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Double-Headed Sulfur-Linked Amino Acids As First Inhibitors for Betaine-Homocysteine S-Methyltransferase 2
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SYSNO ASEP 0379825 Document Type J - Journal Article R&D Document Type Journal Article Subsidiary J Článek ve WOS Title Double-Headed Sulfur-Linked Amino Acids As First Inhibitors for Betaine-Homocysteine S-Methyltransferase 2 Author(s) Mládková, Jana (UOCHB-X)
Vaněk, Václav (UOCHB-X) RID, ORCID
Buděšínský, Miloš (UOCHB-X) RID, ORCID
Elbert, Tomáš (UOCHB-X) RID, ORCID
Demianova, Zuzana (UOCHB-X)
Garrow, T. A. (US)
Jiráček, Jiří (UOCHB-X) RID, ORCIDNumber of authors 7 Source Title Journal of Medicinal Chemistry. - : American Chemical Society - ISSN 0022-2623
Roč. 55, č. 15 (2012), s. 6822-6831Number of pages 10 s. Language eng - English Country US - United States Keywords betaine ; homocysteine ; methionine ; BHMT ; inhibitor Subject RIV CE - Biochemistry R&D Projects GA203/09/1919 GA ČR - Czech Science Foundation (CSF) GAP207/10/1277 GA ČR - Czech Science Foundation (CSF) Institutional support UOCHB-X - RVO:61388963 UT WOS 000307264100015 DOI 10.1021/jm300571h Annotation 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 tested them 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. Workplace Institute of Organic Chemistry and Biochemistry Contact asep@uochb.cas.cz ; Kateřina Šperková, Tel.: 232 002 584 ; Jana Procházková, Tel.: 220 183 418 Year of Publishing 2013
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