Discovery and Characterization of Novel Selective Inhibitors of Carbonic Anhydrase IX

2014 ◽  
Vol 57 (22) ◽  
pp. 9435-9446 ◽  
Author(s):  
Virginija Dudutienė ◽  
Jurgita Matulienė ◽  
Alexey Smirnov ◽  
David D. Timm ◽  
Asta Zubrienė ◽  
...  
Keyword(s):  
Carbonic Anhydrase ◽  
Carbonic Anhydrase Ix ◽  
Selective Inhibitors

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

Metallacarborane Sulfamides: Unconventional, Specific, and Highly Selective Inhibitors of Carbonic Anhydrase IX

2019 ◽  
Vol 62 (21) ◽  
pp. 9560-9575 ◽  
Author(s):  
Bohumír Grüner ◽  
Jiří Brynda ◽  
Viswanath Das ◽  
Václav Šícha ◽  
Jana Štěpánková ◽  
...  
Keyword(s):  
Carbonic Anhydrase ◽  
Carbonic Anhydrase Ix ◽  
Selective Inhibitors

scholarly journals Isolation and characterization of monoclonal antibodies against human carbonic anhydrase-IX

mAbs ◽  
2021 ◽  
Vol 13 (1) ◽  
Author(s):  
Anne E.G. Lenferink ◽  
Paul C. McDonald ◽  
Christiane Cantin ◽  
Suzanne Grothé ◽  
Mylene Gosselin ◽  
...  
Keyword(s):  
Monoclonal Antibodies ◽  
Carbonic Anhydrase ◽  
Carbonic Anhydrase Ix ◽  
Isolation And Characterization ◽  
Human Carbonic Anhydrase

scholarly journals α,γ-Diketocarboxylic Acids and Their Esters Act as Carbonic Anhydrase IX and XII Selective Inhibitors

2019 ◽  
Vol 10 (4) ◽  
pp. 661-665 ◽  
Author(s):  
Alessio Nocentini ◽  
Alessia Lucidi ◽  
Francesca Perut ◽  
Annamaria Massa ◽  
Daniela Tomaselli ◽  
...  
Keyword(s):  
Carbonic Anhydrase ◽  
Carbonic Anhydrase Ix ◽  
Selective Inhibitors

scholarly journals Cobalt Bis(dicarbollide) Alkylsulfonamides: Potent and Highly Selective Inhibitors of Tumor Specific Carbonic Anhydrase IX

ChemPlusChem ◽  
2020 ◽  
Author(s):  
Bohumír Grüner ◽  
Michael Kugler ◽  
Suzan El Anwar ◽  
Josef Holub ◽  
Jan Nekvinda ◽  
...  
Keyword(s):  
Carbonic Anhydrase ◽  
Carbonic Anhydrase Ix ◽  
Selective Inhibitors

Sulfonamido carboranes as highly selective inhibitors of cancer-specific carbonic anhydrase IX

2020 ◽  
Vol 200 ◽  
pp. 112460 ◽  
Author(s):  
Jana Dvořanová ◽  
Michael Kugler ◽  
Josef Holub ◽  
Václav Šícha ◽  
Viswanath Das ◽  
...  
Keyword(s):  
Carbonic Anhydrase ◽  
Carbonic Anhydrase Ix ◽  
Selective Inhibitors

scholarly journals Novel benzoyl thioureido benzene sulfonamides as highly potent and selective inhibitors of carbonic anhydrase IX: optimization and bioactive studies

MedChemComm ◽  
2018 ◽  
Vol 9 (12) ◽  
pp. 2100-2105 ◽  
Author(s):  
Li Liu ◽  
Wanqi Wang ◽  
Jin Huang ◽  
Zhenjiang Zhao ◽  
Honglin Li ◽  
...  
Keyword(s):  
Carbonic Anhydrase ◽  
Inhibitory Activity ◽  
Carbonic Anhydrase Ix ◽  
Selective Inhibitors ◽  
Ca Ix

Novel benzoyl thioureido benzene sulfonamides as CA IX inhibitors such as 6a displayed inhibitory activity against CA IX with an IC50 value of 0.48 nM and about 1500-fold selectivity over CA II were reported.

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