Selective inhibition of miR-21 by phage display screened peptide.
Selective inhibition of miR-21 by phage display screened peptide.
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DOI：
10.1093/nar/gkv185
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发表时间：
2015-04-30
影响因子：
14.9
通讯作者：
Maiti S
中科院分区：
文献类型：
--
作者：
Bose D;Nahar S;Rai MK;Ray A;Chakraborty K;Maiti S
miRNA是基因表达的节点调节因子，并且miRNA的失调与包括癌症在内的不同疾病有因果关系。因此，调节miRNA表达具有治疗重要性。目前正在探索小分子下调miRNA的潜力。肽已经显示出对它们的靶标具有更好的效力和选择性，但是它们在靶向和调节miRNA方面的潜力仍然未被探索。在此，使用噬菌体展示，我们发现了针对pre-miR-21的非常选择性的肽。有趣的是，该肽具有下调miR-21的潜力，通过与pre-miR-21结合并阻碍Dicer加工。它对细胞内的miR-21具有选择性。通过拮抗miR-21功能，该肽能够增加其靶蛋白的表达，从而增加细胞凋亡并抑制细胞增殖、侵袭和迁移。这种肽可以进一步探索其体内抗癌活性，甚至可以扩展到临床研究。
miRNAs are nodal regulators of gene expression and deregulation of miRNAs is causally associated with different diseases, including cancer. Modulation of miRNA expression is thus of therapeutic importance. Small molecules are currently being explored for their potential to downregulate miRNAs. Peptides have shown to have better potency and selectivity toward their targets but their potential in targeting and modulating miRNAs remain unexplored. Herein, using phage display we found a very selective peptide against pre-miR-21. Interestingly, the peptide has the potential to downregulate miR-21, by binding to pre-miR-21 and hindering Dicer processing. It is selective towards miR-21 inside the cell. By antagonising miR-21 function, the peptide is able to increase the expression of its target proteins and thereby increase apoptosis and suppress cell proliferation, invasion and migration. This peptide can further be explored for its anti-cancer activity in vivo and may be even extended to clinical studies.
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DOI：
10.1261/rna.042911.113
发表时间：
2014-04
期刊：
RNA (New York, N.Y.)
影响因子：
--
作者：
Diaz JP;Chirayil R;Chirayil S;Tom M;Head KJ;Luebke KJ
通讯作者：
Luebke KJ
影响因子：
3.7
作者：
Brown M;Suryawanshi H;Hafner M;Farazi TA;Tuschl T
通讯作者：
Tuschl T
影响因子：
4.6
作者：
Lamichhane, Tek N.;Abeydeera, N. Dinuka;Chow, Christine S.
通讯作者：
Chow, Christine S.
影响因子：
5.2
作者：
Gelman, MA;Richter, S;Rana, TM
通讯作者：
Rana, TM
影响因子：
64.8
作者：
Castanotto, Daniela;Rossi, John J.
通讯作者：
Rossi, John J.