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Aldo-keto reductase 1C3 - assessment as a new target for the treatment of endometriosis
ID
Lanišnik-Rižner, Tea
(
Author
),
ID
Penning, Trevor M.
(
Author
)
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MD5: 43017A1204C6323E3D06E2DF35B1770D
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https://www.sciencedirect.com/science/article/pii/S1043661819314732
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Abstract
Endometriosis is a common gynecological disorder, which is treated surgically and/ or pharmacologically with an unmet clinical need for new therapeutics. A completed phase I trial and a recent phase II trial that investigated the steroidal aldo-keto reductase 1C3 (AKR1C3) inhibitor BAY1128688 in endometriosis patients prompted this critical assessment on the role of AKR1C3 in endometriosis. This review includes an introduction to endometriosis with emphasis on the roles of prostaglandins and progesterone in its pathophysiology. This is followed by an overview of the major enzymatic activities and physiological functions of AKR1C3 and of the data published to date on the expression of AKR1C3 in endometriosis at the mRNA and protein levels. The review concludes with the rationale for using AKR1C3 inhibitors, a discussion of the effects of AKR1C3 inhibition on the pathophysiology of endometriosis and a brief overview of other drugs under clinical investigation for this indication.
Language:
English
Keywords:
progesterone
,
androgens
,
endometriosis
,
prostaglandin F$_2$$_α$
,
9α
,
11β-prostaglandin F$_2$
,
geranylgeranial
,
9-cis-retinoic acid
Work type:
Article
Typology:
1.02 - Review Article
Organization:
MF - Faculty of Medicine
Publication status:
Published
Publication version:
Version of Record
Year:
2020
Number of pages:
14 str.
Numbering:
Vol. 152, art. 104446
PID:
20.500.12556/RUL-128777
UDC:
618.1
ISSN on article:
1096-1186
DOI:
10.1016/j.phrs.2019.104446
COBISS.SI-ID:
34486233
Publication date in RUL:
28.07.2021
Views:
957
Downloads:
209
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Record is a part of a journal
Title:
Pharmacological research
Shortened title:
Pharmacol. res.
Publisher:
Elsevier
ISSN:
1096-1186
COBISS.SI-ID:
53047811
Licences
License:
CC BY-NC-ND 4.0, Creative Commons Attribution-NonCommercial-NoDerivatives 4.0 International
Link:
http://creativecommons.org/licenses/by-nc-nd/4.0/
Description:
The most restrictive Creative Commons license. This only allows people to download and share the work for no commercial gain and for no other purposes.
Secondary language
Language:
Slovenian
Keywords:
progesteron
,
androgeni
,
endometrioza
Projects
Funder:
ARRS - Slovenian Research Agency
Project number:
J3-8212
Name:
Vloga intrakrinega delovanja estrogenov pri hormonsko odvisnih boleznih – pomen za zdravljenje
Funder:
Other - Other funder or multiple funders
Project number:
P30-ES013508
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