Abstract
A series of shape-modified flexible nucleosides ('fleximers', 1, 2, and 3) was modeled, synthesized and subsequently assayed against S-adenosyl-L-homocysteine hydrolase (SAHase). No inhibitory activity was observed for the adenosine fleximer, which served as a substrate, but moderate inhibitory activity was exhibited by the guanosine fleximers. This is the first known report of a guanosine nucleoside analogue possessing activity against SAHase.
MeSH terms
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Adenosine / analogs & derivatives
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Adenosine / metabolism
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Adenosine / pharmacology
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Adenosylhomocysteinase / antagonists & inhibitors*
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Calorimetry / methods
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Enzyme Inhibitors / chemical synthesis
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Enzyme Inhibitors / chemistry
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Enzyme Inhibitors / pharmacology
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Guanosine / analogs & derivatives*
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Guanosine / chemical synthesis
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Guanosine / pharmacology*
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Hydrogen Bonding
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Hydrolysis
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Inosine / analogs & derivatives
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Inosine / chemical synthesis
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Inosine / pharmacology
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Kinetics
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Models, Molecular
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Thermodynamics
Substances
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Enzyme Inhibitors
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Guanosine
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Inosine
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Adenosylhomocysteinase
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Adenosine