A cellular thermal shift assay (CETSA) protocol identifies and resolves antimalarial drug targets in P. falciparum. Defining drug targets in malaria Different classes of malaria drugs have been used for decades, even though the mechanisms of action have ...
J. Dziekan+9 more
semanticscholar +1 more source
Pyrazolo[4,3-e][1,2,4]triazines: Purine Analogues with Electronic Absorption in the Visible Region
Synthesis of several pryrazolo[4,3-e][1,2,4]-triazines is described. Theabsorption spectrum of some 5-substituted derivatives was found to extend to the visibleregion.
Jacek Wierzchowski+2 more
doaj +1 more source
Plasmodium falciparum parasites are killed by a transition state analogue of purine nucleoside phosphorylase in a primate animal model. [PDF]
Plasmodium falciparum causes most of the one million annual deaths from malaria. Drug resistance is widespread and novel agents against new targets are needed to support combination-therapy approaches promoted by the World Health Organization. Plasmodium
MarĂa B Cassera+11 more
doaj +1 more source
Ethenoguanines undergo glycosylation by nucleoside 2'-deoxyribosyltransferases at non-natural sites. [PDF]
Deoxyribosyl transferases and functionally related purine nucleoside phosphorylases are used extensively for synthesis of non-natural deoxynucleosides as pharmaceuticals or standards for characterizing and quantitating DNA adducts.
Wenjie Ye+10 more
doaj +1 more source
A UV/Vis Spectroscopy-Based Assay for Monitoring of Transformations Between Nucleosides and Nucleobases [PDF]
Efficient reaction monitoring is crucial for data acquisition in kinetic and mechanistic studies. However, for conversions of nucleosides to their corresponding nucleobases, as observed in enzymatically catalyzed nucleoside phosphorylation reactions, the
Giessmann, Robert T.+5 more
core +1 more source
Design and Synthesis of New Modified Flexible Purine Bases as Potential Inhibitors of Human PNP
The great interest in studying the structure of human purine nucleoside phosphorylase (hPNP) and the continued search for effective inhibitors is due to the importance of the enzyme as a target in the therapy of T-cell proliferative diseases. In addition,
Anastasia Khandazhinskaya+7 more
doaj +1 more source
Nucleoside-dependent synthesis of organic phosphorus compounds by rat liver nuclei [PDF]
a) A modified procedure of the WIDNELL and TATA8 method yields rat liver nuclei manifesting a high degree of purity and activity. b) These nuclei contain a nucleoside-dependent phosphorylating activity that is readily released and apparently unrelated to
Utsumi, Kozo
core +1 more source
Ischemic nucleotide breakdown increases during cardiac development due to drop in adenosine anabolism/catabolism ratio [PDF]
Our earlier work on reperfusion showed that adult rat hearts released almost twice as much purine nucleosides and oxypurines as newborn hearts did [Am J Physiol 254 (1988) H1091].
Huizer, T. (Tom)+3 more
core +2 more sources
Purine nucleoside phosphorylase (PNP) deficiency is a rare autosomal recessive primary immunodeficiency disorder characterized by decreased numbers of T-cells, variable B-cell abnormalities, decreased amount of serum uric acid and PNP enzyme activity ...
Saba Fekrvand+4 more
semanticscholar +1 more source
Despite a wealth of potential applications inside target cells, protein-based therapeutics are largely limited to extracellular targets due to the inability of proteins to readily cross biological membranes and enter the cytosol.
Minyoung Park+8 more
semanticscholar +1 more source