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AS 1411 (AGRO-100) is an oligonucleotide aptamer targeting nucleoproteins. AS 1411 inhibits tumor cell proliferation by affecting the activity of nucleoprotein-containing complexes and can be used as a carrier to precisely deliver nanoparticles, oligonucleotides and small molecules to cancer cells. AS 1411 reduces PRMT5 expression to inhibit tumor growth in DU145 prostate cancer cells. AS 1411 works by blocking the binding of nucleoproteins to bcl-2 mRNA in MCF-7 breast cancer cells. AS 1411-coupled Jin nanospheres can inhibit breast cancer cell proliferation in vitro and in mouse models, has the ability to cross the blood-brain barrier with low tissue toxicity[1][2][3]. | [in vivo]
AS 1411 coupled with gold nanospheres (GNS) shows antitumor activity in a mouse model of breast cancer cell xenografts[3]. | Animal Model: | Female nude mice bearing MDA-MB-231 xenografts[3] | | Dosage: | 22 μg; once a day; 12 days | | Administration: | Intravenous injection (i.v.) | | Result: | Took up and retained in tumors and cleared in normal tissues. |
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Bcl-2 | [References]
[1] Teng Y, et al. AS1411 alters the localization of a complex containing protein arginine methyltransferase 5 and nucleolin. Cancer Res. 2007;67(21):10491-10500. DOI:10.1158/0008-5472.CAN-06-4206
[2] Soundararajan S, et al. The nucleolin targeting aptamer AS1411 destabilizes Bcl-2 messenger RNA in human breast cancer cells. Cancer Res. 2008;68(7):2358-2365. DOI:10.1158/0008-5472.CAN-07-5723
[3] Mohammad T Malik, et al. AS1411-conjugated gold nanospheres and their potential for breast cancer therapy. Oncotarget. 2015 Sep 8;6(26):22270-81. DOI:10.18632/oncotarget.4207 |
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