GRO-29A(GRO-29A) - 药物靶点：IKKγ x NF-κB_专利_临床

概要

基本信息

药物类型

寡核苷酸

别名-

靶点

IKKγ x NF-κB

作用机制

IKKγ抑制剂(inhibitor of nuclear factor kappa B kinase regulatory subunit gamma inhibitors)、NF-κB抑制剂(核因子NF-κB复合体抑制剂)

治疗领域

肿瘤

在研适应症-

非在研适应症

肿瘤

原研机构

University of Louisville

在研机构-

非在研机构

University of Louisville

最高研发阶段终止临床前

首次获批日期-

最高研发阶段(中国)-

特殊审评-

关联

100 项与 GRO-29A 相关的临床结果

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100 项与 GRO-29A 相关的转化医学

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100 项与 GRO-29A 相关的专利（医药）

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1

项与 GRO-29A 相关的文献（医药）

2021-02-07·Journal of Drug Targeting3区 · 医学

Polypod-like structured guanine-rich oligonucleotide aptamer as a selective and cytotoxic nanostructured DNA to cancer cells

3区 · 医学

Article

作者: Nishikawa, Makiya ; Tanishita, Sohei ; Sakuma, Shinji ; Hayashi, Emi ; Matsushita, Nao ; Nishino, Manato ; Mohri, Kohta

Guanine-rich oligonucleotide (GRO) can be developed as an effective anticancer agent owing to its high selectivity, affinity and antiproliferative activity in cancer cells. In this study, to increase the potency of GRO29A, a 29-mer GRO aptamer against nucleolin, an overexpressed protein in cancer cells, GRO29A was incorporated into three or six pods of polypod-like structured DNA (polypodna), tripodna or hexapodna, respectively. The polypod-like structured GROs, tri-G3, consisting of one tripodna and three GRO29A, or hexa-G1, hexa-G3 or hexa-G6, each of which comprises one hexapodna and one, three or six GRO29A, respectively, were designed. Tri-G3, hexa-G1 and hexa-G3 were prepared in high yield, except for hexa-G6. Polypod-like structured GROs had quadruplex structures under physiological salt conditions, and degraded at a slower rate in buffer containing serum. Cellular interaction experiments using fluorescently labelled DNA samples showed that the uptake of hexa-G3 by nucleolin-positive MCF-7 cells was more than 2-fold higher than GRO29A, and the interaction was increasingly dependent on the number of GRO29A in the structures. Hexa-G3 inhibited the proliferation of MCF-7 cells in more than 40%, but not of CHO cells. These results indicate that polypod-like structured GROs are useful DNA aptamers with high selectivity and cytotoxicity against nucleolin-positive cancer cells.

100 项与 GRO-29A 相关的药物交易

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