1. Acetazolamide-based [18F]-PET tracer: In vivo validation of carbonic anhydrase IX as a sole target for imaging of CA-IX expressing hypoxic solid tumors.
- Author
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More, Kunal N., Lee, Jun Young, Kim, Dong-Yeon, Cho, Nam-Chul, Pyo, Ayoung, Yun, Misun, Kim, Hyeon Sik, Kim, Hangun, Ko, Kwangseok, Park, Jeong-Hoon, and Chang, Dong-Jo
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ACETAZOLAMIDE , *CARBONIC anhydrase , *LYASES , *TUMOR treatment , *TARGETED drug delivery , *THERAPEUTICS - Abstract
Carbonic anhydrase IX is overexpressed in many solid tumors including hypoxic tumors and is a potential target for cancer therapy and diagnosis. Reported imaging agents targeting CA-IX are successful mostly in clear cell renal carcinoma as SKRC-52 and no candidate was approved yet in clinical trials for imaging of CA-IX. To validate CA-IX as a valid target for imaging of hypoxic tumor, we designed and synthesized novel [ 18 F]-PET tracer ( 1 ) based on acetazolamide which is one of the well-known CA-IX inhibitors and performed imaging study in CA-IX expressing hypoxic tumor model as 4T1 and HT-29 in vivo models other than SKRC-52. [ 18 F]-acetazolamide ( 1 ) was found to be insufficient for the specific accumulation in CA-IX expressing tumor. This study might be useful to understand in vivo behavior of acetazolamide PET tracer and can contribute to the development of successful PET imaging agents targeting CA-IX in future. Additional study is needed to understand the mechanism of poor targeting of CA-IX, as if CA-IX is not reliable as a sole target for imaging of CA-IX expressing hypoxic solid tumors. [ABSTRACT FROM AUTHOR]
- Published
- 2018
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