Numerous steroids are essential plant, animal, and human hormones. The medical and industrial applications of these hormones require the identification of new synthetic routes, including biotransformations. The metabolic fate of a steroid can be complicated; it may be transformed into a variety of substituted derivatives. This may be because a steroid molecule can adopt several possible orienta...

The c-Abl tyrosine kinase is inhibited by mechanisms that are poorly understood. Disruption of these mechanisms in the Bcr-Abl oncoprotein leads to several forms of human leukemia. We found that like Src kinases, c-Abl 1b is activated by phosphotyrosine ligands. Ligand-activated c-Abl is particularly sensitive to the anti-cancer drug STI-571/Gleevec/imatinib (STI-571). The SH2 domain-phosphoryl...

Improved synthesis of 3b-acetoxy-9, 10-seco-19, 8(8)-spiro-5(10), 6-cholestadiene has been reported after reacting cholecalciferol acetate with dimethylbutadiene by incorporating BF3·OEt2, SnCl4, ZnBr2, p-TsOH in toluene under Diels-Alder condition to get better yields. Agarose gel electrophoresis showed the potential in vitro DNA damaging nature while as the comet assay depicted the genotoxic ...

Peroxisome proliferators-activated receptors (PPARα, γ and δ) are potentially effective targets for Type 2 diabetes mellitus therapy. The severe effects of known glitazones and the successfully approved agents (saroglitazar and lobeglitazone) motivated us to study novelly potent PPARs drugs with improved safety profile. In this work, we received 15 carboxylic acids based on the combination prin...

Animals are routinely subjected to painful procedures, such as tail docking for puppies, castration for piglets, dehorning for dairy calves, and surgery for laboratory rats. Disease and injury, such as tumours in mice and sole ulcers on the feet of dairy cows, may also cause pain. In this paper we describe some of the ways in which the pain that animals experience can be recognized and quantifi...

The signaling output of protein kinase C (PKC) is exquisitely controlled, with its disruption resulting in pathophysiologies. Identifying the structural basis for autoinhibition is central to developing effective therapies for cancer, where PKC activity needs to be enhanced, or neurodegenerative diseases, where PKC activity should be inhibited. Here, we reinterpret a previously reported crystal...

Pig production has changed dramatically over the last several decades, and most piglets are now raised on industrialized commercial operations that confine thousands of animals on one site. In these facilities, piglets are born and reared under conditions that dramatically contrast with the natural environment they are biologically adapted to fit. In nature, a mother sow builds a nest of twigs ...

An α-amido cyclobutanone possessing a C10 hydrocarbon tail was designed as potential transition-state mimetic for the quorum-quenching metallo-γ-lactonase autoinducer inactivator A (AiiA) with support of in-house modeling techniques and found to be competitive inhibitor dicobalt(II) AiiA an inhibition constant Ki = 0.007 ± 0.002 mM. The catalytic mechanism further explored using our product-bas...

It has become increasingly clear that pig producers face difficulties to implement the EU legislation on animal welfare. The switch from individual sow stalls to group housing of gestating sows from January 2013 is one clear example of the difficulties found in several Member States (MS) to implement the current ‘Pig Directive’ (EU-Directive 2008/120/EC). Besides, clear cases of non-compliance,...

The type VI secretion system (T6SS) is a multiprotein complex that delivers toxin effectors in both prokaryotic and eukaryotic cells. It is constituted of a long cytoplasmic structure-the tail-made of stacked Hcp hexamers and wrapped by a contractile sheath. Contraction of the sheath propels the inner tube capped by the VgrG spike protein toward the target cell. This tubular structure is built ...