Selection of progesterone derivatives specific to membrane progesterone receptors
Polikarpova AV, Maslakova AA, Levina IS, Kulikova LE, Kuznetsov YV, Guseva AA, Shchelkunova TA, Zavarzin IV, Smirnova OV (2017)
Publication Type: Journal article
Publication year: 2017
Journal
Book Volume: 82
Pages Range: 140-148
Journal Issue: 2
DOI: 10.1134/S0006297917020055
Abstract
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.
Involved external institutions
Lomonosov Moscow State University / Московский государственный университет имени М.В.Ломоносова
Russian Federation (RU)
Russian Academy of Sciences / Росси́йская акаде́мия нау́к (RAS)
Russian Federation (RU)
Russian Federation (RU)
Russian Academy of Sciences / Росси́йская акаде́мия нау́к (RAS)
Russian Federation (RU)
How to cite
APA:
Polikarpova, A.V., Maslakova, A.A., Levina, I.S., Kulikova, L.E., Kuznetsov, Y.V., Guseva, A.A.,... Smirnova, O.V. (2017). Selection of progesterone derivatives specific to membrane progesterone receptors. Biochemistry-Moscow, 82(2), 140-148. https://dx.doi.org/10.1134/S0006297917020055
MLA:
Polikarpova, A. V., et al. "Selection of progesterone derivatives specific to membrane progesterone receptors." Biochemistry-Moscow 82.2 (2017): 140-148.
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