Synthesis and enzymatic evaluation of the guanosine analogue 2-amino-6-mercapto-7-methylpurine ribonucleoside (MESG): insights into the phosphorolysis reaction mechanism based on the blueprint transition state: SN1 or SN2?

A modified experimental procedure for the synthesis of MESG (2-amino-6-mercapto-7-methylpurine ribonucleoside) 1 has been successfully performed and its full characterization is presented. High resolution ESI(+)-MSMS indicates both the nucleoside bond cleavage as the main fragmentation in the gas phase and a possible SN1 mechanism. Ab initio transition state calculations based on the blue print transition state support this mechanistic rationale and discard an alternative SN2 mechanism. Assays using purine nucleoside phosphorylase (PNP) enzyme (human and M. tuberculosis sources) indicate its efficiency in the phosphorolysis of MESG and allow the quantitative determination of inorganic phosphate in real time assay.

Ionic liquids for the nuclear industry: A radiochemical, structural, and electrochemical investigation

The applicability of ionic liquids within the nuclear industry has been investigated. The radiation stability of ionic liquids containing dialkylimidazolium cations has been tested through with alpha, beta and gamma irradiation. The results of these tests suggest that imidazolium salts have stabilities similar to alkylbenzenes and greater than tetrabutylphosphate / odorless kerosene (TBP/OK) mixtures. The oxidative dissolution of uranium dioxide and the anodic dissolution of uranium metal and plutonium metal have been carried out in various ionic liquid media (C) 2002 American Chemical Society.

Insights into the binding and activation sites of the receptors for cholecystokinin and gastrin

CCK receptors represent potential targets in a number of diseases. Knowledge of CCK receptor binding sites is a prerequisite for the understanding of the molecular basis for their ligand recognition, partial agonism, ligand-induced trafficking of signalling. In the current paper, we report studies from our laboratory and others which have provided new data on the molecularbasis of the pharmacology and functioning of CCK1 and CCK2 receptors. It has been shown that: 1) homologous regions of the two receptors are involved in the binding site of CCK, however, positioning of CCK slightly differs in agreement with distinct phannacophores of CCK toward the two receptors and receptor sequence variations; 2) Binding sites of most of non-peptide agonists/ antagonist are buried in the pocket formed by transmembrane helices and overlap that of CCK; Aromatic amino acids within and near the binding site, especially in helix VI, are involved in receptor activation; 4) Like for other members of family A of G-protein coupled receptors, residues of the binding sites as well as of conserved motifs such as E/DRY, NPXXY are crucial for receptor activation. (c) 2007 Elsevier B.V. All rights reserved.

Insights into torpor and behavioural thermoregulation of the endangered Juliana's golden mole

The cryptic, subterranean ways of golden moles (Chrysochloridae) hamper studies of their biology in the field. Ten species appear on the IUCN red list, but the dearth of information available for most inhibits effective conservation planning. New techniques are consequently required to further our understanding and facilitate informed conservation management decisions. We studied the endangered Juliana's golden mole Neamblysomus julianae and aimed to evaluate the feasibility of using implantable temperature sensing transmitters to remotely acquire physiological and behavioural data. We also aimed to assess potential body temperature (T-b) fluctuations in relation to ambient soil temperature (T-a) in order to assess the potential use of torpor. Hourly observations revealed that T-b was remarkably changeable, ranging from 27 to 33 degrees C. In several instances T-b declined during periods of low T-a. Such 'shallow torpor' may result in a daily energy saving of c. 20%. Behavioural thermoregulation was used during periods of high T-a by selecting cooler microclimates, while passive heating was used to raise T-b early morning when T-a was increasing. In contrast to anecdotal reports of nocturnal patterns of activity, our results suggest that activity is flexible, being primarily dependent on T-a. These results exemplify how behavioural patterns and microclimatic conditions can be examined in this and other subterranean mammal species, the results of which can be used in the urgently required conservation planning of endangered Chrysochlorid species.