Powered by OpenAIRE graph
Found an issue? Give us feedback
image/svg+xml art designer at PLoS, modified by Wikipedia users Nina, Beao, JakobVoss, and AnonMoos Open Access logo, converted into svg, designed by PLoS. This version with transparent background. http://commons.wikimedia.org/wiki/File:Open_Access_logo_PLoS_white.svg art designer at PLoS, modified by Wikipedia users Nina, Beao, JakobVoss, and AnonMoos http://www.plos.org/ Acta Naturaearrow_drop_down
image/svg+xml art designer at PLoS, modified by Wikipedia users Nina, Beao, JakobVoss, and AnonMoos Open Access logo, converted into svg, designed by PLoS. This version with transparent background. http://commons.wikimedia.org/wiki/File:Open_Access_logo_PLoS_white.svg art designer at PLoS, modified by Wikipedia users Nina, Beao, JakobVoss, and AnonMoos http://www.plos.org/
addClaim

This Research product is the result of merged Research products in OpenAIRE.

You have already added 0 works in your ORCID record related to the merged Research product.

Ингибирование поли(ADP-рибозо)- полимеразы метаболитом нуклеиновых кислот 7-метилгуанином

Ингибирование поли(ADP-рибозо)- полимеразы метаболитом нуклеиновых кислот 7-метилгуанином

Abstract

Способность метаболита нуклеиновых кислот 7-метилгуанина ингибировать поли(ADP-рибозо)полимеразу 1 (ПАРП-1) и поли(ADP-рибозо)полимеразу 2 (ПАРП-2) выявлена in silico и изучена экспериментально. Показано, что для эффективного связывания пуриновых производных с ПАРП важна аминогруппа в положении 2 и метильная группа в положении 7. Активность ПАРП-1 и ПАРП-2 подавляется 7-метилгуанином со значениями IC50 150 и 50 мкМ соответственно. В ПАРП-ингибирующей концентрации 7-метилгуанин не токсичен, но способен усиливать апоптотическую гибель BRCA1-дефицитных клеток рака молочной железы под воздействием цисплатина и доксорубицина широко используемых ДНКповреждающих химиотерапевтических препаратов. 7-Метилгуанин имеет привлекательный предсказанный профиль фармакокинетики и токсичности и может рассматриваться в качестве дополнительного компонента химиотерапии.

Keywords

ДОКИНГ,ИНГИБИТОРЫ ПАРП,МОЛЕКУЛЯРНОЕ МОДЕЛИРОВАНИЕ

  • BIP!
    Impact byBIP!
    selected citations
    These citations are derived from selected sources.
    This is an alternative to the "Influence" indicator, which also reflects the overall/total impact of an article in the research community at large, based on the underlying citation network (diachronically).
    0
    popularity
    This indicator reflects the "current" impact/attention (the "hype") of an article in the research community at large, based on the underlying citation network.
    Average
    influence
    This indicator reflects the overall/total impact of an article in the research community at large, based on the underlying citation network (diachronically).
    Average
    impulse
    This indicator reflects the initial momentum of an article directly after its publication, based on the underlying citation network.
    Average
Powered by OpenAIRE graph
Found an issue? Give us feedback
selected citations
These citations are derived from selected sources.
This is an alternative to the "Influence" indicator, which also reflects the overall/total impact of an article in the research community at large, based on the underlying citation network (diachronically).
BIP!Citations provided by BIP!
popularity
This indicator reflects the "current" impact/attention (the "hype") of an article in the research community at large, based on the underlying citation network.
BIP!Popularity provided by BIP!
influence
This indicator reflects the overall/total impact of an article in the research community at large, based on the underlying citation network (diachronically).
BIP!Influence provided by BIP!
impulse
This indicator reflects the initial momentum of an article directly after its publication, based on the underlying citation network.
BIP!Impulse provided by BIP!
0
Average
Average
Average
bronze