Unusual activity pattern of leucine aminopeptidase inhibitors based on phosphorus containing derivatives of methionine and norleucine
The result's identifiers
Result code in IS VaVaI
<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F61388963%3A_____%2F11%3A00359040" target="_blank" >RIV/61388963:_____/11:00359040 - isvavai.cz</a>
Result on the web
<a href="http://dx.doi.org/10.3109/14756366.2010.482047" target="_blank" >http://dx.doi.org/10.3109/14756366.2010.482047</a>
DOI - Digital Object Identifier
<a href="http://dx.doi.org/10.3109/14756366.2010.482047" target="_blank" >10.3109/14756366.2010.482047</a>
Alternative languages
Result language
angličtina
Original language name
Unusual activity pattern of leucine aminopeptidase inhibitors based on phosphorus containing derivatives of methionine and norleucine
Original language description
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 peptidaseisolated 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.
Czech name
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Czech description
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Classification
Type
J<sub>x</sub> - Unclassified - Peer-reviewed scientific article (Jimp, Jsc and Jost)
CEP classification
CC - Organic chemistry
OECD FORD branch
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Result continuities
Project
Result was created during the realization of more than one project. More information in the Projects tab.
Continuities
Z - Vyzkumny zamer (s odkazem do CEZ)
Others
Publication year
2011
Confidentiality
S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů
Data specific for result type
Name of the periodical
Journal of Enzyme Inhibition and Medicinal Chemistry
ISSN
1475-6366
e-ISSN
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Volume of the periodical
26
Issue of the periodical within the volume
2
Country of publishing house
GB - UNITED KINGDOM
Number of pages
7
Pages from-to
155-161
UT code for WoS article
000288441700001
EID of the result in the Scopus database
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