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Unusual activity pattern of leucine aminopeptidase inhibitors based on phosphorus containing derivatives of methionine and norleucine
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SYSNO ASEP 0359040 Document Type J - Journal Article R&D Document Type Journal Article Subsidiary J Článek ve WOS Title Unusual activity pattern of leucine aminopeptidase inhibitors based on phosphorus containing derivatives of methionine and norleucine Author(s) 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)Number of authors 6 Source Title Journal of Enzyme Inhibition and Medicinal Chemistry. - : Taylor & Francis - ISSN 1475-6366
Roč. 26, č. 2 (2011), s. 155-161Number of pages 7 s. Language eng - English Country GB - United Kingdom Keywords aminophosphonates ; aminophospinates ; methionine ; norleucine ; phosphorus containing dipeptides ; cytosolic leucine aminopeptidase ; inhibitors Subject RIV CC - Organic Chemistry R&D Projects GA203/06/1405 GA ČR - Czech Science Foundation (CSF) LC06077 GA MŠMT - Ministry of Education, Youth and Sports (MEYS) CEZ AV0Z40550506 - UOCHB-X (2005-2011) UT WOS 000288441700001 DOI 10.3109/14756366.2010.482047 Annotation 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. Workplace Institute of Organic Chemistry and Biochemistry Contact asep@uochb.cas.cz ; Kateřina Šperková, Tel.: 232 002 584 ; Viktorie Chládková, Tel.: 232 002 434 Year of Publishing 2012
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