Selection of progesterone derivatives specific to membrane progesterone receptors
- Авторы: 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
-
Учреждения:
- Lomonosov Moscow State University
- Zelinsky Institute of Organic Chemistry
- Выпуск: Том 82, № 2 (2017)
- Страницы: 140-148
- Раздел: Article
- URL: https://journals.rcsi.science/0006-2979/article/view/151244
- DOI: https://doi.org/10.1134/S0006297917020055
- ID: 151244
Цитировать
Аннотация
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.
Об авторах
A. Polikarpova
Lomonosov Moscow State University
Автор, ответственный за переписку.
Email: kairo911@gmail.com
Россия, Moscow, 119991
A. Maslakova
Lomonosov Moscow State University
Email: kairo911@gmail.com
Россия, Moscow, 119991
I. Levina
Zelinsky Institute of Organic Chemistry
Email: kairo911@gmail.com
Россия, Moscow, 117913
L. Kulikova
Zelinsky Institute of Organic Chemistry
Email: kairo911@gmail.com
Россия, Moscow, 117913
Y. Kuznetsov
Zelinsky Institute of Organic Chemistry
Email: kairo911@gmail.com
Россия, Moscow, 117913
A. Guseva
Lomonosov Moscow State University
Email: kairo911@gmail.com
Россия, Moscow, 119991
T. Shchelkunova
Lomonosov Moscow State University
Email: kairo911@gmail.com
Россия, Moscow, 119991
I. Zavarzin
Zelinsky Institute of Organic Chemistry
Email: kairo911@gmail.com
Россия, Moscow, 117913
O. Smirnova
Lomonosov Moscow State University
Email: kairo911@gmail.com
Россия, Moscow, 119991
![](/img/style/loading.gif)