Carbonic Anhydrase

The first topical carbonic anhydrase inhibitor for clinical use Dorzolamide HCl (Axon 1517) has been prescribed widely for the treatment of glaucoma and ocular hypertension. It inhibits carbonic anhydrase II (CA-II; EC 4.2.1.1) selectively, which is the main CA iso-enzyme involved in aqueous humor secretion. Inhibition of CA-II in the ciliary processes of the eye decreases aqueous humor secretion, presumably by slowing the formation of bicarbonate ions with subsequent reduction in sodium and fluid transport. Dorzolamide also accumulates in red blood cells as a result of CA-II binding, as CA-II is found predominantly in erythrocytes. However, sufficient CA-II activity remains so that adverse effects due to systemic CA inhibition are not observed[1]. Membrane-associated carbonic anhydrase (CA, EC 4.2.1.1) IX (CA IX) is strongly overexpressed in a broad range of tumor types, and the expression of CA IX negatively correlates with the prognosis of cancer patients. In normal tissues CA IX expression is much more restricted with abundant expression mainly present in the mucosa of the glandular stomach[2].


[1] Dorzolamide. A review of its pharmacology and therapeutic potential in the management of glaucoma and ocular hypertension. J.A. Balfour, M.I. Wilde. Drugs Aging. 1997, 10, 384-403.
[2] R.G. Gieling et al. Antimetastatic effect of sulfamate carbonic anhydrase IX inhibitors in breast carcinoma xenografts. J Med Chem. 2012, 55(11), 5591-600.

 

 

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Axon ID Name Description From price
2662 CAIX Inhibitor S4 Carbonic anhydrase (CA) IX/XII inhibitor  Recently added €90.00
1517 Dorzolamide hydrochloride Carbonic anhydrase inhibitor €70.00
2208 Gallic acid Multi-affinity drug. Antioxidant. €50.00

3 Item(s)

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