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 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 Carbonic Anhydrase IX in Renal Cell Carcinoma, Implications for Disease Management

2020 ◽  
Vol 21 (19) ◽  
pp. 7146
Author(s):  
Jean Courcier ◽  
Alexandre de la Taille ◽  
Maya Nourieh ◽  
Ingrid Leguerney ◽  
Nathalie Lassau ◽  
...  
Keyword(s):  
Renal Cell Carcinoma ◽  
Molecular Imaging ◽  
Carbonic Anhydrase ◽  
Cell Carcinoma ◽  
Renal Cell ◽  
Renal Carcinoma ◽  
Current Knowledge ◽  
Checkpoint Inhibitors ◽  
Hypoxia Inducible Factor ◽  
Carbonic Anhydrase Ix

Carbonic Anhydrase IX (CAIX) is a well-described enzyme in renal cell carcinoma, with its expression being regulated by the hypoxia-inducible factor 1 alpha, it is known for interfering with hypoxia processes. Renal carcinoma encompasses a broad spectrum of histological entities and is also described as a heterogeneous malignant tumor. Recently, various combinations of checkpoint inhibitors and targeted therapies have been validated to manage this disease. Reliable markers to confirm the diagnosis, estimate the prognosis, predict or monitor the treatment response are required. Molecular imaging developments allow a comprehensive analysis of the tumor, overcoming the spatial heterogeneity issue. CAIX, being highly expressed at the tumor cell surfaces of clear cell renal carcinoma, also represents a potential treatment target. In this manuscript we reviewed the current knowledge from the literature on the pathophysiological interactions between renal cell carcinoma and CAIX, the role of CAIX as a marker for diagnosis, prognosis, treatment monitoring and molecular imaging, and the potential target for therapeutic strategies.

scholarly journals Is carbonic anhydrase IX a validated target for molecular imaging of cancer and hypoxia?

2015 ◽  
Vol 11 (10) ◽  
pp. 1531-1541 ◽  
Author(s):  
Jianbo Li ◽  
Guojian Zhang ◽  
Xuemei Wang ◽  
Xiao-Feng Li
Keyword(s):  
Molecular Imaging ◽  
Carbonic Anhydrase ◽  
Carbonic Anhydrase Ix

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

Molecular imaging and carbonic anhydrase IX-targeted radioimmunotherapy in clear cell renal cell carcinoma

Immunotherapy ◽  
2013 ◽  
Vol 5 (5) ◽  
pp. 489-495 ◽  
Author(s):  
Stijn Muselaers ◽  
Peter Mulders ◽  
Egbert Oosterwijk ◽  
Wim Oyen ◽  
Otto Boerman
Keyword(s):  
Renal Cell Carcinoma ◽  
Molecular Imaging ◽  
Carbonic Anhydrase ◽  
Cell Carcinoma ◽  
Renal Cell ◽  
Clear Cell ◽  
Carbonic Anhydrase Ix ◽  
Cell Renal Cell Carcinoma
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