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1.
Biol Pharm Bull ; 33(2): 301-6, 2010.
Article in English | MEDLINE | ID: mdl-20118557

ABSTRACT

Timolol, a beta-blocker, has been shown to be an effective ocular hypotensive agent when used alone or with carbonic anhydrase inhibitor on ocular hypertensive or open angle glaucoma patients. The effect of timolol hemihydrate on the CO(2) hydration activities of human carbonic anhydrase (HCA) I and II and their reaction mechanisms were investigated. Timolol activates the enzyme activities of HCA I and HCA II. In HCA I and II, the enzyme kinetic results clearly showed that timolol increases the value of V(max) but does not influence the value of K(m). The enzyme kinetic method showed that timolol noncompetitively activates HCA I and II activities through the formation of a ternary complex consisting of the enzyme, the substrate, and timolol. These results indicate that timolol binds apart from the narrow cavity of the active site. AutoDocking results showed that timolol binds at the entrance of the active site cavity in a region where the proton shuttle residue, His 64, of HCA I or II, is placed. The enzyme kinetic and AutoDocking results showed that timolol might weakly bind near the proton shuttle residue, His 64, to accelerate the proton transfer rate from His 64 to the buffer components. It is known that efficient activators of carbonic anhydrase possess a bulky aromatic/heterocyclic moiety and a primary/secondary amino group in their molecular structure. Timolol has a heterocyclic moiety and a secondary amino group, which are typical structures in efficient activators of carbonic anhydrase.


Subject(s)
Carbonic Anhydrase II/metabolism , Carbonic Anhydrase I/metabolism , Timolol/pharmacology , Binding Sites/drug effects , Binding Sites/physiology , Enzyme Activation/drug effects , Enzyme Activation/physiology , Humans
2.
Opt Lett ; 34(2): 175-7, 2009 Jan 15.
Article in English | MEDLINE | ID: mdl-19148246

ABSTRACT

A solar-pumped 100 W class laser that features high efficiency and low cost owing to the use of a Fresnel lens and a chromium codoped neodymium YAG ceramic laser medium was developed. A laser output of about 80 W was achieved with combination of a 4 m(2) Fresnel lens and a pumping cavity as a secondary power concentrator. This output corresponds to 4.3% of conversion efficiency from solar power into laser, and the maximum output from a unit area of Fresnel lens was 20 W/m(2), which is 2.8 times larger than previous results with mirror-type concentrator.

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