Selection of progesterone derivatives specific to membrane progesterone receptors
- 作者: Polikarpova A.1, Maslakova A.1, Levina I.2, Kulikova L.2, Kuznetsov Y.2, Guseva A.1, Shchelkunova T.1, Zavarzin I.2, Smirnova O.1
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隶属关系:
- Lomonosov Moscow State University
- Zelinsky Institute of Organic Chemistry
- 期: 卷 82, 编号 2 (2017)
- 页面: 140-148
- 栏目: Article
- URL: https://journals.rcsi.science/0006-2979/article/view/151244
- DOI: https://doi.org/10.1134/S0006297917020055
- ID: 151244
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详细
The search of selective agonists and antagonists of membrane progesterone receptors (mPRs) is a starting point for the study of progesterone signal transduction mechanisms mediated by mPRs, distinct from nuclear receptors. According to preliminary data, the ligand affinity for mPRs differs significantly from that for classical nuclear progesterone receptors (nPRs), which might indicate structural differences in the ligand-binding pocket of these proteins. In the present work, we analyzed the affinity of several progesterone derivatives for mPRs of human pancreatic adenocarcinoma BxPC3 cell line that is characterized by a high level of mPR mRNA expression and by the absence of expression of nPR mRNA. The values were compared with the affinity of these compounds for nPRs. All tested compounds showed almost no affinity for nPRs, whereas their selectivity towards mPRs was different. Derivatives with an additional 19-hydroxyl group and removed 3-keto group had the highest selectivity for mPRs. These results suggest these compounds as the most selective progesterone analogs for studying the mechanisms of progestin action via mPRs.
作者简介
A. Polikarpova
Lomonosov Moscow State University
编辑信件的主要联系方式.
Email: kairo911@gmail.com
俄罗斯联邦, Moscow, 119991
A. Maslakova
Lomonosov Moscow State University
Email: kairo911@gmail.com
俄罗斯联邦, Moscow, 119991
I. Levina
Zelinsky Institute of Organic Chemistry
Email: kairo911@gmail.com
俄罗斯联邦, Moscow, 117913
L. Kulikova
Zelinsky Institute of Organic Chemistry
Email: kairo911@gmail.com
俄罗斯联邦, Moscow, 117913
Y. Kuznetsov
Zelinsky Institute of Organic Chemistry
Email: kairo911@gmail.com
俄罗斯联邦, Moscow, 117913
A. Guseva
Lomonosov Moscow State University
Email: kairo911@gmail.com
俄罗斯联邦, Moscow, 119991
T. Shchelkunova
Lomonosov Moscow State University
Email: kairo911@gmail.com
俄罗斯联邦, Moscow, 119991
I. Zavarzin
Zelinsky Institute of Organic Chemistry
Email: kairo911@gmail.com
俄罗斯联邦, Moscow, 117913
O. Smirnova
Lomonosov Moscow State University
Email: kairo911@gmail.com
俄罗斯联邦, Moscow, 119991