Conformational transitions of the serotonin 5-HT receptor.

The serotonin 5-HT receptor is a pentameric ligand-gated ion channel (pLGIC). It belongs to a large family of receptors that function as allosteric signal transducers across the plasma membrane; upon binding of neurotransmitter molecules to extracellular sites, the receptors undergo complex conformational transitions that result in transient opening of a pore permeable to ions. 5-HT receptors are therapeutic targets for emesis and nausea, irritable bowel syndrome and depression.

Sensitive Versatile Fluorogenic Transmembrane Peptide Substrates for Rhomboid Intramembrane Proteases.

Rhomboid proteases are increasingly being explored as potential drug targets, but their potent and specific inhibitors are not available, and strategies for inhibitor development are hampered by the lack of widely usable and easily modifiable activity assays. Here we address this bottleneck and report on the development of new fluorogenic transmembrane peptide substrates, which are cleaved by several unrelated rhomboid proteases, can be used both in detergent micelles and in liposomes, and contain red-shifted fluorophores that are suitable for high-throughput screening of compound libraries. We show that nearly the entire transmembrane domain of the substrate is important for efficient cleavage, implying that it extensively interacts with the enzyme.

[Occupational regulations of the use of terpene compounds in the air of the workplace].

Based on results of 15-years complex study, the authors present toxicological and hygienic characteristics of terpene compounds (with mono- and bicyclic structure) and their compositions. The article deals with toxicodynamics and toxicokinetics of terpenoids, dependence of toxic properties on the chemical structure. The article also touches upon studies of biologic and specific (sensibilizing activity, embryotoxic and gonadotropic, membranotropic) effects of terpenoids.

[An experimental validation of the maximum permissible concentration of a mixture of mono- and bicyclic terpenoid alcohols in water].

The maximum permissible concentrations (MPC) of Viterol in water were established, which was equal to 0.14 mg/l. Its organoleptic and general sanitary thresholds were determined at the same level.

[Allergenic properties of various natural and modified colofonies].

Natural tall colophony and its modification by monoethanolamine are moderate allergens at intracutaneous and epicutaneous ways of sensibilization reproduction. In the conditions of 30-days inhalational exposure in concentrations on the level of Limch modified by monoethanolamine colophony does not cause sensitization; while the modified tall colophony induces a weakly expressed allergic effect in experimental guinea pigs--albinos.