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Biochemical Characterization of an Arabinoside Monophosphate Specific 5'-Nucleotidase-like Enzyme from .
Biomolecules
October 2024
Henan Engineering Research Center of Bioconversion Technology of Functional Microbes, College of Life Science, Henan Normal University, Xinxiang 453007, China.
To investigate the function of the gene in the pentostatin and vidarabine (Ara-A) biosynthetic gene cluster in NRRL 3238, PenF was recombinantly expressed and characterized. Enzymatic characterization of the enzyme demonstrated that PenF exhibited metal-dependent nucleoside 5'-monophosphatase activity, showing a substrate preference for arabinose nucleoside 5'-monophosphate over 2'-deoxyribonucleoside 5'-monophosphate and ribonucleoside 5'-monophosphate. Metal ions such as Mg and Mn significantly enhanced enzyme activity, whereas Zn, Cu, and Ca inhibited it.
View Article and Find Full Text PDFThe metabolic engineering of Escherichia coli for the high-yield production of hypoxanthine.
Microb Cell Fact
November 2024
College of Biotechnology, Tianjin University of Science & Technology, Tianjin, 300457, P. R. China.
Background: Hypoxanthine, prevalent in animals and plants, is used in the production of food additives, nucleoside antiviral drugs, and disease diagnosis. Current biological fermentation methods synthesize quantities insufficient to meet industrial demands. Therefore, this study aimed to develop a strain capable of industrial-scale production of hypoxanthine.
View Article and Find Full Text PDFEctonucleotidase inhibitors: an updated patent review (2017-2023).
Expert Opin Ther Pat
November 2024
Institute of Intelligent Machines, Hefei Institutes of Physical Science, Chinese Academy of Sciences, Hefei, China.
Article Synopsis
- The main enzymes responsible for breaking down nucleotides at the cell surface are NTPDases, ENPPs, alkaline phosphatases, and e5'NT, which can influence various health conditions like cancer and inflammation, making them potential therapeutic targets.
- This review focuses on ectonucleotidase inhibitors, including both nucleoside/nucleotide analogues and bicyclic compounds, that have been patented between 2017 and 2023, highlighting their chemistry and clinical applications.
- The review emphasizes the importance of nucleotides in regulating key physiological processes and discusses the therapeutic potential of small molecules that affect ectonucleotidase activity, including advancements in combination therapy and selectivity.
Adenosine Metabolism Pathway Alterations in Frontal Cortical Neurons in Schizophrenia.
Cells
October 2024
Department of Neurosciences & Psychiatry, University of Toledo College of Medicine and Life Sciences, Toledo, OH 43614, USA.
Schizophrenia is a neuropsychiatric illness characterized by altered neurotransmission, in which adenosine, a modulator of glutamate and dopamine, plays a critical role that is relatively unexplored in the human brain. In the present study, postmortem human brain tissue from the anterior cingulate cortex (ACC) of individuals with schizophrenia ( = 20) and sex- and age-matched control subjects without psychiatric illness ( = 20) was obtained from the Bronx-Mount Sinai NIH Brain and Tissue Repository. Enriched populations of ACC pyramidal neurons were isolated using laser microdissection (LMD).
View Article and Find Full Text PDFDesign, synthesis and structure-activity relationship of malonic acid non-nucleoside derivatives as potent CD73 inhibitors.
Bioorg Med Chem Lett
November 2024
Shanghai Key Laboratory of New Drug Design, School of Pharmacy, East China University of Science and Technology, Shanghai 200237, China. Electronic address:
High levels of extracellular adenosine in tumor microenvironment (TME) has extensive immunosuppressive effect. CD73 catalyzes the conversion of AMP into adenosine and regulates its production. Inhibiting CD73 can reduce the level of adenosine and reverse adenosine-mediated immune suppression.
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