scholarly journals Copper-Free ‘Click’ Chemistry-Based Synthesis and Characterization of Carbonic Anhydrase-IX Anchored Albumin-Paclitaxel Nanoparticles for Targeting Tumor Hypoxia

2018 ◽  
Vol 19 (3) ◽  
pp. 838 ◽  
Author(s):  
Katyayani Tatiparti ◽  
Samaresh Sau ◽  
Kaustubh Gawde ◽  
Arun Iyer
Keyword(s):  
Carbonic Anhydrase ◽  
Click Chemistry ◽  
Tumor Hypoxia ◽  
Carbonic Anhydrase Ix ◽  
Synthesis And Characterization

The synthesis and characterization of novel coumarin-containing cyanine dyes via “Click” chemistry

2008 ◽  
Vol 34 (2-3) ◽  
pp. 229-239 ◽  
Author(s):  
Wen-Hai Zhan ◽  
Jian-Li Hua ◽  
Ying-Hua Jin ◽  
Xin Teng ◽  
He Tian
Keyword(s):  
Click Chemistry ◽  
Cyanine Dyes ◽  
Synthesis And Characterization

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 Synthesis and characterization of hydrogel microsphere matrices with tunable bioactivity using click chemistry

2016 ◽  
Vol 4 ◽  
Author(s):  
Jivan Faraz ◽  
Yegappan Ramanathan ◽  
Wyman Omar ◽  
Pearce Hannah ◽  
Gaharwar Akhilesh ◽  
...  
Keyword(s):  
Click Chemistry ◽  
Synthesis And Characterization ◽  
Hydrogel Microsphere

scholarly journals Sortase-mediated site-specific modification of interleukin-2 for the generation of a tumor targeting acetazolamide-cytokine conjugate

2020 ◽  
Author(s):  
Baptiste Gouyou ◽  
J Millul ◽  
A Villa ◽  
S Cazzamalli ◽  
D Neri ◽  
...  
Keyword(s):  
Carbonic Anhydrase ◽  
Tumor Targeting ◽  
Interleukin 2 ◽  
Industrial Applications ◽  
Carbonic Anhydrase Ix ◽  
Site Specific ◽  
Tumor Bearing ◽  
Bioactive Proteins

1.AbstractSmall ligands specific to tumor-associated antigens can be used as alternatives to antibodies for the delivery of small payloads such as radionuclides, cytotoxic drugs and fluorophores. Their use as delivery moiety of bioactive proteins like cytokines remains largely unexplored. Here, we describe the preparation and in vivo characterization of the first small molecule-cytokine conjugate targeting carbonic anhydrase IX (CAIX), a marker of renal cell carcinoma and hypoxia. Site-specific conjugation between interleukin-2 and acetazolamide was obtained by Sortase A-mediated transpeptidation. Binding of the conjugate to the cognate CAIX antigen was confirmed by surface plasmon resonance. The in vivo targeting of structures expressing carbonic anhydrase IX was assessed by biodistribution experiments in tumor bearing mice. Optimization of manufacturability and tumor targeting performance of acetazolamide-cytokine products will be required in order to enable industrial applications.Graphical abstract

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