Garvey, Edward P. published the artcileNucleotide and Nucleoside Analogs as Inhibitors of Cytosolic 5′-Nucleotidase I from Heart, Recommanded Product: Diethyltrichloromethylphosphonate, the publication is Biochemistry (1998), 37(25), 9043-9051, database is CAplus and MEDLINE.
Substrate and product specificity studies were used to develop inhibitors of the cytosolic 5′-nucleotidase I (c-N-I) from myocardium. As measured by Vmax/Km, c-N-I preferred pyrimidine 2′-deoxyribonucleotides as substrates with thymidine monophosphate (TMP) being the most efficient. In product inhibition studies, thymidine inhibited noncompetitively and inorganic phosphate inhibited competitively, consistent with an ordered release of nucleoside prior to phosphate. Mirroring nucleotide substrate specificities, pyrimidine nucleosides were more potent product inhibitors than purine nucleosides. Thus, pyrimidine nucleotide and nucleoside analogs were developed as inhibitors. Phosphonate analogs of TMP were synthesized by a novel method. The most potent was the 5′-phosphonate of 3′-deoxythymidine (ddT) (apparent Ki value of 63 nM). In addition, pyrimidine nucleoside analogs were inhibitors with 5-ethynyl-2′,3′-dideoxyuridine being the most potent (apparent Ki value of 3.7 μM). The most potent nucleotide and nucleoside inhibitor were both greater than 1000-fold more potent inhibiting c-N-I than the cytosolic 5′-nucleotidase II. The nucleoside analog was also greater than 1000-fold more potent against c-N-I than the membrane ecto-5′-nucleotidase (e-N). Because the phosphonate analogs measurably inhibited e-N (apparent Ki values of 6-12 μM), the selectivity of the phosphonates for c-N-I vs. e-N was less (40-200-fold). Because of the high selectivity for c-N-I vs. both of the other 5′-nucleotidases, the nucleoside inhibitors of c-N-I may be useful biochem. tools in discerning the role that c-N-I plays in generating adenosine within myocardium.
Biochemistry published new progress about 866-23-9. 866-23-9 belongs to chlorides-buliding-blocks, auxiliary class Aliphatic Chain, name is Diethyltrichloromethylphosphonate, and the molecular formula is C5H10Cl3O3P, Recommanded Product: Diethyltrichloromethylphosphonate.
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https://en.wikipedia.org/wiki/Chloride,
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