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Statements

Subject Item
n2:RIV%2F61388963%3A_____%2F12%3A00379825%21RIV13-AV0-61388963
rdf:type
skos:Concept n14:Vysledek
dcterms: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.
dcterms: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
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
skos:notation
RIV/61388963:_____/12:00379825!RIV13-AV0-61388963
n14:predkladatel
n15:ico%3A61388963
n3:aktivita
n16:P n16:I
n3:aktivity
I, P(GA203/09/1919), P(GAP207/10/1277)
n3:cisloPeriodika
15
n3:dodaniDat
n4:2013
n3:domaciTvurceVysledku
n6:7989776 n6:3046486 Demianova, Zuzana n6:9726411 n6:6236219 n6:9729232
n3:druhVysledku
n17:J
n3:duvernostUdaju
n19:S
n3:entitaPredkladatele
n12:predkladatel
n3:idSjednocenehoVysledku
132131
n3:idVysledku
RIV/61388963:_____/12:00379825
n3:jazykVysledku
n9:eng
n3:klicovaSlova
betaine; homocysteine; methionine; BHMT; inhibitor
n3:klicoveSlovo
n11:BHMT n11:inhibitor n11:homocysteine n11:betaine n11:methionine
n3:kodStatuVydavatele
US - Spojené státy americké
n3:kontrolniKodProRIV
[6C409884FF3B]
n3:nazevZdroje
Journal of Medicinal Chemistry
n3:obor
n13:CE
n3:pocetDomacichTvurcuVysledku
6
n3:pocetTvurcuVysledku
7
n3:projekt
n18:GAP207%2F10%2F1277 n18:GA203%2F09%2F1919
n3:rokUplatneniVysledku
n4:2012
n3:svazekPeriodika
55
n3:tvurceVysledku
Buděšínský, Miloš Demianova, Zuzana Mládková, Jana Vaněk, Václav Elbert, Tomáš Jiráček, Jiří Garrow, T. A.
n3:wos
000307264100015
s:issn
0022-2623
s:numberOfPages
10
n7:doi
10.1021/jm300571h