Xanthophyllomyces dendrorhous is an excellent industrial source for production of natural astaxanthin, but the yield of astaxanthin is relative low due to the contradiction between biomass weight and astaxanthin accumulation. Glutamate, a metabolite connecting nitrogen and carbon metabolisms, is...

Glutamate, the main excitatory neurotransmitter in the vertebrate brain, exerts its actions through specific membrane receptors present in neurons and glial cells. Over-stimulation of glutamate receptors results in neuronal death, phenomena known as excitotoxicity. A family of sodium-dependent, ...

EphA2, which belongs to the Eph family of receptor tyrosine kinases, is overexpressed in a variety of human cancers. Serine 897 (S897) phosphorylation of EphA2 is known to promote cancer cell migration and proliferation in a ligand-independent manner. In this study, we show that glucose deprivat...

The work was aimed at the development of a biosensor array for the simultaneous determination of six solutes (glutamate, glucose, choline, acetylcholine, lactate, and pyruvate) in aqueous solutions. Enzymes selective for these substrates were immobilized on the surface of amperometric platinum d...

A novel functional polyamide containing azo, azomethine groups and pyridine ring was synthesized using a novel azomethine based dicarboxylic acid by direct polycondensation reaction. Polyacrylic acid-co-poly-2-acrylamido-2-methylpropanesulfonic acid (PAA-co-PAMPS) as anionic water-soluble polyme...

The tri-n-butyltin(IV) complexes of 2-[(E)-2-(3-formyl-4-hydroxyphenyl)-1-diazenyl]benzoic acid and 4-[((E)-1-{2-hydroxy-5-[(E)-2-(2-carboxyphenyl)-1-diazenyl]phenyl}methylidene)amino]aryls (aryls = 4-CH3, 4-Br, 4-Cl, 4-OCH3) have been synthesized and characterized by 1H, 13C, 119Sn NMR, IR and ...

Synthesis and photophysical properties of a novel pyrazoline – containing fluorophore, 3-naphthyl-1-phenyl-5-(4-carboxyphenyl)-2-pyrazoline (NPCP) A, and its proline derivative (NPCP-P) B are presented in this work. The highlight of this fluorescent dye is that, it can be prepared from availabl...

Reaction of 4-aminoantipyrine with 2-mercaptobenzoic acid afforded a proton transfer derivative, 1-phenyl-2,3-dimethyl-5-oxo-1,2-dihydro-1H-pyrazol-4-ammonium 2[(2-carboxyphenyl) disulfanyl]benzoate, (HAAP+⋅HTBA−), via the oxidation of 2-mercaptobenzoic acid into 2,2′-dithiobis(benzoic acid). T...

p-Coumaric acid (4-hydroxycinnamic acid) and methyl p-coumarate (methyl 4-hydroxycinnamate) inhibit the oxidation of l-tyrosine catalyzed by mushroom tyrosinase. However, both were oxidized as monophenol substrate analogues at an extremely slow rate. This oxidation was significantly accelerated ...

In addition to playing a key role in the response to environmental changes, cell walls are also considered as a valuable feedstock for cellulosic ethanol. Here we explored the effects of the stress-response hormones, salicylic acid and methyl jasmonate, on cell wall biosynthesis and biomass dige...

Class I phosphoinositide 3-kinases (PI3Ks), particularly PI3Kγ, have become attractive drug targets for inflammatory and autoimmune disorders such as rheumatoid arthritis. Herein, we describe the synthesis and the structure–activity relationships (SAR) of a series of 2-amino-5-oxadiazolyl thia...

An efficient synthesis of (S)- and (R)-3-hydroxypiperidin-2-ones from methyl 5-nitro-2-oxopentanoate is described. A one-pot enzyme catalysed hydrolysis of the ester and reduction of the ketone gave enantiopure 2-hydroxy-5-nitropentanoic acids which on esterification, catalytic hydrogenation ove...

We have made a novel series of pyrazolo[1,5-a]pyridines as PI3 kinase inhibitors, and demonstrated their selectivity for the p110α isoform over the other Class Ia PI3 kinases. We investigated the SAR around the pyrazolo[1,5-a]pyridine ring system, and found compound 5x to be a particularly pote...

The serine–threonine kinase CDK9 is a target of emerging interest for the development of anti-cancer drugs. There are multiple lines of evidence linking CDK9 activity to cancer, including the essential role this kinase plays in transcriptional regulation through phosphorylation of the C-termina...

Six organotin compounds with 4,4′-thiodibenzenethiol (LH2) of the type RnSnL4−nSnRn (n = 3: R = Me 1, Ph 2, PhCH2 3, n = 2: R = Me 4, Ph 5, PhCH2 6) have been synthesized. All compounds were characterized by elemental analysis, IR and NMR (1H, 13C, and 119Sn) spectra. The structures of compound...

From analyses of 77 K fluorescence and fluorescence excitation spectra of styrene and three deuterium substituted isomers, it is concluded that the S0 ∌ S1 transition is of a 1A1 ∌ 1A1 nature (in C2v).

Infrared and Raman spectra of C6H5CHCH2, C6H5CDCD2, C6D5CHCH2, and C6D5CDCD2 liquids are analyzed to assign their fundamental vibrations.

It has been recently reported that the peptide Ac–Glu–Thr–Lys–Thr–Tyr–Phe–Trp–Lys–NH2, analogue of the Glu1811–Lys1818 region of A3 light chain of blood coagulation factor VIII, presents in vitro significant anticoagulant activity. The encapsulation of this peptide into different polyv...

A simple synthetic method for the preparation of optically active pyrimidinyl α-amino acids is presented. A nucleophilic ipso-substitution reaction between 2-(benzylsulfonyl)-4-isopropoxypyrimidines and a nucleophilic side chain of several protected natural α-amino acids is investigated to obt...

P2Y12 plays an important role in platelet aggregation, which makes it an interesting target for antithrombotic agents. Compounds that antagonize P2Y12 include the active metabolites of thienopyridines and molecules that are structurally related to ATP, which is an antagonist of P2Y12. During the...