scholarly journals A Flexible Synthesis of 68Ga-Labeled Carbonic Anhydrase IX (CAIX)-Targeted Molecules via CBT/1,2-Aminothiol Click Reaction

Molecules ◽  
2018 ◽  
Vol 24 (1) ◽  
pp. 23 ◽  
Author(s):  
Kuo-Ting Chen ◽  
Kevin Nguyen ◽  
Christian Ieritano ◽  
Feng Gao ◽  
Yann Seimbille
Keyword(s):  
Carbonic Anhydrase ◽  
Half Life ◽  
Reaction Rate ◽  
Click Reaction ◽  
Tumor Hypoxia ◽  
Carbonic Anhydrase Ix ◽  
Reaction Conditions ◽  
Positron Emitter ◽  
Radiochemical Yields ◽  
Gallium 68

We herein describe a flexible synthesis of a small library of 68Ga-labeled CAIX-targeted molecules via an orthogonal 2-cyanobenzothiazole (CBT)/1,2-aminothiol click reaction. Three novel CBT-functionalized chelators (1–3) were successfully synthesized and labeled with the positron emitter gallium-68. Cross-ligation between the pre-labeled bifunctional chelators (BFCs) and the 1,2-aminothiol-acetazolamide derivatives (8 and 9) yielded six new 68Ga-labeled CAIX ligands with high radiochemical yields. The click reaction conditions were optimized to improve the reaction rate for applications with short half-life radionuclides. Overall, our methodology allows for a simple and efficient radiosynthetic route to produce a variety of 68Ga-labeled imaging agents for tumor hypoxia.

scholarly journals Effect of distributional heterogeneity on the analysis of tumor hypoxia based on carbonic anhydrase IX

2007 ◽  
Vol 87 (12) ◽  
pp. 1206-1217 ◽  
Author(s):  
Vladimir V Iakovlev ◽  
Melania Pintilie ◽  
Andrew Morrison ◽  
Anthony W Fyles ◽  
Richard P Hill ◽  
...  
Keyword(s):  
Carbonic Anhydrase ◽  
Tumor Hypoxia ◽  
Carbonic Anhydrase Ix

scholarly journals Targeting Tumor Hypoxia: Suppression of Breast Tumor Growth and Metastasis by Novel Carbonic Anhydrase IX Inhibitors

2011 ◽  
Vol 71 (9) ◽  
pp. 3364-3376 ◽  
Author(s):  
Yuanmei Lou ◽  
Paul C. McDonald ◽  
Arusha Oloumi ◽  
Stephen Chia ◽  
Christina Ostlund ◽  
...  
Keyword(s):  
Carbonic Anhydrase ◽  
Tumor Growth ◽  
Breast Tumor ◽  
Tumor Hypoxia ◽  
Carbonic Anhydrase Ix ◽  
Tumor Growth And Metastasis

scholarly journals Synthesis and biological evaluation of a 99mTc-labelled sulfonamide conjugate for in vivo visualization of carbonic anhydrase IX expression in tumor hypoxia

2010 ◽  
Vol 37 (5) ◽  
pp. 557-564 ◽  
Author(s):  
Vamsidhar Akurathi ◽  
Ludwig Dubois ◽  
Natasja G. Lieuwes ◽  
Satish K. Chitneni ◽  
Bernard J. Cleynhens ◽  
...  
Keyword(s):  
Carbonic Anhydrase ◽  
Tumor Hypoxia ◽  
Biological Evaluation ◽  
Carbonic Anhydrase Ix ◽  
Synthesis And Biological Evaluation

scholarly journals Carbonic Anhydrase IX—Mouse versus Human

2019 ◽  
Vol 21 (1) ◽  
pp. 246
Author(s):  
Martina Takacova ◽  
Monika Barathova ◽  
Miriam Zatovicova ◽  
Tereza Golias ◽  
Ivana Kajanova ◽  
...  
Keyword(s):  
Transcriptional Regulation ◽  
Carbonic Anhydrase ◽  
Functional Properties ◽  
Ph Regulation ◽  
Tumor Hypoxia ◽  
Data Interpretation ◽  
Tissue Expression ◽  
Carbonic Anhydrase Ix ◽  
Ca Ix ◽  
Cell Adhesion And Migration

In contrast to human carbonic anhydrase IX (hCA IX) that has been extensively studied with respect to its molecular and functional properties as well as regulation and expression, the mouse ortholog has been investigated primarily in relation to tissue distribution and characterization of CA IX-deficient mice. Thus, no data describing transcriptional regulation and functional properties of the mouse CA IX (mCA IX) have been published so far, despite its evident potential as a biomarker/target in pre-clinical animal models of tumor hypoxia. Here, we investigated for the first time, the transcriptional regulation of the Car9 gene with a detailed description of its promoter. Moreover, we performed a functional analysis of the mCA IX protein focused on pH regulation, cell–cell adhesion, and migration. Finally, we revealed an absence of a soluble extracellular form of mCA IX and provided the first experimental evidence of mCA IX presence in exosomes. In conclusion, though the protein characteristics of hCA IX and mCA IX are highly similar, and the transcription of both genes is predominantly governed by hypoxia, some attributes of transcriptional regulation are specific for either human or mouse and as such, could result in different tissue expression and data interpretation.

Albumin/sulfonamide stabilized iron porphyrin metal organic framework nanocomposites: targeting tumor hypoxia by carbonic anhydrase IX inhibition and T1–T2 dual mode MRI guided photodynamic/photothermal therapy

2018 ◽  
Vol 6 (2) ◽  
pp. 265-276 ◽  
Author(s):  
Wei Zhu ◽  
Yao Liu ◽  
Zhe Yang ◽  
Li Zhang ◽  
Liji Xiao ◽  
...  
Keyword(s):  
Carbonic Anhydrase ◽  
Photothermal Therapy ◽  
Metal Organic Framework ◽  
Tumor Hypoxia ◽  
Carbonic Anhydrase Ix ◽  
Iron Porphyrin ◽  
Dual Mode ◽  
Metal Organic ◽  
Mri Guided ◽  
Organic Framework

We report BSA and SA stabilized iron porphyrin MOF nanocomposites with tremendous potential in tumor hypoxic imaging guided PDT and PTT.

Synthesis and SAR of Novel Re/99mTc-Labeled Benzenesulfonamide Carbonic Anhydrase IX Inhibitors for Molecular Imaging of Tumor Hypoxia

2013 ◽  
Vol 56 (2) ◽  
pp. 510-520 ◽  
Author(s):  
Genliang Lu ◽  
Shawn M. Hillier ◽  
Kevin P. Maresca ◽  
Craig N. Zimmerman ◽  
William C. Eckelman ◽  
...  
Keyword(s):  
Molecular Imaging ◽  
Carbonic Anhydrase ◽  
Tumor Hypoxia ◽  
Carbonic Anhydrase Ix

scholarly journals In Vivo Imaging and Quantification of Carbonic Anhydrase IX Expression as an Endogenous Biomarker of Tumor Hypoxia

PLoS ONE ◽  
2012 ◽  
Vol 7 (11) ◽  
pp. e50860 ◽  
Author(s):  
Bagna Bao ◽  
Kevin Groves ◽  
Jun Zhang ◽  
Emma Handy ◽  
Paul Kennedy ◽  
...  
Keyword(s):  
Carbonic Anhydrase ◽  
In Vivo Imaging ◽  
Tumor Hypoxia ◽  
Carbonic Anhydrase Ix
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