Acyclic nucleoside phosphonates with adenine nucleobase inhibit Trypanosoma brucei adenine phosphoribosyltransferase in vitro
نویسندگان
چکیده
منابع مشابه
Acyclic adenine nucleoside phosphonates in plasma determined by high-performance liquid chromatography with fluorescence detection.
9-(2-Phosphonylmethoxyethyl)adenine (PMEA), (S)-9-(3-hydroxy-2-phosphonylmethoxypropyl)adenine (HPMPA), and (R,S)-9-(3-fluoro-2-phosphonylmethoxypropyl)adenine (FPMPA) are selective antiviral agents with activity against a broad spectrum of DNA viruses and retroviruses. A highly sensitive method has been developed to determine concentrations of these compounds in human plasma. Plasma samples co...
متن کاملTrypanosoma brucei adenine-phosphoribosyltransferases mediate adenine salvage and aminopurinol susceptibility but not adenine toxicity☆
African trypanosomes, like all obligate parasitic protozoa, cannot synthesize purines de novo and import purines from their hosts to build nucleic acids. The purine salvage pathways of Trypanosoma brucei being redundant, none of the involved enzymes is likely to be essential. Nevertheless they can be of pharmacological interest due to their role in activation of purine nucleobase or nucleoside ...
متن کاملAdenine phosphoribosyltransferase deficiency
Key-words Disease name and synonyms Definition Excluded diseases Diagnosis criteria Differential diagnosis Prevalence Molecular defect Clinical description Management including treatment Etiology Diagnostic methods Antenatal diagnosis Unresolved questions References Abstract Adenine phosphoribosyltransferase (APRT) catalyzes the synthesis of AMP (adenosine monophosphate) from adenine and 5'-pho...
متن کاملHuman Adenine Phosphoribosyltransferase
Human adenine phosphoribosyltransferase has been purified 33,000-fold from erythrocytes to a specific activity of 9.58 pmoles of AMP formed per mg of protein per min. The native enzyme has a molecular weight of 34,000 and is composed of three subunits of equal molecular weight which appear to be associated by noncovalent forces. The highly purified enzyme is maximally active over a broad pH ran...
متن کاملKinetic studies of adenine phosphoribosyltransferase.
The mechanism of reaction of adenine phosphoribosyltransferase from Ehrlich ascites tumor cells was investigated kinetically by initial velocity and product inhibition studies. The data are consistent with a mechanism in which 5-phosphoribosylpyrophosphate reacts with the enzyme to form an intermediate, presumably an enzyme-ribose 5-phosphate complex, with which adenine then reacts to form aden...
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ژورنال
عنوان ژورنال: Scientific Reports
سال: 2021
ISSN: 2045-2322
DOI: 10.1038/s41598-021-91747-6