1 h post-injection with high tumor-to-background levels (>100 tumor-to-blood and -muscle) achieved within 24 h. Biodistribution studies demonstrated a maximum tumor uptake of 19.3% injected dose per gram of radioactivity at 4 h. Tumor-to-blood, -muscle and -kidney ratios were 129.6 ± 18.8, 84.3 ± 21.0 and 2.1 ± 0.3, respectively, at 8 h post-injection. At 24 h a tumor-to-kidney ratio of 7.1 ± 2.5 was achieved. These results indicate pharmacokinetics superior to those of previously reported imaging agents binding to CAIX. [(64)Cu]XYIMSR-06 is a new low-molecular-weight PET ligand targeting CAIX, which can image localized and metastatic ccRCC. Impact Journals LLC 2016-07-14 /pmc/articles/PMC5302928/ /pubmed/27437764 http://dx.doi.org/10.18632/oncotarget.10602 Text en Copyright: © 2016 Minn et al. http://creativecommons.org/licenses/by/2.5/ This is an open-access article distributed under the terms of the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original author and source are credited.
spellingShingle Research Paper
Minn, Il
Koo, Soo Min
Lee, Hye Soo
Brummet, Mary
Rowe, Steven P.
Gorin, Michael A.
Sysa-Shah, Polina
Lewis, William D.
Ahn, Hye-Hyun
Wang, Yuchuan
Banerjee, Sangeeta Ray
Mease, Ronnie C.
Nimmagadda, Sridhar
Allaf, Mohamad E.
Pomper, Martin G.
Yang, Xing
[(64)Cu]XYIMSR-06: A dual-motif CAIX ligand for PET imaging of clear cell renal cell carcinoma
title [(64)Cu]XYIMSR-06: A dual-motif CAIX ligand for PET imaging of clear cell renal cell carcinoma
title_full [(64)Cu]XYIMSR-06: A dual-motif CAIX ligand for PET imaging of clear cell renal cell carcinoma
title_fullStr [(64)Cu]XYIMSR-06: A dual-motif CAIX ligand for PET imaging of clear cell renal cell carcinoma
title_full_unstemmed [(64)Cu]XYIMSR-06: A dual-motif CAIX ligand for PET imaging of clear cell renal cell carcinoma
title_short [(64)Cu]XYIMSR-06: A dual-motif CAIX ligand for PET imaging of clear cell renal cell carcinoma
title_sort [(64)cu]xyimsr-06: a dual-motif caix ligand for pet imaging of clear cell renal cell carcinoma
topic Research Paper
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5302928/
https://www.ncbi.nlm.nih.gov/pubmed/27437764
http://dx.doi.org/10.18632/oncotarget.10602
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