AKR1C3 Inhibitory Potency of Naturally-occurring Amaryllidaceae Alkaloids of Different Structural Types
The result's identifiers
Result code in IS VaVaI
<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F00216208%3A11160%2F17%3A10364760" target="_blank" >RIV/00216208:11160/17:10364760 - isvavai.cz</a>
Result on the web
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DOI - Digital Object Identifier
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Alternative languages
Result language
angličtina
Original language name
AKR1C3 Inhibitory Potency of Naturally-occurring Amaryllidaceae Alkaloids of Different Structural Types
Original language description
Aldo-keto reductase 1C3 (AKR1C3) is an important human enzyme that participates in the reduction of steroids and prostaglandins, which leads to proliferative signaling. AKR1C3 is frequently upregulated in various cancers, and this enzyme has been suggested as a therapeutic target for the treatment of these pathological conditions. The fact that the isoquinoline alkaloid stylopine has been identified as a potent AKR1C3 inhibitor has prompted us to screen a library of diverse types of Amaryllidaceae alkaloids, which biogenetically are isoquinoline alkaloids, on a recombinant form of AKRIC3. From the tested compounds, only tazettine showed moderate AKR1C3 inhibitory potency with an IC50 value of 15.8 +/- 1.2 mu M. Tazettine is a common Amaryllidaceae alkaloid, which could be used as a model substance for the further development of either analogues or related compounds with better inhibition potency.
Czech name
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Czech description
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Classification
Type
J<sub>imp</sub> - Article in a specialist periodical, which is included in the Web of Science database
CEP classification
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OECD FORD branch
30104 - Pharmacology and pharmacy
Result continuities
Project
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Continuities
S - Specificky vyzkum na vysokych skolach<br>I - Institucionalni podpora na dlouhodoby koncepcni rozvoj vyzkumne organizace
Others
Publication year
2017
Confidentiality
S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů
Data specific for result type
Name of the periodical
Natural Product Communications
ISSN
1934-578X
e-ISSN
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Volume of the periodical
12
Issue of the periodical within the volume
2
Country of publishing house
US - UNITED STATES
Number of pages
2
Pages from-to
245-246
UT code for WoS article
000395229200028
EID of the result in the Scopus database
2-s2.0-85019119655