Double-Headed Sulfur-Linked Amino Acids As First Inhibitors for Betaine-Homocysteine S-Methyltransferase 2

Result code in IS VaVaI
<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F61388963%3A_____%2F12%3A00379825" target="_blank" >RIV/61388963:_____/12:00379825 - isvavai.cz</a>
Result on the web
<a href="http://dx.doi.org/10.1021/jm300571h" target="_blank" >http://dx.doi.org/10.1021/jm300571h</a>
DOI - Digital Object Identifier
<a href="http://dx.doi.org/10.1021/jm300571h" target="_blank" >10.1021/jm300571h</a>

Result language
angličtina
Original language name
Double-Headed Sulfur-Linked Amino Acids As First Inhibitors for Betaine-Homocysteine S-Methyltransferase 2
Original language description
BHMT-2 methyltransferase catalyzes the transfer of a methyl group from S-methylmethionine to L-homocysteine, yielding two molecules of L-methionine. In this study, we have prepared the first series of BHMT-2 inhibitors to be described, and we have testedthem with human recombinant BHMT-2 that has been stabilized by copurification with human recombinant BHMT. Among the compounds synthesized, (2S,8RS,11RS)-5-thia-2,11-diamino-8-methyldodecanedioic acid was the most potent (Ki app about 77 nM) and selective inhibitor of BHMT-2. This compound may be useful in future in vivo studies to probe the physiological significance of BHMT-2 in sulfur amino acid metabolism.
Czech name
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Czech description
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Type
J<sub>x</sub> - Unclassified - Peer-reviewed scientific article (Jimp, Jsc and Jost)
CEP classification
CE - Biochemistry
OECD FORD branch
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Project
Result was created during the realization of more than one project. More information in the Projects tab.
Continuities
I - Institucionalni podpora na dlouhodoby koncepcni rozvoj vyzkumne organizace

Publication year
2012
Confidentiality
S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů

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