ALL libraries (COBIB.SI union bibliographic/catalogue database)
-
Derivatives of pyrimidine, phthalimide and anthranilic acid as inhibitors of human hydroxysteroid dehydrogenase AKR1C1Brožič, Petra ...Human hydroxysteroid dehydrogenase (HSD) AKR1C1 is a member of the aldo-keto reductase superfamily, and it functions mainly as a 20_-HSD. It catalyzes the reduction of the potent progesterone to the ... weak 20_-hydroxyprogesterone, and of 3_,5_-tetrahydroprogesterone (5_-THPč allopregnanolone) to 5_-pregnane-3_,20_-diol. AKR1C1 thus decreases the levels of progesterone and 5_-THP in peripheral tissue. Progesterone inhibits cell proliferation, stimulates differentiation of endometrial cells, and is also important for maintenance of pregnancy, while 5_-THP allosterically modulates the activity of the _-aminobutyric acid receptor. Inhibitors of AKR1C1 are thus potential agents for treatment of endometrial cancer and endometriosis, as well as other diseases like premenstrual syndrome, catamenial epilepsy and depressive disorders.We have synthesized a series of pyrimidine, phthalimido and athranilic acid derivatives, and have here examined their inhibitory properties towards AKR1C1. A commonaldo- keto reductase substrate, 1-acenaphthenol,was used to monitor theNAD+-dependent oxidation catalyzed by AKR1C1. The most potent inhibitors of AKR1C1 were the pyrimidine derivative N-benzyl- 2-(2-(4-methoxybenzyl)-6-oxo-1,6-dihydropyrimidin-4-yl)acetamide (Ki=17_M) and the anthranilic acid derivative 2-(((2_,3-dichlorobiphenyl-4-yl)carbonyl)(methyl)amino)benzoic acid (Ki =33_M), both of which are non-competitive inhibitors.Source: Enzymology and molecular biology of carbonyl metabolism : [14th international workshop, Kranjska Gora, Slovenia, July 8 - 12, 2008] (Vol. 178, issues 1-3, 2009, str. 158-164)Type of material - conference contributionPublish date - 2009Language - englishCOBISS.SI-ID - 2480497
source: Enzymology and molecular biology of carbonyl metabolism : [14th international workshop, Kranjska Gora, Slovenia, July 8 - 12, 2008] (Vol. 178, issues 1-3, 2009, str. 158-164)
Shelf entry
Permalink
- URL:
Impact factor
Access to the JCR database is permitted only to users from Slovenia. Your current IP address is not on the list of IP addresses with access permission, and authentication with the relevant AAI accout is required.
Year | Impact factor | Edition | Category | Classification | ||||
---|---|---|---|---|---|---|---|---|
JCR | SNIP | JCR | SNIP | JCR | SNIP | JCR | SNIP |
Select the library membership card:
If the library membership card is not in the list,
add a new one.
DRS, in which the journal is indexed
Database name | Field | Year |
---|
Links to authors' personal bibliographies | Links to information on researchers in the SICRIS system |
---|---|
Brožič, Petra | 27575 |
Cesar, Jožko | 19062 |
Kovač, Andreja, farmacevtka, 1979- | 27782 |
Davies, Matthew | |
Johnson, A.P. | |
Fishwick, Colin W.G. | |
Lanišnik-Rižner, Tea | 11699 |
Gobec, Stanislav, 1970- | 15284 |
Source: Personal bibliographies
and: SICRIS
Select pickup location:
Material pickup by post
Delivery address:
Address is missing from the member's data.
The address retrieval service is currently unavailable, please try again.
By clicking the "OK" button, you will confirm the pickup location selected above and complete the reservation process.
By clicking the "OK" button, you will confirm the above pickup location and delivery address, and complete the reservation process.
By clicking the "OK" button, you will confirm the address selected above and complete the reservation process.
Notification
Automatic login and reservation service currently not available. You can reserve the material on the Biblos portal or try again here later.
Subject headings in COBISS General List of Subject Headings
Select pickup location
The material from the parent unit is free. If the material is delivered to the pickup location from another unit, the library may charge you for this service.
Pickup location | Material status | Reservation |
---|
Reservation in progress
Please wait a moment.
Reservation was successful.
Reservation failed.
Reservation...
Membership card:
Pickup location: