scholarly journals Synthesis, characterization, crystal structure and bioactivities of novel enamine and pyrrole derivatives endowed with acetylcholinesterase, α-glycosidase and human carbonic anhydrase inhibition effects

2021 ◽  
pp. 144-156
Author(s):  
İlhami Gülçin ◽  
Abel Maharramov ◽  
Malahat Kurbanova ◽  
Parham Taslimi ◽  
Yeliz Demir ◽  
...  
Keyword(s):  
Crystal Structure ◽  
Carbonic Anhydrase ◽  
Pyrrole Derivatives ◽  
Carbonic Anhydrase Inhibition ◽  
Human Carbonic Anhydrase

scholarly journals Azobenzene-based inhibitors of human carbonic anhydrase II

2015 ◽  
Vol 11 ◽  
pp. 1129-1135 ◽  
Author(s):  
Leander Simon Runtsch ◽  
David Michael Barber ◽  
Peter Mayer ◽  
Michael Groll ◽  
Dirk Trauner ◽  
...  
Keyword(s):  
Crystal Structure ◽  
Catalytic Activity ◽  
Carbonic Anhydrase ◽  
Drug Class ◽  
Carbonic Anhydrase Ii ◽  
Carbonic Anhydrases ◽  
X Ray ◽  
X Ray Crystallography ◽  
Human Carbonic Anhydrase

Aryl sulfonamides are a widely used drug class for the inhibition of carbonic anhydrases. In the context of our program of photochromic pharmacophores we were interested in the exploration of azobenzene-containing sulfonamides to block the catalytic activity of human carbonic anhydrase II (hCAII). Herein, we report the synthesis and in vitro evaluation of a small library of nine photochromic sulfonamides towards hCAII. All molecules are azobenzene-4-sulfonamides, which are substituted by different functional groups in the 4´-position and were characterized by X-ray crystallography. We aimed to investigate the influence of electron-donating or electron-withdrawing substituents on the inhibitory constant K i. With the aid of an hCAII crystal structure bound to one of the synthesized azobenzenes, we found that the electronic structure does not strongly affect inhibition. Taken together, all compounds are strong blockers of hCAII with K i = 25–65 nM that are potentially photochromic and thus combine studies from chemical synthesis, crystallography and enzyme kinetics.

scholarly journals Crystal structure of human carbonic anhydrase-related protein VIII reveals the basis for catalytic silencing

2009 ◽  
Vol 76 (2) ◽  
pp. 507-511 ◽  
Author(s):  
Sarah S. Picaud ◽  
João R. C. Muniz ◽  
Anneke Kramm ◽  
Ewa S. Pilka ◽  
Grazyna Kochan ◽  
...  
Keyword(s):  
Crystal Structure ◽  
Carbonic Anhydrase ◽  
Related Protein ◽  
Human Carbonic Anhydrase

Crystal Structure of Human Carbonic Anhydrase C

1972 ◽  
Vol 235 (57) ◽  
pp. 131-137 ◽  
Author(s):  
A. LILJAS ◽  
K. K. KANNAN ◽  
P.-C. BERGSTÉN ◽  
I. WAARA ◽  
K. FRIDBORG ◽  
...  
Keyword(s):  
Crystal Structure ◽  
Carbonic Anhydrase ◽  
Human Carbonic Anhydrase

Crystal Structure of a Zinc-Activated Variant of Human Carbonic Anhydrase I, CA I Michigan 1:  Evidence for a Second Zinc Binding Site Involving Arginine Coordination

Biochemistry ◽  
2002 ◽  
Vol 41 (20) ◽  
pp. 6237-6244 ◽  
Author(s):  
Marta Ferraroni ◽  
Silvia Tilli ◽  
Fabrizio Briganti ◽  
W. Richard Chegwidden ◽  
Claudiu T. Supuran ◽  
...  
Keyword(s):  
Crystal Structure ◽  
Carbonic Anhydrase ◽  
Binding Site ◽  
Zinc Binding ◽  
Carbonic Anhydrase I ◽  
Zinc Binding Site ◽  
Human Carbonic Anhydrase
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