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
Functional and genetic evidence that nucleoside transport is highly conserved in Leishmania species: Implications for pyrimidine-based chemotherapy [PDF]
Leishmania pyrimidine salvage is replete with opportunities for therapeutic intervention with enzyme inhibitors or antimetabolites. Their uptake into cells depends upon specific transporters; therefore it is essential to establish whether various ...
Ali, Juma A.M.+7 more
core +2 more sources
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
María 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
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
Anatomical Distribution of Nucleoside System in the Human Brain and Implications for Therapy [PDF]
Nucleosides have a wide range of physiological and pathophysiological roles in the human brain as modulators of a variety of neural functions. For example, adenosine, inosine, guanosine, and uridine participate in the mechanisms underlying memory ...
Dobolyi, Árpád, Kovács, Zsolt
core +1 more source
A β-Fluoroamine Inhibitor of Purine Nucleoside Phosphorylase [PDF]
The potent immucillin purine nucleoside phosphorylase (PNP ) inhibitors F-DADMe-ImmH [(3S,4S)-3], and [(3R,4R)-3] are synthesized in seven steps. Cycloaddition to a fluoroalkene and an enzymic resolution are the key features of the construction of the fluoropyrrolidines 11, from which the immucillins are assembled by use of a three-component Mannich ...
Graeme J. Gainsford+5 more
openaire +3 more sources
Altered deoxyribonucleotide pools in T-lymphoblastoid cells expressing the multisubstrate nucleoside kinase of Drosophila melanogaster [PDF]
The multisubstrate nucleoside kinase of Drosophila melanogaster (Dm-dNK) can be expressed in human solid tumor cells and its unique enzymatic properties makes this enzyme a suicide gene candidate.
Balzarini, J+4 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