Biochemistry

Folding energetics and oligomerization of polytopic α-helical transmembrane proteins
While interactions of single-span transmembrane helices have been studied to a significant extent in the past years, the folding of polytopic α-helical transmembrane proteins as well as their oligomerization, are far less analyzed and understood. The goal of the few thus far performed thermodynamic studies, in which unfolding of polytopic TM proteins was described, was to achieve a mild, poten...


Fourier Transform Infrared (FTIR) Study and Thermal Decomposition Kinetics of Sorghum bicolour Glume and Albizia pedicellaris Residues
An investigation into the thermal decomposition kinetics, by thermogravimetric analysis, of an agricultural and a forestry residue was carried out using distributed activation energy model (DAEM) and Friedman’s differential technique. Preliminarily, Fourier transform infrared spectroscopy alongside proximate, ultimate and heating value was used in the characterisation of the biomass resources...
Preventive DNA repair by sanitizing the cellular (deoxy)nucleoside triphosphate pool
The occurrence of modified bases in DNA is attributed to some major factors: incorporation of altered nucleotide building blocks and chemical reactions or radiation effects on bases within the DNA structure. Several enzyme families are involved in preventing incorporation of non-canonical bases playing a “sanitizing” role. The catalytic mechanism of action of these enzymes has been revealed...


Competitive antagonism of insect GABA receptors by 4-substituted 5-(4-piperidyl)-3-isothiazolols
Γ-Aminobutyric acid (GABA) receptors are important targets of parasiticides/insecticides. Several 4-substituted analogs of the partial GABAA receptor agonist 5-(4-piperidyl)-3-isothiazolol (Thio-4-PIOL) were synthesized and examined for their antagonism of insect GABA receptors expressed in Drosophila S2 cells or Xenopus oocytes. Thio-4-PIOL showed weak antagonism of three insect GABA receptor...
Exploiting the Anti-HIV 6-Desfluoroquinolones to Design Multiple Ligands
It is getting clearer that many drugs effective in different therapeutic areas act on multiple rather than single targets. The application of polypharmacology concepts might have numerous advantages especially for disease such as HIV/AIDS, where the rapid emergence of resistance requires a complex combination of more than one drug. In this paper, we have designed three hybrid molecules combinin...


Risk Evaluation of Selective Renal Arterial Embolization in the Treatment of Delayed Hemorrhage from Renal Artery Pseudoaneurysm After Partial Nephrectomy
Renal-artery pseudoaneurysm (RAP) is a well-described complication of partial nephrectomy. We aimed to evaluate the occurrence rate of delayed hemorrhage from RAP after partial nephrectomy, and to investigate the efficacy and safety of selective renal arterial embolization. Between January 2000 and December 2010, 426 partial nephrectomies were performed at our institution for treatment of small...
Redox-Triggered Self-Assembly of Gadolinium-Based MRI Probes for Sensing Reducing Environment
Controlled self-assembly of small molecule gadolinium (Gd) complexes into nanoparticles (GdNPs) is emerging as an effective approach to design activatable magnetic resonance imaging (MRI) probes and amplify the r1 relaxivity. Herein, we employ a reduction-controlled macrocyclization reaction and self-assembly to develop a redox activated Gd-based MRI probe for sensing a reducing environment. Up...

Heavy metals induce oxidative stress and trigger oxidative stress-mediated heat shock proteins (hsps) modulation in the intertidal copepod Tigriopus japonicus
Heat shock proteins (hsps) are induced by a wide range of environmental stressors including heavy metals in aquatic organisms. However, the effect of heavy metals on zooplankton at the molecular level remains still unclear. In this study, we measured the intracellular reactive oxygen species (ROS) level and the antioxidant enzyme activities for 96h after exposure to five heavy metals: arsenic (...
Sequential and Parallel Dual Labeling of Nanoparticles Using Click Chemistry
Bioorthogonal ‘click’ reactions have recently emerged as promising tools for chemistry and biological applications. By using a combination of two different ‘click’ reactions, ‘double-click’ strategies have been developed to attach multiple labels onto biomacromolecules. These strategies require multi-step modifications of the biomacromolecules that can lead to heterogeneity in the f...

Inhibitory effects of p-alkylaminophenol on melanogenesis
Melanin protects the skin against ultraviolet (UV) rays. It is produced in excess by UV radiation, which causes skin disorders and pigmentation. Retinoic acid (RA) decreases the levels of epidermal melanin by suppressing the expression of melanogenic enzymes including tyrosinase, which is the rate-limiting enzyme in melanin synthesis. However, RA shows inflammatory effects on the skin. In an ef...
Antitumor efficacy, pharmacokinetic and biodistribution studies of the anticancer peptide CIGB-552 in mouse models
Accumulation of the COMMD1 protein as a druggable pharmacology event to target cancer cells has not been evaluated so far in cancer animal models. We have previously demonstrated that a second-generation peptide, with cell-penetrating capacity, termed CIGB-552, was able to induce apoptosis mediated by stabilization of COMMDHere, we explore the antitumor effect by subcutaneous administration of ...

Enhancement of rutin production in fagopyrum tataricum hairy root cultures with its endophytic fungal elicitors
Tartary buckwheat (Fagopyrum tataricum) is a potentially important source of rutin, a natural bioactive flavonoid with antihyperglycemic, antioxidative, antihypertensive, and anti-inflammatory properties. This study examines the effects of endophytic fungi on rutin production in the hairy root cultures of F. tataricum. Without obvious changes in the appearance of the hairy roots, the exogenous ...
Cost-effective and efficient apparatus for electroelution of micro- and macrogram quantities of proteins from polyacrylamide gels
Protein recovery from gel electrophoresis plays a significant role in functional genomics and proteomics. To assist in this, a simple, cost-effective, and efficient apparatus for electroelution of proteins has been designed. The performance of the apparatus was demonstrated using the proteins bovine serum albumin (BSA), phosphorylase, ovalbumin, pepsin, and trypsinogen. In all the cases the yie...
Investigation on the influence of (Z)-3-(2-(3-chlorophenyl)hydrazono)-5,6-dihydroxyindolin-2-one (PT2) on β-amyloid(1-40) aggregation and toxicity
In Alzheimer’s disease (AD), native Aβ protein monomers aggregate through the formation of a variety of water-soluble, toxic oligomers, ultimately leading to insoluble fibrillar deposits. The inhibition of oligomers formation and/or their dissociation into non-toxic monomers, are considered an attractive strategy for the prevention and treatment of AD. A number of studies have demonstrated t...
G-quadruplex formation of FXYD1 pre-mRNA indicates the possiblity of regulating expression of its protein product
G-quadruplexes are higher-order nucleic acid structures formed of square-planar arrangements of four guanine bases held together by Hoogsteen-type hydrogen bonds. Stacks of guanine tetrads are stabilised by intercalating potassium ions. FXYD1 encodes for phospholemman, a regulatory subunit of the cardiac Na+/K+-ATPase. Computational sequence analysis of FXYD1 pre-mRNA predicted the formation of...