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Inhibitors of aldo-keto reductases AKR1C1-AKR1C4
Brožič, Petra (Avtor), Turk, Samo (Avtor), Lanišnik-Rižner, Tea (Avtor), Gobec, Stanislav (Avtor)

URLURL - Predstavitvena datoteka, za dostop obiščite http://www.benthamscience.com/contents.php?JCode=CMC&Vol=00000018&Iss=00000017#3168246 Novo okno

Izvleček
The AKR1C aldo-keto reductases (AKR1C1-AKR1C4) are enzymes that interconvert steroidal hormones between their active and inactive forms. In this manner, they can regulate the occupancy and trans-activation of the androgen, estrogen and progesterone receptors. The AKR1C isoforms also have important roles in the production and inactivation of neurosteroids and prostaglandins, and in the metabolism of xenobiotics. They thus represent important emerging drug targets for the development of agents for the treatment of hormone-dependent forms of cancer, like breast, prostate and endometrial cancers, and other diseases, like premenstrual syndrome, endometriosis, catamenial epilepsy and depressive disorders. We present here the physiological roles of these enzymes, along with their structural properties and an overview of the recent developments regarding their inhibitors. The most important strategies of inhibitor design are described, which include the screening of banks of natural compounds (like cinnamic acids, flavonoids, jasmonates, and related compounds), the screening of and structural modifications to non-steroidal anti-inflammatory drugs, the substrate-inspireddesign of steroidal and nonsteroidal inhibitors, and computer-assisted structure-based inhibitor design.

Jezik:Angleški jezik
Ključne besede:aldo-keto reduktaza, AKR1C1, AKR1C4, steroidni hormoni, inhibitorji
Vrsta gradiva:Delo ni kategorizirano (r6)
Tipologija:1.02 - Pregledni znanstveni članek
Organizacija:FFA - Fakulteta za farmacijo
Leto izida:2011
Št. strani:str. 2554-2565
Številčenje:Vol. 18, no. 17
UDK:615.2
ISSN pri članku:0929-8673
COBISS.SI-ID:3023985 Povezava se odpre v novem oknu
Število ogledov:528
Število prenosov:112
Metapodatki:XML RDF-CHPDL DC-XML DC-RDF
 
Skupna ocena:(0 glasov)
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Gradivo je del revije

Naslov:Current medicinal chemistry
Skrajšan naslov:Curr. med. chem.
Založnik:Bentham Science Publishers
ISSN:0929-8673
COBISS.SI-ID:16840197 Novo okno

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