Selection of progesterone derivatives specific to membrane progesterone receptors
- Autores: 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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Afiliações:
- Lomonosov Moscow State University
- Zelinsky Institute of Organic Chemistry
- Edição: Volume 82, Nº 2 (2017)
- Páginas: 140-148
- Seção: Article
- URL: https://journals.rcsi.science/0006-2979/article/view/151244
- DOI: https://doi.org/10.1134/S0006297917020055
- ID: 151244
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Resumo
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.
Sobre autores
A. Polikarpova
Lomonosov Moscow State University
Autor responsável pela correspondência
Email: kairo911@gmail.com
Rússia, Moscow, 119991
A. Maslakova
Lomonosov Moscow State University
Email: kairo911@gmail.com
Rússia, Moscow, 119991
I. Levina
Zelinsky Institute of Organic Chemistry
Email: kairo911@gmail.com
Rússia, Moscow, 117913
L. Kulikova
Zelinsky Institute of Organic Chemistry
Email: kairo911@gmail.com
Rússia, Moscow, 117913
Y. Kuznetsov
Zelinsky Institute of Organic Chemistry
Email: kairo911@gmail.com
Rússia, Moscow, 117913
A. Guseva
Lomonosov Moscow State University
Email: kairo911@gmail.com
Rússia, Moscow, 119991
T. Shchelkunova
Lomonosov Moscow State University
Email: kairo911@gmail.com
Rússia, Moscow, 119991
I. Zavarzin
Zelinsky Institute of Organic Chemistry
Email: kairo911@gmail.com
Rússia, Moscow, 117913
O. Smirnova
Lomonosov Moscow State University
Email: kairo911@gmail.com
Rússia, Moscow, 119991
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