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Carbonic anhydrases: novel therapeutic applications for inhibitors and activators
  • C. Supuran
  • Biology, Chemistry
    Nature Reviews Drug Discovery
  • 1 February 2008
TLDR
The biological rationale for the novel uses of inhibitors or activators of CA activity in multiple diseases is discussed, and progress in the development of specific modulators of the relevant CA isoforms is highlighted, some of which are now being evaluated in clinical trials.
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Carbonic anhydrase inhibitors.
TLDR
The use of such enzyme inhibitors as antiglaucoma drugs will be discussed in detail, together with the recent developments that led to isozyme-specific and organ-selective inhibitors.
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Carbonic anhydrases--an overview.
  • C. Supuran
  • Biology
    Current pharmaceutical design
  • 29 February 2008
TLDR
Several important physiological and physio-pathological functions are played by CA isozymes present in organisms all over the phylogenetic tree, related to respiration and transport of CO(2)/bicarbonate between metabolizing tissues and the lungs, pH andCO(2) homeostasis, electrolyte secretion in a variety of tissues/organs, biosynthetic reactions, etc.
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Interfering with pH regulation in tumours as a therapeutic strategy
TLDR
Key pH regulators in tumour cells include: isoforms 2, 9 and 12 of carbonic anhydrase, isoforms of anion exchangers, Na+/HCO3− co-transporters, Na+./H+ exchanger, monocarboxylate transporters and the vacuolar ATPase.
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Hypoxia activates the capacity of tumor‐associated carbonic anhydrase IX to acidify extracellular pH
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Crystal structure of the catalytic domain of the tumor-associated human carbonic anhydrase IX
TLDR
On the basis of the structural differences observed between CA IX and the other membrane-associated α-CAs, further prospects for the rational drug design of isozyme-specific CA inhibitors are proposed, given that inhibition of this enzyme shows antitumor activity both in vitro and in vivo.
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Carbonic Anhydrase in the Scleractinian Coral Stylophora pistillata
TLDR
STPCA is a secreted form of α-CA, which possesses a CA catalytic function, similar to the secreted human CAVI, and its localization at the calicoblastic ectoderm level supports the role of STPCA in the calcification process.
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Multiple binding modes of inhibitors to carbonic anhydrases: how to design specific drugs targeting 15 different isoforms?
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Unexpected nanomolar inhibition of carbonic anhydrase by COX-2-selective celecoxib: new pharmacological opportunities due to related binding site recognition.
TLDR
An unexpected nanomolar affinity is demonstrated of the COX-2 specific arylsulfonamide-type celecoxib and valdecoxib for isoenzymes of the totally unrelated carbonic anhydrase (CA) family, such as CA I, II, IV, and IX, whereas the rofecoxib methyl sulfone-type has no effect.
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Direct extracellular interaction between carbonic anhydrase IV and the human NBC1 sodium/bicarbonate co-transporter.
TLDR
It is concluded that CAIV binds EC4 of NBC1, and this interaction is essential for full NBC1 activity, which maximizes the transmembrane HCO(3)(-) gradient local to NBC1 and thereby activates the transport rate.
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