RGD-based Therapy: Principles of Selectivityстатья

Статья опубликована в высокорейтинговом журнале

Информация о цитировании статьи получена из Scopus, Web of Science
Статья опубликована в журнале из списка Web of Science и/или Scopus
Дата последнего поиска статьи во внешних источниках: 20 апреля 2016 г.

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1. Полный текст RUBTSOV-REPRINT-CPD.pdf 808,1 КБ 10 марта 2016 [krimsy]

[1] Rubtsov M. A., Syrkina M. S., Gjumrakch A. Rgd-based therapy: Principles of selectivity // Current Pharmaceutical Design. — 2016. — Vol. 22, no. 7. — P. 925–932. Design of selective anticancer agents targeting RGD-binding integrin receptors is known to be one of the perspective directions in molecular medicine especially in oncology. Significant progress in the development and application of such agents is already obvious. A great number of publications declare significant effects on both in vitro and in vivo experimental models. However the specific mechanism of action is generally not fully elucidated as well as the exact target responsible for the achievement of stated effects is not defined sufficiently well. To date 8 types of integrin receptors capable to recognize RGD-motif in natural ligands has been identified (namely IIb3, v1, v3, v5, v6, v8, 51, 81). Even so the estimation of the affinity of one particular RGDbearing anticancer agent is often based on the determination of the binding efficacy to only one or rarely two integrin receptors. Traditionally the range of targets is restricted by the integrins which are known to be highly expressed in a particular model system. While potential interactions of such an agent with other RGD-recognizing receptors usually remain beyond the research. Nonetheless such interactions may also affect the viability and behavior of cancer cells. In this paper we are going to review and discuss the principles of selectivity achievement in case of RGD-bearing natural ligands and the applicability of these principles in anticancer drug design. [ DOI ]

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