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Title: Chemical modification of a synthetic small molecule boosts its biological efficacy against pluripotency genes in mouse fibroblasts.
Authors: Saha, Abhijit
Pandian, Ganesh N
Sato, Shinsuke
Taniguchi, Junichi
Kawamoto, Yusuke
Hashiya, Kaori
Bando, Toshikazu
Sugiyama, Hiroshi  kyouindb  KAKEN_id
Author's alias: 板東, 俊和
Keywords: biological activity
cellular uptake
gene expression
polyamides
transcription
Issue Date: 8-Jul-2014
Publisher: wiley
Journal title: ChemMedChem
Volume: 9
Issue: 10
Start page: 2374
End page: 2380
Abstract: A synthetic transcriptional activator encompassing both sequence-specific pyrrole-imidazole polyamides (PIPs) and an epigenetic activator (suberoylanilide hydroxamic acid) was recently shown to induce the endogenous expression of core pluripotency genes in mouse embryonic fibroblasts (MEFs). Microarray data analysis suggested Oct-3/4 as the probable target pathway of the activator. However, the expression levels in MEFs treated with the activator were relatively lower than those in mouse embryonic stem cells. Herein, we report studies carried out to improve the efficacy of the activator and show that the biological activity was significantly (p<0.05) improved against the core pluripotency genes after the incorporation of an isophthalic acid (IPA) at the C terminus. The resultant IPA conjugate dramatically induced Oct-3/4 and demonstrated a new chemical strategy for developing PIP conjugates as next-generation genetic switches.
Rights: This is the peer reviewed version of the following article: Saha, A., Pandian, G. N., Sato, S., Taniguchi, J., Kawamoto, Y., Hashiya, K., Bando, T. and Sugiyama, H. (2014), Chemical Modification of a Synthetic Small Molecule Boosts Its Biological Efficacy against Pluripotency Genes in Mouse Fibroblasts. ChemMedChem, 9: 2374–2380, which has been published in final form at http://dx.doi.org/10.1002/cmdc.201402117. This article may be used for non-commercial purposes in accordance with Wiley Terms and Conditions for Self-Archiving.
This is not the published version. Please cite only the published version. この論文は出版社版でありません。引用の際には出版社版をご確認ご利用ください。
URI: http://hdl.handle.net/2433/200213
DOI(Published Version): 10.1002/cmdc.201402117
PubMed ID: 25044886
Appears in Collections:Journal Articles

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