Synthetic Amine Linkers for Efficient Sortagging.

Enzymatic site-specific bioconjugation techniques, in particular sortase-mediated ligation, are increasingly used to generate conjugated proteins for a wide array of applications. Extension of the utility and practicality of sortagging for diverse purposes is critically dependent on further improvement of the efficiency of sortagging reactions with a wider structural variety of substrates. We present a comprehensive comparative mass spectrometry screening study of synthetic nonpeptidic incoming amine nucleophile substrates of Sortase A enzyme.

Genotoxic Effects of Exposure to Water-Soluble Fraction of Diesel Fuel in Sand Dollar Gametes.

Pollution of marine areas with oil and oil products is steadily growing. As part of this connection, the study of the impact of petroleum hydrocarbons on marine hydrobionts is an urgent issue of modern ecotoxicology. In our study, the genotoxic effect of the water-soluble fraction of diesel fuel at different concentrations on the gametes of the sand dollar was evaluated.

Exposure of adult sand dollars (Scaphechinus mirabilis) (Agassiz, 1864) to copper oxide nanoparticles induces gamete DNA damage.

The increase in the number of products containing nanoparticles (NPs) poses a real threat to the environment. Recently, more evidence has been added to predictive models about the presence of NPs in various natural and anthropogenic systems. The acute toxicity of most aquatic NPs has now been well documented.

Strained contacts with the cell membrane may influence ligand affinity to G protein coupled receptors: a case of free fatty acid receptor 1 agonists.

A set of 1,3,4-thiadiazole-2-carboxamides bearing a substituted biphenyl in the amide portion was synthesised and tested for agonistic activity towards free fatty acid receptor 1 (FFA1). The observed activity trends were impossible to rationalised based solely on the docking energy scores of Glide SP. On the contrary, when the phospholipid cell membrane bilayer was reconstructed around FFA1, it became apparent that inactive compounds displayed significant strained contacts with the membrane while for active compounds the strain was noticeably lower.

Exploration of the nitrogen heterocyclic periphery around the core of the advanced FFA1 agonist fasiglifam (TAK-875).

Three types of heterocyclic moieties-piperidines fused to a heteroaromatic moiety-were explored as potential periphery motifs for the pharmacophoric core of fasiglifam (TAK-875), with fasiglifam being the most advanced agonist of free fatty acid receptor 1, a promising target for therapeutic intervention in type 2 diabetes. Several observed structure-activity relationship trends were corroborated by in silico docking results. Balanced selection based on potency and Caco-2 permeability advanced six compounds to cellular efficacy tests (glucose-stimulated insulin secretion in rat insulinoma INS1E cells).

Sea Urchin Embryogenesis as Bioindicators of Marine Pollution in Impact Areas of the Sea of Japan/East Sea and the Sea of Okhotsk.

The embryogenesis of the sea urchin sand dollar Scaphechinus mirabilis was used as bioindicators of seawater quality from the impact areas of the Sea of Japan/East Sea (Peter the Great Bay) and the Sea of Okhotsk (northwestern shelf of Sakhalin Island and western shelf of Kamchatka Peninsula). Fertilization membrane formation, first cleavage, blastula formation, gastrulation, and 2-armed and 4-armed pluteus formation have been analyzed and a number of abnormalities were calculated. Number of embryogenesis anomalies in sand dollar larvae exposed to sea water from different stations in Peter the Great Bay corresponds to pollution level at each area.

Influence of water pollution on the growth and pigment concentration of the microalgae Phaeodactylum tricornutum Bohlin (Bacillariophyta).

The aim of the work was to study the influence of the water taken from one of the most polluted parts of the Peter the Great Bay (the Japan Sea), the Nakhodka Bay, on the growth and chlorophyll a concentration in the cells of microalga P. tricornutum Bohlin (Bacillariophyta). The estimation of the dynamics of cell number growth and chlorophyll a concentration in the cells of microalga grown in the water from the Nakhodka Bay was made.