Impact of climate change and anthropogenic activities on aquatic ecosystem - A review.

All living things depend on their natural environment, either directly or indirectly, for their high quality of life, growth, nutrition, and development. Due to the fast emissions of greenhouse gases (GHGs), the Earth's climate system is being negatively impacted by global warming. Stresses caused by climate change, such as rising and hotter seas, increased droughts and floods, and acrid waters, threaten the world's most populated areas and aquatic ecosystems.

New cathepsin D inhibitor library utilizing hydroxyethyl isosteres with cyclic tertiary amines.

The design and synthesis of hydroxyethylamine isosteres as inhibitors of cathepsin D based on SAR data have been accomplished. A library of 96 of these hydroxyethylamine isosteres are described and many have proven to be very potent inhibitors of human cathepsin D activity as measured using a fluorometric assay technique, via peptide substrate Ac-Glu-Glu(Edans)-Lys-Pro-Ile-Cys-Phe-Phe-Arg-Leu-Gly-Lys(Methyl Red)-Glu-NH(2). Compounds showing strongest inhibition of cathepsin D activity were those that contain a hydroxyethyl-N'-2- or N'-(4-chlorophenyl)piperazine moiety (IC(50) values range from 0.

Inhibition of a viral enzyme by a small-molecule dimer disruptor.

We identified small-molecule dimer disruptors that inhibit an essential dimeric protease of human Kaposi's sarcoma-associated herpesvirus (KSHV) by screening an alpha-helical mimetic library. Next, we synthesized a second generation of low-micromolar inhibitors with improved potency and solubility. Complementary methods including size exclusion chromatography and 1H-13C HSQC titration using selectively labeled 13C-Met samples revealed that monomeric protease is enriched in the presence of inhibitor.