Flexibility of the coordination geometry at the N-site of Cu(II)2 human serum-transferrin induced by the different orientations of Arg124.

The ESR spectra of dicupric human serum-transferrin (serum-Tf) were measured from -20 to 37°C in the liquid state (56% glycerol at pH 7.6). Two coordination geometries (types B-1 and B-2) with different ESR parameters were present at the N-site.

[Coordination chemical studies on the zinc enzymes].

The metal dissociation constants of bovine carbonic anhydrase II, bovine carboxypeptidase A, rat aminopeptidase B, and rat dipeptidyl peptidase III were measured using metal buffer solutions. The zinc dissociation constants of bovine carbonic anhydrase II, bovine carboxypeptidase A, rat aminopeptidase B, and rat dipeptidyl peptidase III were 5.8×10(-14), 3.

Antioxidant effects of the highly-substituted carbazole alkaloids and their related carbazoles.

Antioxidant activities of 3-oxygenated and 3,4-dioxygenated carbazole alkaloids and their related carbazoles were comprehensively evaluated. In all assay systems, the 3,8-dihydroxycarbazoles carbazomadurin A (2) and B (3), and their synthetic precursors 2a and 3a exhibited higher antioxidant activities than the 3-monohydroxycarbazoles carazostatin (1), and the synthetic precursors 4a and 4b of carquinostatin A (4). In particular, 2a and 3a exhibited strong scavenging activities due to the reducing ability of formyl group at the C-5 position of carbazoles.

[Analysis of daily reports of practical training in pharmacology using text mining].

  The text mining and full-text searching function were used to analyze the digitalized daily reports of the practical training in pharmacology submitted to the web system in Fukuyama University. Collocations connected to the word "inspection" were searched in the daily reports using the text mining and the full-text search functions of the system. Many collocation groups connected to "inspection" were found in the daily reports and the greatest number of collocations was associated with "preparation of drugs".

In rat dipeptidyl peptidase III, His⁵⁶⁸ is essential for catalysis, and Glu⁵⁰⁷ or Glu⁵¹² stabilizes the coordination bond between His⁴⁵⁵ or His⁴⁵⁰ and zinc ion.

Dipeptidyl peptidase (DPP) III is a zinc-dependent exopeptidase that has a unique motif, "HELLGH," as the zinc-binding site. In the present study, a three-dimensional (3D) model of rat DPP III was generated with the X-ray crystal structure of human DPP III (PDB: 3FVY [Dobrovetsky E. et al.

Useful Extend-release Chitosan Tablets with High Antioxidant Activity.

The antioxidant properties of different low molecular weight (LMW) chitosans (CS1; 22 kDa, CS2; 38 kDa, CS3; 52 kDa, CS4; 81 kDa) were examined for possible use in extended-release tablets. The criteria used were the ability of the chitosans to reduce Cu, and hydroxyl and superoxide radicals and N-centered radicals derived from 1,1'-diphenyl-2-picrylhydrazyl, via the use of ESR spectrometry. CS2 showed the highest scavenging activity.

Timolol activates the enzyme activities of human carbonic anhydrase I and II.

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.

The mechanisms by which latanoprost free acid inhibits human carbonic anhydrase I and II.

Latanoprost, a prostaglandin F2 alpha analogue, has been shown to be an effective ocular hypotensive agent when used alone on ocular hypertensive or open angle glaucoma patients. Carbonic anhydrase (CA) inhibitors are also used to reduce ocular hypertension by decreasing aqueous humor secretion, and are given in combination with prostaglandin F2 alpha analogue. It has been shown that prostaglandin F2 alpha, Minprostin F2 alpha, has been shown to increase the carbonic anhydrase (CA) activity and blood pressure.

Aspartic acid 405 contributes to the substrate specificity of aminopeptidase B.

Aminopeptidase B (EC 3.4.11.

The metal-binding motif of dipeptidyl peptidase III directly influences the enzyme activity in the copper derivative of dipeptidyl peptidase III.

The zinc-binding motif (HELLGH) of dipeptidyl peptidase III (DPP III) is different from the common zinc-binding motif (HExxH) of metallopeptidases. To clarify the importance of the zinc-binding motif part of DPP III for enzymatic activity, we measured the recovery of the enzyme activity of apo-Leu(453)-deleted dipeptidyl peptidase III (apo-Leu(453)-del-DPP III), which has a motif (HELGH) like that of the common peptidase (HExxH), in the presence of various metal ions. The enzyme activity of apo-Leu(453)-deleted DPP III could not be recovered by the addition of cupric ions, while apo-DPP III could be easily reactivated by the addition of cupric ions.