Search results for "Nucleosides"
showing 10 items of 66 documents
Insight into non-nucleoside triazole-based systems as viral polymerases inhibitors
2023
Viruses have been recognized as the etiological agents responsible for many pathological conditions ranging from asymptomatic infections to serious diseases, even leading to death. For this reason, many efforts have been made to identify selective viral targets with the aim of developing efficient therapeutic strategies, devoid of drug-resistance issues. Considering their crucial role in the viral life cycle, polymerases are very attractive targets. Among the classes of compounds explored as viral polymerases inhibitors, here we present an overview of non-nucleoside triazole-based compounds identified in the last fifteen years. Furthermore, the structure-activity relationships (SAR) of the …
Presence of phosphorylatedO-ribosyl-adenosine In T-ψ-stem of yeast methlonine initiator tRNA
1989
We report in this paper on isolation and characterization of two unknown nucleosides G* and [A*] located in the T-psi-stem of yeast methionine initiator tRNA, using the combined means of HPLC protocols, real time UV-absorption spectrum, and post-run mass spectrometry by electron impact or fast atom bombardment. The G* nucleoside in position 65 was identified as unmodified guanosine. The structure of the unknown [A*] in position 64 was characterized as an isomeric form of O-ribosyl-adenosine by comparison of its chromatographic, UV-spectral and mass spectrometric properties with those of authentic O-alpha-ribofuranosyl-(1"----2')-adenosine isolated from biosynthetic poly(adenosine diphosphat…
Extreme nucleoside concentrations in a marine annelid: a novel nucleoside storing cell in the polychaete Nereis virens.
2010
A new type of free coelomic cell was isolated from the coelomic fluid of the polychaete Nereis virens. This cell type was present only during sexual maturation and only in males with fully developed spermatozoa. In vivo acridine orange staining and electron microscopy showed that this cell type consists mainly of a large acidic vacuole with a very low proportion of cytoplasm. This cell type stores extremely high concentration of purine nucleosides reaching concentrations of >700 millimolar on a cell weight basis. The nucleoside concentrations are the highest reported from any living cell so far. Inosine (280-711 micromol/g cell mass), guanosine (8-109 micromol/g), deoxyinosine (3-26 micromo…
On the Use of Metal Purine Derivatives (M=Ir, Rh) for the Selective Labeling of Nucleosides and Nucleotides
2014
The reactions of neutral or cationic IrIII and RhIII derivatives of phenyl purine nucleobases with unsymmetrical alkynes produce new metallacycles in a predictable manner, which allows for the incorporation of either photoactive (anthracene or pyrene) or electroactive (ferrocene) labels in the nucleotide or nucleoside moiety. The reported methodology (metalation of the purine derivative and subsequent marker insertion) could be used for the postfunctionalization and unambiguous labeling of oligonucleotides.
Synthesis and preliminary biological evaluation of a new pyridocarbazole derivative covalently linked to a thymidine nucleoside as a potential target…
2003
The therapy of human cancer is one of the more pursued goals by medicinal chemistry research. Most of the compounds clinically used as a treatment owe their efficacy to their cytotoxic interaction (direct or indirect) with nuclear DNA. This interaction results in the inhibition of DNA synthesis and the degradation of nucleic strands. Ellipticine is a naturally occurring 6H-pyrido[4,3-b]carbazole alkaloid endowed with antitumor activity, and several ellipticine derivatives have been used in clinical trials. We previously reported some 1,4-dimethyl-9H-carbazole derivatives structurally related to ellipticine. The purpose of our research was to transform the pyridocarbazole in a prodrug so tha…
Partial purification and some properties of a nucleoside phosphotransferase of chick embryos.
1978
A nucleoside phosphotransferase purified about 40fold from chick embryos utilizes efficiently as phosphate donors deoxyribonucleoside and pyrimidine ribonucleoside monophosphates, whereas the pyrimidine deoxyribonucleoside appear to be the preferred acceptors of phosphate. The enzyme is very unstable to heat, dilution and dialysis. A marked enhancement in the stability is caused by nucleotides and it seems associated with the formation of an aggregated state of the protein.
Unified model for the ultrafast decay of pyrimidine nucleobases.
2006
Ultrafast decay processes detected after absorption of UV radiation in gas-phase pyrimidine nucleobases uracil, thymine, and cytosine are ascribed to the barrierless character of the pathway along the low-lying 1(pipi*) hypersurface connecting the Franck-Condon region with an out-of-plane distorted ethene-like conical intersection with the ground state. Longer lifetime decays and low quantum yield emission are on the other hand related to the presence of a 1(pipi*) state planar minimum on the S1 surface and the barriers to access other conical intersections. A unified model for the three systems is established on the basis of accurate multiconfigurational CASPT2 calculations, whereas the ef…
Pseudouridine: Still mysterious, but never a fake (uridine)!
2014
International audience; Pseudouridine () is the most abundant of >150 nucleoside modifications in RNA. Although was discovered as the first modified nucleoside more than half a century ago, neither the enzymatic mechanism of its formation, nor the function of this modification are fully elucidated. We present the consistent picture of synthases, their substrates and their substrate positions in model organisms of all domains of life as it has emerged to date and point out the challenges that remain concerning higher eukaryotes and the elucidation of the enzymatic mechanism.
On the function of modified nucleosides in the RNA world.
1998
Presumably ribosome and transfer RNA (tRNA) evolved from a pre-existing function in the RNA stage of life and were secondarily adapted for protein synthesis. Various possible initial functions of the primitive ribosome (protoribosome) have been suggested. The initial function of the primitive ribosome and primitive genetic translation would have been quite similar. It is possible that, initially, both functions coexisted in the protoribosome. Given that the three-dimensional structure of ribosomal RNAs shows only minor variations throughout time, it is, then, most likely that present ribosomes can still recall (remember) the most important parts of the mechanism of their initial function. A…
Long-term stability study of clofarabine injection concentrate and diluted clofarabine infusion solutions
2011
Purpose: The aim of this study was to investigate the physicochemical stability of clofarabine (CAFdA) injection concentrate and ready-to-use CAFdA infusion solutions over a prolonged period of 28 days. Methods: To determine the stability of CAFdA infusion solutions, the injection concentrate (Evoltra®, 1 mg/mL, Genzyme) was diluted either with 0.9% sodium chloride or 5% glucose infusion solution. The resulting concentrations of 0.2 mg/mL or 0.6 mg/mL, respectively, were chosen to represent the lower and upper limit of the ordinary concentration range. Test solutions were stored under refrigeration (2–8°C) or at room temperature either light protected or exposed to light. CAFdA concentrati…