Gene/Protein
Disease
Symptom
Drug
Enzyme
Compound
Pivot Concepts:
Gene/Protein
Disease
Symptom
Drug
Enzyme
Compound
Target Concepts:
Gene/Protein
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Query: UNIPROT:P35218 (
CA V
)
101
document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)
The inhibition of the metalloenzyme carbonic anhydrase (CA, EC 4.2.1.1) with three phenols was investigated. Phenol was an effective CA I-IV, IX, XII and XIV inhibitor (K(I)s of 2.7-11.5 microM) and a less effective one against the other isoforms,
CA VA
, VB, VI, VII, and XIII (K(I)s of 208-710 micraoM). 3,5-Difluorophenol was an effective inhibitor of CA III, IV, IX, and XIV (K(I)s of 0.71-10.7 microM) being a weaker one for CA I, II, VA, VB, VI, VII, XII, and XIII (K(I)s of 33.9-163 microM). Clioquinol (5-chloro-7-iodo-8-quinolinol) was the best phenol inhibitor against all isozymes, with inhibition constants in the range of 3.3-16.0 microM. These data prove that the phenol OH moiety can be considered as a new 'zinc-
water
binding group' for the design of CA inhibitors possessing a different inhibition mechanism as compared to the classical sulfonamide inhibitors that bind the metal ion within the active site cavity.
...
PMID:Carbonic anhydrase inhibitors: interactions of phenols with the 12 catalytically active mammalian isoforms (CA I-XIV). 1824 85
Carbonic anhydrase inhibitors are used to treat glaucoma and cancers. Carbonic anhydrases perform a crucial role in the conversion of carbon dioxide and
water
into bicarbonate and protons. However, there is little information about carbonic anhydrase isoforms during the process of ageing. Mitochondrial dysfunction is implicit in ageing brain and muscle. We have interrogated isolated mitochondrial fractions from young adult and middle aged mouse brain and skeletal muscle. We find an increase of tissue specific carbonic anhydrases in mitochondria from middle-aged brain and skeletal muscle. Mitochondrial carbonic anhydrase II was measured in the Purkinje cell degeneration (
pcd
5J
) mouse model. In
pcd
5J
we find
mitochondrial carbonic anhydrase
II is also elevated in brain from young adults undergoing a process of neurodegeneration. We show
C.elegans
exposed to carbonic anhydrase II have a dose related shorter lifespan suggesting that high CAII levels are in themselves life limiting. We show for the first time that the mitochondrial content of brain and skeletal tissue are exposed to significantly higher levels of active carbonic anhydrases as early as in middle-age. Carbonic anhydrases associated with mitochondria could be targeted to specifically modulate age related impairments and disease.
...
PMID:Mitochondrial proteomic profiling reveals increased carbonic anhydrase II in aging and neurodegeneration. 2774 11
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