Pancreastatin (PST) is a biologically active peptide isolated first from porcine pancreas. Its origin takes place in chromogranin A proteolysis within the neuroendocrine and gastrointestinal systems. Although ample metabolic effects, such as modulation of secretion of different glands, as well a...

BackgroundNeuroendocrine tumors (NETs) of the duodenum are rare, heterogeneous, and often indolent neoplasms. We hypothesized that elevated pancreastatin levels are an indicator of a poor prognosis in well-differentiated duodenal NETs.

AimsTo investigate the role of pancreastatin inhibitor (PSTi8) in lipid homeostasis and insulin sensitivity in dexamethasone induced fatty liver disease associated type 2 diabetes.

We have reported previously the localization of the 49 amino acid peptide pancreastatin to all identifiable endocrine cells of porcine gut, pancreas and adrenal, thyroid and pituitary glands. In this study, we have investigated the occurrence of pancreastatin in a series of human neuroendocrine ...

A radioimmunoassay of human pancreastatin was developed using a rabbit antiserum that selectively recognized the C-terminal amidated end of the peptide, and it was used for the identification of the molecular forms of pancreastatin in human gut (stomach, duodenum, small intestine, colon) and end...

Effects of synthetic human pancreastatin-52 and human pancreastatin-29 on pancreatic secretion and blood flow were examined in rats and dogs. Synthetic human pancreastatin-52 and human pancreastatin-29 were equally potent in suppressing the release of amylase stimulated by cholecystokinin in rat...

5′-Triphosphate 2′-5′-oligoadenylate (2–5A) is the central player in the 2–5A system that is an innate immunity pathway in response to the presence of infectious agents. Intracellular endoribonuclease RNase L activated by 2–5A cleaves viral and cellular RNA resulting in apoptosis. The majo...

The aim of this study is to investigate the effect of different concentrations of adenosine 5′-triphosphate (ATP) as a stabilizing agent on the physicochemical and biological behavior of AgNPs. The results revealed that the size of distribution and dispersion of AgNPs were controlled by changes...

This work reports on a novel time-resolved fluorescent aptasensing platform for the quantitative monitoring of adenosine 5′-triphosphate (ATP) by interaction of dispersive/agglomerate gold nanoparticles (AuNPs) with terbium ion-coordinated carbon dots (Tb-CDs). To construct such a fluorescent n...

While enzyme activity is often regulated by a combination of substrate/effector availability and quaternary structure, many cytosolic enzymes may be further regulated through oligomerization into filaments. Cytidine-5′-triphosphate (CTP) synthase (CTPS) forms such filaments—a process that is p...

A fully automated chemical method for the parallel and high-throughput solid-phase synthesis of 5′-triphosphate and 5′-diphosphate oligonucleotides is described. The desired full-length oligonucleotides were first constructed using standard automated DNA/RNA solid-phase synthesis procedures. T...

5-[(p-Carborane-2-yl)ethynyl]-2′-deoxyuridine 5′-O-triphosphate was synthesized and used as a good substrate in enzymatic construction of carborane-modified DNA or oligonucleotides containing up to 21 carborane moieties in primer extension reactions by DNA polymerases.

We describe an efficient method for the synthesis of (E)-5-[3-Aminoallyl]-uridine-5′-triphosphate, AA-UTP that combines the advantage of one-pot triphosphate formation and fluorous solid-phase extraction.

As an archetype C-nucleoside, pyrazofurin possesses broad-spectrum antiviral and antitumor activities. However, the presence of the acidic enol in the nucleobase of pyrazofurin poses a huge challenge to the conventional NTP synthetic methods. On the basis of a selective phosphorylation method an...

IntroductionLes médicaments périmés engendrent un important coût financier et leur consommation peuvent être liée à de multiples morbidités et toxicités. L’objectif de ce travail est de décrire les attitudes des marocains devant un médicament avec une date de péremption expirée.

A series of benzimidazole derivatives with a phenylcyclohexyl acetic acid group as DGAT-1 inhibitors was developed. Among the benzimidazole series, compound 5k showed submicromolar in vitro activity toward human and mouse DGAT-1, good selectivity toward DGAT-2, human liver metabolic stability, a...

A study of the effects in vitro of 1-(1-phenylcyclohexyl)piperidine·HCl (Sernyl) has shown that with succinate, α-ketoglutarate, β-hydroxybutyrate, or citrate as the substrate, the oxygen uptake by homogenates of rat liver was stimulated by 0·2 and 0·5 mM concentrations of the drug. Experim...

We have investigated the effects of Sernylan, a dissociative anaesthetic, on both the bulbo-spinal and spinal reflexes of cats. Cats decerebrated at the precollilcular level were used to investigate the interaction of bulbo-spinal with spinal reflexes. Conditioning stimuli were delivered to the ...

The current work discloses a novel cyclohexylarylamine chemotype with potent inhibition of the serotonin, norepinephrine, and dopamine transporters and potential for treatment of major depressive disorder. Optimized compounds 1 (SERT, NET, DAT, IC50 = 169, 85, 21 nM) and 42 (SERT, NET, DAT IC50 ...

Novel chiral cyclohexylaryl amines were developed with potent reuptake inhibition against the serotonin, norepinephrine and dopamine transporters and activity at 10 and 30 mpk PO in the mouse tail suspension test. Prototype compound 31 (SERT, NET, DAT IC50 ⩽ 1, 21, 28 nM) was highly brain penetr...