Počet záznamů: 1
Unusual activity pattern of leucine aminopeptidase inhibitors based on phosphorus containing derivatives of methionine and norleucine
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SYSNO ASEP 0359040 Druh ASEP J - Článek v odborném periodiku Zařazení RIV J - Článek v odborném periodiku Poddruh J Článek ve WOS Název Unusual activity pattern of leucine aminopeptidase inhibitors based on phosphorus containing derivatives of methionine and norleucine Tvůrce(i) Pícha, Jan (UOCHB-X) RID, ORCID
Liboska, Radek (UOCHB-X) RID, ORCID
Buděšínský, Miloš (UOCHB-X) RID, ORCID
Jiráček, Jiří (UOCHB-X) RID, ORCID
Pawelczak, M. (PL)
Mucha, A. (PL)Celkový počet autorů 6 Zdroj.dok. Journal of Enzyme Inhibition and Medicinal Chemistry. - : Taylor & Francis - ISSN 1475-6366
Roč. 26, č. 2 (2011), s. 155-161Poč.str. 7 s. Jazyk dok. eng - angličtina Země vyd. GB - Velká Británie Klíč. slova aminophosphonates ; aminophospinates ; methionine ; norleucine ; phosphorus containing dipeptides ; cytosolic leucine aminopeptidase ; inhibitors Vědní obor RIV CC - Organická chemie CEP GA203/06/1405 GA ČR - Grantová agentura ČR LC06077 GA MŠMT - Ministerstvo školství, mládeže a tělovýchovy CEZ AV0Z40550506 - UOCHB-X (2005-2011) UT WOS 000288441700001 DOI 10.3109/14756366.2010.482047 Anotace Ligands containing bulky aliphatic P1 residues exhibit a high affinity towards cytosolic leucine aminopeptidase, a bizinc protease of biomedical significance. According to this specificity, a series of phosphonic and phosphinic compounds have been put forward as novel putative inhibitors of the enzyme. These phosphonic and phosphinic compounds were derivatives of methionine and norleucine as both single amino acids and dipeptides. The designed inhibitors were synthesised and tested towards the peptidase isolated from porcine kidneys using an improved separation procedure affording superior homogeneity. Unexpectedly, organophosphorus derivatives of methionine and norleucine exhibited moderate activity with Ki values in the micromolar range. Pracoviště Ústav organické chemie a biochemie Kontakt asep@uochb.cas.cz ; Kateřina Šperková, Tel.: 232 002 584 ; Viktorie Chládková, Tel.: 232 002 434 Rok sběru 2012
Počet záznamů: 1