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

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About: Double-Headed Sulfur-Linked Amino Acids As First Inhibitors for Betaine-Homocysteine S-Methyltransferase 2 Goto Sponge NotDistinct Permalink

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rdf:type	skos:Concept http://linked.opendata.cz/ontology/domain/vavai/Vysledek
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 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. 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. (en)
Title	Double-Headed Sulfur-Linked Amino Acids As First Inhibitors for Betaine-Homocysteine S-Methyltransferase 2 Double-Headed Sulfur-Linked Amino Acids As First Inhibitors for Betaine-Homocysteine S-Methyltransferase 2 (en)
skos:prefLabel	Double-Headed Sulfur-Linked Amino Acids As First Inhibitors for Betaine-Homocysteine S-Methyltransferase 2 Double-Headed Sulfur-Linked Amino Acids As First Inhibitors for Betaine-Homocysteine S-Methyltransferase 2 (en)
skos:notation	RIV/61388963:_____/12:00379825!RIV13-AV0-61388963
http://linked.open...avai/riv/aktivita	I P
http://linked.open...avai/riv/aktivity	I, P(GA203/09/1919), P(GAP207/10/1277)
http://linked.open...iv/cisloPeriodika	15
http://linked.open...vai/riv/dodaniDat	2013
http://linked.open...aciTvurceVysledku	Buděšínský, Miloš Elbert, Tomáš Jiráček, Jiří Mládková, Jana Vaněk, Václav Demianova, Zuzana
http://linked.open.../riv/druhVysledku	J - Článek v odborném periodiku
http://linked.open...iv/duvernostUdaju	S - Úplné a pravdivé údaje nepodléhající ochraně podle zvláštních právních předpisů
http://linked.open...titaPredkladatele	Ústav organické chemie a biochemie AV ČR, v. v. i.
http://linked.open...dnocenehoVysledku	132131
http://linked.open...ai/riv/idVysledku	RIV/61388963:_____/12:00379825
http://linked.open...riv/jazykVysledku	eng - angličtina
http://linked.open.../riv/klicovaSlova	betaine; homocysteine; methionine; BHMT; inhibitor (en)
http://linked.open.../riv/klicoveSlovo	homocysteine betaine methionine BHMT inhibitor
http://linked.open...odStatuVydavatele	US - Spojené státy americké
http://linked.open...ontrolniKodProRIV	[6C409884FF3B]
http://linked.open...i/riv/nazevZdroje	Journal of Medicinal Chemistry
http://linked.open...in/vavai/riv/obor	CE
http://linked.open...ichTvurcuVysledku	6 (xsd:int)
http://linked.open...cetTvurcuVysledku	7 (xsd:int)
http://linked.open...vavai/riv/projekt	Development of methods for configuration determination at chiral sulfur, nitrogen or phosphorus atom using NMR spectroscopy and ab initio calculations New inhibitors for human methyltransferases BHMT and BHMT-2 to study their physiological functions
http://linked.open...UplatneniVysledku	2012
http://linked.open...v/svazekPeriodika	55
http://linked.open...iv/tvurceVysledku	Buděšínský, Miloš Elbert, Tomáš Vaněk, Václav Jiráček, Jiří Demianova, Zuzana Garrow, T. A. Mládková, Jana
http://linked.open...ain/vavai/riv/wos	000307264100015
issn	0022-2623
number of pages	10 (xsd:int)
http://bibframe.org/vocab/doi	10.1021/jm300571h

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