The molecular features of non-peptidic nucleophilic substrates and acceptor proteins determine the efficiency of sortagging.

Sortase A-mediated ligation (SML) or "sortagging" has become a popular technology to selectively introduce structurally diverse protein modifications. Despite the great progress in the optimization of the reaction conditions and design of miscellaneous C- or N-terminal protein modification strategies, the reported yields of conjugates are highly variable. In this study, we have systematically investigated C-terminal protein sortagging efficiency using a combination of several rationally selected and modified acceptor proteins and a panel of incoming surrogate non-peptidic amine nucleophile substrates varying in the structural features of their amino linker parts and cargo molecules.

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.