A bombyxin gene encoding precursor molecule for bombyxin-IV, one of the insulin-related neurosecretory peptide of the silkmoth Bombyx mori, has been cloned and characterized. The nucleotide sequence of this gene and its deduced amino acid sequence deviate moderately from those characterized prev...

The implementation of direct and mild catalytic synthesis of products from benign materials using inexpensive catalysts is a major goal of chemists. Herein, a mild O2-interrupted hydrogen borrowing strategy using easily accessible and high efficient cobalt complex was reported for direct synthes...

An N-methylpyridinium-4-boronic ester acts as a catalyst for dehydrative glycosidations of 2-deoxy sugar-derived hemiacetals. The catalytic protocol is tolerant of functionalized acceptors, including alcohols bearing isopropylidene ketal, tert-butyl carbamate or benzyl carbamate groups. The resu...

A series of (1-(benzyl (aryl) amino) cyclohexyl) methyl esters 7a-n were prepared and screened for their anticonvulsant profile. Screening of these esters 7a-n and their starting alcohols 6a and 6b revealed that compound 7k was the most potent one in the scPTZ screening test with an ED50 value o...

The bridged diacetato complex [Cu2(O)(H2O)2(OOCCH3)2] has been obtained by reacting aqueous solutions of Cu(OOCCH3)2 · H2O and urea at about 70°C. The reaction product was characterized through elemental analysis and i.r. measurements. The i.r. spectrum shows the characteristic bands of coordi...

Tetracarboxylatoplatinum(IV) complexes are interesting representatives of potential anticancer active platinum(IV) drugs. Revealing higher kinetic inertness in comparison to their cytotoxic platinum(II) counterparts, they offer an opportunity to reduce toxic and deactivating side reactions. Plat...

Two novel dichloro Cu(II) complexes of (R,R)-N1,N2-bis((5-methylthiophen-2-yl)methyl)cyclohexane-1,2-diamine (MTCHD) and (R,R)-N1,N2-bis((5-methylfuran-2-yl)methyl)cyclohexane-1,2-diamine (MFCHD) ligands have been synthesised and structurally characterised using X-ray diffraction. The geometry a...

In-situ confocal Raman spectroscopy combined with relative humidity (RH) control technique was used to study the sequential dehydration process of insulin crystals. By gradually decreasing the ambient RH of the insulin crystal, the content of the hydration water in the crystal was quantitatively...

Based on the extensive structural comparisons among the determined structures of the different species and crystal forms of insulin and its derivatives in our laboratory, it was suggested that the binding interaction with the receptor molecule should take place mainly on an amphipathic surface o...

Earliest events in the aggregation process, such as single molecule reconfiguration, are extremely important and the most difficult to characterize in experiments. To this end, we have used well-tempered bias exchange metadynamics simulations to determine the equilibrium ensembles of an insulin ...

We report here the inhibition of amyloid fibrillation of human insulin in vitro by Morin hydrate, a naturally occurring small molecule. Using spectroscopic assays and transmission electron microscopy, we found that Morin hydrate effectively inhibits insulin amyloid fibrillation in a dose depende...

The binding of insulin to the insulin binding aptamer (IBA) was investigated with different spectroscopy techniques (UV/vis absorption, fluorescence, resonance light-scattering spectra (RLS), synchronous fluorescence, and three-dimensional fluorescence). The thermodynamic parameters (Kb, ΔH, Δ...

The effects of 2-[(4-acetylphenyl)amino]-3-chloro-1,4-naphthalenedione (NQ-Y15), a synthetic 1,4-naphthoquinone derivative, on platelet activity and its mechanism of action were investigated. NQ-Y15 caused a concentration-dependent inhibition of the aggregation induced by thrombin, collagen, ara...

Publisher SummaryThis chapter discusses the types of investigations with major emphasis on recent studies that include elucidation of complete or partial amino acid sequences of the enzymes from several sources. L-Glutamate dehydrogenases catalyze the interconversion of α-ketoglutarate and L-gl...

A method of solid phase reaction analysis is described using an in situ cleavage process (TFA vapour) followed by MALDI-TOF MS analysis. The process is demonstrated by the solid phase synthesis of a depsipeptide based on the antibiotic Lysobactin.

ObjectiveTo explore the ability of Synechocystis sp. PCC6803 in transforming 6-deoxypseudoanisatin.

A series of pyrido[2,3-b]pyrazin-3(4H)-one based derivatives were designed as inhibitors of aldose reductase (ALR2), the enzyme which plays a key role in the development of diabetes complications as well as in the oxidative stress processes associated with diabetes and other pathologies. Most of...

Human immunodeficiency virus (HIV) reverse transcriptase (RT) associated ribonuclease H (RNase H) is the only HIV enzymatic function not targeted by current antiviral drugs. Although various chemotypes have been reported to inhibit HIV RNase H, few have shown significant antiviral activities. We...

Synthesis of amides of 7-methyl-3-phenyl-2,4-dioxo-1,2,3,4-tetrahydropyrido[2,3-d]pyrimidine-5-carboxylic acid (6–10) and their 1-[2-hydroxy-3(4-phenyl-1-piperazinyl)propyl] derivatives (11–15) are described. Some of them displayed strong analgesic activity.

Synthesis of N,N-dialkyl(dialkenyl)amides of 7-methyl-3-phenyl-2,4-dioxo-1,2,3,4-tetrahydropyrido[2,3-d]pyrimidine-5-carboxylic acid (5–9) and their 1-[2-hydroxy-3-(4-phenyl-1-piperazinyl)propyl] derivatives (10–14) is described. Compounds 10–14 were tested for analgesic and sedative activiti...