Heterocyclic periphery in the design of carbonic anhydrase inhibitors: 1,2,4-Oxadiazol-5-yl benzenesulfonamides as potent and selective inhibitors of cytosolic h CA II and membrane-bound h CA IX isoforms

2018 ◽  
Vol 76 ◽  
pp. 88-97 ◽  
Author(s):  
Mikhail Krasavin ◽  
Anton Shetnev ◽  
Tatyana Sharonova ◽  
Sergey Baykov ◽  
Tiziano Tuccinardi ◽  
...  
Keyword(s):  
Carbonic Anhydrase ◽  
Selective Inhibitors ◽  
Carbonic Anhydrase Inhibitors ◽  
Ca Ix ◽  
Membrane Bound

Indanesulfonamides as Carbonic Anhydrase Inhibitors. Toward Structure-Based Design of Selective Inhibitors of the Tumor-Associated Isozyme CA IX

2006 ◽  
Vol 49 (9) ◽  
pp. 2743-2749 ◽  
Author(s):  
Anne Thiry ◽  
Marie Ledecq ◽  
Alessandro Cecchi ◽  
Jean-Michel Dogné ◽  
Johan Wouters ◽  
...  
Keyword(s):  
Carbonic Anhydrase ◽  
Selective Inhibitors ◽  
Carbonic Anhydrase Inhibitors ◽  
Ca Ix

Expression of membrane-associated carbonic anhydrase isoforms IV, IX, XII, and XIV in the rabbit: induction of CA IV and IX during maturation

2005 ◽  
Vol 288 (5) ◽  
pp. R1256-R1263 ◽  
Author(s):  
Jeffrey M. Purkerson ◽  
George J. Schwartz
Keyword(s):  
Skeletal Muscle ◽  
Carbonic Anhydrase ◽  
Gall Bladder ◽  
Plasma Membranes ◽  
Rabbit Kidney ◽  
Α Subunit ◽  
Anion Transporters ◽  
Ca Ix ◽  
Membrane Bound ◽  
Physiological Demands

Several carbonic anhydrase (CA) isoforms are associated with plasma membranes. It is probable that these enzymes interact with anion transporters to facilitate the movement of HCO3− into or out of the cell. A better knowledge of CA isoform expression in a given tissue would facilitate a systematic examination of any associations with such transporters. We examined the expression of CAs IV, IX, XII, and XIV mRNAs in rabbit tissues, including kidney, heart, lung, skeletal muscle, liver, pancreas, gall bladder, stomach, small intestine, colon, and spleen, using quantitative real-time reverse transcription polymerase chain reaction (RT-PCR). CA IV mRNA was mainly in kidney, heart, lung, colon, and gall bladder. CA IX mRNA was restricted to stomach, gall bladder, duodenum, and early jejunum. CA XII mRNA was found in kidney and colon. CA XIV mRNA was localized to heart, lung, skeletal muscle, and liver. The data indicate that there are different patterns of CA expression in various tissues: CA IX was expressed in the proximal gastrointestinal tract, whereas CA XII and CA IV were more distal. CA IV and CA XII are important kidney isoforms. CA XIV was abundant in metabolically active tissues such as liver, heart, lung, and skeletal muscle. Some significant species differences were noted in the expression of some of these isoforms; for example, CA XIV is not expressed in rabbit kidney, despite being abundant in mouse kidney. Maturational studies showed that the expression of CA IX mRNA and protein increased markedly with weaning (∼3–4 postnatal wk) and was well correlated with the maturational expression of the α-subunit of the gastric H+,K+-ATPase, suggesting that function of CA IX and the gastric H+ pump might be linked in the digestion of adult foodstuffs. The unique pattern of membrane-bound CA isoforms suggests different functional associations with transporters, depending on the physiological demands on the tissue.

scholarly journals Structure of the carbonic anhydrase VI (CA6) gene: evidence for two distinct groups within the α-CA gene family

1999 ◽  
Vol 344 (2) ◽  
pp. 385-390 ◽  
Author(s):  
Weiping JIANG ◽  
Dwijendra GUPTA
Keyword(s):  
Carbonic Anhydrase ◽  
Untranslated Region ◽  
Sequence Similarity ◽  
Ca Ix ◽  
Its Gene ◽  
Exon 1 ◽  
Membrane Bound ◽  
Mature Enzyme ◽  
Gene Structures ◽  
Carbonic Anhydrase Vi

The secreted carbonic anhydrase (CA VI) is believed to be one of the oldest mammalian CAs in evolutionary terms. To elucidate its gene structure and compare it with other members of the α-CA family, we cloned genomic fragments encoding the bovine CA6 gene and determined its exon/intron organization. The gene spans approx. 25 kb and consists of eight exons and seven introns. Exon 1 encodes the 5′ untranslated region, the signal peptide and the N-terminus of the mature enzyme. Exon 8 encodes the 3′ untranslated region and the C-terminal extension that is unique to CA VI. Exons 2-7 encode the CA domain, which shows significant sequence similarity to other CAs. Two distinct groups exist in the α-CA family on the basis of a comparison of the known gene structures. One group consists of the cytoplasmic (CA I, II, III and VII) and mitochondrial (CA V) members. The other group consists of the membrane-bound (CA IV and IX) and secreted (CA VI) members. In particular, the seven exon/intron boundaries in the CA domain of the CA6 gene are conserved in the CA9 gene, which encodes the multidomain protein CA IX that is overexpressed in tumours and has transforming potential.

Carbonic Anhydrase Inhibitors. Comparison of Aliphatic Sulfamate/Bis-sulfamate Adducts with Isozymes II and IX as a Platform for Designing Tight-Binding, More Isoform-Selective Inhibitors

2009 ◽  
Vol 52 (19) ◽  
pp. 5990-5998 ◽  
Author(s):  
Rosa Maria Vitale ◽  
Vincenzo Alterio ◽  
Alessio Innocenti ◽  
Jean-Yves Winum ◽  
Simona Maria Monti ◽  
...  
Keyword(s):  
Carbonic Anhydrase ◽  
Tight Binding ◽  
Selective Inhibitors ◽  
Carbonic Anhydrase Inhibitors

Carbonic anhydrase inhibitors: inhibition of the tumor-associated isozyme IX with fluorine-containing sulfonamides. The first subnanomolar CA IX inhibitor discovered

2004 ◽  
Vol 14 (9) ◽  
pp. 2351-2356 ◽  
Author(s):  
Daniela Vullo ◽  
Andrea Scozzafava ◽  
Silvia Pastorekova ◽  
Jaromir Pastorek ◽  
Claudiu T Supuran
Keyword(s):  
Carbonic Anhydrase ◽  
Carbonic Anhydrase Inhibitors ◽  
Ca Ix
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