Carbonic anhydrase inhibitors: Inhibition of the tumor-associated isozymes IX and XII with a library of aromatic and heteroaromatic sulfonamides

Biochemical Characterization of CA IX, One of the Most Active Carbonic Anhydrase Isozymes

“…The production and purification of this glutathione S-transferase fusion protein in Escherichia coli has already been described (25). A sample of recombinant human CA IX protein produced in murine myeloma cell line NS0 was purchased from R&D Systems (Minneapolis, MN) and used in the mass spectrometric analyses.…”

Crystal structure of N-(4-(3-cyclohexyl-5-methyl-2,4-dioxoimidazolidin- 1-ylsulfonyl)phenyl)acetamide, C18H23N3O5S

“…The clinically useful sulfonamides are derived from sulfanilamide, which is similar to para-aminobenzoic acid, afactor required by bacteria for folic acid synthesis [1]. Sulfanilamide was introduced in therapy about half acentury ago for prevention and cure of bacterial infections in humans, and so many derivatives of sulfanilamide have been developed [2][3][4][5]. In the title molecule ( figure, top), the C2-O1 bond lengths (1.205(3).Å)i sl onger than that of standard C=O double bond length 1.170 Å,while the C2-N1 bond distance (1.364(4) Å)is shorter than atypical C-Nbond length (ca.…”

Differentialin vitroinhibition effects of some antibiotics on tumor associated carbonic anhydrase isozymes of hCA-IX and hCA-XII

“…The final CA domains of CA IX and CA-XII was further purified by Sepharose 4B-L-tyrosine-sulfonamide affinity gel [23] with 129.15 and 92.29 fold purifications for CA-IX and CA-XII, respectively. The amount of enzyme being determined by spectrophotometric measurements and its activity by stoppedflow experiments, with CO 2 as substrate [11].…”

“…However, no evidence of a direct relationship between malignant transformation and CA expression has been presented for CAs I through VII. It appears that only the recently characterized isoform CA IX and CA XII is an exception which their expression was asociated with tumorigenesis [11].…”