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The 2′-deoxy (2a) and 2′-ara-fluoro (3a) derivatives of zebularine (1-(β-D-ribofuranosyl)-dihydropyrimidin-2-one, 1a) were phosphorylated in high yield to the 5′-nucleotides 2b and 3b, respectively, and characterized by HPLC, enzyme degradation, 1 H, 13 C and 31 P NMR, and high resolution...
Several analogs 5, 6, 7, 8, 10 and 11 of the C-terminal fragment of a peptide antibiotic Sch 37137 were designed and tested as inhibitors of glucosamine-6-phosphate synthase from Succharomyces cerevisiae . From IC 50 values and kinetic parameters of inhibition of glucosamine-6-phosphate synthase...
A kinetic analysis of the inhibition of human salivary α-amylase (EC 188.8.131.52) by wheat seed ( Triticum aestivum ) type II α-amylase inhibitor revealed the inhibition was slow and tight-binding. The inhibition was competitive with an inhibition binding constant of the α-amylase inhibitor for...
Rat peritoneal macrophages were cultured with a specific and potent phospholipase A 2 activator A 23187, with 1-stearoyl-2-( 3 H)arachidonoyl-sn-GPC as source of ( 3 H) arachidonic acid, and with a dialkyl-GPC, at 2, 10 or 20 μml M . Four dialkyl-GPCs were prepared by chemical synthesis....
A new p56 idk tyrosine kinase inhibitor WIN 61651 (1,4-dihydro-7-(4-methyl-1-piperizinyl)-1-(4-(4-methyl-1-piperizinyl))phenyl-4-oxo-3-quinolinecarboxamide) is described. WIN 61651, which is competitive with AP, demonstrates selectivity for the lymphoid restricted tyrosine kinase p56 lck over...
Some intercalating and nonintercalating drugs have been tested as inhibitorrs on the DNA synthesis reaction catalyzed by avian myeloblastosis virus (AMV) reverse transcriptase, in the presence of poly-riboadenylic acid (poly(rA)) and poly(2′-Huoro-2′-deoxyadenylic acid) (poly(dM)) as...
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