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| {{STRUCTURE_2h5l| PDB=2h5l | SCENE= }} | | {{STRUCTURE_2h5l| PDB=2h5l | SCENE= }} |
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| '''S-Adenosylhomocysteine hydrolase containing NAD and 3-deaza-D-eritadenine'''
| | ===S-Adenosylhomocysteine hydrolase containing NAD and 3-deaza-D-eritadenine=== |
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| ==Overview==
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| d-Eritadenine (DEA) is a potent inhibitor of S-adenosyl-l-homocysteine hydrolase (SAHH) and has hypocholesterolemic activity. We have hypothesized that 3-deaza-DEA (C3-DEA) and its analogues retain high level of SAHH inhibitory activity and have resistance to deamination and glycosidic bond hydrolysis in vivo. Such C3-DEA analogues would have much higher hypocholesterolemic activity. C3-DEA, and its methyl ester (C3-OMeDEA) and its methyl amido (C3-NMeDEA) were synthesized to examine their SAHH inhibitory and hypocholesterolemic activities. A crystal structure of SAHH containing C3-DEA was determined and confirmed that DEA and C3-DEA bound to the same site of SAHH with the same binding mode. The SAHH inhibitory activities of C3-DEA (K(I)=1.5 microM) and C3-OMeDEA (K(I)=1.5 microM) are significantly lower than that of DEA (K(I)=30 nM), while rats fed by C3-DEA and C3-OMeDEA decrease the total plasma cholesterol and phospholipids by 36-40% and 23%, respectively, which is similar to the level of reductions (42% and 27%) by DEA. C3-NMeDEA lost most of the SAHH inhibitory activity (K(I)=30 microM) and dietary C3-NMeDEA does not decrease cholesterol and phospholipid in plasma but decreases the triacylglycerol level by 16%. DEA and C3-DEA analogues are neither substrates nor inhibitors of adenosine deaminase.
| | The line below this paragraph, {{ABSTRACT_PUBMED_17214973}}, adds the Publication Abstract to the page |
| | (as it appears on PubMed at http://www.pubmed.gov), where 17214973 is the PubMed ID number. |
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| | {{ABSTRACT_PUBMED_17214973}} |
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| ==About this Structure== | | ==About this Structure== |
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| [[Category: Inhibitor]] | | [[Category: Inhibitor]] |
| [[Category: S-adenosylhomocysteine]] | | [[Category: S-adenosylhomocysteine]] |
| ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun May 4 05:53:39 2008'' | | |
| | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Jul 28 12:05:17 2008'' |
