scholarly journals Bioavailability, tissue distribution, and excretion characteristics of the novel carbonic anhydrase inhibitor tolsultazolamide in rats

2013 ◽  
Vol 35 (2) ◽  
pp. 275-282 ◽  
Author(s):  
Jin-da Wang ◽  
Yong-ping Shi ◽  
Jing Yin ◽  
Zhi-yuan Pan ◽  
Wen-yu Cui ◽  
...  
Keyword(s):  
Carbonic Anhydrase ◽  
Tissue Distribution ◽  
Carbonic Anhydrase Inhibitor ◽  
The Novel

The Effect of a Carbonic Anhydrase Inhibitor, Diamox, On Human Pancreatic Secretion

1955 ◽  
Vol 29 (2) ◽  
pp. 262-279 ◽  
Author(s):  
David A. Dreiling ◽  
Henry D. Janowitz ◽  
Mark Halpern
Keyword(s):  
Carbonic Anhydrase ◽  
Pancreatic Secretion ◽  
Carbonic Anhydrase Inhibitor

The Carbonic Anhydrase Inhibitor E7070 Sensitizes Glioblastoma Cells to Radio- and Chemotherapy and Reduces Tumor Growth

2021 ◽  
Author(s):  
Silvia A. Teixeira ◽  
Mariano S. Viapiano ◽  
Augusto F. Andrade ◽  
Mohan S. Nandhu ◽  
Julia A. Pezuk ◽  
...  
Keyword(s):  
Carbonic Anhydrase ◽  
Tumor Growth ◽  
Carbonic Anhydrase Inhibitor ◽  
Glioblastoma Cells

scholarly journals The Influence of Varying Fluorination Patterns on the Thermodynamics and Kinetics of Benzenesulfonamide Binding to Human Carbonic Anhydrase II

Biomolecules ◽  
2020 ◽  
Vol 10 (4) ◽  
pp. 509 ◽  
Author(s):  
Steffen Glöckner ◽  
Khang Ngo ◽  
Björn Wagner ◽  
Andreas Heine ◽  
Gerhard Klebe
Keyword(s):  
Carbonic Anhydrase ◽  
Carbonic Anhydrase Ii ◽  
The Novel ◽  
Binding Modes ◽  
X Ray ◽  
Structure Activity ◽  
Small Set ◽  
Novel Method ◽  
Human Carbonic Anhydrase ◽  
Kinetics Of

The fluorination of lead-like compounds is a common tool in medicinal chemistry to alter molecular properties in various ways and with different goals. We herein present a detailed study of the binding of fluorinated benzenesulfonamides to human Carbonic Anhydrase II by complementing macromolecular X-ray crystallographic observations with thermodynamic and kinetic data collected with the novel method of kinITC. Our findings comprise so far unknown alternative binding modes in the crystalline state for some of the investigated compounds as well as complex thermodynamic and kinetic structure-activity relationships. They suggest that fluorination of the benzenesulfonamide core is especially advantageous in one position with respect to the kinetic signatures of binding and that a higher degree of fluorination does not necessarily provide for a higher affinity or more favorable kinetic binding profiles. Lastly, we propose a relationship between the kinetics of binding and ligand acidity based on a small set of compounds with similar substitution patterns.

Polypharmacology of epacadostat: a potent and selective inhibitor of the tumor associated carbonic anhydrases IX and XII

2019 ◽  
Vol 55 (40) ◽  
pp. 5720-5723 ◽  
Author(s):  
Andrea Angeli ◽  
Marta Ferraroni ◽  
Alessio Nocentini ◽  
Silvia Selleri ◽  
Paola Gratteri ◽  
...  
Keyword(s):  
Carbonic Anhydrase ◽  
Selective Inhibitor ◽  
Carbonic Anhydrase Inhibitor ◽  
Carbonic Anhydrases ◽  
Indoleamine 2,3 Dioxygenase

Epacadostat (EPA), a selective indoleamine-2,3-dioxygenase 1 (IDO1) inhibitor, has been investigatedin vitroas a human (h) Carbonic Anhydrase Inhibitor (CAI).

Structural modulation of the biological activity of gold nanoparticles functionalized with a carbonic anhydrase inhibitor

2013 ◽  
Vol 36 (5) ◽  
Author(s):  
Francesca Bellissima ◽  
Fabrizio Carta ◽  
Alessio Innocenti ◽  
Andrea Scozzafava ◽  
Piero Baglioni ◽  
...  
Keyword(s):  
Gold Nanoparticles ◽  
Biological Activity ◽  
Carbonic Anhydrase ◽  
Carbonic Anhydrase Inhibitor ◽  
Structural Modulation
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