|
ИСТИНА |
Войти в систему Регистрация |
ИПМех РАН |
||
3- and 19-oximes of 16alpha,17alpha-cyclohexanoprogesterone derivatives: synthesis and interactions with progesterone receptor and other proteinsстатья
Информация о цитировании статьи получена из
Web of Science,
Scopus
Статья опубликована в журнале из списка Web of Science и/или Scopus
Дата последнего поиска статьи во внешних источниках: 18 июля 2013 г.
- Авторы: Levina I.S., Pokrovskaya E.V., Kulikova L.E., Kamernitzky A.V., Kachala V.V., Smirnov A.N.
- Журнал: Steroids
- Том: 73
- Номер: 8
- Год издания: 2008
- Издательство: Elsevier BV
- Местоположение издательства: Netherlands
- Первая страница: 815
- Последняя страница: 827
- Аннотация: Series of 3- and 19-oximes of 16alpha,17alpha-cyclohexanoprogesterone derivatives (pregna-d’-pentaranes) have been synthesized with the aim of probing the surfaces of progesterone receptor’s and two other protein ligand binding pockets neighboring to 3- and 19-positions of steroid core. The same derivatives were also studied as possible intermediates for attachment to matrixes. The data on affinity constants suggest the presence of hydrophobic cavities with hydrophilic necks in the progesterone receptor and serum pentaranophylin near C19 of bound ligand and the lack of such a cavity in uterine pentaranophylin. Any of 3-oxime substitutions were found to significantly diminish the ligand affinity for the progesterone receptor. It was also found that some of these modifications, in the Z-configuration particularly, might increase the affinity for serum and uterine pentaranophylins. The latter finding suggests the presence of large cavities near C3 of bound ligand in these proteins and interchangeability between 3-keto and 3-oxime groups in ligand-protein interactions.
- Добавил в систему: Смирнов Александр Николаевич